Latest research on MDV3100

Enzalutamide is an androgen receptor inhibitor for the treatment of castration-resistant prostate cancer. FDA approved on August 31, 2012.

Latest findings

MDV3100, ARN-509 and Bicalutamide were gifts from Dr. [source, 2015]
We verified that Flutamide and MJC13 indeed displayed similar actions at selected DHT-induced genes by qRT-PCR and also compared effects of both compounds with the second generation AR antagonists MDV3100 and ARN-509 [17,18]. [source, 2015]
Numerous novel anti-androgens and androgen depleting agents are being introduced into the clinic, including enzalutamide (MDV3100), ARN-509, and the CYP17 inhibitor abiraterone (Potter et al, 1995; Tran et al, 2009; Clegg et al, 2012). [source, 2015]
Three standard of care compounds widely used against PrCa were added as controls; namely, the androgen receptor antagonist enzalutamide (MDV3100), the C17α-hydroxylase/C17,20-lyase inhibitor abiraterone (Zytiga), and the classic mitotic inhibitor Paclitaxel. [source, 2015]
Development of enzalutamide, formerly MDV3100, originated from the non-steroidal scaffolding chemical RU59063 where it was structurally and biochemically optimized for its use as an AR antagonist. [source, 2015]
The early results seen with enzalutamide therapy led to the international phase III AFFIRM trial (A Study Evaluating the Efficacy and Safety of the investigational drug MDV3100); a randomized, double-blind, placebo controlled trial in men with prostate cancer who had received one or two previous chemotherapy treatments, one of which was Docetaxel. [source, 2015]
Methylselenol and MDV3100 synergistically inhibited full length AR and AR-V7 in prostate cancer cells [39]. [source, 2015]
Drug concentrations of Abiraterone and MDV3100 were chosen which gave maximally 20% reductions in viability when administered as single agents (Abiraterone: 1 μM for LNCaP and VCaP, MDV3100: 1 μM for LNCaP and 100 nM for VCaP). [source, 2015]
LNCaP-abl did not show a significant response to either Abiraterone or MDV3100 and thus were excluded from these experiments (data not shown). [source, 2015]
As hypothesized, combining siRNA against IMPDH2 with Abiraterone or MDV3100 had additive effects in both lines (Figure 3C). [source, 2015]