Galeterone - CAS 851983-85-2
Catalog number:
851983-85-2
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
Inquire
Targets:
Cytochrome P450
Description:
Galeterone (TOK-001 or VN/124-1) is a novel antiandrogen under development by Tokai Pharmaceuticals for the treatment of prostate cancer. It possesses a unique dual mechanism of action, acting as both anandrogen receptor antagonist and an inhibitor of CYP17A1, an enzyme required for the biosynthesis of theandrogens.
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Synonyms:
Galeterone; TOK-001; TOK 001; VN 124; VN/124-1;
MSDS:
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Current Developer:
Tokai Pharmaceutcials.
1.Galeterone and VNPT55 induce proteasomal degradation of AR/AR-V7, induce significant apoptosis via cytochrome c release and suppress growth of castration resistant prostate cancer xenografts in vivo.
Kwegyir-Afful AK1,2, Ramalingam S1,2, Purushottamachar P1,2, Ramamurthy VP1,2, Njar VC1,2,3. Oncotarget. 2015 Sep 29;6(29):27440-60. doi: 10.18632/oncotarget.4578.
Galeterone (Gal) is a first-in-class multi-target oral small molecule that will soon enter pivotal phase III clinical trials in castration resistant prostate cancer (CRPC) patients. Gal disrupts androgen receptor (AR) signaling via inhibition of CYP17, AR antagonism and AR degradation. Resistance to current therapy is attributed to up-regulation of full-length AR (fAR), splice variants AR (AR-Vs) and AR mutations. The effects of gal and VNPT55 were analyzed on f-AR and AR-Vs (AR-V7/ARv567es) in LNCaP, CWR22Rv1 and DU145 (transfected with AR-Vs) human PC cells in vitro and CRPC tumor xenografts. Galeterone/VNPT55 decreased fAR/AR-V7 mRNA levels and implicates Mdm2/CHIP enhanced ubiquitination of posttranslational modified receptors, targeting them for proteasomal degradation. Gal and VNPT55 also induced significant apoptosis in PC cells via increased Bax/Bcl2 ratio, cytochrome-c release with concomitant cleavage of caspase 3 and PARP. More importantly, gal and VNPT55 exhibited strong in vivo anti-CRPC activities, with no apparent host toxicities.
2.Androgen Receptor Modulation Optimized for Response (ARMOR) Phase I and II Studies: Galeterone for the Treatment of Castration-Resistant Prostate Cancer.
Montgomery B1, Eisenberger MA2, Rettig MB3, Chu F4, Pili R5, Stephenson JJ6, Vogelzang NJ7, Koletsky AJ8, Nordquist LT9, Edenfield WJ10, Mamlouk K11, Ferrante KJ11, Taplin ME12. Clin Cancer Res. 2016 Mar 15;22(6):1356-63. doi: 10.1158/1078-0432.CCR-15-1432. Epub 2015 Nov 2.
PURPOSE: Galeterone is a selective, multitargeted agent that inhibits CYP17, antagonizes the androgen receptor (AR), and reduces AR expression in prostate cancer cells by causing an increase in AR protein degradation. These open-label phase I and II studies [Androgen Receptor Modulation Optimized for Response-1 (ARMOR1) and ARMOR2 part 1] evaluated the efficacy and safety of galeterone in patients with treatment-naive nonmetastatic or metastatic castration-resistant prostate cancer (CRPC) and established a dose for further study.
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CAS 851983-85-2 Galeterone

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