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Preclinical pharmacokinetics and metabolism of 6-(4-(2,5-difluorophenyl)oxazol-5-yl)-3-isopropyl-[1,2,4]-triazolo[4,3-a]pyridine, a novel and selective p38alpha inhibitor: identification of an active metabolite in preclinical species and human liver microsomes.
Kalgutkar AS, Hatch HL, Kosea F, Nguyen HT, Choo EF, McClure KF, Taylor TJ, Henne KR, Kuperman AV, Dombroski MA, Letavic MA. Kalgutkar AS, et al. Among authors: choo ef. Biopharm Drug Dispos. 2006 Nov;27(8):371-86. doi: 10.1002/bdd.520. Biopharm Drug Dispos. 2006. PMID: 16944451
Pharmacodynamics of 2-[4-[(1E)-1-(hydroxyimino)-2,3-dihydro-1H-inden-5-yl]-3-(pyridine-4-yl)-1H-pyrazol-1-yl]ethan-1-ol (GDC-0879), a potent and selective B-Raf kinase inhibitor: understanding relationships between systemic concentrations, phosphorylated mitogen-activated protein kinase kinase 1 inhibition, and efficacy.
Wong H, Belvin M, Herter S, Hoeflich KP, Murray LJ, Wong L, Choo EF. Wong H, et al. Among authors: choo ef. J Pharmacol Exp Ther. 2009 Apr;329(1):360-7. doi: 10.1124/jpet.108.148189. Epub 2009 Jan 15. J Pharmacol Exp Ther. 2009. PMID: 19147858
Antitumor efficacy of the novel RAF inhibitor GDC-0879 is predicted by BRAFV600E mutational status and sustained extracellular signal-regulated kinase/mitogen-activated protein kinase pathway suppression.
Hoeflich KP, Herter S, Tien J, Wong L, Berry L, Chan J, O'Brien C, Modrusan Z, Seshagiri S, Lackner M, Stern H, Choo E, Murray L, Friedman LS, Belvin M. Hoeflich KP, et al. Cancer Res. 2009 Apr 1;69(7):3042-51. doi: 10.1158/0008-5472.CAN-08-3563. Epub 2009 Mar 10. Cancer Res. 2009. PMID: 19276360
Potent and selective aminopyrimidine-based B-Raf inhibitors with favorable physicochemical and pharmacokinetic properties.
Mathieu S, Gradl SN, Ren L, Wen Z, Aliagas I, Gunzner-Toste J, Lee W, Pulk R, Zhao G, Alicke B, Boggs JW, Buckmelter AJ, Choo EF, Dinkel V, Gloor SL, Gould SE, Hansen JD, Hastings G, Hatzivassiliou G, Laird ER, Moreno D, Ran Y, Voegtli WC, Wenglowsky S, Grina J, Rudolph J. Mathieu S, et al. Among authors: choo ef. J Med Chem. 2012 Mar 22;55(6):2869-81. doi: 10.1021/jm300016v. Epub 2012 Feb 29. J Med Chem. 2012. PMID: 22335519
Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor.
Wong H, Vernillet L, Peterson A, Ware JA, Lee L, Martini JF, Yu P, Li C, Del Rosario G, Choo EF, Hoeflich KP, Shi Y, Aftab BT, Aoyama R, Lam ST, Belvin M, Prescott J. Wong H, et al. Among authors: choo ef. Clin Cancer Res. 2012 Jun 1;18(11):3090-9. doi: 10.1158/1078-0432.CCR-12-0445. Epub 2012 Apr 10. Clin Cancer Res. 2012. PMID: 22496205
61 results