Preclinical pharmacokinetics of the novel PI3K inhibitor GDC-0941 and prediction of its pharmacokinetics and efficacy in human

References

• Boxenbaum H. (1982). Interspecies scaling, allometry, physiological time, and the ground plan of pharmacokinetics. J Pharmacokinet Biopharm 10:201–227.
   PubMedGoogle Scholar
• Chalhoub N, Baker SJ. (2009). PTEN and the PI3-kinase pathway in cancer. Annu Rev Pathol 4:127–150.
   PubMed Web of Science ®Google Scholar
• Davies B, Morris T. (1993). Physiological parameters in laboratory animals and humans. Pharm Res 10:1093–1095.
   PubMed Web of Science ®Google Scholar
• Engelman JA. (2009). Targeting PI3K signalling in cancer: opportunities, challenges and limitations. Nat Rev Cancer 9:550–562.
   PubMed Web of Science ®Google Scholar
• Engelman JA, Luo J, Cantley LC. (2006). The evolution of phosphatidylinositol 3-kinases as regulators of growth and metabolism. Nat Rev Genet 7:606–619.
   PubMed Web of Science ®Google Scholar
• Folkes AJ, Ahmadi K, Alderton WK, Alix S, Baker SJ, Box G, Chuckowree IS, Clarke PA, Depledge P, Eccles SA, Friedman LS, Hayes A, Hancox TC, Kugendradas A, Lensun L, Moore P, Olivero AG, Pang J, Patel S, Pergl-Wilson GH, Raynaud FI, Robson A, Saghir N, Salphati L, Sohal S, Ultsch MH, Valenti M, Wallweber HJ, Wan NC, Wiesmann C, Workman P, Zhyvoloup A, Zvelebil MJ, Shuttleworth SJ. (2008). The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer. J Med Chem 51:5522–5532.
   PubMed Web of Science ®Google Scholar
• Ghigo A, Hirsch E. (2008). Isoform selective phosphoinositide 3-kinase gamma and delta inhibitors and their therapeutic potential. Recent Pat Inflamm Allergy Drug Discov 2:1–10.
   PubMedGoogle Scholar
• Gibaldi M, Perrier D. (1982). Pharmacokinetics. New York: Marcel Dekker.
   Google Scholar
• Gibbs JP. (2010). Prediction of exposure-response relationships to support first-in-human study design. AAPS J 12:750–758.
   PubMed Web of Science ®Google Scholar
• Liu P, Cheng H, Roberts TM, Zhao JJ. (2009). Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov 8:627–644.
   PubMed Web of Science ®Google Scholar
• Luo J, Manning BD, Cantley LC. (2003). Targeting the PI3K-Akt pathway in human cancer: rationale and promise. Cancer Cell 4:257–262.
   PubMed Web of Science ®Google Scholar
• Mahmood I, Balian JD. (1996). Interspecies scaling: predicting clearance of drugs in humans. Three different approaches. Xenobiotica 26:887–895.
   PubMed Web of Science ®Google Scholar
• Maira SM, Stauffer F, Brueggen J, Furet P, Schnell C, Fritsch C, Brachmann S, Chène P, De Pover A, Schoemaker K, Fabbro D, Gabriel D, Simonen M, Murphy L, Finan P, Sellers W, García-Echeverría C. (2008). Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. Mol Cancer Ther 7:1851–1863.
   PubMed Web of Science ®Google Scholar
• Obach RS, Baxter JG, Liston TE, Silber BM, Jones BC, MacIntyre F, Rance DJ, Wastall P. (1997). The prediction of human pharmacokinetic parameters from preclinical and in vitro metabolism data. J Pharmacol Exp Ther 283:46–58.
   PubMed Web of Science ®Google Scholar
• Raynaud FI, Eccles SA, Patel S, Alix S, Box G, Chuckowree I, Folkes A, Gowan S, De Haven Brandon A, Di Stefano F, Hayes A, Henley AT, Lensun L, Pergl-Wilson G, Robson A, Saghir N, Zhyvoloup A, McDonald E, Sheldrake P, Shuttleworth S, Valenti M, Wan NC, Clarke PA, Workman P. (2009). Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941. Mol Cancer Ther 8:1725–1738.
   PubMed Web of Science ®Google Scholar
• Salphati L, Lee LB, Pang J, Plise EG, Zhang X. (2010a). Role of P-glycoprotein and breast cancer resistance protein-1 in the brain penetration and brain pharmacodynamic activity of the novel phosphatidylinositol 3-kinase inhibitor GDC-0941. Drug Metab Dispos 38:1422–1426.
   PubMed Web of Science ®Google Scholar
• Salphati L, Wong H, Belvin M, Bradford D, Edgar KA, Prior WW, Sampath D, Wallin JJ. (2010b). Pharmacokinetic-pharmacodynamic modeling of tumor growth inhibition and biomarker modulation by the novel phosphatidylinositol 3-kinase inhibitor GDC-0941. Drug Metab Dispos 38:1436–1442.
   PubMed Web of Science ®Google Scholar
• Sarker D, Kristeleit R, Mazina KE, Ware JA, Yan Y, Dresser M, Derynck MA, de Bono JS. (2009). A phase I study evaluating the pharmacokinetics (PK) and pharmacodynamics (PD) of the oral pan-phosphoinositide-3 kinase (PI3K) inhibitor GDC-0941. J Clin Oncol 27, suppl; abstract 3538.
   Web of Science ®Google Scholar
• Seipelt I, Gerlach M, Baasner S, Blumenstein L, Schmidt P, Mueller G, Aicher B, Engel J, Guenther E, Teifel M. (2010). AEZS-132, a new orally bioavailable PI3K/Erk inhibitor with antitumor effects. Eur J Cancer 8, suppl; abstract 197.
   Google Scholar
• Shapiro G, Molina J, Bendell J, Brana I, Spicer J, Kwak E, Pandya S, Milham R, Houk B, Bell-McGuinn K. (2010). First-in-human study of PF-05212384, a small molecule intravenous dual inhibitor of PI3K and mTOR in patients with advanced cancer: preliminary report on safety and pharmacokinetics. Eur J Cancer 8, suppl; abstract 387.
   Google Scholar
• Wong KK, Engelman JA, Cantley LC. (2010). Targeting the PI3K signaling pathway in cancer. Curr Opin Genet Dev 20:87–90.
   PubMed Web of Science ®Google Scholar