Bicalutamide

Bicalutamide is a non-steroidal androgen receptor inhibitor. It competitively inhibits the action of androgens by binding to cytosol androgen receptors in the target tissue.

• Bicalutamide tablets, USP 50 mg daily are indicated for use in combination therapy with a luteinizing hormone-releasing hormone (LHRH) analog for the treatment of Stage D 2 metastatic carcinoma of the prostate. Bicalutamide tablets, USP 150 mg daily are not approved for use alone or with other treatments [see Clinical Studies (14.2)].

• Bicalutamide is contraindicated in: • Hypersensitivity Bicalutamide is contraindicated in any patient who has shown a hypersensitivity reaction to the drug or any of the tablet’s components. Hypersensitivity reactions including angioneurotic edema and urticaria have been reported.contraindicated

The recommended dose for bicalutamide tablets therapy in combination with an LHRH analog is one 50 mg tablet once daily (morning or evening). (2) 2.1 Recommended Dose and Schedule The recommended dose for bicalutamide tablets therapy in combination with an LHRH analog is one 50 mg tablet once daily (morning or evening), with or without food. It is recommended that bicalutamide tablets be taken at the same time each day. Treatment with bicalutamide tablets should be started at the same time as treatment with an LHRH analog. If a dose of bicalutamide tablets is missed, take the next dose at the scheduled time. Do not take the missed dose and do not double the next dose. 2.2 Dosage Adjustment in Renal Impairment No dosage adjustment is necessary for patients with renal impairment [see Use in Specific Populations (8.7)]. 2.3 Dosage Adjustment in Hepatic Impairment No dosage adjustment is necessary for patients with mild to moderate hepatic impairment. In patients with severe liver impairment (n=4), although there was a 76% increase in the half-life (5.9 and 10.4 days for normal and impaired patients, respectively) of the active enantiomer of bicalutamide, no dosage adjustment is necessary [see Use in Specific Populations (8.6)].

• Severe hepatic injury and fatal hepatic failure have been observed. Monitor serum transaminase levels prior to starting treatment with bicalutamide, at regular intervals for the first four months of treatment and periodically thereafter, and for symptoms or signs suggestive of hepatic dysfunction. Use bicalutamide with caution in patients with hepatic impairment. ( 5.1 ) • Hemorrhage with Concomitant Use of Coumarin Anticoagulant. Closely monitor the Prothrombin Time (PT) and International Normalized Ratio (INR), and adjust the anticoagulant dose as needed. ( 5.2 ) • Gynecomastia and breast pain have been reported during treatment with bicalutamide 150 mg when used as a single agent. ( 5.3 ) • Bicalutamide is used in combination with an LHRH agonist. LHRH agonists have been shown to cause a reduction in glucose tolerance in males. Consideration should be given to monitoring blood glucose in patients receiving bicalutamide in combination with LHRH agonists. ( 5.4 ) • Monitoring Prostate Specific Antigen (PSA) is recommended. Evaluate for clinical progression if PSA increases. ( 5.5 ) 5.1 Hepatitis Cases of death or hospitalization due to severe liver injury (hepatic failure) have been reported postmarketing in association with the use of bicalutamide. Hepatotoxicity in these reports generally occurred within the first three to four months of treatment. Hepatitis or marked increases in liver enzymes leading to drug discontinuation occurred in approximately 1% of bicalutamide patients in controlled clinical trials.

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Adverse reactions that occurred in more than 10% of patients receiving bicalutamide plus an LHRH-A were: hot flashes, pain (including general, back, pelvic and abdominal), asthenia, constipation, infection, nausea, peripheral edema, dyspnea, diarrhea, hematuria, nocturia, and anemia. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Sun Pharmaceutical Industries, Inc. at 1-800-818-4555 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience In patients with advanced prostate cancer treated with bicalutamide in combination with an LHRH analog, the most frequent adverse reaction was hot flashes (53%). In the multi-center, double-blind, controlled clinical trial comparing bicalutamide 50 mg once daily with flutamide 250 mg three times a day, each in combination with an LHRH analog, the following adverse reactions with an incidence of 5% or greater, regardless of causality, have been reported.

• Females and Males of Reproductive Potential: Advise males with female partners of reproductive potential to use effective contraception. ( 8.3 ) • Pediatric patients: Efficacy has not been demonstrated for the treatment of familial male-limited precocious puberty (testotoxicosis). ( 8.4 ) 8.1 Pregnancy Risk Summary Bicalutamide is contraindicated for use in pregnant women because it can cause fetal harm. Bicalutamide is not indicated for use in females. There are no human data on the use of bicalutamide in pregnant women. In animal reproduction studies, oral administration of bicalutamide to pregnant rats during organogenesis caused abnormal development of reproductive organs in male fetuses at exposures approximately 0.7 to 2 times the human exposure at the recommended dose (see Data). Data Animal Data In an embryo-fetal development study in pregnant rats dosed during the period of organogenesis from gestation days 6-15, male fetuses had reduced anogenital distance at doses of 10 mg/kg/day and above (approximately 0.7 to 2 times the human exposure at the recommended dose). In a pre- and post-natal development study, female rats were dosed from gestation day 7-16 and allowed to litter and rear their offspring to weaning.

Metabolism

Absorption Bicalutamide is well-absorbed following oral administration, although the absolute bioavailability is unknown. Coadministration of bicalutamide with food has no clinically significant effect on rate or extent of absorption.

Long-term clinical trials have been conducted with dosages up to 200 mg of bicalutamide daily and these dosages have been well tolerated. A single dose of bicalutamide that results in symptoms of an overdose considered to be life threatening has not been established. There is no specific antidote; treatment of an overdose should be symptomatic. In the management of an overdose with bicalutamide, vomiting may be induced if the patient is alert. It should be remembered that, in this patient population, multiple drugs may have been taken. Dialysis is not likely to be helpful since bicalutamide is highly protein bound and is extensively metabolized. General supportive care, including frequent monitoring of vital signs and close observation of the patient, is indicated.

• Oct 4, 1995NDANDA020498Ani Pharms
• Jul 6, 2009ANDAANDA079089Adaptis
• Jul 6, 2009ANDAANDA078917Accord Hlthcare
• Jul 6, 2009ANDAANDA079110Sun Pharm

The 10 most recently updated of 237 ClinicalTrials.gov registrations naming Bicalutamide as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Pharmacogenomics IND Commercial SNP Clinical Study - Abiraterone and Single Nucleotide Polymorphisms
  Active not recruiting · Phase 2 · Phase 3 · Interventional · 600 enrolled · Han Xu, M.D., Ph.D., FAPCR, Sponsor-Investigator, IRB Chair
  NCT03348670updated 2026-06-10
• An Efficacy and Safety Study of JNJ-56021927 (Apalutamide) in High-risk Prostate Cancer Subjects Receiving Primary Radiation Therapy: ATLAS
  Active not recruiting · Phase 3 · Interventional · 1,503 enrolled · Aragon Pharmaceuticals, Inc.
  NCT02531516updated 2026-06-05
• A Randomized Trial of Bicalutamide in Non-Muscle Invasive Bladder Cancer
  Recruiting · Phase 1 · Interventional · 80 enrolled · University of Wisconsin, Madison
  NCT05521698updated 2026-06-04
• Bicalutamide With or Without Akt Inhibitor MK2206 in Treating Patients With Previously Treated Prostate Cancer
  Active not recruiting · Phase 2 · Interventional · 108 enrolled · National Cancer Institute (NCI)
  NCT01251861updated 2026-05-29
• Bicalutamide Therapy in Young Women With NAFLD and PCOS
  Recruiting · Phase 1 · Interventional · 50 enrolled · University of California, San Francisco
  NCT05979389updated 2026-05-29
• Androgen-responsive POSLUMA-guided Intra-prostatic Boost
  Recruiting · Phase 2 · Interventional · 23 enrolled · Martin T. King, MD, PhD
  NCT07393867updated 2026-05-29
• Trial Comparing Irradiation Plus Long Term Adjuvant Androgen Deprivation With GnRH Antagonist Versus GnRH Agonist Plus Flare Protection in Patients With Very High Risk Localized or Locally Advanced Prostate Cancer
  Active not recruiting · Phase 3 · Interventional · 885 enrolled · European Organisation for Research and Treatment of Cancer - EORTC
  NCT02799706updated 2026-05-22
• Prostate Specific Membrane Antigen (PSMA) Imaging for Detection of Residual and Metastatic Prostate Cancer
  Not yet recruiting · Phase 2 · Interventional · 20 enrolled · Washington University School of Medicine
  NCT07593079updated 2026-05-18
• An Observational Study Conducted in China to Evaluate the Efficacy and Safety of Darolutamide in Combination With Androgen Deprivation Therapy (ADT) for Men With Non-metastatic Prostate Cancer That Progressed Following Prior Bicalutamide + ADT Treatment
  Not yet recruiting · Observational · 800 enrolled · Bayer
  NCT07538843updated 2026-05-15
• Hormone Therapy and Intensity-Modulated Radiation Therapy in Treating Patients With Metastatic Prostate Cancer
  Active not recruiting · Phase 2 · Interventional · 29 enrolled · City of Hope Medical Center
  NCT00544830updated 2026-05-15

Frequently asked questions

How does Bicalutamide work?

Bicalutamide is a non-steroidal androgen receptor inhibitor. It competitively inhibits the action of androgens by binding to cytosol androgen receptors in the target tissue.

What is Bicalutamide used for?

According to FDA labeling, Bicalutamide carries indications including: Bicalutamide tablets, USP 50 mg daily are indicated for use in combination therapy with a luteinizing hormone-releasing hormone (LHRH) analog for the treatment of Stage D 2 metastatic carcinoma of the prostate. Bicalutamide tablets, USP 150 mg daily are not approved for use alone or with other treatments [see Clinical Studies (14.2)].. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Bicalutamide?

Bicalutamide is classified as Anti-androgens, Androgen Receptor Inhibitor, Androgen Receptor Antagonists, Decreased Testosterone Secretion.

What are the brand names for Bicalutamide?

Bicalutamide is marketed under brand names including Casodex.

What are the contraindications for Bicalutamide?

Bicalutamide labeling lists contraindications including: Bicalutamide is contraindicated in: • Hypersensitivity Bicalutamide is contraindicated in any patient who has shown a hypersensitivity reaction to the drug or any of the tablet’s components. Hypersensitivity reactions including angioneurotic edema and urticaria have been reported.. Always consult the full prescribing information and a clinician.