Drug Class Detail

Drug Class Hormone - Anti-androgens

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Darolutamide BAY1841788|ODM-201 Hormone - Anti-androgens 22 Darolutamide (ODM-201) is an androgen receptor antagonist composed of two diastereomers that binds to and prevents nuclear translocation of the androgen receptor, thereby inhibiting expression of genes downstream of androgen receptor signaling that regulate proliferation of prostate cancer cells (PMID: 28490267).
ASN001 Hormone - Anti-androgens 22 ASN001 selectively binds to and inhibits steroid 17-alpha-hydroxylase/C17,20 lyase (CYP17), which potentially leads to decreased androgen production and in turn, growth inhibition of androgen-dependent tumor cells (NCI Drug Dictionary).
UT-155 Hormone - Anti-androgens 22 UT-155 is a selective androgen receptor degrader (SARD), which decreases expression of the androgen receptor (AR), including wild-type and mutant versions, potentially leading to reduced growth of AR-dependent tumors (PMID: 28978635).
Abiraterone Zytiga CB7630 Hormone - Anti-androgens 22 Zytiga (abiraterone) inhibits cytochrome P-450c17, resulting in decreased androgen synthesis (PMID: 25560485). Zytiga (abiraterone) is FDA approved for patients with metastatic castration-resistant prostate cancer (FDA.gov).
D-0502 Hormone - Anti-androgens 22 D-0502 is a selective estrogen receptor degrader (SERD) that prevents cell proliferation of ER-positive cells (AACR; Cancer Res 2018;78(13 Suppl):Abstract nr 5776).
Bicalutamide Casodex Hormone - Anti-androgens 22 Casodex (bicalutamide) is an androgen-receptor antagonist that binds androgen receptors and inhibits androgen binding, therefore inhibits AR-dependent growth of tumor cells (PMID: 9428389). Casodex (bicalutamide) is approved, in combination with a luteinizing hormone-releasing hormone (LHRH) analog, for metastatic carcinoma of the prostate (FDA.gov).
LY01005 Hormone - Anti-androgens 22 Limited information is currently available on LY01005, a putative extended release formulation of Goserelin (Aug 2018).
TRC253 JNJ-63576253 Hormone - Anti-androgens 22 TRC253 binds androgen receptor (AR), including wild-type AR and some mutant versions, resulting in decreased receptor activation and downstream signaling, and potentially leading to decreased growth of AR-expressing tumor cells (NCI Drug Dictionary).
CFG920 Hormone - Anti-androgens 22 CFG920 inhibits CYP17, resulting in decreased androgen production and potentially leading to reduced proliferation of androgen-dependent tumor cells (NCI Drug Dictionary).
Nilutamide Nilandron Anandron Hormone - Anti-androgens 22 Nilandron (nilutamide) is a nonsteroidal antiandrogen, binding to the androgen receptor and blocking agonists, thereby inhibiting androgen-dependent tumor growth (NCI Drug Dictionary).
FL442 Hormone - Anti-androgens 22 FL442 binds to and inhibits the androgen receptor (AR), resulting in reduction of downstream signaling and decreased tumor growth (PMID: 24565895).
VT-464 Hormone - Anti-androgens 22 VT-464 inhibits CYP17 17,20 lyase activity, resulting in decreased androgen production, which may inhibit growth of androgen-dependent tumors (NCI Drug Dictionary).
galeterone TOK-001 Hormone - Anti-androgens 22 Galeterone functions both as an inhibitor of CYP17A1 and anti-androgen (NCI Drug Dictionary). It binds the androgen receptor, acting as an competitive antagonist and also preventing Ar protein binding to chromatin and enhancing degradation of mutant Ar protein (PMID: 24874833 ).
CH5137291 Hormone - Anti-androgens 22 CH5137291 is an androgen receptor (AR) antagonist that additionally inhibits the nuclear translocation of AR, potentially resulting in decreased tumor growth (PMID: 21050768, PMID: 25634071).
AZD3514 Hormone - Anti-androgens 22 AZD3514 binds to androgen receptor (AR) and inhibits its nuclear translocation and activation, and also inhibits AR protein expression, resulting in decreased tumor cell proliferation (PMID: 23861347).
EPI-506 Hormone - Anti-androgens 22 EPI-506, the prodrug for EPI-002, is a small molecule that inhibits the N-terminal domain of the androgen receptor (AR), potentially resulting in decreased AR signaling, including in the context of mutant AR (PMID: 27628492).
Apalutamide Erleada ARN-509|JNJ-56021927 Hormone - Anti-androgens 22 Erleada (apalutamide) is a second-generation antiandgrogen, that binds to the androgen receptor (AR) and inhibits downstream signaling, potentially resulting in decreased growth of AR-expressing tumors (PMID: 22266222, PMID: 23337756). Erleada (apalutamide) is FDA approved for use in patients with non-metastatic castration-resistant prostate cancer (FDA.gov).
Cyproterone Androcur Cyproterone acetate Hormone - Anti-androgens 22 Androcur (cyproterone) is a steroidal androgen receptor (AR) antagonist, which reduces AR activation and growth of androgen-sensitive tumors (NCI Drug Dictionary).
BMS-641988 Hormone - Anti-androgens 22 BMS-641988 is an androgen receptor (AR) antagonist, which inhibits AR signaling, resulting in decreased tumor growth (PMID: 19654297).
Flutamide Eulexin Flutamide USP25 Hormone - Anti-androgens 22 Eulexin (flutamide) is a nonsteroidal antiandrogen that competitively blocks androgen receptors. Eulexin prevents receptor activation and translocation to the nucleus, thus preventing androgen-dependent DNA and protein synthesis, which may prevent tumor cell growth (NCI Drug Dictionary).
Orteronel TAK-700 Hormone - Anti-androgens 22 Orteronel inhibits CYP17A1, resulting in reduced androgen production and potentially leading to decreased growth of androgen-dependent tumors (PMID: 24799061).
Enzalutamide Xtandi MDV3100 Hormone - Anti-androgens 22 Xtandi (enzalutamide) is a second-generation small molecule androgen receptor (AR) inhibitor that inhibits AR signaling, thereby resulting in decreased tumor growth (PMID: 24009414, PMID: 25945058). Xtandi (enzalutamide) is FDA approved for use in patients with castration-resistant prostate cancer (FDA.gov).
Molecular Profile Protein Effect Treatment Approaches