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We discover and develop novel, "best-in-class" inhibitors of CYP17, a validated metalloenzyme involved in prostate cancer.

Publications and Presentations

Publications and Presentations

Publications

“Targeting of CYP17A1 Lyase by VT-464 Inhibits Adrenal and Intratumoral Androgen Biosynthesis and Tumor Growth of Castration Resistant Prostate Cancer” Nature Scientific Reports | 6:35354 | DOI: 10.1038/srep35354 (2016) Sankar N. Maity, Mark A. Titus, Revekka Gyftaki, Guanglin Wu, Jing-Fang Lu, Ramachandran, Elsa M. Li-Ning-Tapia, Christopher J. Logothetis, John C. Araujo & Eleni Efstathiou

Rafferty SW, Eisner JR, Moore WR, Schotzinger RJ, Hoekstra WJ. Highly-selective 4-(1,2,3-triazole)-based P450c17a 17,20-lyase inhibitors. Bioorg Med Chem Lett 2014;24:2444–7.

Toren PJ, Kim S, Pham S, Mangalji A, Adomat H, Tomlinson Guns ES, Zoubeidi A, Moore W, Gleave ME. Anticancer Activity of a Novel Selective CYP17A1 Inhibitor in Preclinical Models of Castrate-Resistant Prostate Cancer. Mol Cancer Ther 2014;14(1);59–69

Presentations

Bardia A, Dacosta NA, Gabrail NY, Lemon S, Danso MA, Ali HA, Fleming RA, Kurman MR, Eisner JR, Moore WR,  Gucalp A, Traina TA. Phase (Ph) 1 study of oral seviteronel (VT-464), a dual CYP17-Lyase (L) inhibitor and androgen receptor (AR) antagonist, in patients (pts) with advanced AR+ triple negative (TNBC) or estrogen receptor (ER)+ breast cancer (BC). J Clin Oncol 34, 2016 (suppl; abstr 1088) [2016 ASCO Annual Meeting]

 

Nordquist LT, Shore ND, De Bono JS, Gupta S, Berry WR, Gillessen S, Liu G, Vogelzang NJ, Efstathiou E, Fleming MT, George DJ, Araujo JC, Zhang J, Kurman MR, Eisner JR, Moore WR. Objective response of the dual CYP17-Lyase (L) inhibitor / androgen receptor (AR) antagonist, VT-464, in patients with CRPC. J Clin Oncol 34, 2016 (suppl 2S; abstr 273) [2016 Genitourinary Cancers Symposium]

 

Shore ND, Nordquist LT, Gupta S, Fleming MT, Berry WR, Zhang J, Kurman MR, Eisner JR, Moore WR. Once-nightly (QD) dual CYP17-Lyase (L) inhibitor / androgen receptor (AR) antagonist VT-464 in patients with CRPC. J Clin Oncol 34, 2016 (suppl 2S; abstr 343) [2016 Genitourinary Cancers Symposium]

 

Kurman MR, Sager P, Rudoltz MS, Eisner JR, Goodman D, Heyman E, Salvail D, Bell C, Moore WR. Cardiovascular safety profile of VT-464 in patients (pts) with castrate-resistant prostate cancer (CRPC). J Clin Oncol 34, 2016 (suppl 2S; abstr 198) [2016 Genitourinary Cancers Symposium]

 

Gucalp A, Hudis C, Norton L, Patil S, Kurman MR, Eisner JR, Moore WR, Traina TA. A phase 1/2 study of once-daily oral VT-464 in patients with advanced androgen receptor (AR) positive triple negative (TNBC) or estrogen receptor (ER) positive breast cancer (BC). Cancer Res Volume 76, Issue 4 Supplement, pp. OT2-01-03 [2015 San Antonio Breast Cancer Symposium]

 

Ellison SJ, Norris JD, Wardell S, Eisner JR, Hoekstra WJ, Stagg DB, Alley HM, Moore WR, McDonnell DP. Effects of the dual selective CYP17 lyase inhibitor and androgen receptor (AR) antagonist, VT-464, on AR+ and ER+ tumor models in vitro and in vivo. Volume 76, Issue 4 Supplement, pp. P3-14-04 [2015 San Antonio Breast Cancer Symposium]

 

De Bono JS, Pezaro CJ, Gillessen S, Shore ND, Nordquist LT, Efstathiou E, Araujo JC, Berry WR, Liu G,  Vogelzang NJ, Omlin AG, Schotzinger RJ, Eisner JR, Moore WR. The oral CYP17-Lyase (L) inhibitor VT-464 in patients with CRPC. J Clin Oncol 33, 2015 (suppl 7; abstr 187) [2015 Genitourinary Cancers Symposium]

 

Moore WR, Norris JD, Wardell S, Eisner JR, Hoekstra WJ, Schotzinger RJ, McDonnell DP. Direct effects of the selective CYP17 lyase (L) inhibitor, VT-464, on the androgen receptor (AR) and its oral activity in an F876L tumor mouse xenograft model. J Clin Oncol 33, 2015 (suppl 7; abstr 263) [2015 Genitourinary Cancers Symposium]

 

Toren PJ, Pham S, Kim S, Adomat H, Zoubeidi A, Moore W, Gleave ME. Anti-cancer activity of a novel CYP17 inhibitor in pre-clinical models of castrate resistant prostate cancer. [2014 American Urological Association Annual Meeting]

 

Maity SN, Titus M, Wu G, Lu J-F, Ramachandran S, Eisner JR, Rafferty SW, Schotzinger RJ, Moore WR, Logothetis CJ, Araujo JC, Efstathiou E. Efficacy of VT-464, a Novel Selective Inhibitor of Cytochrome P450 17,20 lyase, in Castrate-Resistant Prostate Cancer. [AACR 2013 Annual Conference].

 

Figg WD, Spencer SD, Pisle ST, Pressler HM, Troutman SM, Eisner JR, Rafferty SW, Schotzinger RJ, Moore WR. Activity of oral VT-464, a selective CYP17-lyase inhibitor, in the LNCaP prostate cancer xenograft.. J Clin Oncol 30, 2012 (suppl; abstr 4671) [2012 Genitourinary Cancers Symposium]

 

Eisner JR, Abbott DH, Bird IM, Rafferty SW, Moore WR, Schotzinger RJ. VT-464: A novel, selective inhibitor of P450c17(CYP17)-17,20 lyase for castration-refractory prostate cancer (CRPC). J Clin Oncol 30, 2012 (suppl 5; abstr 198) [2012 Genitourinary Cancers Symposium]