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MDV3100 is an experimental androgen receptor antagonist drug developed by the pharmaceutical company Medivation for the treatment of hormone-refractory prostate cancer[1] currently in Phase 3 clinical trials.[2][3] Results so far have been encouraging; Medivation has reported up to an 89% decrease in prostate specific antigen serum levels after a month of taking the medicine.[4]


Preclinical pharmacology

MDV3100 has approximately fivefold higher binding affinity for the androgen receptor (AR) compared to the antiandrogen bicalutamide.[5] As opposed to bicalutamide, MDV3100 does not promote translocation of AR to the nucleus and in addition prevents binding of AR to DNA and AR to coactivator proteins.[5]

When LNCaP cells (a prostate cancer cell line) were treated with MDV3100, the expression of androgen dependent genes PSA and TMPRSS2 was down regulated in contrast to bicalutamide where the expression was upregulated.[5] In VCaP cells which over express androgen receptors, MDV3100 induced apoptosis whereas bicalutamide did not.[5] Furthermore MDV3100 behaves as an antagonist of the W741C mutant androgen receptor in contrast to bicalutamide which behaves as a pure agonist when bound to the W741C mutant.[5]

Clinical studies

MDV 3100 was found clinically active for metastatic castration-resistant prostate cancer patients in a phase II trial. PSA level decreased more than 50 percent in 40/65 chemo-naive patients and 38/75 chemotherapy-trated patients.[6]

Medivation is conducting an international phase III trial beginning in September 2009.[2][3] In addition, there is an additional phase II study commencing in 2010 that will compare mdv3100 with bicalutamide in hormone-naive metastatic prostate cancer patients.


  1. "Medivation's MDV3100 Shown to Be Effective in a Preclinical Model of Hormone-Refractory Prostate Cancer". Press release. Medivation, Inc.. 2007-02-26. Retrieved 2009-05-10. 
  2. 2.0 2.1 "Medivation Announces Initiation of Phase 3 Clinical Trial of MDV3100 in Advanced Prostate Cancer". 2009-09-23. 
  3. 3.0 3.1 "NCT00974311"., United States National Institutes of Health. Retrieved 2009-10-29. "Safety and Efficacy Study of MDV3100 in Patients With Castration-Resistant Prostate Cancer Who Have Been Previously Treated With Docetaxel-based Chemotherapy (AFFIRM)" 
  4. "Medivation's MDV3100 Demonstrates Substantial PSA Reductions In First Patient Groups Treated In Phase 1-2 Hormone Refractory Prostate Cancer Trial". Medical News Today. 2007-11-06. Retrieved 2009-05-10. 
  5. 5.0 5.1 5.2 5.3 5.4 Tran C, Ouk S, Clegg NJ, Chen Y, Watson PA, Arora V, Wongvipat J, Smith-Jones PM, Yoo D, Kwon A, Wasielewska T, Welsbie D, Chen CD, Higano CS, Beer TM, Hung DT, Scher HI, Jung ME, Sawyers CL (May 2009). [Expression error: Missing operand for > "Development of a second-generation antiandrogen for treatment of advanced prostate cancer"]. Science 324 (5928): 787–90. doi:10.1126/science.1168175. PMID 19359544. 
  6. Scher HI, Beer TM, Higano CS, Taplin M, Efstathiou E, Anand A, Hung D, Hirmand M, Fleisher M (2009). "Antitumor activity of MDV3100 in a phase I/II study of castration-resistant prostate cancer (CRPC)". J Clin Oncol 27 (15s): abstr 5011. 

See also

  • Abiraterone
  • TOK-001, a small molecule, oral drug, that is both an androgen receptor antagonist and CYP17 inhibitor (a combination MOA of abiraterone and mdv3100). Currently being tested in early phase I/II clinical trials for HRPC and sponsored by Tokai Pharmaceuticals.


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