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Products are for research use only. Not for human use. We do not sell to patients.

Signaling Pathway

Enzalutamide

HY-70002

(MDV3100; MDV-3100; MDV 3100)

Enzalutamide
Enzalutamide Chemical Structure

Enzalutamide (MDV3100) is androgen-receptor antagonist inhibitor. Enzalutamide is highly recommended inhibitor in AR research.Enzalutamide is useful for treatment of hormone-refractory prostate cancer.

Price and Availability of Enzalutamide
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5 mg $132 In-stock
50 mg $275 In-stock
500 mg $660 In-stock
>1000 mg Get quote
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Enzalutamide Data Sheet

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Purity: 99.02%

Cell Cycle/DNA Damage

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Biological Activity of Enzalutamide

Enzalutamide (MDV3100) is androgen-receptor antagonist inhibitor. Enzalutamide is highly recommended inhibitor in AR research.Enzalutamide is useful for treatment of hormone-refractory prostate cancer.

Clinical Information

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References on Enzalutamide

1 . Shapiro D, Tareen B.Current and emerging treatments in the management of castration-resistant prostate cancer.Expert Rev Anticancer Ther. 2012 Jul;12(7):951-64.
Abstract
Historically, patients diagnosed with castration-resistant prostate cancer (CRPC) have had poor survival rates. In recent years there have been significant advances in the treatment of CRPC. In addition to cytotoxic chemotherapy, treating physicians and their patients now have the option of several new agents that target not only androgen- and cytotoxic-mediated pathways, but also the patient's own immune system. In this review, we discuss the existing US FDA-approved therapies, a wide range of experimental treatments that are currently in development, and also palliative options for patients with symptoms secondary to metastatic disease. We also discuss the progression-free survival, overall survival, PSA levels and other end points used in clinical trials in order to evaluate and compare novel therapeutic options for CRPC. Currently, docetaxel and sipuleucel-T are the first line treatment options for patients with CRPC; approved second-line treatments for first line treatment failure are limited to cabazitaxel and abiraterone acetate. Recently, a few experimental agents, MDV3100 and radium-223, have demonstrated efficacy in improving overall survival in patients who had previously failed chemotherapy. These agents, and possibly others introduced in this review, are positioned to change the treatment landscape for CRPC.

2 . Schweizer MT, Antonarakis ES.Abiraterone and other novel androgen-directed strategies for the treatment of prostate cancer: a new era of hormonal therapies is born.Ther Adv Urol. 2012 Aug;4(4):167-78.
Abstract
The number of life-prolonging therapies proven effective in the treatment of metastatic castrate-resistant prostate cancer (CRPC) has been limited until recently. In the past 2 years several such therapies have come to market. In 2010, the autologous immunotherapy sipuleucel-T and the next-generation taxane cabazitaxel were approved in this setting. However, abundant evidence has shown that CRPC growth continues to be driven through androgen-dependent signaling. Both of these drugs fail to take advantage of this targetable oncogenic pathway. Potent specific inhibitors of cytochrome P450-17 have been engineered with the aim of suppressing androgen synthesis beyond that seen with the luteinizing hormone-releasing hormone agonists/antagonists. Abiraterone acetate was developed by rational design based on a pregnenolone parent structure. Its approval by the US Food and Drug Administration (FDA) was granted in 2011 based on phase III data demonstrating an overall survival advantage compared with placebo. More recently, other drugs that act along the androgen signaling pathway, such as orteronel (TAK-700), galeterone (TOK-001), enzalutamide (MDV3100) and ARN-509, have shown promise in clinical trials. Some of these are expected to gain FDA approval in the near future. Here, we review abiraterone and other novel androgen-directed therapeutic strategies for the management of advanced prostate cancer.

3 . Kohli M, Qin R, Jimenez R, Dehm SM.Biomarker-based targeting of the androgen-androgen receptor axis in advanced prostate cancer.Adv Urol. 2012;2012:781459. Epub 2012 Aug 22.
Abstract
Recent therapeutic advances for managing advanced prostate cancer include the successful targeting of the androgen-AR axis with several new drugs in castrate resistant prostate cancer including abiraterone acetate and enzalutamide (MDV3100). This translational progress from "bench to bed-side" has resulted in an enlarging repertoire of novel and traditional drug choices now available for use in advanced prostate cancer therapeutics, which has had a positive clinical impact in prolonging longevity and quality of life of advanced prostate cancer patients. In order to further the clinical utility of these drugs, development of predictive biomarkers guiding individual therapeutic choices remains an ongoing challenge. This paper will summarize the potential in developing predictive biomarkers based on the pathophysiology of the androgen-AR axis in tumor tissue from patients with advanced prostate cancer as well as inherited variation in the patient's genome. Specific examples of rational clinical trial designs incorporating potential predictive biomarkers from these pathways will illustrate several aspects of pharmacogenetic and pharmacogenomic predictive biomarker development in advanced prostate cancer therapeutics.

4 . Scher HI, Fizazi K, Saad F, Taplin ME, Sternberg CN, Miller MD, de Wit R, Mulders P, Chi KN, Shore ND, Armstrong AJ, Flaig TW, Fléchon A, Mainwaring P, Fleming M, Hainsworth JD, Hirmand M, Selby B, Seely L, de Bono JS; the AFFIRM Investigators.Increased Survival with Enzalutamide in Prostate Cancer after Chemotherapy.N Engl J Med. 2012 Aug 15.
Abstract
Background Enzalutamide (formerly called MDV3100) targets multiple steps in the androgen-receptor-signaling pathway, the major driver of prostate-cancer growth. We aimed to evaluate whether enzalutamide prolongs survival in men with castration-resistant prostate cancer after chemotherapy. Methods In our phase 3, double-blind, placebo-controlled trial, we stratified 1199 men with castration-resistant prostate cancer after chemotherapy according to the Eastern Cooperative Oncology Group performance-status score and pain intensity. We randomly assigned them, in a 2:1 ratio, to receive oral enzalutamide at a dose of 160 mg per day (800 patients) or placebo (399 patients). The primary end point was overall survival. Results The study was stopped after a planned interim analysis at the time of 520 deaths. The median overall survival was 18.4 months (95% confidence interval [CI], 17.3 to not yet reached) in the enzalutamide group versus 13.6 months (95% CI, 11.3 to 15.8) in the placebo group (hazard ratio for death in the enzalutamide group, 0.63; 95% CI, 0.53 to 0.75; P<0.001). The superiority of enzalutamide over placebo was shown with respect to all secondary end points: the proportion of patients with a reduction in the prostate-specific antigen (PSA) level by 50% or more (54% vs. 2%, P<0.001), the soft-tissue response rate (29% vs. 4%, P<0.001), the quality-of-life response rate (43% vs. 18%, P<0.001), the time to PSA progression (8.3 vs. 3.0 months; hazard ratio, 0.25; P<0.001), radiographic progression-free survival (8.3 vs. 2.9 months; hazard ratio, 0.40; P<0.001), and the time to the first skeletal-related event (16.7 vs. 13.3 months; hazard ratio, 0.69; P<0.001). Rates of fatigue, diarrhea, and hot flashes were higher in the enzalutamide group. Seizures were reported in five patients (0.6%) receiving enzalutamide. Conclusions Enzalutamide significantly prolonged the survival of men with metastatic castration-resistant prostate cancer after chemotherapy. (Funded by Medivation and Astellas Pharma Global Development; AFFIRM ClinicalTrials.gov number, NCT00974311 .).

5 . Tran C, Ouk S, Clegg NJ, Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science 324 (5928): 787-90.
Abstract
Metastatic prostate cancer is treated with drugs that antagonize androgen action, but most patients progress to a more aggressive form of the disease called castration-resistant prostate cancer, driven by elevated expression of the androgen receptor. Here we characterize the diarylthiohydantoins RD162 and MDV3100, two compounds optimized from a screen for nonsteroidal antiandrogens that retain activity in the setting of increased androgen receptor expression. Both compounds bind to the androgen receptor with greater relative affinity than the clinically used antiandrogen bicalutamide, reduce the efficiency of its nuclear translocation, and impair both DNA binding to androgen response elements and recruitment of coactivators. RD162 and MDV3100 are orally available and induce tumor regression in mouse models of castration-resistant human prostate cancer. ...

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