Bicalutamide

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Bicalutamide

Clinical data
Pregnancy category	US: X (Contraindicated)
Routes of administration	Oral
ATC code	L02BB03 (WHO)
Legal status
Legal status	In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability	well absorbed
Protein binding	96%
Metabolism	hepatic
Elimination half-life	5.8 days
Identifiers
IUPAC name N-[4-cyano-3-(trifluoromethyl)phenyl]- 3-(4-fluorophenyl)sulfonyl-2- hydroxy-2-methyl- propanamide
CAS Number	90357-06-5
PubChem CID	56069
DrugBank	APRD00042
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C18H14F4N2O4S
Molar mass	430.374 g/mol

Bicalutamide (marketed as Casodex®, Cosudex®, Calutide®, Kalumid®) is an oral non-steroidal anti-androgen for prostate cancer. It was first launched in 1995 as a combination treatment (with surgical or medical castration) for advanced prostate cancer and subsequently launched as monotherapy for the treatment of earlier stages of the disease.

It is marketed by AstraZeneca with the brand names Casodex and Cosudex. Bicalutamide is recommended 50 mg once daily in combination with an LHRH analogue or surgical castration.

Description

Bicalutamide is an oral non-steroidal anti-androgen with the empirical formula C₁₈H₁₄N₂O₄F₄S and is an off-white powder that is practically insoluble in water.

Indications and use

For the treatment of stage D2 metastatic prostate cancer in combination with a luteinizing hormone-releasing hormone analogue or as a monotherapy. Has been used in clinical trials for ovarian cancer.

Contraindications and precautions

Bicalutamide is contra-indicated in females and children and must not be given to any patient who has shown a hypersensitivity reaction to its use.

Adverse reactions

Adverse reactions include reproductive system and breast disorders, breast tenderness, gynaecomastia, hot flushes, gastrointestinal disorders, diarrhoea, nausea, hepatic changes (elevated levels of transaminases, jaundice), asthenia and pruritus.

External links

• Casodex, Cosudex (manufacturer's website)
• Bicalutamide (patient information)