Castration 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)
Metastatic castration-resistant prostate carcinoma that progresses during or after treatment with the cytostatic drug docetaxel or for the treatment of metastatic castration-resistant prostate carcinoma with asymptomatic or mildly asymptomatic progression after failure of androgen deprivation therapy if chemotherapy is not yet clinically indicated. (altmeyers.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)
1 Although patients with recurrent disease initially respond to androgen deprivation therapy (ADT), most will go on to develop castration-resistant prostate cancer (CRPC) in which the disease becomes refractory to traditional hormone therapies and cancer growth continues despite castrate levels of testosterone. (touchoncology.com)
In the trial, this agent was highly tolerable across all tested dose levels, with adverse effects (AEs) largely resembling those of other androgen receptor (AR) antagonists and androgen deprivation therapy (ADT), Laccetti explains. (onclive.com)
Androgen deprivation therapy induces apoptosis or cell cycle arrest in prostate cancer (PCa) cells. (oncotarget.com)
Androgen deprivation therapy (ADT) is a first-line therapy for locally advanced and metastatic prostate cancer (PCa). (oncotarget.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)
For instance Ibuprofen Lysine (NeoProfen) androgen deprivation therapy[15] coupled with AR antagonists (we.e. anti-androgens) such as for example bicalutamide[16] continues to be used like a first-line treatment for early stage prostate tumor for many years. (buyresearchchemicalss.net)
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)
The approval of darolutamide in Japan is based on the results of the ARAMIS trial, a randomized (2:1), double-blind, placebo-controlled, multi-center Phase III study which evaluated the safety and efficacy of the compound in patients with nmCRPC who are currently being treated with androgen deprivation therapy (ADT) and are at high risk for developing metastatic disease. (orion.fi)

Enzalutamide is an antiandrogen, and acts as an antagonist of the androgen receptor, the biological target of androgens like testosterone and dihydrotestosterone. (wikipedia.org)
There is good evidence that enzalutamide is an effective treatment for increasing overall survival among people with high-risk non-metastatic castration-resistant prostate cancer, particularly those with a PSA doubling time ≤ 6 months. (wikipedia.org)
This is thought to be due to enzalutamide crossing the blood-brain barrier and exerting off-target binding to and inhibition of the GABAA receptor in the central nervous system (it has been found to inhibit the GABAA receptor in vitro (IC50Tooltip half-maximal inhibitory concentration = 3.6 μM) and induces convulsions in animals at high doses). (wikipedia.org)
In addition to seizures, other potentially GABAA receptor-related side effects observed with enzalutamide treatment in clinical trials have included anxiety, insomnia, vertigo, paresthesia, and headache. (wikipedia.org)
NSAA-induced seizures are responsive to benzodiazepine treatment, and it has been suggested that GABAA receptor inhibition by enzalutamide could be treated with these drugs. (wikipedia.org)
The mechanism of action of the side effect is unknown, but it was proposed to a consequence of inhibition of the GABAA receptor by enzalutamide. (wikipedia.org)
In a clinical study of enzalutamide for ERTooltip estrogen receptor-positive breast cancer in women, enzalutamide was found to decrease serum concentrations of the aromatase inhibitors anastrozole and exemestane by 90% and 50%, respectively, which could reduce their effectiveness. (wikipedia.org)
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)
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)
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)
Ralaniten Sensitizes Enzalutamide-Resistant Prostate Cancer to Ionizing Radiation in Prostate Cancer Cells that Express Androgen Receptor Splice Variants. (bcgsc.ca)
The androgen receptor inhibitor, Enzalutamide, proved effective against castration resistance prostate cancer, has demonstrated clinical benefits and increased survival rate in men. (uea.ac.uk)
However, AR mutation (F876L) converts Enzalutamide from antagonist to agonist indicating a rapid evolution of resistance. (uea.ac.uk)
We designed a dataset of Enzalutamide derivatives using Enzalutamide's shape and electrostatic features to match with pharmacophoric features essential for tight binding with the androgen receptor. (uea.ac.uk)
Enzalutamide is a well-tolerated, modern androgen receptor antagonist (ARA) with more enhanced anti-tumor activity compared to previous ARAs. (survivornet.com)
Determine if prostate-specific antigen (PSA)-TRICOM combined with enzalutamide will increase time to progression (as defined by Prostate Cancer Clinical Trials Working Group 2 criteria, incorporated in section 5.2) in chemotherapy-naive metastatic castration resistant prostate cancer patients compared to enzalutamide alone. (survivornet.com)
Among the current treatments, (R)-bicalutamide and enzalutamide are non-steroidal androgen receptor antagonist drugs approved also in the case of castration-resistant forms. (cardiff.ac.uk)
Enzalutamide, a 2nd generation androgen receptor antagonist , inhibits the androgen receptor signaling pathway and is used for the therapy of metastatic castration-resistant prostate cancer. (altmeyers.org)
New drugs including abiraterone acetate (AA) and enzalutamide, effectively target the androgen pathway to arrest aberrant signalling even after multiple therapies. (springeropen.com)
2012 ). Even for the second-generation anti-androgen enzalutamide a ligand binding domain mutation has been identified which converts the drug from an AR antagonist to an AR agonist. (springeropen.com)
Cell lines with experimentally derived AR gene rearrangements displayed high expression of tumor-specific AR-Vs andwere resistant to endocrine therapies, including the AR antagonist enzalutamide. (wustl.edu)
Andrew Laccetti, MD, MS, discusses results from a phase 1 trial of masofaniten monotherapy in patients with metastatic castration-resistant prostate cancer and highlights the rationale for launching a phase 1/2 study evaluating masofaniten in combination with enzalutamide vs enzalutamide alone in this patient population. (onclive.com)
Andrew Laccetti, MD, MS, medical oncologist, assistant attending, Genitourinary Medical Oncology, Memorial Sloan Kettering Cancer Center, discusses results from a phase 1 trial (NCT04421222) of masofaniten (EPI-7386) monotherapy in patients with metastatic castration-resistant prostate cancer (mCRPC) and highlights the rationale for launching a phase 1/2 study (NCT05075577) evaluating masofaniten in combination with enzalutamide (Xtandi) vs enzalutamide alone in this patient population. (onclive.com)
Enzalutamide competes with androgens to bind AR, and inhibits AR binding to AREs and androgen-regulated transcription (9 therefore,16). (azd1152.com)
Utilizing a high-resolution ChIP-exo strategy, we recently discovered that enzalutamide induces AR binding towards the book binding theme 5-NCHKGNnndDCHDGN, stimulating the manifestation of many antagonist-responsive, cancer-relevant genes (e.g. siRNA pool (Dharmacon, ON-TARGETplus Human being GATA2 siRNA SMARTpool) or a control siRNA pool RU.521 (RU320521) (Dharmacon, ON-TARGETplus Non-targeting SMARTpool). (azd1152.com)
on androgen synthesis and/or AR signaling such as for example abiraterone and MDV3100/enzalutamide respectively demonstrate medical advantage to CRPC individuals[20-22]. (buyresearchchemicalss.net)
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)
Prior treatment with first-generation AR antagonists (i.e., bicalutamide, nilutamide, flutamide) before abiraterone or enzalutamide is allowed. (mayo.edu)
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)
Given clinical response to immunotherapies in metastatic RCC, these therapies are being tested as monotherapy and in combination with vascular endothelial growth factor receptor tyrosine kinase inhibitors in the (neo)adjuvant setting. (bvsalud.org)
The binding mechanism of potential androgen receptor inhibitors was further studied by molecular docking, molecular dynamics simulations and MM-GBSA binding free energy calculations and found in agreement with the in vitro studies. (uea.ac.uk)
Standard of care for castration-resistant prostate cancer involves androgen receptor signaling inhibitors (ARSI), but this treatment is largely ineffective because of the development of ARSI drug resistance. (mdedge.com)
BAY 2731954 is currently in Phase I clinical development and designed for patients with cancers that harbor a neurotrophic tyrosine receptor kinase ( NTRK ) gene fusion and have progressed or were intolerant to prior TRK inhibitors. (gdc4gpat.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)

Apalutamide, a nonsteroidal potent androgen receptor antagonist, was safe and effective in patients with non-metastatic castration-resistant prostate cancer (nmCRPC) and metastatic-CRPC (mCRPC) in global studies. (endourology.ph)
Unfortunately, these therapies fail to maintain a durable clinical effectiveness, as patients eventually succumb to castration-resistant prostate cancer (CRPC). (ubc.ca)
Various molecular mechanisms have been implicated in the progression from hormone-sensitive to castration-resistant prostate cancer (CRPC). (escholarship.org)
Therapies for lethal castration-resistant prostate cancer (CRPC) are an unmet medical need. (bcgsc.ca)
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)
Recent breakthrough therapies targeting androgen receptor signalling in castration resistant prostate cancer (CRPC) involve multifunctional androgen receptor (AR) blockade and exhaustive androgen deprivation. (springeropen.com)
AA treatments of AR positive CRPC cell models led to decreased expression of androgen regulated genes such as PSA. (springeropen.com)
Castration-resistant prostate cancer (CRPC) is a lethal stage of the disease that emerges when endocrine therapies are no longer effective at suppressing activity of the androgen receptor (AR) transcription factor. (wustl.edu)
These SARDs exhibit the ability to effectively degrade the androgen receptor, hence offering potential therapeutic benefits in the management of castration-resistant cancer (CRPC). (rhodeislandchronicle.com)
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)
Over the past decade, the treatment landscape in metastatic castration-resistant prostate cancer (CRPC) has markedly changed, with the introduction of three new chemotherapeutic agents. (touchoncology.com)
The mechanism of CRPC is not fully understood, but it may result from multiple pathways, including a loss or androgen receptor (AR) specificity and increased downstream signalling activity that provide multiple targets for therapeutic agents. (touchoncology.com)
The androgen signaling pathway has recently been found to be critical in both hormone-sensitive prostate cancer and CRPC. (touchoncology.com)
a second-generation AR antagonist displaying solid anti-cancer activity with an growing application to individual look after both castration-resistant prostate tumor (CRPC) and hormone RU.521 (RU320521) delicate prostate tumor (HSPC) (9,10). (azd1152.com)
Incredibly this SARD maintained anti-proliferative activity in cell lines resistant to current standard-of-care medicines for castration-resistant prostate tumor (CRPC). (buyresearchchemicalss.net)
Furthermore in CRPC the first-generation anti-androgen medicines such as for example bicalutamide[19] and flutamide[18] may screen AR agonist activity. (buyresearchchemicalss.net)
Hypothesizing that improved AR amounts may drive the introduction of CRPC and taking into consideration Ibuprofen Lysine (NeoProfen) the medical success from the selective estrogen receptor degrader (SERD) fulvestrant[23] we wanted to induce AR degradation via our hydrophobic tagging strategy. (buyresearchchemicalss.net)
Prostate cancer that is treated with ADT but keeps progressing even when the amount of testosterone is reduced to very low levels in the body is known as castration-resistant prostate cancer (CRPC). (orion.fi)

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)
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)
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)

Spironolactone, an aldosterone antagonist, competes with testosterone and dihydrotestosterone at the androgen receptor. (weiss.ge)
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)
Within cells, the hormones are converted to the more potent dihydrotestosterone (DHT) metabolites, which function as intracellular signals operating via the androgen receptor (AR, a ligand-dependent transcription factor), ultimately leading to tumor growth. (touchoncology.com)
Some urologists add a third drug, finasteride, which blocks the conversion of testosterone to a more potent androgen, dihydrotestosterone, or DHT. (bcm.edu)
The androgen receptor (AR)[14] can be a ligand-dependent transcription element that upon binding towards the androgen dihydrotestosterone (DHT) goes through Ibuprofen Lysine (NeoProfen) a conformational modification resulting in homodimerization nuclear translocation and upregulation of gene transcription. (buyresearchchemicalss.net)

This includes the use of Gonadotropin-releasing hormone (Luteinizing-hormone releasing hormone) agonists and antagonists suppressing the production of testosterone, and non-steroidal anti-androgens (e.g. (oncotarget.com)
Referred to as complete androgen blockade, or CAB, this treatment choice combines an orchiectomy or LH-RH antagonist with anti-androgens, drugs that block the effects of adrenal gland hormones by influencing a receptor in the nucleus of the prostate cancer cell. (bcm.edu)

Novel selective androgen receptor degraders (SARDs) were identified in a collaborative effort with Dr. Ramesh Narayanan. (rhodeislandchronicle.com)
To do this we designed some selective androgen receptor degraders (SARDs) predicated on the high affinity AR agonist RU59063[24] linked via a brief PEG linker for an adamantyl group (Shape 1A) a hydrophobic degron been shown to be effective inside our previous use Halotag fusion proteins. (buyresearchchemicalss.net)
A) Constructions of Selective Androgen Receptor Degraders (SARDs) predicated on the androgen receptor agonist RU59063. (buyresearchchemicalss.net)

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)
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)

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)
DHT binds with the androgen receptor and induces transcription of proteins necessary for function and development of the prostate. (abdominalkey.com)
Darolutamide is an androgen receptor inhibitor (ARi) with a distinct chemical structure that binds to the receptor with high affinity and exhibits strong antagonistic activity, thereby inhibiting the receptor function and the growth of prostate cancer cells. (orion.fi)

Castration reduced the expression of R1 mRNA in SNB motoneurons, an effect that was blocked by androgen replacement in castrates. (jneurosci.org)

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

IADT is usually applied when there is a response to treatment with reintroduction of medical castration on progression of disease. (abdominalkey.com)
5-7 Figure 1 presents a simplified disease progression pathway illustrating the conversion of cholesterol to androgen and testosterone. (touchoncology.com)
While initially able to suppressing tumor development this strategy generally leads towards the progression of the AR-dependent however androgen independent type of the condition (i.e. (buyresearchchemicalss.net)

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)
The mode of action of these new compounds is either inhibition of androgen synthesis at the CYP17A1 enzyme covering also adrenal and intracrine androgen sources, or a full androgen receptor (AR) blockade antagonizes the AR function by directly binding this transcription factor with high affinity. (springeropen.com)

In medical castration with gonadotropin-releasing hormone (GnRH) agonists, a flare in serum testosterone may result from an initial short-term surge of luteinizing hormone (LH), worsening the symptoms. (thieme-connect.com)
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)

An open-label, phase 1 study of androgen receptor antagonist, apalutamide in Japanese patients with metastatic castration-resistant prostate cancer. (endourology.ph)
Apalutamide may help fight prostate cancer by blocking the use of androgen by the tumor cells. (dana-farber.org)

In 1998, the first nonsteroidal selective androgen receptor modulators (SARMs) were discovered and documented by Dr. Miller and Dr. Jim Dalton, who now holds the position of Provost, The University of Alabama. (rhodeislandchronicle.com)

The presentation will highlight preclinical data in prostate cancer cell lines that demonstrate the company's glucocorticoid receptor (GR) antagonist, ORIC-101, reversing GR-mediated resistance to an androgen receptor (AR) degrader. (oricpharma.com)
ORIC's lead product candidate, ORIC-101, is a potent and selective small molecule antagonist of the glucocorticoid receptor, which has been linked to resistance to multiple classes of cancer therapeutics across a variety of solid tumors. (oricpharma.com)
Here we set out to analyze whether MCL1, a known mediator of chemotherapy resistance regulates the cellular response to androgen withdrawal. (oncotarget.com)
These outcomes claim that selective AR degradation could be an effective restorative prostate Ibuprofen Lysine (NeoProfen) tumor technique in the framework of AR mutations that confer level of resistance to third era AR antagonists. (buyresearchchemicalss.net)

The primary goal was to evaluate the efficacy of degarelix in achieving and maintaining testosterone suppression to castration levels (≤50 ng/dL) over 1 year. (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)

Within the last three years two alternative anti-androgen strategies reached clinical application offering new options in both pre- and post-chemotherapy setting which emphasises the androgen receptor as sustained therapy target in prostate cancer. (springeropen.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)
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)
Long-term androgen therapy has been demonstrated to prolong the QT interval. (formularywatch.com)
Most prostate cancer cells have receptors for testosterone and are potential targets for hormone therapy. (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)

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)

ADT can be applied by surgical bilateral orchiectomy or medical castration. (abdominalkey.com)
This method is cost saving, offers potentially fewer injections and clinic visits, and is equally as effective as medical castration in controlling prostate cancer. (abdominalkey.com)
Despite this, medical castration is much more frequently used than surgical orchiectomy in North America. (abdominalkey.com)
With medical castration, psychological issues of surgical castration can be avoided. (abdominalkey.com)
ADT can be offered in the form of bilateral orchiectomy (surgical castration) or medical castration. (thieme-connect.com)
Bilateral orchiectomy may be appropriate when a rapid decline in testosterone is needed (e.g., worsening obstructive urinary symptoms and imminent cord compression) or when cost or compliance to medical castration is a concern. (thieme-connect.com)

the glucocorticoid receptor (GR) another steroid receptor not really identified by the mother or father ligand RU59063 isn't degraded in LNCaP cells under circumstances that bring about near-complete degradation from the androgen receptor. (buyresearchchemicalss.net)

That's why medications that lower testosterone levels (for example, leuprolide) and castration are common treatments for men with prostate cancer. (weiss.ge)

One possible strategy is to encapsulate the small molecule drug and the key piece of NXTAR into nanoparticles, perhaps into the same nanoparticle, and shut down the androgen receptor in two different ways. (genengnews.com)

In another oral presentation, new pre-clinical data on the investigational androgen receptor (AR) antagonist darolutamide will be presented. (gdc4gpat.com)
ODM-201 (BAY-1841788) is an investigational oral androgen receptor (AR) antagonist that has a unique chemical structure designed to block the growth of cancer cells through binding to the AR with high affinity and inhibiting the receptor function. (orion.fi)

The morphology of SNB motoneurons is maintained by testicular androgens secreted in adulthood. (jneurosci.org)

Background- Darolutamide is a structurally unique androgen-receptor antagonist that is under development for the treatment of prostate cancer. (carolinaurologicresearchcenter.com)
We evaluated the efficacy of darolutamide for delaying metastasis and death in men with nonmetastatic, castration-resistant prostate cancer. (carolinaurologicresearchcenter.com)
Bayer recently submitted darolutamide for approval in the U.S., EU and Japan based on the data from the Phase III ARAMIS study, which investigated darolutamide in non-metastatic castration-resistant prostate cancer. (gdc4gpat.com)
The Japanese Ministry of Health, Labor and Welfare (MHLW) has granted marketing authorization for darolutamide, under the brand name Nubeqa®, for the treatment of men with non-metastatic castration-resistant prostate cancer (nmCRPC). (orion.fi)

Androgen production takes place mainly in the testes, with a small contribution from the adrenal glands. (abdominalkey.com)
Androgens produced by the adrenal glands are androstenedione and dehydroepiandrosterone. (abdominalkey.com)
The adrenal androgens play a role in the development of castrate resistant prostate cancer. (abdominalkey.com)

About 70 percent of breast cancers contain estrogen receptors and can have their growth stimulated by the presence of estrogen. (sutterhealth.org)

R2A and R2B mRNA expression in SNB cells was not affected by androgen manipulations. (jneurosci.org)
The NMDA receptor has been implicated in many instances of neural plasticity, including estrogen-induced morphological changes of hippocampal pyramidal cells. (jneurosci.org)
In these cells diminished expression of androgen regulated genes was accompanied by an up-regulation of CYP17A1 expression within short-term treatments. (springeropen.com)
Using PCa cellular models in vitro and in vivo we show that MCL1 expression is upregulated in androgen-deprived PCa cells. (oncotarget.com)
The BH3-mimetic Obatoclax induces apoptosis and decreases MCL1 expression in androgen-sensitive PCa cells, while castration-resistant PCa cells are less sensitive and react with an upregulation of MCL1 expression. (oncotarget.com)
Altogether, our results suggest that MCL1 is a key molecule deciding over the fate of PCa cells upon inactivation of androgen receptor signaling. (oncotarget.com)
It is those androgen-insensitive cells that scientists believe eventually grow, reproduce and ultimately cause death. (bcm.edu)
These drugs bind themselves to the receptors on the cancer cells, preventing testosterone from binding to them and promoting cell growth. (sutterhealth.org)
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)
Immature B cells from normal mouse bone marrow were not responsive to the suppressive effect of androgens unless they were cocultured with marrow stromal cells or with supernatants from androgen-treated stromal cells, suggesting that the androgen effects are exerted through marrow stromal elements by production of a diffusible mediator. (jci.org)
The stromal cell requirement for androgen-mediated effects was confirmed in vivo by experiments using chimeric animals created by bone marrow transplantation in which androgen receptor expression was restricted to either the stromal or lymphoid cells of the bone marrow. (jci.org)
Androgens only affected B cell development in chimeric mice with androgen-sensitive stromal cells. (jci.org)
These experiments suggest that effects of androgens on developing B cells are mediated through androgen receptors in bone marrow stromal cells. (jci.org)

Castration of normal male mice induces expansion of the bone marrow B cell population, an effect that can be reversed by androgen replacement. (jci.org)

ORIC-101 was shown to completely reverse these effects and block tumor cell growth and androgen-regulated gene expression. (oricpharma.com)
NTRK gene fusions are genomic alterations resulting in constitutively-activated tropomyosin receptor kinase (TRK) fusion proteins, which may lead to tumor growth. (gdc4gpat.com)
AR regulates RU.521 (RU320521) focus on gene manifestation through binding to androgen reactive components (AREs) in the current presence of androgens (2,15). (azd1152.com)

It is indicated for use in conjunction with castration in the treatment of metastatic castration-resistant prostate cancer (mCRPC), nonmetastatic castration-resistant prostate cancer, and metastatic castration-sensitive prostate cancer (mCSPC). (wikipedia.org)
Men at least 18 years of age who have advanced castration-resistant prostate cancer. (survivornet.com)
Phase III trial has demonstrated a 4.8 month improvement in survival and a 37% risk reduction in death in metastatic castration resistant prostate cancer (mCRPC) patients who have had previous docetaxel. (survivornet.com)
The data come from a review of biochemical and biophysical approaches to blocking androgen receptor activity in castration-resistant prostate cancer. (mdedge.com)
The compound is currently in Phase III study ARAMIS for high-risk non-metastatic castration-resistant prostate cancer (nmCRPC). (orion.fi)
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)

Androgen receptor (AR), a known person in the NR superfamily, takes on an integral part in the development and starting point of prostate tumor (5,6), and several artificial AR antagonists have already been created to inhibit the actions of endogenous AR ligands (i.e. androgens) (7,8). (azd1152.com)

Androgen Receptor (AR)-dependent transcription is a significant drivers of prostate tumor cell proliferation. (buyresearchchemicalss.net)
in androgen-dependent prostate tumor cell lines. (buyresearchchemicalss.net)

4 Evidence has shown that resistant cancer continues to rely on androgen biosynthesis, its binding to the receptor and consequent uptake in order to progress. (touchoncology.com)

These subsequent drugs are designed to aid individuals in situations when conventional androgen receptor antagonists have proven ineffective in the treatment of prostate cancer. (rhodeislandchronicle.com)

Based on these data, ADT alone should no longer be considered sufficient for patients with advanced, castration-sensitive disease. (jnj.com)

Androgen receptor (AR), a transcription factor, is a validated therapeutic target for prostate cancer. (ubc.ca)

Anatomy14

Organisms8

Diseases11

Chemicals and Drugs144

Analytical, Diagnostic and Therapeutic Techniques and Equipment15

Psychiatry and Psychology3

Phenomena and Processes29

Disciplines and Occupations1

Anthropology, Education, Sociology and Social Phenomena1

Information Science3

Health Care1

Deprivation therapy17

Enzalutamide30

Inhibitors8

CRPC18

LHRH4

Dihydrotestosterone5

Anti-androgens2

Selective androgen receptor degraders3

Agonists and antagonists2

Binds3

Blocked by androgen replacement1

Inhibitor of androgen1

Progression3

Inhibition of androgen2

GnRH2

Apalutamide2

Nonsteroidal1

Resistance4

Degarelix2

Therapy8

Transcriptional activity1

Medical castration6

Glucocorticoid receptor1

Leuprolide1

Small molecule1

Investigational2

Testicular1

Darolutamide4

Adrenal3

Cancers1

Cells13

Induces1

Gene3

Resistant prostate6

Inhibit1

Tumor cell2

Biosynthesis1

Treatment of prostate cancer1

Patients1

Transcription factor1