{"entity":{"id":"bicalutamide","kind":"drug","name":"Bicalutamide","aka":[],"tldr":"The old antiandrogen pill used to block the testosterone flare from GnRH agonists and in combined androgen blockade; superseded by enzalutamide-class drugs.","summary":"Bicalutamide is an oral first-generation non-steroidal antiandrogen that competes with testosterone and dihydrotestosterone for the androgen receptor. It has partial agonist activity in tumours with AR amplification or the W741L mutation, which explains the antiandrogen withdrawal response seen when it is stopped. It was approved in the US and EU in 1995 for metastatic prostate cancer in combination with an LHRH agonist, and in the EU a 150 mg monotherapy dose is licensed for locally advanced disease. It is still used to block the testosterone flare at the start of agonist therapy and remains a mainstay in low-resource settings because it is cheap and well tolerated. Enzalutamide-class drugs, which bind the receptor without agonism, have superseded it in most guidelines. Bicalutamide is the old antiandrogen pill whose limits taught the field how to build better ones.","status":"approved","asOf":"2026-09-08","wikipedia":"https://en.wikipedia.org/wiki/Bicalutamide","links":[{"label":"Label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=bicalutamide"}],"tags":["gap-fill","generic"],"related":[],"cancers":["prostate","salivary-duct-carcinoma","tnbc"],"sections":[],"technologies":["androgen-deprivation"],"targets":["androgen-receptor"],"drugs":[],"companies":["astrazeneca"],"institutions":[],"pathways":["ar-signaling"],"terms":[],"trials":["rtog-9601","nct02531516"],"people":[],"bottlenecks":[],"keyPapers":["paper-gucalp-bicalutamide-ar-positive-tbcrc011-ccr-2013"],"journals":[],"dependsOn":[],"notes":[],"brand":"Casodex","modality":"Oral first-generation non-steroidal antiandrogen","mechanism":"Competitive AR antagonist with partial agonist activity in AR-amplified or mutated (W741L) disease; combined with GnRH agonists.","approvals":[{"region":"US","year":1995,"indication":"Metastatic prostate cancer with LHRH analogue"},{"region":"EU","year":1995,"indication":"Advanced prostate cancer; 150 mg for locally advanced"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[{"date":"1995-10-04","type":"accelerated-approval","region":"US","note":"Accelerated approval on a surrogate endpoint, with a confirmatory trial required.","indication":"In combination with an LHRH analogue for advanced prostate cancer"},{"date":"1997-12-12","type":"conversion","region":"US","note":"Confirmed: the accelerated approval of 1995 converted to traditional approval 2.2 years after it was granted.","indication":"In combination with an LHRH analogue for advanced prostate cancer"}]},"route":"/drugs/bicalutamide/","neighbours":{"cancer":[{"id":"apocrine-carcinoma-breast","kind":"cancer","name":"Apocrine carcinoma of the breast","route":"/cancers/apocrine-carcinoma-breast/"},{"id":"prostate-bcr","kind":"cancer","name":"Biochemical recurrence of prostate cancer","route":"/cancers/prostate-bcr/"},{"id":"tnbc-luminal-androgen-receptor","kind":"cancer","name":"Luminal androgen receptor triple-negative breast cancer (LAR)","route":"/cancers/tnbc-luminal-androgen-receptor/"},{"id":"prostate-nmcrpc","kind":"cancer","name":"Non-metastatic castration-resistant prostate cancer","route":"/cancers/prostate-nmcrpc/"},{"id":"prostate","kind":"cancer","name":"Prostate cancer","route":"/cancers/prostate/"},{"id":"salivary-duct-carcinoma","kind":"cancer","name":"Salivary duct carcinoma","route":"/cancers/salivary-duct-carcinoma/"},{"id":"tnbc","kind":"cancer","name":"Triple-negative breast cancer (TNBC)","route":"/cancers/tnbc/"}],"technology":[{"id":"androgen-deprivation","kind":"technology","name":"Androgen deprivation & AR pathway inhibitors","route":"/technologies/androgen-deprivation/"}],"target":[{"id":"androgen-receptor","kind":"target","name":"Androgen receptor","route":"/targets/androgen-receptor/"}],"company":[{"id":"astrazeneca","kind":"company","name":"AstraZeneca","route":"/companies/astrazeneca/"}],"pathway":[{"id":"ar-signaling","kind":"pathway","name":"Androgen receptor signalling","route":"/pathways/ar-signaling/"}],"trial":[{"id":"nct02531516","kind":"trial","name":"An Efficacy and Safety Study of JNJ-56021927 (Apalutamide) in High-risk Prostate Cancer Subjects Receiving Primary Radiation Therapy: ATLAS","route":"/trials/nct02531516/"},{"id":"nct07455903","kind":"trial","name":"Assessing Efficacy of Neoadjuvant ADT in Localized High-Risk Prostate Cancer Patients Utilizing 18F-Flotufolastat PSMA PET/CT","route":"/trials/nct07455903/"},{"id":"nct06365788","kind":"trial","name":"Bicalutamide and Abemaciclib in Inoperable or Metastatic Androgen Receptor-positive Triple-negative Breast Cancer","route":"/trials/nct06365788/"},{"id":"dart-01-05-gicor","kind":"trial","name":"DART 01/05 GICOR","route":"/trials/dart-01-05-gicor/"},{"id":"nct00003653","kind":"trial","name":"Hormone Therapy in Treating Patients With Rising PSA Levels Following Radiation Therapy for Prostate Cancer","route":"/trials/nct00003653/"},{"id":"nct00004054","kind":"trial","name":"Hormone Therapy Plus Radiation Therapy With or Without Combination Chemotherapy in Treating Patients With Prostate Cancer","route":"/trials/nct00004054/"},{"id":"nct00055731","kind":"trial","name":"Hormone Therapy With or Without Docetaxel And Estramustine in Treating Patients With Prostate Cancer That is Locally Advanced or At High Risk of Relapse","route":"/trials/nct00055731/"},{"id":"nct00002633","kind":"trial","name":"Hormone Therapy With or Without Surgery or Radiation Therapy in Treating Patients With Prostate Cancer","route":"/trials/nct00002633/"},{"id":"nct00884273","kind":"trial","name":"Investigation of the Effect of Degarelix in Terms of Prostate Volume Reduction in Prostate Cancer Patients","route":"/trials/nct00884273/"},{"id":"nct00833248","kind":"trial","name":"Neoadjuvant Study Investigating Degarelix in Patients Suffering From Prostate Cancer","route":"/trials/nct00833248/"},{"id":"nct00567580","kind":"trial","name":"Prostate Radiation Therapy or Short-Term Androgen Deprivation Therapy and Pelvic Lymph Node Radiation Therapy With or Without Prostate Radiation Therapy in Treating Patients With a Rising Prostate Specific Antigen (PSA) After Surgery for Prostate Cancer","route":"/trials/nct00567580/"},{"id":"nct00936390","kind":"trial","name":"Radiation Therapy With or Without Androgen-Deprivation Therapy in Treating Patients With Prostate Cancer","route":"/trials/nct00936390/"},{"id":"radicals-hd","kind":"trial","name":"RADICALS-HD","route":"/trials/radicals-hd/"},{"id":"rtog-9601","kind":"trial","name":"RTOG 9601","route":"/trials/rtog-9601/"},{"id":"nct03678025","kind":"trial","name":"Standard Systemic Therapy With or Without Definitive Treatment in Treating Participants With Metastatic Prostate Cancer","route":"/trials/nct03678025/"},{"id":"nct04513717","kind":"trial","name":"Two Studies for Patients With High Risk Prostate Cancer Testing Less Intense Treatment for Patients With a Low Gene Risk Score and Testing a More Intense Treatment for Patients With a High Gene Risk Score, The PREDICT-RT Trial","route":"/trials/nct04513717/"}],"paper":[{"id":"paper-chen-androgen-receptor-overexpression-antiandrogen-resistance-nat-med-2004","kind":"paper","name":"Molecular determinants of resistance to antiandrogen therapy","route":"/key-papers/paper-chen-androgen-receptor-overexpression-antiandrogen-resistance-nat-med-2004/"},{"id":"paper-gucalp-bicalutamide-ar-positive-tbcrc011-ccr-2013","kind":"paper","name":"Phase II trial of bicalutamide in patients with androgen receptor-positive, estrogen receptor-negative metastatic breast cancer","route":"/key-papers/paper-gucalp-bicalutamide-ar-positive-tbcrc011-ccr-2013/"},{"id":"paper-hussain-swog-9346-intermittent-androgen-deprivation-nejm-2013","kind":"paper","name":"SWOG 9346: intermittent versus continuous androgen deprivation in metastatic prostate cancer","route":"/key-papers/paper-hussain-swog-9346-intermittent-androgen-deprivation-nejm-2013/"}],"term":[{"id":"arpi","kind":"term","name":"Androgen receptor pathway inhibitor (ARPI)","route":"/terms/arpi/"},{"id":"androgen-receptor-positive-tnbc","kind":"term","name":"Androgen receptor-positive triple-negative breast cancer","route":"/terms/androgen-receptor-positive-tnbc/"},{"id":"intermittent-androgen-deprivation","kind":"term","name":"Intermittent androgen deprivation (IAD)","route":"/terms/intermittent-androgen-deprivation/"}],"drug":[{"id":"flutamide","kind":"drug","name":"Flutamide","route":"/drugs/flutamide/"},{"id":"nilutamide","kind":"drug","name":"Nilutamide","route":"/drugs/nilutamide/"}],"roadmap":[{"id":"hormonal-therapy-roadmap","kind":"roadmap","name":"Hormonal therapy roadmap: removing the ovaries → tamoxifen → oral degraders switched by a blood test","route":"/roadmaps/hormonal-therapy-roadmap/"}]}}