Bicalutamide(CAS: 90357-06-5)

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.

Indications and use

It has also been used in clinical trials for ovarian cancer. It has also been used in combination with castration.

Most advanced prostate cancer patients eventually become resistant to antiandrogen including bicalutamide therapy.

Bicalutamide is currently tested for treatment of andogen receptor positive ER-/PR- metastatic breast cancer.

Contraindications and precautions

Bicalutamide is contraindicated in patients who have shown a hypersensitivity reaction to its use. Bicalutamide is

a teratogen and must not be handled by females who are or may become pregnant. It is known to cause fetal harm. pg8

Caution is required when used together with other medications that depend on CYP3A4 and CYP2D6 metabolisation.

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(itching).