Disposition of GDC-0879, a B-RAF kinase inhibitor in preclinical species Disposition of G-0879 in preclinical species

Xenobiotica

Volumn 39, Issue 9, 2009, Pages 700-709

  Choo, E F ^a   Driscoll, J P ^a   Feng, J ^a   Liederer, B ^a   Plise, E ^a   Randolph, N ^b   Shin, Y ^a   Wong, S ^a   Ran, Y ^a  

^a GENENTECH INC   (United States)

^b ARRAY BIOPHARMA INC   (United States)

Author keywords

B RAF; Disposition; Pharmacokinetics

Indexed keywords

2 [4 [(1E) 1 (HYDROXYIMINO) 2,3 DIHYDRO 1H INDEN 5 YL] 3 (PYRIDINE 4 YL) 1H PYRAZOL 1 YL]ETHAN 1 OL; DRUG METABOLITE; G 0303748; G 030748; GDC 0879; PROTEIN SERINE THREONINE KINASE INHIBITOR; UNCLASSIFIED DRUG; 2 (4 (1 (HYDROXYIMINO) 2,3 DIHYDRO 1H INDEN 5 YL) 3 (PYRIDIN 4 YL) 1H PYRAZOL 1 YL)ETHAN 1 OL; 2-(4-(1-(HYDROXYIMINO)-2,3-DIHYDRO-1H-INDEN-5-YL)-3-(PYRIDIN-4-YL)-1H-PYRAZOL-1-YL)ETHAN-1-OL; B RAF KINASE; INDENE DERIVATIVE; PLASMA PROTEIN; PROTEIN KINASE INHIBITOR; PYRAZOLE DERIVATIVE;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DOG; DRUG ABSORPTION; DRUG BILE LEVEL; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG CLEARANCE; DRUG DISPOSITION; DRUG DISTRIBUTION; DRUG ELIMINATION; DRUG EXCRETION; DRUG FORMULATION; DRUG HALF LIFE; DRUG METABOLISM; DRUG PROTEIN BINDING; DRUG SOLUBILITY; DRUG URINE LEVEL; FEMALE; FOOD INTAKE; HUMAN; MALE; MAXIMUM PLASMA CONCENTRATION; MONKEY; MOUSE; NONHUMAN; PH; PLASMA PROTEIN BINDING; RAT; SPECIES DIFFERENCE; TIME TO MAXIMUM PLASMA CONCENTRATION; ANIMAL; CHEMISTRY; DRUG ANTAGONISM; DRUG SCREENING; HALF LIFE TIME; MACACA; METABOLIC CLEARANCE RATE; METABOLISM; PROTEIN BINDING; SPRAGUE DAWLEY RAT;

CANIS FAMILIARIS; RATTUS;

ANIMALS; BLOOD PROTEINS; DOGS; DRUG EVALUATION, PRECLINICAL; FEMALE; HALF-LIFE; HUMANS; INDENES; MACACA FASCICULARIS; MALE; METABOLIC CLEARANCE RATE; MICE; PROTEIN BINDING; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS B-RAF; PYRAZOLES; RATS; RATS, SPRAGUE-DAWLEY;

EID: 70350510899     PISSN: 00498254     EISSN: 13665928     Source Type: Journal    
DOI: 10.1080/00498250902991827     Document Type: Article

References (24)

1. Boxenbaum H. (1982). Interspecies scaling, allometry, physiological time, and the ground plan of pharmacokinetics. J Pharmacokinet Biopharmaceut 10:201-227
2. Boyer SJ. (2006). Raf modulators and methods of use. Expert Opin Ther Patent 16:1031-1036
3. Davies H, Bignell GR, Cox C, Stephens P, Edkins S, Clegg S, Teague J, Woffendin H, Garnett MJ, Bottomley W, et al. (2002). Mutations of the BRAF gene in human cancer. Nature 417:949-954
4. Gollob JA, Wilhelm S, Carter C, Kelley SL. (2006). Role of Raf kinase in cancer: therapeutic potential of targeting the Raf/MEK/ERK signal transduction pathway. Sem Oncol 33:392-406.
5. Hansen JD, Grina J, Newhouse B, Welch M, Topalov G, Littman N, Callejo M, Gloor S, Martinson M, Laird E, et al. (2008). Potent and selective pyrazole-based inhibitors of B-Raf kinase. Bioorg Med Chem Lett 18:4692-4695
6. Hoeflich KP, Gray DC, Eby MT, Tien JY, Wong L, Bower J, Gogineni A, Zha J, Cole MJ, Stern HM, et al. (2006). Oncogenic BRAF is required for tumor growth and maintenance in melanoma models. Cancer Res 66:999-1006.
7. Hoeflich KP, Herter S, Tien J, Wong L, Berry L, Chan J, O'brien C, Modrusan Z, Seshagiri S, Lackner M, et al. (2009). 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. Cancer Res 69:3042-3051
8. Khazak V, Astsaturov I, Serebriiskii IG, Golemis EA. (2007). Selective Raf inhibition in cancer therapy. Expert Opin Ther Target 11:1587-1609
9. Lave T, Dupin S, Schmitt C, Chou RC, Jaeck D, Coassolo P. (1997). Integration of in vitro data into allometric scaling to predict hepatic metabolic clearance in man: application to 10 extensively metabolized drugs. J Pharmaceut Sci 86:584-590
10. Lui CY, Amidon GL, Berardi RR, Fleisher D, Youngberg C, Dressman JB. (1986). Comparison of gastrointestinal pH in dogs and humans: implications on the use of the beagle dog as a model for oral absorption in humans. J Pharmaceut Sci 75:271-274
11. Madhunapantula SV, Robertson GP. (2008). Is B-Raf a good therapeutic target for melanoma and other malignancies? Cancer Res 68:5-8.
12. Mahmood I, Balian JD. (1996). Interspecies scaling: predicting clearance of drugs in humans. Three different approaches. Xenobiotica 26:887-895
13. Mercer KE, Pritchard CA. (2003). Raf proteins and cancer: B-Raf is identified as a mutational target. Biochim Biophys Acta 1653:25-40.
14. Panka DJ, Atkins MB, Mier JW. (2006). Targeting the mitogen- activated protein kinase pathway in the treatment of malignant melanoma. Clin Cancer Res 12:2371s-5s.
15. Rowland M, Tozer TN. (1995). Clinical pharmacokinetics: concepts and applications. 3rd ed. Philadelphia, PA: Lippincott Williams & Wilkins.
16. Schreck R, Rapp UR. (2006). Raf kinases: Oncogenesis and drug discovery. Int J Cancer 15;119(10):2261-2271
17. Sebolt-Leopold JS, Herrera R. (2004). Targeting the mitogen-activated protein kinase cascade to treat cancer. Nat Rev Cancer 4:937-947
18. Tibbitts J. (2003). Issues related to the use of canines in toxicologic pathology - issues with pharmacokinetics and metabolism. Toxicol Pathol 31(Suppl.):17-24.
19. Wilhelm SM, Carter C, Tang L, Wilkie D, Mcnabola A, Rong H, Chen C, Zhang X, Vincent P, McHugh M, et al. (2004). BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res 64:7099-7109
20. Wilhelm S, Chien DS. (2002). BAY 43-9006: preclinical data. Curr Pharmaceut Design 8:2255-2257
21. Wong H, Belvin M, Herter S, Hoeflich KP, Murray LJ, Wong L, Choo EF. (2009). 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 1 inhibition, and efficacy. J Pharmacol Exp Ther 329:360-367
22. Yuen ST, Davies H, Chan TL, Ho JW, Bignell GR, Cox C, Stephens P, Edkins S, Tsui WW, Chan AS, et al. (2002). Similarity of the phenotypic patterns associated with BRAF and KRAS mutations in colorectal neoplasia. Cancer Res 62:6451-6455
23. Zebisch A, Troppmair J. (2006). Back to the roots: the remarkable RAF oncogene story. Cell Mol Life Sci 63:1314-1330
24. Zhou R, Moench P, Heran C, Lu X, Mathias N, Faria TN, Wall DA, Hussain MA, Smith RL, Sun D. (2005). pH-dependent dissolution in vitro and absorption in vivo of weakly basic drugs: development of a canine model. Pharmaceut Res 22:188-192