The old antiandrogen pill used to block the testosterone flare from GnRH agonists and in combined androgen blockade; superseded by enzalutamide-class drugs.
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 Enzalutamide-class drugs, which bind the receptor without agonism, have superseded it in most guidelines.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.
Competitive AR antagonist with partial agonist activity in AR-amplified or mutated (W741L) disease; combined with GnRH agonists. Connects to Androgen receptor.
1.Bicalutamide acts on Androgen receptor, the hormone receptor or the enzyme that makes the hormone.
Oral, self-administered, so it is a Part D drug: covered through a stand-alone Part D plan or Medicare Advantage drug benefit, usually on the specialty tier with 25 to 33% coinsurance until the annual cap ($2,000 in 2025, $2,100 in 2026). Generic, low cost.
Multi-source generic on low-cost tiers; usually no prior authorisation. Cash prices without insurance are modest.
Sources: Medicare.gov: Drug coverage (Part D) · Medicare.gov: Costs for Medicare drug coverage (annual out-of-pocket cap). Not medical or financial advice; verify with your plan.
Sources: NICE search: bicalutamide. Funding decisions are indication-specific and change monthly; verify with NICE and your treating team.
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In combination with an LHRH analogue for advanced prostate cancer
Accelerated approval on a surrogate endpoint, with a confirmatory trial required.
In combination with an LHRH analogue for advanced prostate cancer
Confirmed: the accelerated approval of 1995 converted to traditional approval 2.2 years after it was granted.
| Region | Year | Indication |
|---|---|---|
| US | 1995 | Metastatic prostate cancer with LHRH analogue |
| EU | 1995 | Advanced prostate cancer; 150 mg for locally advanced |
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It fixes the AR-positive share of ER-negative disease at about one in eight and shows anti-androgens give modest, non-toxic benefit, the rationale for enzalutamide and later CDK4/6 and PI3K combinations in LAR tumours.
The reason intermittent androgen deprivation is offered as a choice in metastatic disease rather than recommended, and a case study in what an inconclusive non-inferiority trial should say. For a man weighing the side effects, the honest statement is that the quality-of-life gain is real but brief and the survival question is open.
The design specification for the second-generation antiandrogens. A drug for castration-resistant prostate cancer has to stay an antagonist when the receptor is abundant, which is what enzalutamide, apalutamide and darolutamide were engineered to do and what bicalutamide fails to do.
Query for this drug: (TITLE:"Bicalutamide" OR ABSTRACT:"Bicalutamide" OR TITLE:"Casodex" OR ABSTRACT:"Casodex") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Bicalutamide, not a curated reading list.
Shares Assessing Efficacy of Neoadjuvant ADT in Localized High-Risk Prostate Cancer Patients Utilizing 18F-Flotufolastat PSMA PET/CT, Hormone Therapy in Treating Patients With Rising PSA Levels Following Radiation Therapy for Prostate Cancer, Hormone Therapy With or Without Surgery or Radiation Therapy in Treating Patients With Prostate Cancer, Standard Systemic Therapy With or Without Definitive Treatment in Treating Participants With Metastatic Prostate Cancer and the tag generic.
Shares AstraZeneca and the tag generic.
Shares Prostate cancer and the tag generic.
Shares Triple-negative breast cancer (TNBC) and the tag generic.
Shares Triple-negative breast cancer (TNBC) and the tag generic.
Shares Triple-negative breast cancer (TNBC), Prostate cancer and the tag generic.
Shares Standard Systemic Therapy With or Without Definitive Treatment in Treating Participants With Metastatic Prostate Cancer, Prostate cancer and the tag generic.
Shares Hormone Therapy Plus Radiation Therapy With or Without Combination Chemotherapy in Treating Patients With Prostate Cancer and the tag generic.