Unsaturated androstanes which are substituted with one or more hydroxyl groups in any position in the ring system.
The science that investigates the principles governing correct or reliable inference and deals with the canons and criteria of validity in thought and demonstration. This system of reasoning is applicable to any branch of knowledge or study. (Random House Unabridged Dictionary, 2d ed & Sippl, Computer Dictionary, 4th ed)
The branch of psychology which seeks to learn more about the fundamental causes of behavior by studying various psychologic phenomena in controlled experimental situations.
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
Interacting DNA-encoded regulatory subsystems in the GENOME that coordinate input from activator and repressor TRANSCRIPTION FACTORS during development, cell differentiation, or in response to environmental cues. The networks function to ultimately specify expression of particular sets of GENES for specific conditions, times, or locations.
A sterol usually substituted with radioactive iodine. It is an adrenal cortex scanning agent with demonstrated high adrenal concentration and superior adrenal imaging.
The facilitation of a chemical reaction by material (catalyst) that is not consumed by the reaction.
Unsaturated derivatives of the steroid androstane containing at least one double bond at any site in any of the rings.
The edible portions of any animal used for food including domestic mammals (the major ones being cattle, swine, and sheep) along with poultry, fish, shellfish, and game.
Any of various animals that constitute the family Suidae and comprise stout-bodied, short-legged omnivorous mammals with thick skin, usually covered with coarse bristles, a rather long mobile snout, and small tail. Included are the genera Babyrousa, Phacochoerus (wart hogs), and Sus, the latter containing the domestic pig (see SUS SCROFA).
The volatile portions of substances perceptible by the sense of smell. (Grant & Hackh's Chemical Dictionary, 5th ed)
The surgical removal of one or both testicles.
A potent androgenic steroid and major product secreted by the LEYDIG CELLS of the TESTIS. Its production is stimulated by LUTEINIZING HORMONE from the PITUITARY GLAND. In turn, testosterone exerts feedback control of the pituitary LH and FSH secretion. Depending on the tissues, testosterone can be further converted to DIHYDROTESTOSTERONE or ESTRADIOL.
A major C19 steroid produced by the ADRENAL CORTEX. It is also produced in small quantities in the TESTIS and the OVARY. Dehydroepiandrosterone (DHEA) can be converted to TESTOSTERONE; ANDROSTENEDIONE; ESTRADIOL; and ESTRONE. Most of DHEA is sulfated (DEHYDROEPIANDROSTERONE SULFATE) before secretion.
The outer layer of the adrenal gland. It is derived from MESODERM and comprised of three zones (outer ZONA GLOMERULOSA, middle ZONA FASCICULATA, and inner ZONA RETICULARIS) with each producing various steroids preferentially, such as ALDOSTERONE; HYDROCORTISONE; DEHYDROEPIANDROSTERONE; and ANDROSTENEDIONE. Adrenal cortex function is regulated by pituitary ADRENOCORTICOTROPIN.
Compounds that interact with ANDROGEN RECEPTORS in target tissues to bring about the effects similar to those of TESTOSTERONE. Depending on the target tissues, androgenic effects can be on SEX DIFFERENTIATION; male reproductive organs, SPERMATOGENESIS; secondary male SEX CHARACTERISTICS; LIBIDO; development of muscle mass, strength, and power.
Substances used to allow enhanced visualization of tissues.
A delta-4 C19 steroid that is produced not only in the TESTIS, but also in the OVARY and the ADRENAL CORTEX. Depending on the tissue type, androstenedione can serve as a precursor to TESTOSTERONE as well as ESTRONE and ESTRADIOL.
A pair of glands located at the cranial pole of each of the two KIDNEYS. Each adrenal gland is composed of two distinct endocrine tissues with separate embryonic origins, the ADRENAL CORTEX producing STEROIDS and the ADRENAL MEDULLA producing NEUROTRANSMITTERS.
Proteins, generally found in the CYTOPLASM, that specifically bind ANDROGENS and mediate their cellular actions. The complex of the androgen and receptor migrates to the CELL NUCLEUS where it induces transcription of specific segments of DNA.
The circulating form of a major C19 steroid produced primarily by the ADRENAL CORTEX. DHEA sulfate serves as a precursor for TESTOSTERONE; ANDROSTENEDIONE; ESTRADIOL; and ESTRONE.
An aromatized C18 steroid with a 3-hydroxyl group and a 17-ketone, a major mammalian estrogen. It is converted from ANDROSTENEDIONE directly, or from TESTOSTERONE via ESTRADIOL. In humans, it is produced primarily by the cyclic ovaries, PLACENTA, and the ADIPOSE TISSUE of men and postmenopausal women.
The 17-beta-isomer of estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids.
A heteropolysaccharide that is similar in structure to HEPARIN. It accumulates in individuals with MUCOPOLYSACCHARIDOSIS.
Inorganic salts of sulfuric acid.
Inorganic and organic derivatives of sulfuric acid (H2SO4). The salts and esters of sulfuric acid are known as SULFATES and SULFURIC ACID ESTERS respectively.
Organic esters of sulfuric acid.
Enzymes that catalyze the hydrolysis of a phenol sulfate to yield a phenol and sulfate. Arylsulfatase A, B, and C have been separated. A deficiency of arylsulfatases is one of the causes of metachromatic leukodystrophy (LEUKODYSTROPHY, METACHROMATIC). EC 3.1.6.1.
A metabolite of TESTOSTERONE or ANDROSTENEDIONE with a 3-alpha-hydroxyl group and without the double bond. The 3-beta hydroxyl isomer is epiandrosterone.
Glands situated on each side of the prostate that secrete a fluid component of the seminal fluid into the urethra.
Specialized connective tissue composed of fat cells (ADIPOCYTES). It is the site of stored FATS, usually in the form of TRIGLYCERIDES. In mammals, there are two types of adipose tissue, the WHITE FAT and the BROWN FAT. Their relative distributions vary in different species with most adipose tissue being white.
Any behavior associated with conflict between two individuals.

Identification of 17-methyl-18-norandrosta-5,13(17-dien-3beta-ol, the C19 fragment formed by adrenal side chain cleavage of a 20-aryl analog of (20S)-20-hydroxycholesterol. (1/115)

Incubation of (20R)-20-phenyl-5-pregnene-3beta,20-diol, an aromatic analog of (23S)-20-hydroxycholesterol, with an adrenal mitochondrial preparation leads to the formation of four compounds: pregnenolone, phenol, a C8 ketone, acetophenone, and a nonpolar C19 compound. This latter compound has now been identified by reverse isotope dilution analysis and by gas chromatography/mass spectrometry as 17-methyl-18-norandrosta-5,13(17)-dien-3beta-ol. From these results it is evident that enzymatic fission of the C-17,20 bond of this synthetic derivative occurs. On the other hand, when (20S)-20-hydroxy[21-14C]cholesterol was used as substrate, the analogous cleavage did not take place. Thus, substitution of an aromatic group on C-20 facilitates side chain cleavage between that carbon atom and the nucleus whereas neither of the naturally occuring precursors, cholesterol or its 20-hydroxylated counterpart, are metabolized to a C8 fragment.  (+info)

Characterization of ovarian carbonyl reductase gene expression during ovulation in the gonadotropin-primed immature Rat. (2/115)

In this differential-display polymerase chain reaction-based study, four different primer sets generated cDNA fragments of ovarian carbonyl reductase genes that were uniquely expressed during the ovulatory process in eCG-primed immature rats. The temporal pattern of expression of this aldo-keto reductase gene was delineated by extracting ovarian RNA at 0, 2, 4, 8, 12, and 24 h after induction of ovulation via injection of the primed animals with hCG. The results showed that at least four homologous forms of this gene were transcribed during ovulation. Northern blot analyses indicated a 14-fold increase in ovarian mRNA for carbonyl reductase, with expression reaching a peak at 8 h after hCG treatment and then declining to negligible levels during the next 16 h. In situ hybridization revealed that most of the transcription was in the thecal connective tissue of the ovary and was absent from the granulosa layer of ovarian follicles. Treatment of the animals with ovulation-blocking doses of epostane (an inhibitor of progesterone synthesis) or indomethacin (an inhibitor of prostanoid synthesis) did not reduce the expression of ovarian carbonyl reductase. Nevertheless, the temporal pattern of expression of carbonyl reductase after the induction of ovulation suggests that this enzyme activity is at least indirectly associated with the ovulatory process.  (+info)

Involvement of progesterone in gonadotrophin-induced pituitary adenylate cyclase-activating polypeptide gene expression in pre-ovulatory follicles of rat ovary. (3/115)

The present study was designed to determine whether progesterone might have a role in gonadotrophin-induced pituitary adenylate cyclase-activating polypeptide (Pacap) gene expression in rat ovary. Northern blot analysis revealed that treatment of pregnant mare's serum gonadotrophin (PMSG)-primed immature rats with the progestin antagonist RU486 or an inhibitor of 3beta-hydroxysteroid dehydrogenase epostane, 1 h before HCG, resulted in a dose-dependent inhibition of the HCG-induced Pacap gene expression. In-situ hybridization demonstrated that the number of pre-ovulatory follicles expressing Pacap mRNA in their granulosa cells was greatly reduced in ovaries treated with RU486. Moreover, the suppressive effect of RU486 or epostane on the LH-induced Pacap gene expression in cultured pre-ovulatory follicles was reversed by co-treatment with the synthetic progestin R5020. We further cloned the 5'-flanking region of the rat Pacap gene and identified the presence of a consensus progesterone receptor element. When luciferase fusion genes containing Pacap gene promoter were transiently transfected into granulosa cells of pre-ovulatory follicles, luciferase activity was markedly stimulated by LH. Treatment with RU486 or epostane resulted in partial suppression of LH-stimulated PACAP promoter activity. Taken together, these results indicate that progesterone, acting through progesterone receptors, plays a role in gonadotrophin induction of Pacap gene expression in granulosa cells of pre-ovulatory follicles, and thereby may be involved in the process of ovulation.  (+info)

Ovarian expression of a disintegrin and metalloproteinase with thrombospondin motifs during ovulation in the gonadotropin-primed immature rat. (4/115)

Mammalian ovulation is a dynamic process that requires degradation of the collagenous connective tissue in the thecal layers of a mature follicle. In this reverse transcription-polymerase chain reaction differential display study, gonadotropin-primed immature rats were used to detect ovarian expression of a relatively new type of disintegrin and metalloproteinase with thrombospondin motifs (ADAMTS-1) that is known to cleave extracellular matrix in acutely inflamed tissues. Immature Wistar rats were primed with 10 IU eCG s. c., and the temporal pattern of expression of the ADAMTS-1 gene was delineated by extracting ovarian RNA at 0, 2, 4, 8, 12, and 24 h after induction of ovulation by injecting the primed animals with 10 IU hCG s.c. The differential display data, Northern analyses, and in situ hybridization micrographs all showed significant up-regulation of ADAMTS-1 gene expression by 8 h after hCG administration. The in situ data indicated that the ADAMTS-1 mRNA was in the granulosa layer of mature follicles. Expression reached a peak at 12 h and remained elevated at 24 h after hCG. ADAMTS-1 gene expression was impaired by the antiprogesterone agent epostane, but this inhibition could be overcome by exogenous progesterone. ADAMTS-1 expression was not affected when ovulation was blocked by treatment of the animals with the anti-eicosanoid agent indomethacin. In conclusion, the temporal pattern of expression of this gene, and its apparent regulation by progesterone, suggests that ADAMTS-1 has a significant role in the inflammatory events of the ovulatory process.  (+info)

Positive relationship between menstrual synchrony and ability to smell 5alpha-androst-16-en-3alpha-ol. (5/115)

To explore the possibility that compounds which were identified as pheromones in experimental animals mediate human menstrual synchrony, we examined the relationship between menstrual synchrony and the ability to smell putative pheromones, 5alpha-androst-16-en-3alpha-ol (3alpha-androstenol) and 5alpha-androst-16-en-3-one (5alpha-androstenone). When we examined menstrual synchrony among 64 women living together in a college dormitory, we found that 24 (38%) of them became synchronized with room-mates in 3 months. Afterwards, dilution series of 3alpha-androstenol and 5alpha-androstenone and the control odorant (pyridine) were presented to the 64 women and sensitivity to the odors was compared between synchronized and non-synchronized women. No difference was found between the two groups of women in the detection threshold for pyridine, indicating that general olfactory ability did not differ between them. The detection threshold for 3alpha-androstenol of synchronized women was significantly lower than that of non-synchronized women, but no difference in the threshold for 5alpha-androstenone was found between synchronized and non-synchronized women. These results indicate that the women who showed menstrual synchrony had a higher sensitivity to 3alpha-androstenol but not necessarily to 5alpha-androstenone.  (+info)

Effects of 5alpha-androst-16-en-3alpha-ol on the pulsatile secretion of luteinizing hormone in human females. (6/115)

We examined the effects of 5alpha-androst-16-en-3alpha-ol (3alpha-androstenol) on pulsatile luteinizing hormone (LH) secretion in human females. The frequency of the LH pulse in the follicular phase was decreased by exposing the women to 3alpha-androstenol.  (+info)

Humoral pathway for local transfer of the priming pheromone androstenol from the nasal cavity to the brain and hypophysis in anaesthetized gilts. (7/115)

It is generally accepted that pheromones act by stimulating of the dendritic receptors of the olfactory neurones massed in the olfactory epithelium. This study was designed to ascertain whether it is possible for the boar pheromone androstenol (5alpha-androst-16-en-3-ol) to be transported from the nasal cavity of anaesthetized gilts to the brain and hypophysis via local transfer from the blood in the perihypophyseal vascular complex. The experiment was performed on days 18-21 of the porcine oestrous cycle (crossbred gilts, n = 6). Tritiated androstenol (3H-A; total amount 10(8) d.p.m. (758 ng)) was applied for 1 min onto the respiratory part of the nasal mucosa, 4-6 cm from the opening of the nares. Arterial blood samples from the aorta and from the carotid rete were collected every 2 min during the 60 min period following administration of the steroid. Total radioactive venous effluent from the head was removed and an adequate volume of homologous blood was transfused into the heart through the carotid external vein. At the end of the experiment gilts were killed and tissue samples of the hypophysis and some brain structures were collected to measure radioactivity. In addition, corresponding control tissues were collected from three untreated gilts and from three heads of gilts 60 min after 3H-A was applied post mortem into the nasal cavity. The concentration of 3H-A was significantly higher (P < 0.0001) in the arterial blood of the carotid rete than that of aorta. The mean rate of 3H-A counter current transfer from venous to arterial blood in the perihypophyseal vascular complex, expressed as the ratio of the 3H-A concentration in arterial blood of the carotid rete to the 3H-A concentration in blood sampled simultaneously from the aorta, was 1.96 +/- 0.1. The concentration of 3H-A in plasma from the venous effluent from the head ranged from 1.3 to 1.8 pg x ml(-1). During the 60 min period of the experiment, 0.68% of the total applied dose of 3H-A was resorbed from the nasal cavity into the venous blood. Moreover, we found that 3H-A was present in the olfactory bulb (P <0.01), amygdala, septum, hypothalamus, adenohypophysis, neurohypophysis (P > 0.05) and perihypophyseal vascular complex (P < 0.01). These results demonstrate that, in anaesthetized gilts, the boar pheromone androstenol may be resorbed from the nasal mucosa, transferred in the perihypophyseal vascular complex into arterial blood supplying the brain and hypophysis, and then arrested in the hypophysis and certain brain structures. We suggest that in addition to the standard neural pathway for signalling pheromones, another pathway exists whereby androstenol, as a priming pheromone, may be resorbed from the nasal cavity into the bloodstream and then pass locally from the perihypophyseal vascular complex into the arterial blood supplying the brain and hypophysis, thus avoiding the first passage metabolism in the liver.  (+info)

Demonstration of 2-unsaturated C19-steroids in the urine of female Asian elephants, Elephas maximus, and their dependence on ovarian activity. (8/115)

Air-borne volatile substances have been demonstrated to signal oestrus, induce ovulation and synchronize ovarian activity in different mammals. An oestrous-related pheromone of the female Asian elephant (Elephas maximus) is known to induce behavioural responses in elephant bulls. Additional data revealed that timing of oestrus in females with close social relationships tends to be synchronized. Therefore, urine from female Asian elephants might be expected to contain luteal phase-dependent volatile substances, which may function as additional chemical signals in this species. The aim of the present study was to identify such compounds and to investigate their pattern of excretion throughout the ovarian cycle. Urine samples were collected three times a week during the follicular phase and one to three times a week during the luteal phase from five adult female Asian elephants from a total of 13 non-conception cycles and one conception cycle, including the first 72 weeks of pregnancy. A simple headspace solid-phase microextraction method has been developed for quantification of urinary volatile substances and analysis was performed by gas chromatography. The comparison of urine collected during the follicular and the luteal phase indicated the presence of two luteal phase-dependent substances. Mass spectrometry was used to identify one substance as 5alpha-androst-2-en-17-one and a second substance as the corresponding alcoholic compound 5alpha-androst-2-en-17beta-ol. The 5alpha-androst-2-en-17beta-ol and -17-one profiles reflected cyclic ovarian activity with clear (10-20-fold) luteal phase increases. Furthermore, measurements of both compounds were correlated positively with the concentration of urinary pregnanetriol and indicated cycle duration (15.1 +/- 1.2 weeks) similar to that obtained from pregnanetriol measurements (15.2 +/- 1.6 weeks). The results demonstrate the presence of two luteal phase-specific steroidal volatile compounds in elephant urine. One of the substances, 5alpha-androst-2-en-17-one, has been demonstrated in human axillary bacterial isolates. The measurement of both volatile substances in elephant urine can be used for rapid detection of the stage of the ovarian cycle, as the analysis can be completed within 2 h.  (+info)

Abiraterone acetate is a steroidal irreversible inhibitor of CYP17 (17α hydroxylase/C17, 20-lyase), blocking 2 important enzymatic activities in the synthesis of testosterone. The goal of this study is to compare the clinical benefit of abiraterone acetate plus prednisone with placebo plus prednisone in patients with metastatic castration-resistant prostate cancer (CRPC) who have failed one or two chemotherapy regimens, one of which contains docetaxel. All patients involved in the study will be randomized (assigned by chance) into one of two arms and will not know what study drug is being given to them. Study drug randomization allocation will be 2:1 (abiraterone acetate: placebo). The study will be conducted in the United States, Canada, Australia, and the EU. The study will consist of screening, treatment, and follow-up. In this study, patients will receive study treatment (abiraterone acetate or placebo) plus prednisone until progression of clinical disease. Follow-up will continue until ...
3-Keto-5α-abiraterone, also known as 17-(3-pyridyl)-5α-androst-16-en-3-one, is an active metabolite of abiraterone acetate that has been found to possess androgenic activity and to stimulate prostate cancer progression.[1][2] It is formed as follows: abiraterone acetate to abiraterone by esterases; abiraterone to Δ4-abiraterone by 3β-hydroxysteroid dehydrogenase/Δ5-4 isomerase; and Δ4-abiraterone to 3-keto-5α-abiraterone by 5α-reductase.[1][2] 3-Keto-5α-abiraterone may counteract the clinical effectiveness of abiraterone acetate, and so inhibition of its formation using the 5α-reductase inhibitor dutasteride is being investigated as an adjunct to abiraterone acetate in the treatment of prostate cancer.[1][2] ...
Drugs and Targets FDA approves abiraterone acetate in combination with prednisone for high-risk metastatic castration-sensitive prostate cancer. FDA approved abiraterone acetate (Zytiga) tablets in combination with prednisone for metastatic high-risk castration-sensitive prostate cancer (CSPC). The drug is sponsored by Janssen Biotech Inc.. FDA initially approved abiraterone acetate with prednisone in 2011 for patients with metastatic castration-resistant prostate cancer (CRPC) who had received prior chemotherapy, and expanded the indication in 2012 for patients with metastatic CRPC. The latest approval was based on LATITUDE (NCT01715285), a placebo controlled international clinical trial that randomized 1,199 patients with metastatic high-risk CSPC. Patients received either abiraterone acetate, 1,000 mg orally once daily with prednisone 5 mg once daily (n=597), or placebos orally once daily (n=602). Patients in both arms received a gonadotropin releasing hormone or had a bilateral orchiectomy. ...
TY - JOUR. T1 - Quantitation of the anticancer drug abiraterone and its metabolite Δ(4)-abiraterone in human plasma using high-resolution mass spectrometry. AU - Bhatnagar, Atul. AU - McKay, Matthew J.. AU - Crumbaker, Megan. AU - Ahire, Ketan. AU - Karuso, Peter. AU - Gurney, Howard. AU - Molloy, Mark P.. PY - 2018/5/30. Y1 - 2018/5/30. N2 - Abiraterone acetate is administered as a prodrug to patients with metastatic, castration-resistant prostate cancer (mCRPC) and is readily metabolized into the potent 17a-hydroxylase/17,20-lyase (CYP17) enzyme inhibitor and androgen receptor inhibitor abiraterone and Δ(4)-abiraterone (D4A), respectively. To investigate pharmacokinetic variability in abiraterone acetate metabolism we developed highly sensitive liquid chromatography/mass spectrometry (LC/MS) assays for the simultaneous quantitation of abiraterone and D4A in human plasma using high-resolution mass spectrometry (HRMS) on an Orbitrap mass spectrometer. This study demonstrates the quantitative ...
The aim of this study is to evaluate cardiotoxicity of abiraterone acetate (AA) in metastatic castration-resistant prostate cancer patients (pts) with cardiovascular comorbidities or coronary artery disease (CAD) risk factors.
Clinical trial for Castration Resistant Prostatic Cancer | Metastatic Prostate Cancer | Prostate Cancer | Malignant neoplasm of prostate | Recurrent | Early , A Study of Niraparib in Combination With Abiraterone Acetate and Prednisone Versus Abiraterone Acetate and Prednisone for Treatment of Participants With Metastatic Prostate Cancer
99%), and is metabolised in the liver by CYP3A4 and SULT2A1 to inactive metabolites. The drug is excreted in feces (~88%) and urine (~5%), and has a terminal half-life of 12 ± 5 hours. Abiraterone acetate, also known as 17-(3-pyridinyl)androsta-5,16-dien-3β-ol acetate, is a synthetic androstane steroid and a derivative of androstadienol (androsta-5,16-dien-3β-ol), an endogenous androstane pheromone. It is specifically a derivative of androstadienol with a pyridine ring at the C17 position and an acetate ester attached to the C3β hydroxyl group. Abiraterone acetate is the C3β acetate ester of abiraterone. In the early 1990s, Mike Jarman, Elaine Barrie, and Gerry Potter of the Cancer Research UK Centre for Cancer Therapeutics in the Institute of Cancer Research in London set out to develop drug treatments for prostate cancer. Starting from the drug ketoconazole, they developed abiraterone, filing a patent in 1993 and publishing the first paper describing it the following year. Rights for ...
This study investigated the efficacy of abiraterone acetate followed by enzalutamide in patients with chemotherapy-naive metastatic castration-resistant
What is Samtica 250 mg Tablet ?. Samtica belongs to a group of medications called antineoplastics, or anti-cancer medications. It contains a medicine called Abiraterone Acetate. Samtica is a prescription medicine that can be purchased by a patient only against a valid prescription of a healthcare professional. Do not share this cancer medicine with others until the condition is not monitored by a pharmacist.. Samtica 250 mg Tablets Uses :. Samtica (Abiraterone Acetate) is indicated for use in combination with other medicine for the treatment of men with metastatic castration-resistant prostate cancer.. Samtica Abiraterone 250 mg Tablets Work :. Abiraterone is known as an androgen biosynthesis inhibitor. Androgens stimulate prostate cancer cells to grow. The main androgens in the body are testosterone. Almost all testosterone in men is made by the testicles. A very small amount is made by the adrenal glands, which sit above the kidneys. Abiraterone reduces the amount of testosterone made by your ...
The results of the in vitro studies demonstrated that abiraterone acetate, abiraterone, and its major metabolites, abiraterone sulfate and abiraterone sulfate N-oxide, were inhibitors of CYP2C8 activity in human liver microsomes. Of these, abiraterone sulfate exhibited the most potent CYP2C8 inhibitory activity. Although not compared in the same assay, the data suggest that abiraterone sulfate is at least 10-fold more potent than abiraterone and its prodrug as a CYP2C8 inhibitor. Abiraterone acetate and abiraterone sulfate were predicted to have Ki values (inhibition constant = 0.5 × IC50) below 1 µM, which suggest high in vitro potency to cause in vivo drug interaction of at least two-fold (Obach et al., 2005). In a previous study, Cmax of abiraterone, abiraterone sulfate, and N-oxide abiraterone sulfate were reported to be approximately 0.37 µM, 25 µM, and 9.2 µM, respectively, after a single-dose administration of 1000 mg of abiraterone acetate to healthy volunteers (Bernard et al., ...
Phase II multicenter study of abiraterone acetate plus prednisone therapy in patients with docetaxel-treated castration-resistant prostate cancer Academic Article ...
This is an open-label (identity of study drug will be known) extended access study to evaluate the safety and efficacy of continued administration of abiraterone acetate in patients who have completed 12 cycles of abiraterone acetate treatment in Clinical Study COU-AA-001 and continue to receive clinical benefit from this treatment. Patients will continue with the same dose regimen administered at the end of Study COU-AA-001 and will receive a low-dose glucocorticoid daily. Patients will be followed every 3 months for disease progression and survival for up to 3 years following study entry. Safety will be monitored throughout the study up to 30 days after the last dose of study medication ...
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Abiraterone acetate is the generic name for the trade name drug Zytiga®. Buy Abiraterone Acetate - instructions for use, price, analogues, generic
Abiraterone acetate (INN, USAN, BAN, JAN) (brand names Zytiga, Abiratas, Abretone, Abirapro) is a steroidal CYP17A1 inhibitor and by extension androgen synthesis inhibitor which is used in combination with prednisone in metastatic castration-resistant prostate cancer (mCRPC; previously called hormone-resistant or hormone-refractory prostate cancer) - i.e., prostate cancer not responding to androgen deprivation or treatment with androgen receptor antagonists.Wikipedia] A SNP in the CYP17A1 gene, rs2486758, has been reported (in a small study) to potentially indicate mCRPC patients responding better to AA/P therapy. ...
The STAMPEDE trial offers a direct, randomised, comparative analysis of two new standards for patients with hormone naive prostate cancer. This comparison was possible only because of the novel platform design of this protocol. Failure-free and progression-free survival clearly favoured SOC+abiraterone+prednisone, and with less certainty, metastasis-free survival favoured SOC+abiraterone+prednisone. However, the design means that abiraterone was given to progression whereas docetaxel was given as short course at start of therapy, meaning docetaxel patients had more salvage options at relapse, including docetaxel rechallenge. This explains the discrepancy between failure and progression-free survival favouring abiraterone but with no ultimate difference seen on overall or cause-specific survival. The proportion of patients having at least one severe toxicity was similar between the arms but the type of toxicities was quite different.. These data will help clinicians and patients to choose ...
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This trial is investigating the tolerability and efficacy of abiraterone acetate with prednisone in patients with castration resistant prostate cancer.
h4,Background,/h4,Abiraterone acetate (AA) is the prodrug of abiraterone, which inhibits CYP17A1 and testosterone synthesis and prolongs the survival of patients with metastatic castration-resistant prostate cancer (mCRPC). AA plus prednisone (P) (AA+P) is approved for the treatment of patients with mCRPC.,h4,Objective,/h4,To investigate whether long-term use of low-dose P with or without AA leads to corticosteroid-associated adverse events (CA-AEs) in mCRPC patients.,h4,Design, setting, and participants,/h4,The study included 2267 patients in COU-AA-301 and COU-AA-302. We used an inclusive Standardized MedDRA Queries-oriented approach to identify 112 preferred terms for known CA-AEs, and assessed the incidence of CA-AEs during 3-mo exposure intervals and across all P exposure levels.,h4,Intervention,/h4,All 2267 patients received 5mg of P twice daily, and 1333/2267 received AA (1g) plus P.,h4,Results and limitations,/h4,The CA-AE incidence after any P exposure was 25%, 26%, and 23% for any ...
Testosterone Therapy Followed by Enzalutamide or Abiraterone Acetate in Treating Patients with Prostate Cancer That Is Progressing on Combined Androgen Therapies - NCT02090114
Growing evidence from clinical trials of the next-generation androgen receptor (AR) pathway inhibitors abiraterone acetate (AA) and MDV3100 suggests that both c...
Abiraterone acetate is a prodrug of abiraterone, a selective androgen biosynthesis inhibitor that blocks cytochrome P450 17A1 (CYP17A1) and suppresses androgen and estrogen synthesis (1, 2). Used in combination with prednisone, abiraterone acetate is now approved for use in men with metastatic castration-resistant prostate cancer (mCRPC) in both the pre- and post-chemotherapy-treated settings based on demonstrated survival benefit. A review of the outcomes in these populations shows that the response in individual patients ranged from prolonged and durable to none at all, suggesting the presence of molecular alterations in tumors that predict for response. This finding, coupled with the recent approval of several other effective treatments for mCRPC, has highlighted the urgent need for predictive biomarkers that enrich for patient subpopulations in which treatment has a significant effect on clinically meaningful benefits. These associations are best demonstrated in the setting of randomized ...
This page contains brief information about abiraterone acetate and a collection of links to more information about the use of this drug, research results, and ongoing clinical trials.
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Michalski J, Sartor O, Parker C, et al. Radium-223 dichloride (Ra-223) impact on skeletal-related events, external-beam radiotherapy (EBRT), and pain in patients with castration-resistant prostate cancer (CRPC) with bone metastases: Updated results from the phase III ALSYMPCA trial. Proceedings of the 55th Annual Meeting of the American Society of Radiation Oncology. International Journal of Radiation Oncology Biology Physics. 2013; 87(2): S108-S109. Abstract 265.. Smith MR, Saad F, Coleman R et al. Denosumab and bone-metastasis-free survival in men with castration-resistant prostate cancer: results of a phase 3, randomised, placebo-controlled trial. Lancet. Early online publication November 16, 2011.. Basch E, Autio K, Ryan CJ, et al: Abiraterone acetate plus prednisone versus prednisone alone in chemotherapy-naive men with metastatic castration-resistant prostate cancer: patient-reported outcome results of a randomised phase 3 trial. The Lancet Oncology. 2013; 14(12):1193-1199.. Beer TM, ...
Purpose: Abiraterone improves the overall survival of men with metastatic castration-resistant prostate cancer. However, de novo or adaptive resistance to abiraterone limits its activity. Rational combinations of drugs with different mechanisms of action that overcome resistance mechanisms may improve the efficacy of therapy. To that end, we studied the molecular and phenotypic effects of the combination of cabozantinib plus abiraterone.. Experimental Design: Three prostate cancer cell lines were used to interrogate the in vitro molecular and antiproliferative effects of the single agents and combination of cabozantinib and abiraterone. The in vivo impact of the combination was assessed using the LAPC4-CR xenograft mouse model.. Results: In vitro proliferation studies demonstrated single-agent doses between 2 μmol/L and 10 μmol/L for abiraterone and cabozantinib inhibit prostate cancer cell proliferation in a dose-dependent manner, and the anticancer activity of abiraterone is enhanced when ...
In a real-world setting, patients with metastatic castration-resistant prostate cancer who received radium-223 dichloride with abiraterone acetate in a layered fashion experienced a lower rate of symptomatic skeletal events compared with those who received the treatments concurrently.
The US Food and Drug Administration (FDA) today gave the green light for abiraterone acetate to be used in combination with prednisone for the treatment of castration-resistant prostate cancer in patients who have received prior docetaxel chemotherapy. Todays announcement marks the culmination of two decades of work at the ICR to design and develop this drug, ICR Chief Executive Professor Alan Ashworth says. This very significant achievement underlines the importance of drug discovery work in the not-for-profit sector. Abiraterone acetate was invented by Professor Mike Jarman and his colleagues in what is now the Cancer Research UK Cancer Therapeutics Unit at the ICR in Sutton, south of London. Prostate cancer cells need the male hormone testosterone to grow, so the team set out to design a drug that would cut off the source of testosterone. The ICR continued research on abiraterone acetate with The Royal Marsden Hospital after licensing the drug to Ortho Biotech Oncology Research & ...
The FDA announced the approval of Zytiga (abiraterone acetate), made by J&J subsidiary Janssen Biotech, for men with castration-resistant prostate cancer that has spread to other parts of the body, for use prior to receiving chemotherapy. The drug was already approved for castration-resistant prostate cancer in men who had already undergone chemotherapy treatment.. In castration-resistant prostate cancer, the cancer cells continue to grow even when men have undergone drug treatment or surgery to block testosterone, which stimulates the growth.. Todays approval demonstrates the benefit of further evaluation a drug in an earlier disease setting and provides patients and healthcare providers the option of using Zytiga earlier in the course of treatment, FDA Office of Oncology Drug Products director Richard Pazdur said.. ...
ORLANDO -- The investigational drug abiraterone acetate significantly improved outcomes in metastatic castrate-resistant prostate cancer in virtually every study-defined patient subgroup, researchers
Abiraterone acetate (INN, USAN, BAN, JAN) (brand names Zytiga, Abiratas, Abretone, Abirapro) is a steroidal antiandrogen, specifically an androgen synthesis inhibitor, used in combination with prednisone in metastatic castration-resistant prostate cancer (formerly hormone-resistant or hormone-refractory prostate cancer) - i.e., prostate cancer not responding to androgen deprivation or treatment with androgen receptor antagonists. It is a prodrug to the active agent abiraterone, and is marketed under the trade name Zytiga.. ...
Although one patient with recurrent ovarian cancer achieved complete response, the first trial of abiraterone conducted in ovarian cancer was halted early due to low response, according to results from the CORAL phase 2 trial.
Substantial evidence underscores the clinical efficacy of inhibiting CYP17A1-mediated androgen biosynthesis by abiraterone for treatment of prostate oncology. Previous structural analysis and in vitro assays revealed inconsistencies surrounding the nature and potency of CYP17A1 inhibition by abiraterone. Here, we establish that abiraterone is a slow-, tight-binding inhibitor of CYP17A1, with initial weak binding preceding the subsequent slow isomerization to a high-affinity CYP17A1-abiraterone complex. The in vitro inhibition constant of the final high-affinity CYP17A1-abiraterone complex ( ( Ki* = 0.39 nM )yielded a binding free energy of -12.8 kcal/mol that was quantitatively consistent with the in silico prediction of −14.5 kcal/mol. Prolonged suppression of dehydroepiandrosterone (DHEA) concentrations observed in VCaP cells after abiraterone washout corroborated its protracted CYP17A1 engagement. Molecular dynamics simulations illuminated potential structural determinants underlying the ...
TY - BOOK. T1 - Abiraterone for treating newly diagnosed metastatic hormone-naïve prostate cancer.. AU - Cummins, Ewen AU - Aucott, Lorna Sharman. AU - Robertson, Clare. AU - Fraser, Cynthia. AU - Johnston, Rhona. AU - Lam, Thomas. AU - Brazzelli, Miriam Giovanna. PY - 2018. Y1 - 2018. M3 - Commissioned Report. BT - Abiraterone for treating newly diagnosed metastatic hormone-naïve prostate cancer.. PB - Evidence Review Group report in support of NICE STA Programme. London: National Institute for Health and Care Excellence. ER - ...
Buy Zecyte 250 mg Abiraterone tablets from erectilewellness.com used to in men along with another drug called prednisone, Abiraterone tablets.
Twenty-seven pts have been enrolled, 17 were previously treated with ketoconazole. Median baseline PSA and testosterone levels are 24.6 ng/mL and 5.5 ng/dL, respectively. PK data is available from 6 pts at 250 mg (3 fasted, 3 fed), 9 at 500 mg (6 fasted, 3 fed), 6 at 750 mg (3 fasted, 3 fed) as well as in 6 pts at the 1000 mg dose (fasted only). No abiraterone acetate was detectable, suggesting complete conversion to abiraterone. Maximum drug concentration (Cmax) was achieved within 2.1 hours irrespective of dose or fed vs fasted state (p=0.213). At the 500 and 750 mg but not 250 mg doses a significant increase in Cmax and AUC (p=0.010) was observed in the fed pts (a 2-, 5-fold increase at 500mg and 750 mg respectively). The mean terminal t 1/2 was comparable in the fed and fasted groups at all doses (approximately 7-8 hours). Administration of abiraterone acetate with food resulted in lower interpatient variability (up to 2 fold vs 7 fold differences in Cmax and AUC) and a more linear ...
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TY - JOUR. T1 - Sequencing Treatment for Castration-Resistant Prostate Cancer. AU - Handy, Catherine E.. AU - Antonarakis, Emmanuel. PY - 2016/12/1. Y1 - 2016/12/1. N2 - Prostate cancer is the most common non-cutaneous cancer diagnosed in men and the second leading cause of male cancer deaths in the USA. While most cases are diagnosed in early stages, some will present as or progress to metastatic disease and eventually castration-resistant prostate cancer (mCRPC) which has a mortality rate exceeding 50 %. There are currently six approved systemic life-prolonging therapies for use in mCRPC, yet little data to guide sequencing. Clinical factors, including the presence or absence of symptoms and the presence or absence of visceral metastases, should help determine the best therapeutic choice at each treatment node. Those with asymptomatic bone-only disease could be considered for sipuleucel-T, abiraterone, enzalutamide, or docetaxel in the first-line setting. For symptomatic disease, docetaxel ...
Dr. Shore presented on the relationship between quality of live and overall survival in metastatic castrate-resistant prostate cancer patients with Radium-223 administration analyzed by prior docetaxel. Using the functional assessment of cancer therapy-prostate (FACT-P) they were able to create a time dependent model for change in health-related quality of life scores.
Abiraterone acetate United States Pharmacopeia (USP) Reference Standard; CAS Number: 154229-18-2; Synonym: 17-(Pyridin-3-yl)androsta-5,16-dien-3β-yl acetate; Linear Formula: C26H33NO2; find USP-1000818 MSDS, related peer-reviewed papers, technical documents, similar products & more at Sigma-Aldrich.
Docetaxel has been shown to improve survival in patients with metastatic castrate-resistant prostate cancer (mCRPC). There is no clear consensus regarding the optimum duration of chemotherapy. If patients at greater risk of rapid disease relapse could be identified when on chemotherapy, appropriate follow-up strategies could be put into place. The aim of our study was to find prostate specific antigen (PSA) characteristics that predict a shorter disease response to docetaxel chemotherapy. Data from 41 consecutive mCRPC patients treated with three-weekly docetaxel chemotherapy at a single centre between February 2010 and February 2012 were retrospectively analysed. All patients had ≥50 % reduction in their PSA with chemotherapy. The relationship between time to PSA nadir (TTN) and PSA halving time with time to PSA progression and overall chemotherapy response duration was analysed. TTN was a strong predictor of the duration of chemotherapy response and time to PSA progression. When TTN was ...
Paris (France) and Lund (Sweden), 3 October 2012 - Ipsen (Euronext: IPN; ADR: IPSEY) and Active Biotech (NASDAQ OMX NORDIC: ACTI) today announced the initiation of a new phase II proof of concept clinical trial, evaluating the activity of tasquinimod in advanced metastatic castrate resistant prostate cancer patients. The study aims at establishing the clinical efficacy of tasquinimod used as maintenance therapy in patients with metastatic castrate-resistant prostate cancer (mCRPC) who have not progressed after a first line docetaxel based chemotherapy. Karim Fizazi, Head of the Cancer Medicine Department of the Institut Gustave Roussy (IGR) in France and Principal investigator of the study said:In current clinical practice, metastatic castrate-resistant prostate cancer patients with non-progressive disease after docetaxel treatment are not proposed any medication as no reference/standard treatment exists. These patients remain untreated until disease progression. Prolongation of the response to ...
Characterization of genes linked to bone metastasis is critical for identification of novel prognostic or predictive biomarkers and potential therapeutic targets in metastatic castrate-resistant prostate cancer (mCRPC). Although bone marrow core biopsies (BMBx) can be obtained for gene profiling, the procedure itself is invasive and uncommon practice in mCRPC patients. Conversely, circulating tumor cells (CTCs), which are likely to stem from bone metastases, can be isolated from blood. The goals of this exploratory study were to establish a sensitive methodology to analyze gene expression in BMBx and CTCs, and to determine whether the presence or absence of detectable gene expression is concordant in matching samples from mCRPC patients. The CellSearch® platform was used to enrich and enumerate CTCs. Low numbers of PC3 prostate cancer (PCa) cells were spiked into normal blood to assess cell recovery rate. RNA extracted from recovered PC3 cells was amplified using an Eberwine-based procedure to obtain
Kim N. Chi, MD, of BC Cancer, discusses updated results from a phase II study of cabazitaxel vs abiraterone or enzalutamide in patients with poor-prognosis metastatic castration-resistant prostate cancer (Abstract 5003).. ...
References. 1. Heidenreich A, Bastian PJ, Bellmunt J, Bolla M, Joniau S, van der Kwast T, et al. EAU Guidelines on Prostate Cancer. Part II: Treatment of Advanced, Relapsing, and Castration- Resistant Prostate Cancer. Eur Urol. 2014;65:467-79.. 2. Cookson MS, Roth BJ, Dahm P, Engstrom C, Freedland SJ, Hussain M, et al. Castration-resistant prostate cancer: AUA guideline. 2013.. 3. NCCN. NCCN Clinical Practice Guidelines in Oncology. Prostate Cancer. 2014.. 4. Fizazi K, Scher HI, Molina A, Logothetis CJ, Chi KN, Jones RJ, et al. Abiraterone acetate for treatment of metastatic castration-resistant prostate cancer: final overall survival analysis of the COU-AA-301 randomised, double-blind, placebo-controlled phase 3 study. Lancet Oncol. 2012;13:983-92.. 5. Ryan CJ, Smith MR, de Bono JS, Molina A, Logothetis CJ, de Souza P, et al. Abiraterone in metastatic prostate cancer without previous chemotherapy. N Engl J Med. 2013;368:138-48.. 6. Scher HI, Fizazi K, Saad F, Taplin ME, Sternberg CN, Miller K, ...
Excerpt:. In the phase III CA184-095trial reported in the Journal of Clinical Oncology, Tomasz M. Beer, MD, FACP, of the Knight Cancer Institute, Oregon Health and Science University, and colleagues found that ipilimumab (Yervoy) did not increase overall survival vs placebo in men with asymptomatic or minimally symptomatic chemotherapy-naive metastatic castration-resistant prostate cancer without visceral metastases. Ipilimumab was associated with prolonged progression-free survival and a higher prostate-specific antigen (PSA) response rate.. Go to full article.. If youre wondering whether this story applies to your own cancer case or a loved ones, we invite you to use our ASK Cancer Commons service.. ...
Novel genomic alterations in circulating tumor cells, beyond the androgen receptor V7 splice variant, are associated with outcomes and resistance to hormone therapy in metastatic castrate-resistant prostate cancer, researchers suggest.
1 http://www.auanet.org/education/guidelines/prostate-cancer.cfm. 2 Basch E, Autio K, Ryan CJ, et al: Abiraterone acetate plus prednisone versus prednisone alone in chemotherapy-naive men with metastatic castration-resistant prostate cancer: patient-reported outcome results of a randomised phase 3 trial. The Lancet Oncology. 2013; 14(12):1193-1199.. 3 Beer TM, Armstrong AJ, Sternberg CN, et al: Enzalutamide in men with chemotherapy-naive metastatic prostate cancer (mCRPC): Results of phase III PREVAIL study. Presented at the 2014 Genitourinary Cancers Symposium. Journal of Clinical Oncology. 2014; 32 (supplement 4; abstract LBA1).. 4 Nelson J, Banato A, Battistini B, Nisen P. The endothelin axis: emerging role in cancer. Nat Rev Cancer2003;3(2):110-116.. 5 Scher HI, Fizazi K, Saad F et al: Increased survival with enzalutamide in prostate cancer after chemotherapy. N Eng J Med 2012; 367: 1187.. 6 de Bono JS, Logothetis CJ, Molina A et al: Abiraterone and increased survival in metastatic prostate ...
Bayer HealthCare and Orion Corporation, a pharmaceutical company based in Espoo, Finland, have begun to enroll patients in a Phase III trial with ODM-201, an investigational novel oral androgen receptor (AR) inhibitor in clinical development for the treatment of patients with prostate cancer. The study, called ARAMIS, evaluates ODM-201 in men with castration-resistant prostate cancer […]. ...
TY - JOUR. T1 - Re. T2 - Docetaxel and atrasentan versus docetaxel and placebo for men with advanced castration-resistant prostate cancer (SWOG S0421): A randomised phase 3 trial. AU - Taneja, Samir S.. PY - 2014. Y1 - 2014. UR - http://www.scopus.com/inward/record.url?scp=84899456266&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=84899456266&partnerID=8YFLogxK. U2 - 10.1016/j.juro.2013.11.085. DO - 10.1016/j.juro.2013.11.085. M3 - Comment/debate. C2 - 24522033. AN - SCOPUS:84899456266. VL - 191. SP - 656. EP - 658. JO - Journal of Urology. JF - Journal of Urology. SN - 0022-5347. IS - 3. ER - ...
The Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) has recommended darolutamide, an androgen receptor inhibitor (ARi), for marketing authorization in the European Union (EU).. The compound, which is developed jointly by Orion Corporation and Bayer, is recommended for the treatment of men with non-metastatic castration-resistant prostate cancer (nmCRPC), who are at high risk of developing metastatic disease. The final decision of the European Commission on the marketing authorisation is expected in the coming months. The androgen receptor inhibitor (ARi) is already approved in the in the U.S., Brazil and Japan and filings in other regions are underway or planned by Bayer.. Bayer is responsible for global commercialization of darolutamide, with a co-promotion of Bayer and Orion in certain European markets, e.g. in France, Germany, Italy, Spain, the UK, Scandinavia and Finland.. The CHMP recommendation is based on the results of the Phase III ARAMIS ...
TY - JOUR. T1 - EPI-001, A Compound Active against Castration-Resistant Prostate Cancer, Targets Transactivation Unit 5 of the Androgen Receptor. AU - Moll, Eva De. AU - Fenwick, R. Bryn. AU - Phang, Christopher T.W.. AU - Buzon, Victor. AU - Szulc, Elzbieta. AU - De La Fuente, Alex. AU - Escobedo, Albert. AU - Garcia, Jesus. AU - Bertoncini, Carlos W.. AU - Estebanez-Perpina, Eva AU - McEwan, Iain J.. AU - Riera, Antoni. AU - Salvatella, Xavier N1 - ACKNOWLEDGEMENTS We thank J. M. Valverde (IRB) as well as the NMR facilities of the University of Barcelona (CCiT UB) and the Instituto de Química Física Rocasolano (IQFR, CSIC) for their assistance in, respectively, protein production and NMR. This work was supported by IRB, ICREA (X.S.), Obra Social la Caixa (Fellowship to E.D.M. and CancerTec grants to X.S.) MICINN (CTQ2009-08850 to X.S.), MINECO (BIO2012-31043 to X.S.; CTQ2014-56361-P to A.R), Marató de TV3 (102030 to X.S. and 102031 to E.E.P) the COFUND programme of the European Commission ...
On February 14, 2018, the Food and Drug Administration approved apalutamide (Erleada™, Janssen Biotech, Inc.) for patients with non-metastatic castration-resistant prostate cancer (NM-CRPC).
by NewsRx editors, research stated, Prostate-specific membrane antigen (PSMA) is a promising target for the diagnosis of and therapy for metastatic castration-resistant prostate cancer (mCRPC). The aim of this study was to measure overall-survival (OS) in mCRPC patients who received either abiraterone or enzalutamide prior to PSMA therapy.. Our news journalists obtained a quote from the research from University Hospital Bonn, The second aim of this study was to analyse the predictors of OS according to different pre-therapeutic parameters and also the responses to the first cycle of radioligand therapy (RLT) base on PSA level. Patients with mCRPC and a history of therapy with either abiraterone or enzalutamide or both, were included in this study. Different laboratory tests and pre-therapeutic parameters have been included into the analysis. One-hundred patients received a total of 347 cycles of Lu-PSMA (median: three cycles). 69 patients showed a decline in PSA two months after the first ...
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b) In patients who did not receive Flutamide, add it.. c) Prednisone 40mg / day p.o. may relieve pain.. e) Ketokenazol is administered in doses of 200mg x 3 / day. It is associated with nausea, vomiting, liver injury.. f) Abiraterone acetate 1000 mg / daily and prednisone 10 mg / day. Abiraterone acetate is an androgen synthesis inhibitor autocrine and / or paracrine through inhibition of cytochrome P 450. It is used in patients with recurrent prostate cancer after docetaxel treatment ineffective.. F). diethylstilbestrol or some other estrogen (Chlorotrianisene). The funds available are orchiectomy, LHRH agonists (luteinizing hormone releasing hormone) and androgens.. Androgen deprivation therapy (TDA) for localized disease. Overview. Previous neoadjuvant ADT radical prostatectomy is not recommended.. TDA concomitantly administered before or after radiotherapy prolongs survival in selected patients treated with radiotherapy.. All studies of neoadjuvant ADT short term (4-6 months) or long term ...
The second-generation androgen receptor antagonist enzalutamide (XTANDI) significantly improved survival and delayed the time to chemotherapy in men with previously untreated metastatic castrate-resistant prostate cancer, according to a recent study.
This press release contains forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995. These statements are often, but not always, made through the use of words or phrases such as anticipates, expects, plans, believes, intends, and similar words or phrases. These forward-looking statements include, without limitation, statements related to the benefits to be derived from Cougars drug development programs, including the potential advantages of CB7630 and its potential for use in the treatment of CRPC and in second-line hormone and chemotherapy treatment settings. Such statements involve risks and uncertainties that could cause Cougars actual results to differ materially from the anticipated results and expectations expressed in these forward-looking statements. These statements are only predictions based on current information and expectations and involve a number of risks and uncertainties. Actual events or results may differ materially ...
Alpha Androstenol - The Conversation Grease Pheromone Technical information Common name/s: Anol, Alpha-nol Most common chemical name: 5α-Androst-16-en-3α-ol Molecular Weight: 274.44 g/mol CAS Number: 1153-51-1 Known effects from testing and reports Women consistently rated men higher on the attractiveness scale, when exposed to alpha androstenol (a scientific study). However, men were also reported…
PSA progression defined by a minimum of two rising PSA levels with an interval of ≥ 1 week between each determination. Patients who received an anti-androgen must have progression documented by a minimum of two rising PSA levels with an interval of ≥ 1 week between each determination such that at least the second of these rises is ≥ 4 weeks since last flutamide, bicalutamide or nilutamide.. The PSA value at the screening should be ≥ 2 µg/L (2 ng/mL) .. ...
Median overall survival was 73.9 months in the apalutamide group vs 59.9 months in the placebo group (HR = 0.78, 95% confidence interval [CI] = 0.64-0.96, P = 0.016). Hazard ratios favored apalutamide in virtually all subgroups analyzed.. Apalutamide was associated with significant prolongation of time to first cytotoxic chemotherapy (median not reached in either group; HR = 0.63, 95% CI = 0.49-0.81, P = 0.0002).. Median progression-free survival-2 was 55.6 months vs 41.2 months (HR = 0.55, 95% CI = 0.46-0.66, nominal P , .0001). Updated analysis confirmed the benefit of apalutamide in reducing risk of symptomatic progression (median not reached in either group; HR = 0.57, 95% CI = 0.44-0.73, nominal P , .0001). Median times to PSA progression were 40.5 months vs 3.7 months (HR = 0.07, 95% CI = 0.06-0.09], nominal P , .0001).. Safety. Safety was consistent with previous reports. The incidence of adverse events of any grade were 97% in the apalutamide group, 94% in the placebo group, and 90% in ...
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Radium-223 - inwendige bestraling - samen met andere behandelingen als abiraterone of enzalutamine geeft langere overall overleving en minder pijn en betere kwaliteit van leven dan alleen Radium-223 of alleen andere behandelingen bij hormoon resistente vergevorderde prostaatkanker. Xofigo blijkt toch niet zo veilig en veroorzaakt botbreuken en vroegtijdig overlijden. Artikel update 23 januari 2020
Androstenol -- There are two types of this compound, the alpha and beta isomers, each producing slightly different effects. The alpha and beta have nothing to do with the pheromone projecting an alpha aura. Both seem to cause chattiness and friendliness. It is also known to increase sexual appeal making it great for breaking the ice. The alpha isomer produces a friendly atmosphere which makes the user more approachable for women. Androstenol also creates an aura of youth and health, which can help to create a youthful perception for older people.Androstenol also creates a feeling of youthfullness and health which can be a sexual turn on for women. The primary reported response to Androstenol or Androstenol containing products has been an increase in chattiness and friendliness from both sexes, but as mentioned above it can increase sexual attractiveness as well. It has been referred to as an ice-breaker pheromone. If you find anything extra mentioning about Pheromones, do inform us. It is ...
Clinical trial for mCRPC | mCRPC With DNA Damage Repair Deficiencies (DDR) | DDR+ mCRPC , Talazoparib + Enzalutamide vs. Enzalutamide Monotherapy in mCRPC
https://doi.org/10.18632/oncotarget.16463 Francesco Morra, Francesco Merolla, Virginia Napolitano, Gennaro Ilardi, Caterina Miro, Simona Paladino, Stefania Staibano, Aniello Cerrato, Angela Celetti
Reyaz Ur Rasool, Ramakrishnan Natesan, Qu Deng, Shweta Aras, Priti Lal, Samuel Sander Effron, Erick Mitchell-Velasquez, Jessica M Posimo, Shannon Carskadon, Sylvan C Baca, Mark M Pomerantz, Javed Siddiqui, Lauren E Schwartz, Daniel J Lee, Nallasivam Palanisamy, Goutham Narla, Robert B Den, Matthew L Freedman, Donita C. Brady and Irfan A Asangani ...
H&O How common is resistance to abiraterone and enzalutamide in castration-resistant prostate cancer (CRPC)? ESA Approximately 15% to 25% of patients with CRPC do not respond to […]. ...
in 1990 indicating that essential mating pheromones, including androstenols, required activation by skin-associated microbial ...
... androstenols MeSH D04.808.054.079.429.154 - androstenediols MeSH D04.808.054.079.429.154.050 - androstenediol MeSH D04.808. ...
"Androstenols" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH (Medical Subject ... This graph shows the total number of publications written about "Androstenols" by people in Harvard Catalyst Profiles by year, ... Below are the most recent publications written about "Androstenols" by people in Profiles. ... and whether "Androstenols" was a major or minor topic of these publication. ...
Androstenols. *BCRP/ABCG2 Substrates. *Cytochrome P-450 CYP2B6 Substrates. *Cytochrome P-450 CYP2C19 Substrates ...
Categories: Androstenols Image Types: Photo, Illustrations, Video, Color, Black&White, PublicDomain, CopyrightRestricted 1 ...
Androstenols [D04.808.054.079.429]. *Androstenediols [D04.808.054.079.429.154]. *Fluoxymesterone [D04.808.054.079.429.154.349] ...
5[alpha]- and 5[beta]-androstenols also contribute to sex odor. Subsequently, 5[alpha]-androstenone, 5[alpha]-, and 5[beta]- ... androstenols were found in the testes,17,18 fat,4,19,20 submaxillary gland and saliva,14,18 and parotid gland21 of boars. ... androstenols.14 When a mature boar is aroused by the presence of an estrous female or an unfamiliar boar, he champs copious ...
6668 Background: HE2100, androst-5-ene-3β,17β-diol, and HE3204 are naturally occurring and synthetic adrenal steroid hormones… (More) ...
in 1990 indicating that essential mating pheromones, including androstenols, required activation by skin-associated microbial ...
But, Androstenols do break down into Androstenone on human skin. So, pig pheromone or not it, is found in humans and if it ... But, Androstenols do break down into Androstenone on human skin. So, pig pheromone or not it, is found in humans and if it ...
Klootwijk, E. D., Reichold, M., Helip-Wooley, A., Tolaymat, A., Broeker, C., Robinette, S. L., Reinders, J., Peindl, D., Renner, K., Eberhart, K., Assmann, N., Oefner, P. J., Dettmer, K., Sterner, C., Schroeder, J., Zorger, N., Witzgall, R., Reinhold, S. W., Stanescu, H. C., Bockenhauer, D. & 19 others, Jaureguiberry, G., Courtneidge, H., Hall, A. M., Wijeyesekera, A. D., Holmes, E., Nicholson, J. K., OBrien, K., Bernardini, I., Krasnewich, D. M., Arcos-Burgos, M., Izumi, Y., Nonoguchi, H., Jia, Y., Reddy, J. K., Ilyas, M., Unwin, R. J., Gahl, W. A., Warth, R. & Kleta, R., Jan 1 2014, In : New England Journal of Medicine. 370, 2, p. 129-138 10 p.. Research output: Contribution to journal › Article ...
... androstenols MeSH D04.808.054.079.429.154 - androstenediols MeSH D04.808.054.079.429.154.050 - androstenediol MeSH D04.808. ...
TY - JOUR. T1 - Induction of nuclear translocation of constitutive androstane receptor by peroxisome proliferator-activated receptor α synthetic ligands in mouse liver. AU - Guo, Dongsheng. AU - Sarkar, Joy. AU - Suino-Powell, Kelly. AU - Xu, Yong. AU - Matsumoto, Kojiro. AU - Jia, Yuzhi. AU - Yu, Songtao. AU - Khare, Sonal. AU - Haldar, Kasturi. AU - Musunuri, Sambasiva Rao. AU - Foreman, Jennifer E.. AU - Monga, Satdarshan P.S.. AU - Peters, Jeffrey M.. AU - Xu, H. Eric. AU - Reddy, Janardan K. PY - 2007/12/14. Y1 - 2007/12/14. N2 - Peroxisome proliferators activate nuclear receptor peroxisome proliferator-activated receptor α (PPARα) and enhance the transcription of several genes in liver. We report here that synthetic PPARα ligands Wy-14,643, ciprofibrate, clofibrate, and others induce the nuclear translocation of constitutive androstane receptor (CAR) in mouse liver cells in vivo. Adenoviral-enhanced green fluorescent protein-CAR expression demonstrated that PPARα synthetic ligands ...
Androstenols/therapeutic use*. *Antineoplastic Combined Chemotherapy Protocols/adverse effects. *Antineoplastic Combined ...
Androstenols. *abiraterone. Grant support. *G0501019/Medical Research Council/United Kingdom. *Cancer Research UK/United ...
Class Androstenols; Hormonal replacements; Small molecules; Testosterone congeners * Mechanism of Action Protein synthesis ...
Androstenols .. Hydroxyandrostenes .. Unsaturated androstanes which are substituted with one or more hydroxyl groups in any ... D04.210.500.054.079.429 Androstenols .. D04.210.500.054.079.429.625 Dehydroepiandrosterone .. D04.210.500.365 Estranes .. ...
D04.210.500.054.079.429 Androstenols .. D04.210.500.054.079.429.824 Testosterone .. D04.210.500.054.079.429.824.664 ...
Androstenols. *Cytochrome P-450 CYP3A Substrates. *Cytochrome P-450 CYP3A4 Substrates. *Cytochrome P-450 CYP3A4 Substrates ( ...
androstenols*ketocholesterols*hymecromone*lactobacillus rhamnosus*hydroxycholesterols*relaxin*anisoles*hepatocyte nuclear ...
Androstenols. *BCRP/ABCG2 Substrates. *Cytochrome P-450 CYP2B6 Inducers. *Cytochrome P-450 CYP2B6 Substrates ...
16-hydroxydehydroepiandrosterone sulfate: RN given refers to cpd with unspecified sulfate ester linkage locant & (3 beta,16 beta)-isomer
Human semen was examined for the presence of 16-androstenols, 16-androstenones and androgens. Extracts were analysed by gas ... The axillary skin levels of 3 alpha- and 3 beta-androstenols, androstadienol and, in 3 subjects, androstadienone exceeded those ... androstenols] were only found in small amounts (, 0.1 nmol/microliters) in a few subjects. In the second study, prior to ...
Garcìa-Regueiro JA, Diaz I. Evaluation of the Contribution of Skatole, Indole, Androstenone and Androstenols to Boar-Taint in ...
Studies by Froebe et al.[12] in 1990 indicating that essential mating pheromones, including androstenols, required activation ...
The much celebrated combination of Beta and Alpha Androstenols, which purportedly encourages approach-ability, chattiness, and ... The much celebrated combination of Beta and Alpha Androstenols, which purportedly encourages approach-ability, chattiness, and ...
TRUE CONFESSIONS - (unisex) - The much celebrated combination of Beta and Alpha Androstenols, which purportedly encourage ...
TRUE CONFESSIONS - (unisex) The much celebrated combination of Beta and Alpha Androstenols, which purportedly encourage ...
Journal Article 2009; 30(3): 368-372 PubMed PMID: 19855361 Keywords: Adult, Androstenols:blood, Dehydroepiandrosterone:analogs ...
García-Regueiro JA, Diaz I: Evaluation of the Contribution of Skatole, Indole, Androstenone and Androstenols to Boar-Taint in ...
... the much celebrated combination of Beta and Alpha Androstenols, which purportedly encourages approach-ability, chattiness, and ...
  • The much celebrated combination of Beta and Alpha Androstenols, which purportedly encourages approach-ability, chattiness, and deeply intimate communication. (luvpotionperfume.com)
  • To aid in crucial conversations we've included a dose of our exclusive TRUE CONFESSIONS pheromone formula, the much celebrated combination of Beta and Alpha Androstenols, which purportedly encourages approach-ability, chattiness, and deeply intimate communication. (luvpotionperfume.com)
  • This graph shows the total number of publications written about "Androstenols" by people in Harvard Catalyst Profiles by year, and whether "Androstenols" was a major or minor topic of these publication. (harvard.edu)