Bicalutamide
- Atc Codes:L02BB03
- CAS Codes:90357-06-5
- PHARMGKB ID:90357-06-5
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Induces
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Bicalutamide, Casodex; Belgium: Bicalutamide, Casodex; Bulgaria: Bicalan, Bicalodex, Bicatlon, Bicusan, Calumid, Calutide, Casodex; Czech Republic: Atembin, Bicaluplex, Bicalutagen, Bicalutamid, Bicalutamidum, Bicasil, Bikalard, Binabic, Calumid, Casodex, Glanuta, Lanbica, Ormandyl; Denmark: Bicalustad, Bicalutamid, Casodex, Nycolutamid; Estonia: Bicalan, Bicalutamid, Bicalutamide, Calumid; Finland: Bicalutamid, Bicalutamide, Bicavan, Bicusan, Bikalutamidi, Casodex, Kandex; France: Bicalutamide, Casodex, Ormandyl; Germany: Androcal, Bicadex, Bicalid, Bicalon, Bicalut, Bicalutamid, Bicalutamidgen, Bicalutin, Bicamid-GRY, Bicaprostat, Bica-Q, Casodex, Eurobicalutamid, Ribocadex, Tyquin; Greece: Apex, Bicadex, Bicalut, Bicalutamide, Bicamide, Bicaprol, Bicatin, Bikalen, Bilumide, Casodex, Encalor, Omidex, Procure, Verodex, Zarmol; Hungary: Bicalutamid, Bicalutamide, Bicatlon, Bicusan, Bilutamid, Binabic, Calumid, Capro, Casodex, Grommar, Lanbicamid, Sanotamid; Ireland: Bicalinn, Bicalutamide, Biluta, Casodex, Casomide; Italy: Bicalutamide, Casodex, Lutamid, Praxis, Safedex; Latvia: Bicalutamide; Lithuania: Bicalutamid, Bicalutamide; Luxembourg: Casodex; Netherlands: Bicalutamide, Bicamedica, Bilumide, Casodex; Poland: Bicalutamide, Casodex; Portugal: Bicalutamida, Bicastad, Casodex, Ormandyl; Romania: Androbloc, Bicalton, Bicalutamid, Bicalutamida, Calumid, Casodex; Slovakia: Atembin, Bicalutagen, Bicalutamid, Bicalutamide, Bicatleon, Bicusan, Binabic, Calutin, Casodex, Glanuta, Ormandyl; Slovenia: Bikalutamid, Casodex; Spain: Bicalutamida, Bicamylan, Bicarbex, Casodex, Pencial, Probic, Saveprost, Wibical; Sweden: Baculamyl, Bicalustad, Bicalutamid, Bicalutamide, Bictamid, Bikalutamid, Casodex, Nycolutamid; UK: Bicalutamide, Casodex.
North America
Canada: Bicalutamide, Casodex; USA: Casodex.
Latin America
Argentina: Bicalutamida, Bidrostat, Biolutam, Bitakebir, Bosconar, C3CO, Casodex, Codebup, Dimalán, Finaband, Gepeprostín, Liberprost, Raffolutil; Brazil: Casodex, Gepeprostin, Lutamidal; Mexico: Bicalem, Calutol, Casdrogén, Casodex.
Asia
Japan: Casodex.
Drug combinations
Bicalutamide and Leuprolide
Chemistry
Bicalutamide: C~18~H~14~F~4~N~2~O~4~S. Mw: 430.37. (1) Propanamide, N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methyl-, (±)-; (2)(±)-4′-Cyano-α,α,α-trifluoro-3-[(p-fluorophenyl)sulfonyl]-2-methyl-m-lactotoluidide. CAS-90357-06-5 (1994).
Pharmacologic Category
Antineoplastic Agents; Endocrine Therapy; Antiandrogen. (ATC-Code: L02BB03).
Mechanism of action
Pure nonsteroidal antiandrogen that binds to androgen receptors. Specific and competitive inhibitor for the binding of dihydrotestosterone and testosterone. Prevents testosterone stimulation of cell growth in prostate cancer and may produce transient tumor regression through inhibition of androgen-dependent DNA and protein synthesis. Inhibits initial androgenic stimulation and potential exacerbation of symptoms associated with the first month of LHRH analog therapy.
Therapeutic use
In combination therapy with LHRH agonist analogs in treatment of metastatic prostate cancer.
Pregnancy and lactiation implications
Teratogenic in animal studies. Bicalutamide is not indicated for women.
Unlabeled use
Monotherapy for locally-advanced prostate cancer.
Contraindications
Hypersensitivity to bicalutamide or any component of the formulation. Should not be used in women, particularly for conditions that are not serious or life-threatening.
Warnings and precautions
May cause gynecomastia or breast pain. Rare cases of death or hospitalization due to hepatitis reported. Hepatotoxicity generally occurs within the first 3-4 months of use (caution in moderate-to-severe hepatic dysfunction). May lead to spermatogenesis inhibition. Combined therapy with LHRH analog can produce hot flashes, pain (including abdominal, back, and pelvic pain), asthenia, constipation, infection, nausea, dyspnea, diarrhea. Risk of facial flushing is higher in conjunction with alcohol.