Cetrorelix (INN, BAN), or cetrorelix acetate (USAN, JAN), sold under the brand name Cetrotide, is an injectable gonadotropin-releasing hormone (GnRH) antagonist. A synthetic decapeptide, it is used is used in assisted reproduction to inhibit premature luteinizing hormone surges The drug works by blocking the action of GnRH upon the pituitary, thus rapidly suppressing the production and action of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). In addition, cetrorelix can be used to treat hormone-sensitive cancers of the prostate[citation needed] and breast (in pre-/perimenopausal women)[citation needed] and some benign gynaecological disorders (endometriosis, uterine fibroids and endometrial thinning).[citation needed] It is administered as either multiple 0.25 mg daily subcutaneous injections or as a single-dose 3 mg subcutaneous injection. The duration of the 3 mg single dose is four days; if human chorionic gonadotropin (hCG) is not administered within four days, a daily 0.25 ...
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Professional guide for Cetrorelix. Includes: pharmacology, pharmacokinetics, contraindications, interactions, adverse reactions and more.
Ganirelix Acetate Organon is a medicine available in a number of countries worldwide. A list of US medications equivalent to Ganirelix Acetate Organon is available on the Drugs.com website.
Gonadotropin-releasing hormone antagonists (GnRH antagonists) are a class of medications that antagonize the gonadotropin-releasing hormone receptor (GnRH receptor) and thus the action of gonadotropin-releasing hormone (GnRH). Some are similar in structure to natural GnRH (a hormone made by neurons in the hypothalamus) but that have an antagonistic effect. These GnRH antagonists are peptide molecules that are made up multiple, often synthetically produced amino acids. Others are small-molecule, non-peptide compounds. GnRH antagonists compete with natural GnRH for binding to GnRH receptors, thus decreasing or blocking GnRH action in the body. Testosterone promotes growth of many prostate tumors and therefore reducing circulating testosterone to very low (castration) levels is often the treatment goal in the management of men with advanced prostate cancer. GnRH antagonists are used to provide fast suppression of testosterone without the surge in testosterone levels that is seen when treating ...
RU-486 is an abortifacient which is used to terminate early pregnancy. It acts by blocking progesterone receptor. In our earlier study with progesterone, RU-486 was used as a progesterone receptor antagonist to find out the mechanism of progesterone action on melanoma cells. Results indicated that the effect of progesterone was not mediated through progesterone receptor. In the course of experiments, it was observed that RU-486 by itself inhibited mouse melanoma cell growth. Further research work with RU-486 showed a dose dependent inhibition of human melanoma cell growth. The mechanism of inhibition of cell growth was due to apoptosis and this effect of RU-486 was neither mediated through progesterone receptor nor glucocorticoid receptor. This in-vitro study suggested that melanoma also could be a target for RU-486 action, apart from breast, ovary and prostate cancers.
RU-486 is an abortifacient which is used to terminate early pregnancy. It acts by blocking progesterone receptor. In our earlier study with progesterone, RU-486 was used as a progesterone receptor antagonist to find out the mechanism of progesterone action on melanoma cells. Results indicated that the effect of progesterone was not mediated through progesterone receptor. In the course of experiments, it was observed that RU-486 by itself inhibited mouse melanoma cell growth. Further research work with RU-486 showed a dose dependent inhibition of human melanoma cell growth. The mechanism of inhibition of cell growth was due to apoptosis and this effect of RU-486 was neither mediated through progesterone receptor nor glucocorticoid receptor. This in-vitro study suggested that melanoma also could be a target for RU-486 action, apart from breast, ovary and prostate cancers.
Background The differential efficacy between long GnRH agonist with antagonist can partly be due to the preexisting differences in the early antral follicles before ovarian stimulation.Objective To compare the effect of pretreatment by estradiol with GnRH antagonist on antral follicular size coordination and basal hormone levels in GNRH antagonist protocol. Materials And Methods On cycle day 3 (control/day 3), women underwent measurements of early antral follicles by ultrasound and serum FSH and ovarian hormones then were randomized to receive oral estradiol 4mg/day (n=15) or 3mg cetrorelix acetate (n=15) in luteal phase before subsequent antagonist protocol. Participants were re-evaluated as on control/day 3. Results There was a significant reduction of mean follicular sizes in each group after medical intervention (7.63±2.11 Vs. 4.30±0.92 in group A and 8.73±1.96 Vs. 4.13±1.11 in group B) (p=0.0001). The magnitude of follicular size reduction was significantly higher in group B (-4.60±2.04 Vs. -3
Ovarian reserve is related to chronological age; 35 years of age is the accepted threshold for significant decline in assisted reproductive technologies (ART) success with scarce follicular recruitment and poor oocyte retrieval. New therapeutic schemes are sought to improve follicular response in ovarian ageing because of the increasing number of infertile women aged older than 35 years who are trying to get pregnant. The advent of gonadotropin releasing hormone analogue antagonist (GnRHant) offers new perspectives to address the issues related to advanced reproductive age since it prevents premature luteinizing hormone (LH) surges while not causing suppression in the early follicular phase. Gonadotropin releasing hormone analogue antagonists are administered in the latter stage of the ovarian stimulation to prevent LH surge by competitive blockade of gonadotropin releasing hormone (GnRH) receptors, thus producing a marked decrease in LH levels just when the interplay between follicle ...
Cetrorelix is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity. GnRH induces the production and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH) from the gonadotrophic cells of the anterior pituitary. Due to a positive estradiol (E2) feedback at midcycle, GnRH liberation is enhanced resulting in an LH-surge. This LH-surge induces the ovulation of the dominant follicle, resumption of oocyte meiosis and subsequently luteinization as indicated by rising progesterone levels. Cetrorelix competes with natural GnRH for binding to membrane receptors on pituitary cells and thus controls the release of LH and FSH in a dose-dependent manner ...
Cetrorelix showed good safety and tolerability profile Reduction ofte...QUEBEC CITY March 22 2007 /PRNewswire-FirstCall/ - AEternaZentaris ...On the basis of this study Shionogi initiated a 300-patientphase 2b ... We are very pleased with these results which further confirmthe posi...Nippon Kayaku the Companys other Japanese partner hasterminated it...,AEterna,Zentaris,Reports,Positive,Results,with,Cetrorelix,in,BPH,for,Japanese,Phase,2a,Trial,medicine,advanced medical technology,medical laboratory technology,medical device technology,latest medical technology,Health
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Peptides are provided which have improved duration of GnRH antagonistic properties and/or which can be synthesized more economically. These antagonists may be used in the same manner as the compounds of which they are analogs to regulate fertility and to treat steroid-dependent tumors and for other short-term and long-term treatment indications. One particularly effective peptide, a decapeptide analog of the GnRH antagonist Acyline, has the formula: Ac-D-2Nal-D-4Cpa-D-Dpr(methylcarbamoyl)-Ser-4Aph(acetyl)-D-4Aph(acetyl)-Leu-Lys(isopropyl)-Pro-D-Ala-NH2. It continues to exhibit very substantial suppression of LH secretion at 96 hours following injection. Other economically attractive and pharmacologically effective analogs have the formulas: Ac-D-2Nal-D-4Cpa-Xaa3 -Ser-4Aph(acetyl)-D-4Aph(acetyl)-Leu-Lys(isopropyl)-Pro-D-Ala-NH2 ; and Ac-D-2Nal-D-4Cpa-Xaa3 -Ser-4Aph(hydroorotyl)-D-4Aph(acetyl)-Leu-Lys(isopropyl)-Pro-D-Ala-NH.sub.2, wherein Xaa3 is D-Gln or Gln.
Buy Mifepristone (RU486) (CAS 84371-65-3), a PR and GR antagonist. Join researchers using high quality Mifepristone (RU486) from Abcam and achieve your…
Cetrotide (cetrorelix acetate) is used to prevent premature ovulation during controlled ovarian stimulation. It blocks the hormone (gonadotropin-releasing hormone-GnRH) that causes eggs to be released from the ovaries.
Structure and Composition Mode of action Pharmacokinetics Indications Contraindications Side effects Dosage and administration precautions Storage conditions Shelf life ATX G03BA03 Testosterone Pharmacological groups Androgens, anti-androgens Antitumor hormonal and hormone antagonists Nosological classification (ICD-10) E25 adrenal disorders E29 testicular dysfunction 2 Lack of genital response Unspecified M81.9 Osteoporosis N50 Other disorders of male genital organs ...
We tested the hypothesis that daily gavage with mifepristone, a mixed progesterone/glucocorticoid receptor antagonist would alter hypoxic ventilatory response (HVR) in newborn male and female rats....
Background: This retrospective study evaluated the effect of profound pituitary suppression with oral contraceptive pill (OCP) pretreatment in gonadotropin-releasing horm..
Mifepristone is a synthetic steroid compound used as a pharmaceutical. It is a progesterone receptor antagonist used as an abortifacient in the first months of pregnancy, and in smaller doses as an emergency contraceptive. Mifepristone is also a powerful glucocorticoid receptor antagonist, and has occasionally been used in refractory Cushings Syndrome (due to ectopic/neoplastic ACTH/Cortisol secretion). During early trials, it was known as RU-38486 or simply RU-486, its designation at the Roussel Uclaf company, which designed the drug. The drug was initially made available in France, and other countries then followed-often amid controversy. It is marketed under tradenames Mifegyne, Zacafemyl and Mifeprex. ...
Prostate cancer is the most common cancer in males, and the second leading cause of cancer deaths in American men. Most of the mortality associated with this disease is a result of widespread dissemination of tumors cells from the primary tumor mass. In order for metastasis to occur, the cancer cell must overcome multiple barrier which include development, neovascularization, intravastion, adherence or attachment, extravasation, and ectopic growth. As dissemination from the primary tumor mass is a rate-limiting step during metastasis, tumor cells undergo an epithelial to mesenchymal transition (EMT) to acquire enhanced invasiveness and increased motility. A key step within EMT is a loss of cadherin mediated cell-cell adhesion. Unfortunately, current understanding of the regulatory mechanism of this decreased cell-cell adhesion is poorly understood. Herein this work utilizes the LHRH antagonist Cetrorelix to investigate the regulation of E-cadherin expression in invasive prostate cancer cells. We ...
Antagonist Protocol Definition - An antagonist protocol is a process used during in vitro fertilization (IVF) to prevent premature ovulation. It uses...
MIFEPRISTONE: Review the definition, meaning, pronunciation, explanation, synonyms, and antonyms of the term MIFEPRISTONE in the Online Dictionary. What is a 12 letter word that starts with M?
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... Systematic (IUPAC) name 11β-[p-(Dimethylamino)phenyl]-17β-hydroxy-17-(1-propynyl)estra-4,9-dien-3-one Identifiers CAS number
17 beta-hydroxy-7 alpha-methyl-5-estren-3-one: RN given refers to (7alpha,17beta)-isomer; structure given in first source; progestational hormone antagonist
This eMedTV page explains when side effects of mifepristone could be potentially serious and require immediate medical treatment. This article also describes the results of extensive clinical trials that have shown how often reactions to this drug occur.
Learn about Korlym (Mifepristone) may treat, uses, dosage, side effects, drug interactions, warnings, patient labeling, reviews, and related medications.
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ANTIDE (02.11.1999) - Free trademark register information. Search, file and monitor trademarks in Germany, Europe and International.
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Relugolix is a novel, non-peptide, orally active gonadotropin-releasing hormone (GnRH) antagonist with IC50 of 0.33 nM in the presence of 40% fetal bovine serum, TAK-385 possesses higher affinity and potent antagonistic activity compared with TAK-013. - Mechanism of Action & Protocol.
RU-486: RU-486, first trade name for mifepristone, a synthetic steroid drug prescribed for inducing abortion during the early weeks of pregnancy. The name is derived from an
No effective hormonal contraceptive has yet been devised for men. Through their suppressive effect on gonadotropin secretion, GnRH antagonists inhibit both testosterone (T) production and spermatogenesis in animals. Long term administration of an antagonist alone would result in androgen deficiency; this would cause unacceptable physiological and behavioral sequellae in men. Therefore, androgen replacement must be included in any GnRH antagonist regimen used in human male contraception. We tested the hypothesis that the combination of a GnRH antagonist plus T would suppress spermatogenesis in the male primate to azoospermic levels while maintaining normal serum T levels. We examined the effects of the GnRH antagonist Deterelix [N-Ac-DNal(2)1-DpCl-Phe2-DTrp3-DhArg(Et2)6 -DAla10-GnRH], alone and with simultaneous T replacement, on sperm production and serum T levels in adult male monkeys (n = 22). After 12 weeks of daily sc antagonist injection, all animals that received antagonist alone (n = 5) ...
Testosterone promotes growth of many prostate tumors and therefore reducing circulating testosterone to very low (castration) levels is often the treatment goal in the management of men with advanced prostate cancer. GnRH antagonists are used to provide fast suppression of testosterone without the surge in testosterone levels that is seen when treating patients with GnRH agonists.[1] In patients with advanced disease, this surge in testosterone can lead to a flare-up of the tumour, which can precipitate a range of clinical symptoms such as bone pain, urethral obstruction, and spinal cord compression. Drug agencies have issued warnings regarding this phenomenon in the prescribing information for GnRH agonists. As testosterone surge does not occur with GnRH antagonists, there is no need for patients to receive an antiandrogen as flare protection during prostate cancer treatment. GnRH agonists also induce an increase in testosterone levels after each reinjection of the drug - a phenomenon that does ...
Looking for online definition of antiprogestin in the Medical Dictionary? antiprogestin explanation free. What is antiprogestin? Meaning of antiprogestin medical term. What does antiprogestin mean?
The aim of this study is to assess the oocyte yield of infertile women with suspected or known poor ovarian reserve (POR) undergoing a GnRH antagonist protocol for IVF with Merional® starting either with a low (150 IU) or a high dose (450 IU) and adding 100mg of CC (Serophene®) in the early follicular phase of the stimulation (day 3 to 7). To date no RCT has been conducted to compare the reproductive outcome of patients with POR as defined by the ESHRE Bologna criteria after controlled ovarian hyperstimulation with HMG in an GnRH antagonist protocol using low doses versus high doses of HMG and adding CC versus placebo. We hypothesize that adding 100 mg of CC on day 3-7 to a HMG antagonist protocol will lead to an additional increment of endogenous GT thus increasing the oocytes yield after controlled ovarian stimulation due to higher endogenous gonadotropin secretion ...
In addition to its lack of efficacy, it is concerning that the hCG dosage administered to obese patients is sufficiently high to cause certain physiological responses, and the quality of hCG used by many obesity clinics is unknown. A typical dosage used for weight loss programs is the daily dosage of 150 IU for six times per week or weekly dosage of 1000 IU. In a clinical trial of oocyte production, a daily dose of 200 IU has been successfully used for maintaining late follicular phase as a gonadotropin-releasing hormone antagonist.5 The likelihood that hCG administered for weight loss is having reproductive effects is further suggested by the finding of luteinizing hormone/hCG receptors on various tissues.6, 7 Preliminary studies showed that hCG facilitated decidualization of stromal cells of human endometrium,8 which raises concern of possible leiomyoma formation and exacerbation of endometriosis. For males, animal prostate cells expressed HCG receptor gene upon stimulation, and the authors ...
Cisplatin and its derivatives are important drugs in cancer therapy. It has been widely used for its potent cytotoxic effects upon a variety of tumors types including cervical carcinoma. However, the administration of cisplatin is associated with serious side effects, including nephrotoxic and neurotoxic events. There have been several studies aimed at finding drugs able to potentiate the antiproliferative effects of cisplatin without increasing the already serious side effects, but the search has not been successful.. In this work we investigated the ability of a progesterone antagonist, mifepristone, to modulate the cytotoxic effects of cisplatin in cancer cell lines and in a model of cervix cancer in athymic mice. ...
Product Description High Purity Mifepristone CAS No. 84371-65-3 for Anti-Pregnancy Mifepristone Synonyms: Estra-4, 9-dien-3-one, 11-[4-(dimethylamino)- phenyl]-17-hydroxy-17-(1-propynyl)-, (11a, - 17a)-Mifepristone; 17-beta-Hydroxy-11-beta-(4-dimethylaminophenyl-1)-17-alpha-(prop-1-ynyl)oestra-4, 9-dien-3-one Inchi: InChI=1S/C29H35NO2/c1-5-15-29(32)16-14-26-24-12-8-20-17-22(31)11-13-23(20)27(24)25(18-28(26, 29)2)19-6-9-21(10-7-19)30(3)4/h6-7, 9-10, 17, 24-26, 32H, 8, 11-14, 16, 18H2, 1-4H3/t24-, 25+, 26-, 28-, 29-/m0/s1 CAS No.: 84371-65-3 MF: C29H35NO2 MW: 429.59 Purity: 99%min Density: 1.18 g/cm3 Melting Point: 195-198° C Boiling Point:…
Dr. Geoffrey Sher established the first private IVF Center in the US in 1982. For over 30 years he has been advocate for womens reproductive health concerns while trailblazing medical breakthroughs.
In rats, chronic unpredictable, but also acute stress decreased the numbers of adult-generated cells. The reduced proliferation rate after acute stress, however, normalized again already within 24 hrs, whereas most of the structural dynamic changes after chronic stress were at least partly recovered after 3 week of recovery, indicating that the stress mediated reduction in adult cytogenesis is transient and reversible. Apoptosis on the other hand, increased after acute, but was decreased after chronic stress, while the significant reduction in CA3 volume after chronic stress had not yet normalized after an additional 3 weeks recovery period (4). Recent clinical studies that blocked the effects of stress by treating depressed patients with high doses of the GR antagonist RU486, proved very promising as a strong reduction was found in their depressive symptoms (1). Our preliminary data on stressed rats treated with high doses of RU486 for the last 4 days, indicate this clinical effect is mediated ...
The mechanisms of antisteroid action have been extensively studied in recent years, mostly because of the clinical importance of these compounds. One question that was addressed was whether these drugs display a partial agonist activity under certain conditions. This question is important because of its implications for the efficacy of the drug as well as for understanding the molecular mechanisms of the inhibition of the hormone action. These studies were made possible by the availability of expression vectors for the various steroid receptors and by the use of transfection assays. Using such approaches, it was shown that the antiprogestin and antiglucocorticoid RU 486 (27,28) and the antiestrogen tamoxifen (29) display agonist activity under certain conditions. In fact, antiestrogens can be grouped into several classes distinguished by their relative agonist activity, reflecting their differential effect on the receptor conformation (30). Much less is known about the properties of the ...
C. Matthew Peterson, M.D. Progestogens, Progesterone antagonists, progesterone, and androgens: synthesis, classification and uses ...
His return in many ways mirrors that of Steve Jobs, who was forced out of Apple in the 1980s and, with the company he founded struggling, made a historic comeback in 1997 despite still running Pixar ...
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WASHINGTON (CNS) -- Two-month-old Gabriel Caicedo is one of 78 children who have been saved by a new medical protocol being used to reverse the effects of the RU-486 abortion regimen in its early stages.
* Re your editorial A Forward Move for RU-486, March 8: That Roussel Uclaf is talking about U.S. distribution is certainly welcome news. Well, I know I breathed a big sigh of relief. Now we can
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