Drug information of Bicalutamide


Drug group:

Bicalutamide is an anti-androgen. It works in the body by preventing the actions of androgens (male hormones).
Bicalutamide is used together with another hormone to treat prostate cancer.

Mechanism of effect

Androgen receptor inhibitor; pure nonsteroidal antiandrogen that binds to androgen receptors; specifically a competitive inhibitor for the binding of dihydrotestosterone and testosterone; prevents testosterone stimulation of cell growth in prostate cancer


Bicalutamide is an antineoplastic hormonal agent primarily used in the treatment of prostate cancer.


Absorption:Well absorbed; unaffected by food
Metabolism:Extensively hepatic; glucuronidation and oxidation of the R (active) enantiomer to inactive metabolites; the S enantiomer is inactive.
Excretion:Urine and feces
Time to Peak:Active enantiomer: ~31 hours
Protein Binding:96%
Half-Life Elimination:Active enantiomer: ~6 days.

Drug indications

Prostate Cancer


Prostate cancer, metastatic: Adults: Oral: 50 mg once daily (in combination with an LHRH analogue)
Prostate cancer, locally advanced, high recurrence risk (off-label use): Adults: Oral: 150 mg once daily (as monotherapy) (McLeod, 2006). Additional trials may be necessary to further define the role of bicalutamide in this condition.


1-Use with caution in patients with moderate-to-severe hepatic impairment
2-Treatment for metastatic cancer should be started concomitantly with an LHRH analogue.
3-May cause gynecomastia or breast pain at higher (off-label) doses.
4- Anemia may occur with testosterone suppression; monitor CBC periodically as indicated.
5-May lead to spermatogenesis inhibition.

Points of recommendation

1-Dose should be taken at the same time each day, either in the morning or in the evening.
2-May be administered with or without food.

Pregnancy level


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