| Indication |
For treatment (together with surgery or LHRH analogue) of advanced prostatic cancer. |
| 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. |
| Volume of distribution |
Not Available |
| Protein binding |
96% |
| Metabolism |
Bicalutamide undergoes stereo specific metabolism. The S
(inactive) isomer is metabolized primarily by glucuronidation. The R
(active) isomer also undergoes glucuronidation but is predominantly
oxidized to an inactive metabolite followed by glucuronidation. |
| Route of elimination |
Not Available |
| Half life |
5.9 days |
| Clearance |
- Apparent oral cl=0.32 L/h [Normal Males]
|
| Toxicity |
Not Available |
