Treat prostate cancer androgen receptor antagonists. Medical search. Frequent questions

Blocking androgen receptor (AR) transcriptional activity by androgen deprivation therapy (ADT) improves the response to radiotherapy for intermediate and high risk prostate cancer. (bcgsc.ca)
Androgen deprivation therapy (ADT) combined with docetaxel or antiandrogens (abiraterone, enzalutamide, or apalutamide) improved the outcomes in men with metastatic hormone-sensitive prostate cancer (mHSPC). (thieme-connect.com)
1 ] The upfront management of men with metastatic hormone-sensitive prostate cancer (mHSPC) had been with only androgen deprivation therapy (ADT), for a long time, either with medical or surgical castration. (thieme-connect.com)
Neoadjuvant androgen deprivation therapy (NADT) is systemic therapy administered after the diagnosis of prostate cancer but before locoregional therapy such as radical prostatectomy (RP) or radiation. (medscape.com)
However, the NCCN notes that androgen deprivation therapy before, during, and/or after radiation prolongs survival in selected patients who are receiving radiation therapy only. (medscape.com)
However, a meta-analysis of the sequencing of androgen deprivation therapy with radiation therapy in localized prostate cancer concluded that adjuvant androgen deprivation therapy results in superior outcomes, compared with neoadjuvant or concurrent androgen deprivation therapy. (medscape.com)
RARITAN, N.J., February 8, 2021 - The Janssen Pharmaceutical Companies of Johnson & Johnson announced today results from the final analysis of the Phase 3 TITAN study, which demonstrated the continued statistically significant benefit of the addition of ERLEADA ® (apalutamide) to androgen deprivation therapy (ADT) in overall survival (OS) in patients with metastatic castration-sensitive prostate cancer (mCSPC), regardless of extent of disease, when compared to placebo plus ADT. (jnj.com)
The TITAN final analysis further confirms that treatment with apalutamide can prolong overall survival and offer a clear long-term clinical benefit and established safety profile for patients with metastatic prostate cancer who are starting androgen deprivation therapy," said Dr. Kim Chi, Medical Oncologist at BC Cancer - Vancouver and principal investigator of the TITAN study. (jnj.com)
Recent randomized controlled trials (RCTs) examined the role of adding androgen receptor signaling inhibitors (ARSIs), including abiraterone acetate (ABI), apalutamide, darolutamide (DAR), and enzalutamide (ENZ), to docetaxel (DOC) and androgen deprivation therapy (ADT) in patients with metastatic hormone-sensitive prostate cancer (mHSPC). (nih.gov)
Combined with observations of neuroendocrine enrichment in cases of poor clinical response to androgen deprivation therapy, these findings support the notion that the clonal expansion of AR-negative neuroendocrine cells may play a critical role in the development of androgen-insensitive metastatic prostate cancer. (cancernetwork.com)
Aim: To reduce the frequency of the need for hospital visits for patients with prostate cancer (PCa) taking androgen-deprivation therapy during the SARS-CoV-2 (COVID-19) pandemic, we switched them from gonadotropin-releasing hormone (GnRH) antagonist to a long-acting luteinizing hormone-releasing hormone (LH-RH) agonist. (cancerdiagnosisprognosis.org)
Androgen deprivation therapy (ADT) is the mainstream treatment paradigm for metastatic prostate cancer ( Available at: https://uroweb.org/guideline/prostate-cancer ()">1 ). (cancerdiagnosisprognosis.org)
This led the way for use of androgen deprivation therapy (ADT), which is now the backbone of systemic therapy for metastatic prostate cancer. (abdominalkey.com)
Intermittent androgen deprivation therapy (IADT) involves alternating periods of medical castration and treatment free intervals to allow testosterone recovery. (abdominalkey.com)
61 A study by Labarta et al randomized 49 patients to continuous androgen deprivation therapy (CADT) and 51 patients to IADT. (abdominalkey.com)
The new Phase III study ARASENS will evaluate the safety and efficacy of the compound in combination with standard androgen deprivation therapy (ADT) and the chemotherapy docetaxel in men with newly diagnosed metastatic hormone-sensitive prostate cancer (mHSPC), who are starting first line hormone therapy. (orion.fi)
Upon relapse when the disease will metastasize or spread, androgen deprivation therapy (ADT) is the cornerstone of treatment for this hormone-sensitive disease. (orion.fi)
However, the NCCN notes that androgen deprivation therapy before, during, and/or after radiation prolongs survival in selected radiation-managed patients. (medscape.com)

Therapies for lethal castration-resistant prostate cancer (CRPC) are an unmet medical need. (bcgsc.ca)
Unfortunately, these therapies fail to maintain a durable clinical effectiveness, as patients eventually succumb to castration-resistant prostate cancer (CRPC). (ubc.ca)
Once-daily Oral VT-464 in Patients With Castration-Resistant Prostate Cancer Progressing on Enzalutamide or Abiraterone. (mayo.edu)
The goal of this clinical study is to determine the safety and efficacy of VT-464, a lyase-selective inhibitor of CYP17 and an androgen receptor antagonist, in patients with castration-resistant prostate cancer (CRPC) who have been previously treated with enzalutamide or abiraterone. (mayo.edu)
Various molecular mechanisms have been implicated in the progression from hormone-sensitive to castration-resistant prostate cancer (CRPC). (escholarship.org)
Androgen receptor (AR) signaling continues to play a dominant role in all stages of prostate cancer (PC), including castration-resistant prostate cancers (CRPC) that have developed resistance to second-generation AR antagonists such as enzalutamide," the researchers wrote. (genengnews.com)
This clinical trial is for men with progressive metastatic castration-resistant prostate cancer (mCRPC). (survivornet.com)
ERLEADA ® has shown a statistically significant improvement in OS with a consistent safety profile in both approved indications of mCSPC (TITAN) and non-metastatic castration-resistant prostate cancer or nmCRPC (SPARTAN). (jnj.com)
Further studies showed (+)-JJ-74-138 inhibition of castration-resistant PSA expression in all tested castration-resistant prostate cancer (CRPC) cells. (aacrjournals.org)
The compound is currently in Phase III study ARAMIS for high-risk non-metastatic castration-resistant prostate cancer (nmCRPC). (orion.fi)
Despite this first line treatment, most men with metastatic HSPC will eventually progress to castration-resistant prostate cancer (CRPC), which can impact survival and quality of life. (orion.fi)
Castration-resistant prostate cancer (CRPC) usually involves the PI3K/AKT/mTOR pathway and requires targeted therapy. (bjbms.org)

The clinical onset and progression of most CRPC is accompanied by rising levels of serum prostate specific antigen (PSA), a gene transcriptionally regulated by AR. (ubc.ca)
Approximately 20-30% of men with 1 or more positive margins experience relapse, depending on the site of the positive margin, preoperative prostate-specific antigen (PSA) level, Gleason score, and presence of seminal vesical invasion. (medscape.com)
Hormonal treatment of advanced prostate cancer should be consideredfor patients who have stages C and D1 disease, a high risk of recurrenceafter local therapy, or prostate-specific antigen-measured recurrenceafter local treatment. (cancernetwork.com)
Prostate-specific antigen (PSA) levels were assessed as a secondary end point. (formularywatch.com)
Data obtained from patients with androgen- independent prostatic carcinoma have revealed that prostate-specific antigen (PSA) correlates with survival in patients with normal bombesin levels. (cancernetwork.com)
Patients and Methods: We analyzed the medical records of 32 patients with PCa who received ADT and switched from GnRH antagonist to a long-acting LH-RH agonist during the COVID-19 pandemic, evaluating hematological and serological variables, including serum testosterone and prostate-specific antigen. (cancerdiagnosisprognosis.org)
Results: Before and after the switching from GnRH antagonist to LH-RH agonist, the median serum testosterone levels were 0.22 and 0.18 ng/ml, respectively, and the median serum prostate-specific antigen levels were 0.18 and 0.11 ng/ml, respectively. (cancerdiagnosisprognosis.org)
Hormone therapy is restarted once the man's Prostate-Specific Antigen level reaches a certain point, which indicates that the cancer cells are growing again. (sutterhealth.org)
Since prostate cancer is driven by androgen receptor signaling, ADT lowers testosterone levels into a castrate range, resulting in a decrease in prostate-specific antigen (PSA), which is driven by androgen receptor signaling. (abdominalkey.com)
Patients with metastatic prostate cancer and prostate-specific antigen (PSA) of greater than 20 ng/mL received 6 months of induction ADT. (abdominalkey.com)
Trial Description: This study will evaluate the safety and efficacy of a prostate cancer vaccine named Proscavax ( Prostate -specific antigen(PSA) / Interleukin-2(IL-2) / Granulocyte-macrophage colony-stimulating factor(GM-CSF)) in patients with localized prostate cancer . (dana-farber.org)
Selecting initial treatment requires assessing the risk of the disease spreading or progressing, which is based on evaluating the patient's life expectancy, comorbidities, biopsy grade (Gleason score), clinical stage, and prostate-specific antigen (PSA) level. (medscape.com)

Prior use of other 2nd generation CYP17 inhibitors and androgen receptor antagonists are allowed in addition to abiraterone or enzalutamide. (mayo.edu)
The combination of metformin with androgen biosynthesis/AR inhibitors results in caspase-independent apoptotic cell death in addition to inhibition of both cell proliferation and AR signaling. (renalandurologynews.com)
Novel targeted agents to treat CRPC have been developed that inhibit either androgen receptor (AR)-mediated signaling (AR antagonists and inhibitors of androgen synthesis) or non-AR-mediated signaling (inhibitors of Src, mammalian target of rapamycin, chaperone proteins, insulin-like growth factor-1 receptor, vascular endothelial growth factor, and endothelin-A receptor) pathways. (escholarship.org)
5-alpha reductase inhibitors, in general, are no longer being used in the United States because of health concerns, but a number of highly selective 5-alpha reductase inhibitors are still being used by injectionists for some hemophiliacs, neutropenia, and prostate tumors, with risks varying depending on the choice of the injector, testosterone enanthate dosage. (youthparlor.com)
Drugs commonly used for prostate cancer include luteinizing hormone-releasing hormone (LHRH) agonists, LHRH antagonists and androgen synthesis inhibitors. (sutterhealth.org)
People in both treatment method teams were permitted to acquire normal of treatment which include remdesivir, dexamethasone, anti-IL6 receptor antibodies, and JAK inhibitors. (ottawainsectarium.com)
Both the placebo and Sabizabulin treated groups were allowed to receive standard of care, which could include Dexamethasone, Remdesivir and Anti-IL-6 receptor antibodies and JAK inhibitors. (alphastreet.com)

As a whole, these studies provide critical new insight for receptor-based drug design of nonsteroidal AR agonists and antagonists. (rcsb.org)
Incidence of severe cardiac adverse events may be lower with the use of degarelix compared with GnRH agonists,[ 5 ] an ongoing prospective trial is comparing the risk of cardiovascular events with the use of GnRH agonists and antagonists. (thieme-connect.com)
Options forandrogen blockade primarily include orchiectomy, luteinizing hormone-releasing agonists and antagonists, and nonsteroidal antiandrogens.There is some controversy regarding combined androgen blockade,intermittent androgen blockade, and the question of whether earlyandrogen blockade is superior to delayed therapy. (cancernetwork.com)
The predomination of an androgen-independent phenotype canoccur approximately 1 to 2 years afterthe initiation of androgen deprivation.Multiple strategies have been usedto induce serum levels of testosteronesimilar to those following castration.Traditional treatment options for androgenblockade include orchiectomy,luteinizing hormone-releasing hormone(LHRH) agonists and antagonists,nonsteroidal antiandrogens, andestrogens. (cancernetwork.com)
While the net result of the treatments by agonists and antagonists appears to be the same, two characteristic of the antagonists make it essential to determine whether return to fertility may be a problem and of regulatory interest. (biomedcentral.com)

Patients must have undergone orchiectomy, or have been on LHRH agonists or antagonists, for at least 3 months prior to drug initiation. (mayo.edu)
Patients on LHRH agonists/antagonists must remain on these agents for the duration of the study. (mayo.edu)
The advent of safe and reversible forms of androgen deprivation, such as luteinizing hormone-releasing hormone (LHRH) analogues and antiandrogens (AAs), has also contributed to enthusiasm for NADT. (medscape.com)
Must have remained on testosterone suppression for metastatic disease continuously (without treatment breaks) for 540-750 days (approximately 18 to 24 months) from time of first dose of LHRH agonist or antagonist by time of registration. (dana-farber.org)

One mechanism underlying CRPC and resistance to hormonal therapies is the expression of constitutively active splice variant(s) of androgen receptor (AR-Vs) that lack its C-terminus ligand-binding domain. (bcgsc.ca)
These findings support the rationale for therapy that combines a Pin1 inhibitor with ralaniten for treating CRPC. (bcgsc.ca)
Also, this analogue noncompetitively inhibited androgen-stimulated AR activity in C4-2, LN95, and 22Rv1 CRPC cells. (aacrjournals.org)
Androgen receptor splice variant 7 (AR-V7) is an important oncogenic driver and an early diagnostic and prognostic marker, as well as a therapeutic target in hormone-resistant CRPC. (bjbms.org)

3 ] [ 4 ] GnRH antagonist degarelix is not associated with this surge of LH and can be a substitute to a GnRH agonist when a rapid fall in serum testosterone is necessary. (thieme-connect.com)
Conclusion: Switching from GnRH antagonist to a long-acting LH-RH agonist appears to be a reasonable option that does not diminish efficacy or exacerbate adverse events. (cancerdiagnosisprognosis.org)
Other agents, such as the luteinizing hormone-releasing hormone (LH-RH) agonists, leuprorelin acetate and goserelin acetate, and the gonadotropin-releasing hormone (GnRH) antagonist degarelix, must be injected and therefore cannot be sent directly to the patients because the Japanese medical system does not allow patients to inject themselves with these medications. (cancerdiagnosisprognosis.org)
At present, degarelix is the only GnRH antagonist available in Japan. (cancerdiagnosisprognosis.org)
Although degarelix blocks GnRH receptors in the pituitary gland, resulting in a rapid decrease in the production of testosterone, the effects of degarelix on androgen deprivation last for only 1 month ( BJU Int 102(11) (2008)">2 , Eur Urol 57(5) (2010)">3 ). (cancerdiagnosisprognosis.org)
Several prospective and retrospective studies have demonstrated that patients can also be safely switched from GnRH antagonist therapy to LH-RH agonist therapy without any adverse clinical or oncological effects ( Oncol Ther 5(1) (2017)">7 - Basic Clin Androl 28 (2018)">10 ). (cancerdiagnosisprognosis.org)
In order to reduce the frequency of required hospital visits for our patients during the COVID-19 pandemic, we switched them from the GnRH antagonist degarelix to long-acting LH-RH agonists. (cancerdiagnosisprognosis.org)
An oral therapeutic option with strong efficacy that also reduces cardiovascular risk compared to that of conventional GnRH agonist therapy would be a critical achievement for men with advanced prostate cancer. (myovant.com)
Antagonistic analogues of GnRH for the treatment of prostate cancer may be used clinically in persons for whom return to fertility after such treatment is important or desirable. (biomedcentral.com)
The purpose of this study was, therefore, to evaluate the effects of a long term treatment with orntide, a GnRH antagonist, on testosterone levels and fertility in male rats. (biomedcentral.com)
These results suggest that lack of fertility due to testosterone suppression is reversible after cessation of treatment with this GnRH antagonist. (biomedcentral.com)
They act by hyper-stimulation of GnRH receptors on the gonadotroph cells of the pituitary, resulting in an initial phase of elevated levels of testosterone and androgens, followed by down-regulation of the receptors. (biomedcentral.com)
These are GnRH antagonists, which immediately block the GnRH receptors to access by native GnRH peptides. (biomedcentral.com)
This report is an evaluation of the effect of a long term treatment with a GnRH antagonist, orntide acetate, on the fertility of male rats. (biomedcentral.com)

Among patients treated with degarelix, 98.3% (95% CI, 94.8%-99.4%) of patients in the 240/160-mg dose group and 97.2% (95% CI, 93.5%-98.8%) of patients in the 240/80-mg dose group achieved this end point compared with 96.4% (95% CI, 92.5%-98.2%) of patients treated with leuprolide. (formularywatch.com)
Testosterone suppression to castration levels occurred more rapidly among degarelix patients, with 96% of degarelix-treated patients achieving this end point by Day 3 compared with 0 leuprolide-treated patients. (formularywatch.com)

Recently, our laboratory discovered selective androgen receptor modulators, which structurally resemble the nonsteroidal AR antagonists bicalutamide and hydroxyflutamide but act as agonists for the androgen receptor in a tissue-selective manner. (rcsb.org)
To investigate why subtle structural changes to both the ligand and the receptor (i.e. mutations) result in drastic changes in activity, we studied structure-activity relationships for nonsteroidal AR ligands through crystallography and site-directed mutagenesis, comparing bound conformations of R-bicalutamide, hydroxyflutamide, and two previously reported nonsteroidal androgens, S-1 and R-3. (rcsb.org)
Prior treatment with first-generation AR antagonists (i.e., bicalutamide, nilutamide, flutamide) before abiraterone or enzalutamide is allowed. (mayo.edu)
Estrogen receptor antagonists, such as flutamide and bicalutamide, bind to estrogen receptors in the brain that have been reprogrammed by androgens. (youthparlor.com)
The relative binding affinity of nilutamide at the androgen receptor is less than that of bicalutamide, but similar to that of hydroxuflutamide. (drugbank.com)

Metformin, a widely used oral anti-diabetic drug, enhanced the anti-prostate cancer activity of abiraterone and enzalutamide. (renalandurologynews.com)
Metformin, a widely used oral anti-diabetic drug, enhanced the anti-prostate cancer activity of abiraterone and enzalutamide, a study presented at the American Association for Cancer Research (AACR) Annual Meeting 2016 has shown. (renalandurologynews.com)
Because metformin has been reported to reduce prostate cancer-related death in patients with prostate cancer and type 2 diabetes , researchers at the University of Maryland in Baltimore sought to explore the effects of metformin with abiraterone or enzalutamide in preclinical models. (renalandurologynews.com)
Both agents also increased androgen receptor (AR) and AR variant AR-V7, which is involved in the development of resistance to abiraterone and enzalutamide. (renalandurologynews.com)
Xie Y, Wawng L, Hussain A. Metformin enhances the anti-prostate cancer activity of abiraterone and enzalutamide. (renalandurologynews.com)

Ralaniten Sensitizes Enzalutamide-Resistant Prostate Cancer to Ionizing Radiation in Prostate Cancer Cells that Express Androgen Receptor Splice Variants. (bcgsc.ca)
Combination therapies using ralaniten with ionizing radiation were evaluated for effects on proliferation, colony formation, cell cycle, DNA damage, and Western blot analyses in human prostate cancer cells that express both full-length AR and AR-Vs. Ralaniten and a potent next-generation analog (EPI-7170) decreased expression of DNA repair genes whereas enzalutamide had no effect. (bcgsc.ca)
Ralaniten and EPI-7170 sensitized prostate cancer cells that express full-length AR and AR-Vs to radiotherapy whereas enzalutamide had no added benefit. (bcgsc.ca)
Their findings are published in the journal Cancer Research in a paper titled, " Loss of long noncoding RNA NXTAR in prostate cancer augments androgen receptor expression and enzalutamide resistance . (genengnews.com)
Here, we show that (+)-JJ-74-138 is more potent than JJ-450 in the inhibition of androgen-independent AR activity in enzalutamide-resistant LN95 cells. (aacrjournals.org)

According to the research - conducted in mice implanted with human prostate tumor samples - restoring this so-called long noncoding RNA could be a new strategy to treat prostate cancer that has developed resistance to hormonal therapies. (genengnews.com)
This approach is dependent on most prostatecancer cells being androgen-dependent, but androgen-independentcells may arise after several years of hormonal therapy. (cancernetwork.com)
Although hormonal therapy is an importanttreatment modality for advanced prostate cancer, long-termtreatment carries significant side effects that need to be considered. (cancernetwork.com)
M ore than 60 years haveelapsed since Huggins andHodges[1] first recognizedthe hormonal dependence of prostatecancer. (cancernetwork.com)
Although hormonal treatment is an important palliative measure in the management of patients with advanced prostate carcinoma, the vast majority of cases end in relapse due to overgrowth of androgen-independent tumor cell populations [1]. (cancernetwork.com)
Some hormonal therapies decrease the amount of hormones produced by the body, while others block the action of the hormones on cancer cells. (sutterhealth.org)
Steroids, man-made formulations of the male sex hormone testosterone, to treat hormonal issues, such as delayed puberty, and to retard the muscle-wasting effects of certain diseases. (chicagonewsdaily.com)
Nilutamide is an antineoplastic hormonal agent primarily used in the treatment of prostate cancer. (drugbank.com)
Advanced and metastatic prostate cancers require systemic therapies, including hormonal inhibition, chemotherapy, and targeted agents. (bjbms.org)
The usual treatment for patients with metastatic prostate cancer is to receive hormonal medications including a medication to decrease testosterone levels in the body and a potent oral hormonal medication to block growth signals from male hormones (like testosterone) in the cancer cells. (dana-farber.org)
Natural Estrogen with Pomegranate Extract is a multi-component phytoestrogen compound that addresses all the currently identified hormonal components of androgen mediated hair loss. (hairloss-research.org)

Additionally, lessons learned through the application of these technologies to prostate cancer may subsequently influence therapeutic development in other solid tumors. (escholarship.org)
A study from Washington University School of Medicine in St. Louis has identified an RNA molecule that suppresses prostate tumors. (genengnews.com)
In this study, we identified a long noncoding RNA (lncRNA), NXTAR (LOC105373241), that is located convergent with the AR gene and is repressed in human prostate tumors and cell lines. (genengnews.com)
This means that in all the prostate cancer samples that we study, we rarely find NXTAR, because it is suppressed by the heavy presence of the androgen receptor in these types of tumors. (genengnews.com)
The researchers demonstrated restoring NXTAR expression caused the tumors to shrink using human prostate tumor samples implanted in mice. (genengnews.com)
Androgen hormones are the predominant stimulators of growth in tumors of the prostate. (corcept.com)
Janssen is focused on addressing areas of unmet need in both prostate cancer and solid tumors, and this year's ESMO Annual Congress provides an opportunity to share these important study results for both approved and investigational therapies," said Mark Wildgust, Ph.D., Vice President, Global Medical Affairs, Oncology, Janssen Research & Development, LLC. (jnj.com)
Ogsiveo will be available within five to 10 business days to treat patients with desmoid tumors. (formularywatch.com)
The availability of an anti-androgen receptor (AR) monoclonal antibody has allowed the identification of both AR-positive and AR-negative neuroendocrine subpopulations in both benign and malignant tumors [5]. (cancernetwork.com)

All current AR-targeting therapies inhibit the growth of prostate cancer cells by blocking the ligand-binding domain (LBD), where androgen binds to activate the receptor. (ubc.ca)
2]The premise of androgen ablationrelies on growth of most prostate carcinomacells being androgen-dependent.The androgen receptor expressedby these cells binds dihydrotestosterone,which is then transported intothe nucleus, leading to a cascade ofevents that induces cellular growth. (cancernetwork.com)
DHT binds with the androgen receptor and induces transcription of proteins necessary for function and development of the prostate. (abdominalkey.com)

Rapid Abstract Session: Prostate Cancer, February 11, 3:30 PM-4:15 PM EST). (jnj.com)

Androgen receptor (AR) is one of the predominant nuclear hormone receptors in invasive breast cancer and can be explored as a biomarker of response for targeted anti-androgen therapy, especially in the setting of triple negative breast cancer (TNBC). (ecancer.org)

Development of novel small molecule inhibitor of androgen. (ubc.ca)

Clinically approved AR antagonists compete with dihydrotestosterone (DHT) for binding to the ligand-binding domain (LBD) of AR, and patients eventually develop resistance to these treatments. (aacrjournals.org)

Initial results from the TITAN study presented at the 2019 American Society of Clinical Oncology Genitourinary Cancers Symposium (ASCO GU) and simultaneously published in The New England Journal of Medicine showed the addition of ERLEADA ® (apalutamide) to ADT compared to placebo plus ADT significantly improved the dual primary endpoints of OS and radiographic progression-free survival (rPFS) in patients with mCSPC. (jnj.com)
Apalutamide may help fight prostate cancer by blocking the use of androgen by the tumor cells. (dana-farber.org)
Trial Description: This phase III trial studies whether adding apalutamide to the usual treatment improves outcome in patients with lymph node positive prostate cancer after surgery. (dana-farber.org)

Pin1 inhibition improves the efficacy of ralaniten compounds that bind to the N-terminal domain of androgen receptor. (bcgsc.ca)
Finally, a human prostate cancer cell line model resistant to growth inhibition by EPI-002 was generated, allowing future studies to investigate mechanisms of resistance against AR inhibition through the NTD. (ubc.ca)
Oral contraceptives decrease circulating levels of androgens by direct inhibition of androgen production in the ovaries and by a marked increase in the hepatic. (weiss.ge)
First, LY294002 inhibition can obviously alleviate the mouse psoriatic skin inflammation both in skin structural and histopathological characteristics, which is similar to the changes found in IL-17A antibody-treated mice. (bvsalud.org)
This blockade of androgen receptors may result in growth arrest or transient tumor regression through inhibition of androgen-dependent DNA and protein synthesis. (drugbank.com)
In a review of risperidone/olanzapine-induced mania, it was speculated the cause was due to 5-HT /D receptor occu- pancy.6 However, ziprasidone differs from the older atypicalsin its profound 5-HT and 5-HT/norepinephrine (NE) reuptake inhibition effect-similar to amitriptyline and imipramine. (pdftreatment.com)
It functions to reduce DHT, Androstendione via 17BHSD inhibition/Enterolactone production, Prolactin, and modulates estrogen in such a way as to neutralize its role in hair loss and prostate cancer development. (hairloss-research.org)

Spironolactone, an aldosterone antagonist, competes with testosterone and dihydrotestosterone at the androgen receptor. (weiss.ge)
It is also noted that by maintaining very high estrogen levels, it can trigger breast cancer and endometrial cancer, for spironolactone bodybuilding. (youthparlor.com)
The diuretic effect of spironolactone is mediated through its action as a specific pharmacologic antagonist of aldosterone, primarily by competitive binding of receptors at the aldosterone-dependent sodium-potassium exchange site in the distal convoluted renal tubule. (nih.gov)
Relative to spironolactone, their binding affinities to the aldosterone receptors in rat kidney slices were 0.19, 0.86, and 0.06, respectively. (nih.gov)

Nilutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). (drugbank.com)
Proxalutamide is a nonsteroidal antiandrogen - specifically, a selective high-affinity silent antagonist of the androgen receptor - that is under development for the potential treatment of COVID-19, prostate cancer, and breast cancer. (kintor.com.cn)

This warrants further exploration of the predictive and prognostic significance of its expression amongst TNBC and the potential for targeted therapy, specifically androgen antagonists to improve the outcome of this disease with limited therapeutic options. (ecancer.org)
As with any therapy, the ultimate benefit of NADT in prostate cancer will be determined only through properly designed trials with long-term follow-up. (medscape.com)
Three databases and meetings abstracts were queried in April 2022 for RCTs analyzing patients treated with first-line combination systemic therapy for mHSPC. (nih.gov)
Long-term androgen therapy has been demonstrated to prolong the QT interval. (formularywatch.com)
Hormone replacement therapy (HRT), for both men and women, treats such problems. (youthparlor.com)
Several types of cancer can be treated with hormone therapy, including prostate cancer , breast cancer and endometrial cancer . (sutterhealth.org)
If hormone therapy is an option for the type of cancer you have, your doctor will talk with you about how this kind of therapy might benefit you, as well as the potential side effects. (sutterhealth.org)
Most prostate cancer cells have receptors for testosterone and are potential targets for hormone therapy. (sutterhealth.org)
Hormone therapy often can slow down the growth of prostate cancer for quite a while, and can sometimes shrink a tumor. (sutterhealth.org)
But in most cases, some prostate cancer cells will eventually lose their need for the testosterone "fuel" and will continue to grow anyway, making hormone therapy ineffective. (sutterhealth.org)
For that reason, hormone therapy is not seen as a cure for prostate cancer. (sutterhealth.org)
Surgical castration, removal of the testes, is another form of hormone therapy for prostate cancer. (sutterhealth.org)
Before prescribing hormone therapy, your doctor will likely have a tissue sample from your biopsy or surgery tested for estrogen receptors. (sutterhealth.org)
If they are present, the cancer is termed estrogen-receptor positive, or ER-positive, and might respond to hormone therapy. (sutterhealth.org)
Today, doctors have several options for treating breast cancer with hormone therapy. (sutterhealth.org)
Men with newly diagnosed metastatic hormone-sensitive prostate cancer (mHSPC) will start their treatment with hormone therapy, such as ADT or a combination of the chemotherapy docetaxel and ADT. (orion.fi)
Available at: http://www.cancer.gov/types/prostate/prostate-hormone-therapy-fact-sheet. (orion.fi)
Local-regional therapy, i.e., surgery is beneficial in early-stage prostate cancer management. (bjbms.org)
Most benefits were demonstrated in cyclin dependent-kinase 12 ( CDK12) mutated cell lines when treated with anti-programmed cell death protein 1 (PD1) therapy. (bjbms.org)
This phase II trial examines antiandrogen therapy interruptions in patients with hormone-sensitive prostate cancer that has spread to other places in the body (metastatic) responding exceptionally well to androgen receptor-pathway inhibitor therapy. (dana-farber.org)
Patients whose cancer is responding exceptionally well to this therapy may take a break from these medications according to their doctor's guidance. (dana-farber.org)
Prior local therapy for prostate cancer (either before or after diagnosis of metastatic disease) is permitted. (dana-farber.org)
Trial Description: This phase III trial compares less intense hormone therapy and radiation therapy to usual hormone therapy and radiation therapy in treating patients with high risk prostate cancer and low gene risk score. (dana-farber.org)
Current concerns regarding prostate cancer progression have led to a renewed interest in the use of neoadjuvant androgen deprivation (NAD) therapy prior to radical prostatectomy ( RP ). (medscape.com)
However, neoadjuvant therapy may provide an important paradigm for the discovery of active agents for the treatment of prostate carcinoma, in addition to improving clinical outcomes for men with early, high-risk disease. (medscape.com)
A multidisciplinary approach with a team of oncologists and urologists will be critical to making advances in the arena of neoadjuvant therapy for prostate carcinoma and to aiding in the efficient evaluation of new therapies. (medscape.com)

At the time of diagnosis, most men have localized prostate cancer, meaning their cancer is confined to the prostate gland and can be treated with curative surgery or radiotherapy. (orion.fi)
Prostate cancer (PCa) is the second most common male cancer and about 50% of all PCa patients received radiotherapy (RT), despite some of them develop radioresistance. (frontiersin.org)
One of the treatments applied in cancer is radiotherapy (RT), a therapeutic modality that uses ionizing radiation to induce damage in unwanted cells. (frontiersin.org)

In cancers that express glucocorticoid receptors (GRs), such as pancreatic, ovarian, and breast cancers, cortisol suppresses programmed cell death (apoptosis). (corcept.com)

Testosterone then goes to prostate epithelial cells, where it is converted into dihydrotestosterone (DHT) by the enzyme 5-alpha reductase. (abdominalkey.com)
Researchers know now that the major cause of prostate enlargement and prostate cancer is the transformation of testosterone into dihydrotestosterone and that this can often be blocked and/or reversed by the use of certain natural herbs and nutritional supplementation. (lifex.com)

Although many patients with prostate cancer are treated with therapies that block hormones that fuel tumor growth, most patients develop resistance to these therapies. (genengnews.com)
We are hoping to develop both this (R)-9b drug and NXTAR into new therapies for prostate cancer patients who have developed resistance to the front-line treatments," Mahajan said. (genengnews.com)
Cancer researchers have developed several hormone-based therapies that can interrupt those cancer growth-promoting pathways. (sutterhealth.org)
This review summarizes the pathophysiological mechanisms and available targeted therapies for prostate cancer. (bjbms.org)

That's why medications that lower testosterone levels (for example, leuprolide) and castration are common treatments for men with prostate cancer. (weiss.ge)
50 ng/dL) through 48 weeks, compared to 88.8% of men treated with leuprolide acetate. (myovant.com)

Blocking the ability of estrogen to stimulate cell growth - Selective estrogen receptor modulators (SERMs) bind to the estrogen receptors on the cells, preventing estrogen from binding. (sutterhealth.org)

The diterpenoids blocked androgen-dependent AR transcriptional activity with a structure-activity relationship, reduced androgen-regulated gene expression, and inhibited the proliferation of androgen-sensitive prostate cancer cells. (ubc.ca)

Present study was designed to establish a causal connection between changes in the cell-cell junction protein expression at the blood-testis barrier and alterations in the adult rat testis histology following an anti-androgen flutamide exposure. (biomedcentral.com)
As shown by examination of semi-thin and ultrathin sections, cell surface occupied by the basal ES connecting neighboring Sertoli cells and the number of gap and tight junctions coexisting with the basal ES were apparently reduced in flutamide-treated rats. (biomedcentral.com)
0.05) in flutamide-treated rats compared to the controls. (biomedcentral.com)

Breast cancer has been identified as a heterogeneous disease with marked differences in morphology, molecular biology, clinical findings and outcome [ 1 , 2 ]. (ecancer.org)
However, owing to the inaccuracy of clinical staging, approximately 50% of men with clinical stage T1 or T2 prostate cancer have tumor extension outside of the prostate capsule, and 5-40% have positive surgical margins. (medscape.com)
In patients with clinically localized prostate cancer, the National Comprehensive Cancer Network (NCCN) strongly discourages the use of NADT before RP outside of a clinical trial. (medscape.com)
The TITAN final analysis data confirm the long-term clinical benefit and consistent safety profile of ERLEADA ® plus ADT without a compromise in health-related quality of life," said Mary Guckert, RN, MSN, Vice President, Development Leader, Prostate Cancer, Janssen Research & Development, LLC. (jnj.com)
This review will examine the evidence for the neuroendocrine progression of prostate cancer and the clinical utility of chemothera- peutic agents that are being investigated for the management of late stage disease. (cancernetwork.com)
The clinical relevance of immunohistological detection of neuroendocrine tissue in prostate cancer patients has been the focus of many investigators. (cancernetwork.com)
Search clinical trials for adult and pediatric cancers and blood disorders offered through Dana-Farber and our clinical partners. (dana-farber.org)
Dr. Tong Youzhi, the founder, Chairman, and CEO of Kintor Pharma, commented, "We would like to give special thanks to President Dr. Hongzhou Lu and his team in the Third People's Hospital of Shenzhen for the first patient enrollment and dosing in proxalutamide's phase III clinical trial for treating COVID-19 outpatients in China, which is a very important step for this multi-regional clinical trial. (kintor.com.cn)
In the last years, extensive investigation on miRNomics have shown to have great advantages in cancer personalized medicine regarding diagnosis, treatment and even clinical outcomes. (frontiersin.org)
Surgical cure for prostate cancer can be expected only if the entire tumor is excised, and in men with clinical stage T1 or T2 prostate cancer, 50% have tumor extension outside the prostatic capsule and 40% have positive surgical margins. (medscape.com)

Of 61 TNBC cases analysed, 37.7% were AR positive and 62.3% were AR negative, making the latter to become quadruple negative breast cancers. (ecancer.org)
About 70 percent of breast cancers contain estrogen receptors and can have their growth stimulated by the presence of estrogen. (sutterhealth.org)

The adrenal androgens play a role in the development of castrate resistant prostate cancer. (abdominalkey.com)

0.5 ng/ml), can be achieved with or without blockade agents for androgen receptor ( Available at: https://uroweb.org/guideline/prostate-cancer ()">1 ). (cancerdiagnosisprognosis.org)

Those concerns regarding prostate cancer progression have led to a renewed interest in the use of NADT prior to RP. (medscape.com)
Preliminary data suggests that these markers may contribute to prostate cancer progression. (cancernetwork.com)
Androgen receptor (AR) is a ligand-activated transcription factor that plays a pivotal role in the development and progression of many severe diseases such as prostate cancer, muscle atrophy, and osteoporosis. (big.ac.cn)
The goal of the study is to determine if vaccine administration results in a change in the rate of prostate cancer progression when compared to a no-treatment control group of active surveillance patients. (dana-farber.org)
Some of these patients have incompletely resected cancer and, therefore, are at an increased risk for local recurrence and progression. (medscape.com)
In addition, obesity is associated with progression (but not incidence) of tumour microenvironment through prostate cancer. (who.int)

If no estrogen receptors are present, the cancer is termed ER-negative. (sutterhealth.org)

The mechanism by which the androgen receptor (AR) distinguishes between agonist and antagonist ligands is poorly understood. (rcsb.org)

For example, the hormone testosterone is necessary for normal prostate function, but it can also promote the growth of prostate cancer cells. (sutterhealth.org)
The role of androgens in the growth of prostate cancer was demonstrated by Huggins in 1941. (abdominalkey.com)

Moreover, FKBP52 is also implicated in the regulation of other hormone receptors so these compounds could be used to treat other hormone-dependent diseases such as diabetes or even used as contraceptives. (nih.gov)

A prodrug of ralaniten, ralaniten acetate (EPI-506), was under development for the treatment of prostate cancer. (wikipedia.org)

With the goal of finding potential therapeutic compounds that inhibit the FKBP52-mediated activation of AR, several small molecules were tested and found to be antagonists of FKBP52 and to inhibit AR activity in prostate cells. (nih.gov)

Based on Global Cancer Observatory (GLOBOCAN) 2020, more than 1.4 million new cases of PCa and 375,304 associated deaths were recorded ( 12 ). (frontiersin.org)

That serum testosterone levels useful in treating patients with extra shots until the FDA grants EUA for booster shots, which is expected in September (see below for more information about. (chicagonewsdaily.com)
After recovery of normal serum testosterone levels in the treated animals, each rat was housed with two proven breeder, but drug-naive, females. (biomedcentral.com)

To generate a prostate cancer cell line model that developed resistance to EPI-002, LNCaP human prostate cancer cells were cultured under chronic EPI-002 exposure. (ubc.ca)
With depot-steroid injections data from human trials (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. (chicagonewsdaily.com)

Dr. Sadar is an expert witness for Astellas, Pfizer, and University of California on patents covering Xtandi®, used for the treatment of prostate cancer in the USA with global sales greater than $3.5 billion per year. (bcgsc.ca)
In a proportion of prostate cancer patients, there is evidence of metastatic disease at diagnosis or the disease recurs as distant metastasis despite standard curative treatment. (thieme-connect.com)
These compounds can serve as therapeutics for the treatment of prostate cancer and benign prostate enlargement. (nih.gov)
This agent was approved on December 24, 2008, for the treatment of patients with advanced prostate cancer. (formularywatch.com)
We have also sought to enable more virtual and telephone interaction with our patients with prostate cancer during their treatment. (cancerdiagnosisprognosis.org)
A faster effect in lowering testosterone for prostate cancer patients can be clinically significant - likewise, a more rapid testosterone recovery after stopping treatment, could potentially improve a patient's quality of life," said Neal Shore, M.D., medical director of the Carolina Urologic Research Center, HERO program steering committee member, presenter of the ASCO data, and lead author on the NEJM paper. (myovant.com)
Both of these findings could make a meaningful difference in the treatment journey for men with advanced prostate cancer. (myovant.com)
The concern is heightened by the likelihood that antagonists will be used for treatment of benign prostatic hypertrophy, a condition in men who might wish at some future time to sire offspring. (biomedcentral.com)
Trial Description: This trial is testing whether molecularly targeted oral medications called talazoparib and tazemetostat can be safely combined for the treatment of prostate cancer , and whether the combination is effective in shrinking or preventing the growth of metastatic prostate cancer . (dana-farber.org)
Treatment protocols for prostate cancer are provided below, including general treatment recommendations and those for localized prostate cancer, for recurrent disease, and for advanced or metastatic disease. (medscape.com)

The immunophilin protein FKBP52 is part of a protein complex that helps fold the androgen receptor (AR) protein, a target for treating prostate cancer, and enhances its activity. (nih.gov)
AR is presently the main target for treating prostate cancer. (aacrjournals.org)

Androgen receptor (AR), a transcription factor, is a validated therapeutic target for prostate cancer. (ubc.ca)
Triple negative breast cancer (TNBC) is defined by the absence of expression for oestrogen receptor (ER), progesterone receptor (PR) and human epidermal growth factor receptor-2 (HER2) which has limited targeted therapeutic options. (ecancer.org)
The relationship between miRNAs and cancer was demonstrated for the first time in 2002, with miRNAs being stated as a potential mechanism that may contribute to improve some cancer therapeutic approaches through restoring or blocking the miRNAs function ( 11 ). (frontiersin.org)

However, the proportion of neuroendocrine differentiation was found to be much higher in follow-up studies and it is now thought that 50% to 100% of all prostate neoplasms (including benign prostatic tissue) contain at least some neuroendocrine cells [3,5]. (cancernetwork.com)
Consequently, Nilutamide blocks the action of androgens of adrenal and testicular origin that stimulate the growth of normal and malignant prostatic tissue. (drugbank.com)

Blocking ovarian function - Estrogen production in the ovaries is prevented by surgically removing the ovaries (oophorectomy) or treating them with luteinizing hormone-releasing hormones. (sutterhealth.org)
The most common genetic syndromes associated with prostate cancer risk are BRCA -associated hereditary breast and ovarian cancer (HBOC) and Lynch syndrome. (bjbms.org)

In contrast, metformin inhibited AR, AR-V7, and PSA expression in a dose-dependent manner and induced apoptosis in prostate cancer cells. (renalandurologynews.com)
In accord, no difference in the apoptosis and proliferation level was found between control and treated groups. (biomedcentral.com)

Anatomy10

Organisms5

Diseases19

Chemicals and Drugs72

Analytical, Diagnostic and Therapeutic Techniques and Equipment27

Phenomena and Processes26

Disciplines and Occupations1

Information Science2

Health Care8

Deprivation therapy18

Castration-resistant12

Antigen12

Inhibitors7

Agonists and antagonists5

LHRH4

CRPC4

GnRH14

Degarelix2

Bicalutamide5

Abiraterone5

Enzalutamide5

Hormonal11

Tumors9

Binds3

Abstract1

Anti-androgen therapy1

Inhibitor of androgen1

Ligand-bindin1

Apalutamide3

Inhibition7

Spironolactone4

Nonsteroidal2

Therapy26

Radiotherapy3

Glucocorticoid receptors1

Dihydrotestosterone2

Therapies4

Leuprolide2

Selective1

Transcriptional activity1

Flutamide3

Clinical10

Breast cancers2

Resistant Prostate Cancer1

Blockade1

Progression6

Estrogen receptors1

Ligands1

Growth of prostate cancer2

Hormone receptors1

Acetate1

Inhibit1

20201

Testosterone levels2

LNCaP2

Treatment10

Target for treating prosta2

Therapeutic3

Prostatic tissue2

Ovarian2

Apoptosis2