MDV-3100

• CAT Number: A001158
• CAS Number: 915087-33-1
• Molecular Formula: C21H16F4N4O2S
• Molecular Weight: 464.43
• Purity: ≥95%
• Target: Androgen Receptor
• Solubility: >23.2mg/mL in DMSO
• Storage: 3 years -20C powder
• IUPAC Name: 4-[3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-sulfanylideneimidazolidin-1-yl]-2-fluoro-N-methylbenzamide
• InChI: InChI=1S/C21H16F4N4O2S/c1-20(2)18(31)28(12-5-4-11(10-26)15(8-12)21(23,24)25)19(32)29(20)13-6-7-14(16(22)9-13)17(30)27-3/h4-9H,1-3H3,(H,27,30)
• InChIKey: WXCXUHSOUPDCQV-UHFFFAOYSA-N
• SMILES: CC1(C(=O)N(C(=S)N1C2=CC(=C(C=C2)C(=O)NC)F)C3=CC(=C(C=C3)C#N)C(F)(F)F)C

Enzalutamide (CAS 915087-33-1), also known as MDV3100, is an orally bioavailable, organic, non-steroidal small molecule targeting the androgen receptor (AR) with potential antineoplastic activity. Through a mechanism that is reported to be different from other approved AR antagonists, selective androgen receptor modulator MDV3100 inhibits the activity of prostate cancer cell ARs, which may result in a reduction in prostate cancer cell proliferation and, correspondingly, a reduction in the serum prostate specific antigen (PSA) level. In August 2012, the United States (U.S.) Food and Drug Administration (FDA) approved enzalutamide for the treatment of castration-resistant prostate cancer.

Overview of Clinical Research

Enzalutamide is an androgen receptor antagonist. The phase III study on prostate cancer starts in 2020.

Reference

1: El-Amm J, Patel N, Freeman A, Aragon-Ching JB. Metastatic Castration-Resistant Prostate Cancer: Critical Review of Enzalutamide. Clin Med Insights Oncol. 2013 Aug 21;7:235-245. Review. PubMed PMID: 24179414; PubMed Central PMCID: PMC3813614.
2: Pal SK, Stein CA, Sartor O. Enzalutamide for the treatment of prostate cancer. Expert Opin Pharmacother. 2013 Apr;14(5):679-85. doi: 10.1517/14656566.2013.775251. Epub 2013 Feb 27. Review. PubMed PMID: 23441761.
3: Ha YS, Goodin S, DiPaola RS, Kim IY. Enzalutamide for the treatment of castration-resistant prostate cancer. Drugs Today (Barc). 2013 Jan;49(1):7-13. doi: 10.1358/dot.2013.49.1.1910724. Review. PubMed PMID: 23362491.
4: Rawlinson A, Mohammed A, Miller M, Kunkler R. The role of enzalutamide in the treatment of castration-resistant prostate cancer. Future Oncol. 2012 Sep;8(9):1073-81. doi: 10.2217/fon.12.99. Review. PubMed PMID: 23030482.