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A Phase I Dose-Escalation Study Evaluating the Safety Tolerability and Pharmacokinetics of CUDC-427, a Potent, Oral, Monovalent IAP Antagonist, in Patients with Refractory Solid Tumors.
Tolcher AW, Bendell JC, Papadopoulos KP, Burris HA, Patnaik A, Fairbrother WJ, Wong H, Budha N, Darbonne WC, Peale F, Mamounas M, Royer-Joo S, Yu R, Portera CC, Infante JR. Tolcher AW, et al. Among authors: fairbrother wj. Clin Cancer Res. 2016 Sep 15;22(18):4567-73. doi: 10.1158/1078-0432.CCR-16-0308. Epub 2016 Apr 13. Clin Cancer Res. 2016. PMID: 27076626 Clinical Trial.
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: fairbrother wj. 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. Among authors: fairbrother wj. Toxicol Sci. 2012 Nov;130(1):205-13. doi: 10.1093/toxsci/kfs235. Epub 2012 Jul 28. Toxicol Sci. 2012. PMID: 22843607
Toxicity profile of small-molecule IAP antagonist GDC-0152 is linked to TNF-α pharmacology.
Erickson RI, Tarrant J, Cain G, Lewin-Koh SC, Dybdal N, Wong H, Blackwood E, West K, Steigerwalt R, Mamounas M, Flygare JA, Amemiya K, Dambach D, Fairbrother WJ, Diaz D. Erickson RI, et al. Among authors: fairbrother wj. Toxicol Sci. 2013 Jan;131(1):247-58. doi: 10.1093/toxsci/kfs265. Epub 2012 Sep 5. Toxicol Sci. 2013. PMID: 22956632
126 results