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Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
Flygare JA, Beresini M, Budha N, Chan H, Chan IT, Cheeti S, Cohen F, Deshayes K, Doerner K, Eckhardt SG, Elliott LO, Feng B, Franklin MC, Reisner SF, Gazzard L, Halladay J, Hymowitz SG, La H, LoRusso P, Maurer B, Murray L, Plise E, Quan C, Stephan JP, Young SG, Tom J, Tsui V, Um J, Varfolomeev E, Vucic D, Wagner AJ, Wallweber HJ, Wang L, Ware J, Wen Z, Wong H, Wong JM, Wong M, Wong S, Yu R, Zobel K, Fairbrother WJ. Flygare JA, et al. Among authors: budha n. J Med Chem. 2012 May 10;55(9):4101-13. doi: 10.1021/jm300060k. Epub 2012 Mar 28. J Med Chem. 2012. PMID: 22413863 Free PMC article.
Dogs are more sensitive to antagonists of inhibitor of apoptosis proteins than rats and humans: a translational toxicokinetic/toxicodynamic analysis.
Wong H, Budha NR, West K, Blackwood E, Ware JA, Yu R, Darbonne WC, Gould SE, Steigerwalt R, Erickson R, Hop CE, LoRusso P, Eckhardt SG, Wagner A, Chan IT, Mamounas M, Flygare JA, Fairbrother WJ. Wong H, et al. Toxicol Sci. 2012 Nov;130(1):205-13. doi: 10.1093/toxsci/kfs235. Epub 2012 Jul 28. Toxicol Sci. 2012. PMID: 22843607
Evaluation of metabolism and disposition of GDC-0152 in rats using 14C labeling strategy at two different positions: a novel formation of hippuric acid from 4-phenyl-5-amino-1,2,3-thiadiazole.
Yue Q, Mulder T, Rudewicz PJ, Solon E, Budha N, Ware JA, Lyssikatos J, Hop CE, Wong H, Khojasteh SC. Yue Q, et al. Among authors: budha n. Drug Metab Dispos. 2013 Feb;41(2):508-17. doi: 10.1124/dmd.112.047019. Epub 2012 Dec 4. Drug Metab Dispos. 2013. PMID: 23223496
Learning and confirming with preclinical studies: modeling and simulation in the discovery of GDC-0917, an inhibitor of apoptosis proteins antagonist.
Wong H, Gould SE, Budha N, Darbonne WC, Kadel EE 3rd, La H, Alicke B, Halladay JS, Erickson R, Portera C, Tolcher AW, Infante JR, Mamounas M, Flygare JA, Hop CE, Fairbrother WJ. Wong H, et al. Among authors: budha n. Drug Metab Dispos. 2013 Dec;41(12):2104-13. doi: 10.1124/dmd.113.053926. Epub 2013 Sep 16. Drug Metab Dispos. 2013. PMID: 24041744 Clinical Trial.
44 results