High Purity USP Standard 98% Raw Material Powder Bicalutamide CAS 90357-06-5 with good price and safe delivery

Bicalutamide More Info

Bicalutamide is a non-steroidal anti-androgen medication primarily used in the treatment of prostate cancer. It is marketed under the brand name Casodex and is known for its selective inhibition of androgen receptors.

Mechanism of Action

Bicalutamide functions as a competitive antagonist of the androgen receptor (AR). By binding to the AR, it inhibits the action of androgens such as testosterone and dihydrotestosterone (DHT), which are critical for the growth of prostate cancer cells. This blockade leads to a reduction in androgen-mediated cellular proliferation and promotes apoptosis in prostate cancer cells . Bicalutamide's unique mechanism also involves accessing an additional binding pocket adjacent to the hormone binding site, which further enhances its antagonistic effects on AR activity.

Applications

Prostate Cancer Treatment: It is indicated for metastatic prostate cancer, often in combination with a gonadotropin-releasing hormone (GnRH) analogue or surgical castration. It can also be used as monotherapy for locally advanced nonmetastatic prostate cancer.
Other Uses: Limited applications include treatment for excessive hair growth in women, as part of feminizing hormone therapy for transgender women, and to manage conditions like gonadotropin-independent early puberty in boys.

Routes of Administration

Bicalutamide is administered orally, typically at a dosage of 150 mg once daily for prostate cancer treatment. The absorption of bicalutamide is not significantly affected by food intake.

Safety and Side Effects

Bicalutamide can cause various side effects, some of which may be serious. Common side effects include:
Hot flashes
Fatigue
Nausea and vomiting
Anemia
Breast pain or swelling
Changes in liver function (hepatotoxicity) leading to symptoms like jaundice, dark urine, and abdominal pain.
Severe allergic reactions can occur, manifesting as difficulty breathing, swelling, or hives. Additionally, bicalutamide may lead to lung inflammation (interstitial lung disease), characterized by cough and difficulty breathing.

Pharmacokinetics

Absorption: Well-absorbed after oral administration, with peak plasma concentrations reached within 4 to 12 weeks of therapy. However, absorption diminishes at higher doses.
Distribution: Approximately 96% protein-bound, primarily to albumin. Bicalutamide crosses the blood-brain barrier, allowing it to exert effects in the central nervous system.
Metabolism: Bicalutamide undergoes stereospecific metabolism in the liver, with the active (R)-isomer being oxidized to inactive metabolites while the inactive (S)-isomer is primarily glucuronidated.
Elimination Half-life: The half-life ranges from approximately 5.9 days after a single dose to about 7 to 10 days with repeated administration. Bicalutamide and its metabolites are eliminated through urine and feces.
Clearance: The apparent oral clearance is approximately 0.32 L/h in normal males. Ethnicity can influence pharmacokinetics; for instance, higher steady-state concentrations have been observed in Japanese populations compared to Caucasians.

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