Introduction
Bicalutamide is an oral non-steroidal anti-androgen for prostate cancer. It is comprised of a racemic mixture that is a 50:50 composition of the (R)-bicalutamide and (S)-bicalutamide enantionmers. Bicalutamide binds to the androgen receptor.
Uses
Bicalutamide is an androgen receptor inhibitor used to treat Stage D2 metastatic carcinoma of the prostate.
For treatment (together with surgery or LHRH analogue) of advanced prostatic cancer.
Associated Conditions
Pharmacodynamics
Bicalutamide is an antineoplastic hormonal agent primarily used in the treatment of prostate cancer. Bicalutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). Consequently, Bicalutamide blocks the action of androgens of adrenal and testicular origin which stimulate the growth of normal and malignant prostatic tissue. Prostate cancer is mostly androgen-dependent and can be treated with surgical or chemical castration. To date, antiandrogen monotherapy has not consistently been shown to be equivalent to castration.
Mechanism of Action
Bicalutamide competes with androgen for the binding of androgen receptors, consequently blocking the action of androgens of adrenal and testicular origin which stimulate the growth of normal and malignant prostatic tissue.
Absorption
Bicalutamide is well-absorbed following oral administration, although the absolute bioavailability is unknown.
Protein Binding
96%
Half Life
5.9 days
Clearance
- Apparent oral cl=0.32 L/h [Normal Males]
Food Interactions
- Take at the same time every day.
- Take with or without food. Food does not significantly affect absorption.
Dosage
Pediatric Use: The safety and effectiveness of Bicalutamide in pediatric patients have not been established.
Hepatic Impairment: Bicalutamide is extensively metabolized by the liver. It should be used with caution in patients with moderate-to-severe hepatic impairment.
