Bicalutamide (marketed as Casodex, Cosudex, Calutide, Kalumid) is a non-steriodal Androgen Receptor (AR) inhibitor. Bicalutamide (CDX) is inhibited by non-genomic, transcription-independent stimulation of PI3K/AKT phosphorylation by androgens. Bicalutamide displays peripheral selectivity and does not effect serum levels of LH and testosterone. Bicalutamide exhibits potent anticancer activity in vivo. Bicalutamide acts as a pure anti-androgen by binding to the androgen receptor (AR) and preventing the activation of the AR and subsequent upregulation of androgen responsive genes by androgenic hormones. In addition, bicalutamide accelerates the degradation of the androgen receptor. Bicalutamide is induces cell death by a pathway that is independent of changes in mitochondrial membrane potential and Bcl-2 action. Bicalutamide is currently tested for treatment of andogen receptor positive ER-/PR- metastatic breast cancer.
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|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
A phase II evaluation of goserelin and bicalutamide in patients with ovarian cancer in second or higher complete clinical disease remission.
Levine D, et al. Cancer. 2007 Dec 1;110(11):2448-56. PMID: 17918264.
The preclinical development of bicalutamide: pharmacodynamics and mechanism of action.
Furr BJ, et al. Urology. 1996 Jan;47(1A Suppl):13-25; discussion 29-32. PMID: 8560673.
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