Jefferies & Co. analyst Biren Amin said MDV3100 could have an advantage in survival. Patients treated with Zytiga had median survival of 4.6 months compared to placebo at the end of late-stage testing, but he noted that median survival was 3.9 months after an early analysis like the one Medivation and Astellas reported Thursday. Amin said patients treated with MDV3100 could also have greater survival when a final analysis is complete.
MDV3100 has approximately fivefold higher binding affinity for the androgen receptor (AR) compared to the antiandrogen bicalutamide. 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.
In addition, first generation AR antagonists such as bicalutamide (also called Casodex®) or flutamide demonstrate agonist properties in cells engineered to express higher AR levels. The partial agonism of these compounds is a potential liability
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