Active Ingredient History
Bicalutamide (brand name Casodex) is an oral non-steroidal anti-androgen for prostate cancer. It is indicated for use in combination therapy with a luteinizing hormone-releasing hormone (LHRH) analog for the treatment of Stage D2 metastatic carcinoma of the prostate. Bicalutamide competitively inhibits the action of androgens by binding to cytosol androgen receptors in the target tissue. Prostatic carcinoma is known to be androgen sensitive and responds to treatment that counteracts the effect of androgen and/or removes the source of androgen. When CASODEX is combined with luteinizing hormone releasing hormone (LHRH) analog therapy, the suppression of serum testosterone induced by the LHRH analog is not affected. Bicalutamide is well-absorbed following oral administration, although the absolute bioavailability is unknown. Bicalutamide undergoes stereospecific metabolism. The S (inactive) isomer is metabolized primarily by glucuronidation. The R (active) isomer also undergoes glucuronidation but is predominantly oxidized to an inactive metabolite followed by glucuronidation. Both the parent and metabolite glucuronides are eliminated in the urine and feces. The S-enantiomer is rapidly cleared relative to the R-enantiomer, with the R-enantiomer accounting for about 99% of total steady-state plasma levels. NCATS
Drug Pricing (per unit)
Note: This drug pricing data is preliminary, incomplete, and may contain errors.
Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
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Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
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Prostatic Neoplasms (approved 1995)
Androgens (Phase 2)
Breast Neoplasms (Phase 3)
Carcinoma (Phase 2)
Carcinoma, Transitional Cell (Phase 2)
Castration (Phase 3)
Coronavirus Infections (Phase 1)
COVID-19 (Phase 3)
Drugs, Generic (Phase 1)
Erectile Dysfunction (Phase 2)
Fallopian Tube Neoplasms (Phase 2)
Gynecology (Phase 2)
Hamartoma (Phase 2)
Healthy Volunteers (Phase 1)
Hirsutism (Phase 1)
Hormones (Phase 2)
Intestinal Neoplasms (Phase 3)
Lower Urinary Tract Symptoms (Phase 2)
Neoplasm Metastasis (Phase 3)
Neoplasms (Phase 3)
Non-alcoholic Fatty Liver Disease (Phase 1)
Ovarian Neoplasms (Phase 2)
Polycystic Ovary Syndrome (Phase 1)
Prostate (Phase 2)
Prostatic Neoplasms (Phase 4)
Puberty, Precocious (Phase 2)
Salivary Gland Neoplasms (Phase 2)
Severe Acute Respiratory Syndrome (Phase 1)
Sexual Dysfunction, Physiological (Phase 3)
Triple Negative Breast Neoplasms (Phase 1/Phase 2)
Urinary Bladder Neoplasms (Phase 2)
Urination Disorders (Phase 3)
Trial | Phase | Start Date | Organizations | Indications |
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