edgepedia

Hormonal and endocrine therapy

32 articles

Abiraterone

Abiraterone is a steroidal drug that inhibits CYP17A1, an enzyme required for androgen biosynthesis, and is used with prednisone to treat advanced prostate cancer, first US approved in 2011.

Abiraterone/prednisone regimen

The abiraterone/prednisone regimen is a combination drug treatment for metastatic prostate cancer in which abiraterone acetate, an androgen biosynthesis inhibitor, is given with prednisone on androgen deprivation therapy.

AFFIRM trial

AFFIRM trial (NCT00974311): phase 3 study of enzalutamide (MDV3100) versus placebo in 1,199 men with metastatic castration-resistant prostate cancer after docetaxel; median survival 18.4 vs 13.6 months. Distinct from the atrial fibrillation AFFIRM trial.

Amcenestrant

Amcenestrant (SAR439859) is Sanofi's oral selective estrogen receptor degrader for ER-positive breast cancer; its AMEERA program failed phase 2/3 endpoints and development was discontinued in August 2022.

Androgen deprivation therapy

Androgen deprivation therapy (ADT) is a prostate cancer treatment that suppresses testosterone or blocks androgen receptors to slow tumor growth, used from recurrence to metastatic disease.

Apalutamide

Apalutamide (ARN-509, Erleada) is Janssen's oral androgen receptor inhibitor for prostate cancer; FDA approved February 2018 for nmCRPC after SPARTAN doubled metastasis-free survival, expanded 2019 to mCSPC after TITAN.

CFG920 (LAE001)

CFG920 (LAE001, lapiteronel) is an oral non-steroidal dual CYP17A1/CYP11B2 inhibitor for prostate cancer, discovered by Novartis and licensed worldwide to Laekna in 2017.

Chemohormonal therapy

Chemohormonal therapy is a cancer treatment combining chemotherapy with hormonal therapy, principally six cycles of docetaxel added to androgen deprivation therapy, which prolongs survival in metastatic hormone-sensitive prostate cancer.

Darolutamide

Darolutamide (Nubeqa, ODM-201) is an oral androgen receptor inhibitor by Bayer for prostate cancer, approved 2019 (US) and 2020 (EU), with low brain penetration, few drug interactions, and favorable tolerability versus enzalutamide and apalutamide.

Degarelix

Degarelix (Firmagon, FE200486) is an injectable GnRH antagonist peptide by Ferring for advanced hormone-dependent prostate cancer; 240 mg then 80 mg monthly, rapid castration without flare, main drawback injection-site reactions.

Deutenzalutamide soft capsules

Deutenzalutamide soft capsules (氘恩扎鲁胺软胶囊, Haina'an, HC-1119) are Hinova Pharmaceuticals' deuterated enzalutamide analog, an androgen receptor inhibitor approved in China in May 2025 for mCRPC after abiraterone and chemotherapy, dosed 80 mg daily.

Diethylstilbestrol diphosphate

Diethylstilbestrol diphosphate (fosfestrol, DESP; brands Stilphostrol, Honvan) is the diphosphate ester prodrug of the synthetic estrogen DES, used mainly for prostate cancer; discontinued in the US, thrombosis is a key toxicity.

Docetaxel plus enzalutamide

Docetaxel plus enzalutamide is a combination regimen for advanced prostate cancer pairing the chemotherapy docetaxel with the androgen receptor inhibitor enzalutamide, studied in metastatic disease but not approved as a combination.

Droloxifene

Droloxifene (3-hydroxytamoxifen), a phenolic tamoxifen analogue SERM with 10-60x higher ER affinity and a ~24 h half-life, was inferior to tamoxifen in phase III breast cancer trials and never registered.

Elacestrant

Elacestrant (Orserdu, Korserdu; RAD1901) is an oral selective estrogen receptor degrader approved by the FDA in January 2023 for ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer after endocrine therapy, based on the phase III EMERALD trial.

Everolimus and letrozole regimen

The everolimus and letrozole regimen is an oral combination therapy for hormone receptor-positive, HER2-negative breast cancer, pairing the mTOR inhibitor everolimus with letrozole to overcome endocrine resistance.

Fulvestrant regimen

The fulvestrant regimen is a hormonal cancer treatment for hormone receptor-positive advanced breast cancer, in which fulvestrant 500 mg is injected monthly, alone or combined with the CDK4/6 inhibitor abemaciclib.

Galeterone

Galeterone (TOK-001, VN/124-1) is a steroidal CYP17A1 inhibitor, androgen receptor antagonist, and AR degrader developed for prostate cancer; its phase 3 ARMOR3-SV trial versus enzalutamide in AR-V7-positive metastatic CRPC stopped early and development was discontinued.

Giredestrant

Giredestrant (GDC-9545), Roche's investigational oral SERD for ER-positive, HER2-negative breast cancer; full ER antagonist that immobilizes then degrades the receptor; positive phase III lidERA and evERA trials, FDA NDAs under priority review.

Glufosfamide

Glufosfamide (beta-D-glucosyl-isophosphoramide mustard, D19575) is an investigational glucose-conjugated alkylating prodrug of ifosfamide mustard, cleaved by intracellular glucosidases; tested through phase III mainly in pancreatic cancer without approval.

Hexestrol

Hexestrol (hexoestrol, CAS 84-16-2) is a synthetic non-steroidal estrogen, a hydrogenated diethylstilbestrol derivative used as a hormonal antineoplastic agent, carcinogenic in hamsters and a Lassa virus entry inhibitor.

JMKX002992 (oral AR degrader)

JMKX002992 (JMKX-002992) is an oral PROTAC androgen receptor degrader for prostate cancer from Jemincare, licensed worldwide to Roche/Genentech in 2022 for $60M upfront and up to $650M total.

Nilutamide

Nilutamide (Nilandron) is a first-generation nonsteroidal antiandrogen, FDA approved 9 September 1996, used with surgical castration for Stage D2 metastatic prostate cancer; 300 mg/day for 30 days then 150 mg daily, half-life about 56 hours.

Ovarian suppression

Ovarian suppression, also called ovarian function suppression, is a treatment that stops the ovaries from producing estrogen, used to treat hormone-receptor-positive breast cancer in premenopausal women.

Palazestrant

Palazestrant (OP-1250) is Olema Oncology's investigational oral complete estrogen receptor antagonist (CERAN) and selective ER degrader (SERD) for ER+/HER2- metastatic breast cancer, in phase 3 trials OPERA-01 and OPERA-02.

Pruxelutamide

Pruxelutamide (proxalutamide, GT0918), a second-generation androgen receptor antagonist from Suzhou Kintor, developed for prostate cancer and trialed for breast cancer and COVID-19.

Rezvilutamide

Rezvilutamide (SHR3680, Ariane) is an oral nonsteroidal androgen receptor antagonist by Jiangsu Hengrui, approved in China in 2022 for high-volume metastatic hormone-sensitive prostate cancer based on the CHART trial versus bicalutamide.

Tamoxifen regimen

A tamoxifen regimen is a drug treatment schedule built around oral tamoxifen, 20 mg daily, given for about 5 years to treat hormone receptor-positive breast cancer and reduce recurrence.

Testolactone

Testolactone (Teslac, Δ1-testololactone) is a first-generation steroidal aromatase inhibitor used 1970-2008 for advanced breast cancer, precocious puberty, and gynecomastia; discontinued after more potent inhibitors emerged.

Tibremciclib tartrate capsules

Tibremciclib tartrate capsules (泰瑞西利, BPI-16350, brand name Kangmeina) are an oral CDK4/6 inhibitor developed by Betta Pharmaceuticals of Hangzhou, approved in China in 2025 for advanced breast cancer.