MDV3100
A Novel Mechanism of Action
In vitro data provide evidence that MDV3100 has a novel mechanism of action making it the first triple-acting, oral androgen receptor antagonist.
See Androgen Receptor Inhibitors chart below.
Watch this short animation. (English)
Overexpression of the androgen receptor is believed to contribute to the progression of hormone-resistant prostate cancer. The first triple-acting, oral androgen receptor antagonist, MDV3100 has been shown in preclinical studies to provide more complete suppression of the androgen receptor pathway than bicalutamide, the most commonly used androgen receptor antagonist.
Specifically, MDV3100 slows growth and induces cell death in bicalutamide-resistant cancers via three complementary actions:
- blocks testosterone binding to the androgen receptor
- impedes movement of the androgen receptor complex to the nucleus of prostate cancer cells
- inhibits binding to DNA
| Androgen Receptor Inhibitors (Based on in vitro data) |
||
| MDV3100 | Bicalutamide | |
|---|---|---|
| Blocks Androgen Receptor |  |
 |
| Impedes Nuclear Translocation | |
 |
| Prevents DNA Binding | |
|
| Induces Cancer Cell Death in Resistant Setting | |
|
Science 8 May 2009:Vol. 324. no. 5928, pp. 787 - 790 DOI: 10.1126/science.1168175
Find out more about MDV3100 at medivation.com
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