Pharmacokinetic evaluation of axitinib

Expert Opinion on Drug Metabolism and Toxicology

Volumn 8, Issue 2, 2012, Pages 259-270

  Patson, Brian ^a   Cohen, Roger B ^a   Olszanski, Anthony J ^a  

^a FOX CHASE CANCER CENTER   (United States)

Author keywords

AG 013736; angiogenesis; axitinib; vascular endothelial growth factor; VEGF; VEGFR

Indexed keywords

AXITINIB; BEVACIZUMAB; BIOLOGICAL MARKER; CARBOPLATIN; DOCETAXEL; FLUOROURACIL; FOLINIC ACID; GEMCITABINE; IRINOTECAN; OXALIPLATIN; PACLITAXEL; PAZOPANIB; PLACEBO; SORAFENIB; SUNITINIB;

ABDOMINAL PAIN; ANEMIA; ANOREXIA; ASTHENIA; BONE MARROW SUPPRESSION; BREAST CANCER; CANCER COMBINATION CHEMOTHERAPY; COLORECTAL CANCER; DECREASED APPETITE; DIARRHEA; DRUG ABSORPTION; DRUG DOSE ESCALATION; DRUG DOSE TITRATION; DRUG EFFICACY; DRUG MECHANISM; DRUG METABOLISM; DRUG SAFETY; DRUG TOLERABILITY; DYSPHONIA; ERYTHROCYTOSIS; FATIGUE; FEBRILE NEUTROPENIA; GASTROINTESTINAL STROMAL TUMOR; HAIR COLOR; HAND FOOT SYNDROME; HEMOPTYSIS; HOARSENESS; HUMAN; HYPERTENSION; HYPOPHOSPHATEMIA; HYPOTHYROIDISM; KIDNEY CARCINOMA; LIVER CELL CARCINOMA; LIVER FUNCTION TEST; LUNG NON SMALL CELL CANCER; MELANOMA; MUCOSA INFLAMMATION; MULTIPLE CYCLE TREATMENT; NAUSEA; NEUROENDOCRINE TUMOR; NONHUMAN; NUCLEAR MAGNETIC RESONANCE IMAGING; PANCREAS CANCER; PANCREAS TUMOR; PERIPHERAL EDEMA; PHARMACODYNAMICS; PROTEINURIA; RASH; REVIEW; SEIZURE; SIDE EFFECT; STOMATITIS; THROMBOEMBOLISM; THYROID CANCER; VOMITING;

ANIMALS; CARCINOMA, NON-SMALL-CELL LUNG; CLINICAL TRIALS AS TOPIC; HUMANS; IMIDAZOLES; INDAZOLES; KIDNEY NEOPLASMS; LUNG NEOPLASMS; MAGNETIC RESONANCE IMAGING; PANCREATIC NEOPLASMS; PROTEIN KINASE INHIBITORS; THYROID NEOPLASMS;

EID: 84856082820     PISSN: 17425255     EISSN: 17447607     Source Type: Journal    
DOI: 10.1517/17425255.2012.652947     Document Type: Review

References (43)

1. Hicklin DJ, Ellis LM. Role of the vascular endothelial growth factor pathway in tumor growth and angiogenesis. J Clin Oncol 2005;23:1011-27 (Pubitemid 46202320)
2. Ferrara N, Gerber HP, LeCouter J. The biology of VEGFR and its receptors. Nat Med 2003;9:669-76
3. Hurwitz H, Fehrenbacher L, Novotny W, et al. Bevacizumab plus irinotecan, fluorouracil, and leucovorin for metastatic colorectal cancer. N Engl J Med 2004;350:2335-42 (Pubitemid 38702844)
4. Mendel DB, Laird AD, Xin X, et al. In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors. Clin Cancer Res 2003;9:327-37 (Pubitemid 36109749)
5. Wilhelm SM, Carter C, Tang L, et al. 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 2004;64:7099-109 (Pubitemid 39331023)
6. Hu-Lowe DD, Zou HY, Grazzini ML, et al. Nonclinical antiangiogenesis and antitumor activities of axitinib (AG- 013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2, 3. Clin Cancer Res 2008;14:7272-83.
7. Rugo HS, Herbst RS, Liu G, et al. Phase I trial of the oral antiangiogenesis agent AG-013736 in patients with advanced solid tumors: pharmacokinetic and clinical results. J Clin Oncol 2005;23:5474-83.
8. Pithavala YK, Tortorici M, Toh M, et al. Effect of rifampin on the pharmacokinetics of Axitinib (AG-013736) in Japanese and Caucasian healthy volunteers. Cancer Chemother Pharmacol 2010;65:563-70
9. Poller B, Iusuf D, Sparidans RW, et al. Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. Drug Metab Dispos 2011;39:729-35
10. Mignogna C, Staibano S, Altieri V, et al. Prognostic significance of multidrug-resistance protein (MDR-1) in renal clear cell carcinomas: a five year follow-up analysis. BMC Cancer 2006;6:293
11. Pithavala YK, Tong W, Mount J, et al. Effect of ketoconazole on the pharmacokinetics of axitinib in healthy volunteers. Invest New Drugs 2010:1-9
12. Hoskins JM, Goldberg RM, Qu P, et al. UGT1A1.*28 genotype and irinotecan-induced neutropenia: dose matters. J Natl Cancer Inst 2007;99:1290-5 (Pubitemid 47394168)
13. Tortorici M, Chen Y, Hee B, et al. Effect of food on the pharmacokinetics (PK) of axitinib in healthy volunteers (HVs). Ejc Suppl 2010;8(5):71-1 Meeting Abstract: 273
14. Rixe O, Bukowski RM, Michaelson MD, et al. Axitinib treatment in patients with cytokine-refractory metastatic renal-cell cancer: a phase II study. Lancet Oncol 2007;8:975-84 (Pubitemid 47629888)
15. Rini BI, Wilding G, Hudes G, et al. Phase II study of axitinib in sorafenib-refractory metastatic renal cell carcinoma. J Clin Oncol 2009;27:4462-8
16. Rini BI, Escudier B, Tomczak P, et al. Comparative effectiveness of axitinib versus sorafenib in advanced renal cell carcinoma (AXIS): a randomised phase 3 trial. Lancet 2011
17. Cohen EE, Rosen LS, Vokes EE, et al. Axitinib is an active treatment for all histologic subtypes of advanced thyroid cancer: results from a phase II study. J Clin Oncol 2008;26:4708-13
18. Schiller JH, Larson T, Ou SH, et al. Efficacy and safety of axitinib in patients with advanced non-small-cell lung cancer: results from a phase II study. J Clin Oncol 2009;27:3836-41
19. Rini BI, Schiller JH, Fruehauf JP, et al. Diastolic blood pressure as a biomarker of axitinib efficacy in solid tumors. Clin Cancer Res 2011;17:3841-9
20. Fruehauf J, Lutzky J, McDermott D, et al. Multicenter, phase ii study of axitinib, a selective second-generation inhibitor of vascular endothelial growth factor receptors 1, 2, and 3, in patients with metastatic melanoma. Clin Cancer Res 2011;17:7462-9
21. Spano JP, Chodkiewicz C, Maurel J, et al. Efficacy of gemcitabine plus axitinib compared with gemcitabine alone in patients with advanced pancreatic cancer: an open-label randomised phase II study. Lancet 2008;371:2101-8
22. Kindler HL, Ioka T, Richel DJ, et al. Axitinib plus gemcitabine versus placebo plus gemcitabine in patients with advanced pancreatic adenocarcinoma: a double-blind randomised phase 3 study. Lancet Oncol 2011;12:256-62
23. Rugo HS, Stopeck AT, Joy AA, et al. Randomized, placebo-controlled, double-blind, phase ii study of axitinib plus docetaxel versus docetaxel plus placebo in patients with metastatic breast cancer. J Clin Oncol 2011;29:2459-65
24. Bendell JC, Tournigand C, Bednarczyk M, et al. Axitinib or bevacizumab (bev) plus FOLFOX or FOLFIRI as second-line therapy in patients (pts) with metastatic colorectal cancer (mCRC) [abstracts 29]. ASCO Meeting; 2011. p. 478
25. Llovet JM, Ricci S, Mazzaferro V, et al. Sorafenib in advanced hepatocellular carcinoma. N Engl J Med 2008;359:378-90
26. Motzer RJ, Hutson TE, Tomczak P, et al. Sunitinib versus interferon alfa in metastatic renal-cell carcinoma. N Engl J Med 2007;356:115-24 (Pubitemid 46089672)
27. Rixe O, Billemont B, Izzedine H. Hypertension as a predictive factor of Sunitinib activity. Ann Oncol 2007;18:1117 (Pubitemid 47050505)
28. Rixe O, Dutcher JP, Motzer RJ, et al. Association between diastolic blood pressure (Dbp) >= 90 Mmhg and efficacy in patients (Pts) with metastatic renal cell carcinoma (Mrcc) receiving axitinib (Ag-013736; Ag). Ann Oncol 2008;19:189-9
29. Therasse P, Arbuck SG, Eisenhauer EA, et al. New guidelines to evaluate the response to treatment in solid tumors. European Organization for Research and Treatment Of Cancer, National Cancer Institute Of The United states, National Cancer Institute Of Canada. J Natl Cancer Inst 2000;92:205-16 (Pubitemid 30099779)
30. Yuh WT. An exciting and challenging role for the advanced contrast MR imaging. J Magn Reson Imaging 1999;10:221-2 (Pubitemid 29463103)
31. Taylor JS, Tofts PS, Port R, et al. MR imaging of tumor microcirculation: promise for the new millennium. J Magn Reson Imaging 1999;10:903-7
32. Padhani AR. Dynamic contrast-enhanced MRI in clinical oncology: current status and future directions. J Magn Reson Imaging 2002;16:407-22 (Pubitemid 35167876)
33. Checkley D, Tessier JJ, Kendrew J, et al. Use of dynamic contrast-enhanced MRI to evaluate acute treatment with ZD6474, a VEGFR signalling inhibitor, in PC-3 prostate tumours. Br J Cancer 2003;89:1889-95 (Pubitemid 37533265)
34. Mukohara T, Nakajima H, Mukai H, et al. Effect of axitinib (AG 013736) on fatigue, thyroid stimulating hormone, and biomarkers: a phase I study in Japanese patients. Cancer Sci 2010;101:963-8
35. Desai J, Yassa L, Marqusee E, et al. Hypothyroidism after sunitinib treatment for patients with gastrointestinal stromal tumors. Ann Intern Med 2006;145:660-4 (Pubitemid 46768841)
36. Hoh C, Infante JR, Burris HA, et al. Axitinib inhibition of [18F] fluorothymidine (FLT) uptake in patients (pts) with colorectal cancer (CRC): Implications for cytotoxic chemotherapy combinations [abstracts 29]. ASCO Meeting; 2011. p. 3591
37. Blanke CD, Rankin C, Demetri GD, et al. Phase III randomized, intergroup trial assessing imatinib mesylate at two dose levels in patients with unresectable or metastatic gastrointestinal stromal tumors expressing the kit receptor tyrosine kinase: S0033. J Clin Oncol 2008;26:626-32 (Pubitemid 351264358)
38. Saltz LB, Clarke S, Diaz-Rubio E, et al. Bevacizumab in combination with oxaliplatin-based chemotherapy as first-line therapy in metastatic colorectal cancer: a randomized phase III study. J Clin Oncol 2008;26:2013-19
39. Axitinib (AG 013736) As Second Line Therapy For Metastatic Renal Cell Cancer, U.S. National Institutes of Health, 2010
40. Schmidinger M, Bellmunt J. Plethora of agents, plethora of targets, plethora of side effects in metastatic renal cell carcinoma. Cancer Treat Rev 2010;36:416-24
41. Hamberg P, Verweij J, Sleijfer S. (Pre-) clinical pharmacology and activity of pazopanib, a novel multikinase angiogenesis inhibitor. Oncologist 2010;15:539-47
42. Kumar R, Knick VB, Rudolph SK, et al. Pharmacokinetic-pharmacodynamic correlation from mouse to human with pazopanib, a multikinase angiogenesis inhibitor with potent antitumor and antiangiogenic activity. Mol Cancer Ther 2007;6:2012-21 (Pubitemid 47052491)
43. Chow LQ, Eckhardt SG. Sunitinib: from rational design to clinical efficacy. J Clin Oncol 2007;25:884-96. (Pubitemid 350002890)