Dose selection, pharmacokinetics, and pharmacodynamics of BRAF inhibitor dabrafenib (GSK2118436)

Clinical Cancer Research

Volumn 20, Issue 17, 2014, Pages 4449-4458

  Falchook, Gerald S ^a   Long, Georgina V ^b,c   Kurzrock, Razelle ^d   Kim, Kevin B ^a   Arkenau, H Tobias ^e   Brown, Michael P ^f   Hamid, Omid ^g   Infante, Jeffrey R ^h   Millward, Michael ⁱ   Pavlick, Anna ^j   Chin, Melvin T ^k   O'Day, Steven J ^g   Blackman, Samuel C ^l   Martin, Curtis ^l   Lebowitz, Peter ^l   Ma, Bo ^l   Ouellet, Daniele ^l   Kefford, Richard F ^b,c  

^a UNIVERSITY OF TEXAS MD ANDERSON CANCER CENTER   (United States)

^b UNIVERSITY OF SYDNEY   (Australia)

^c WESTMEAD HOSPITAL   (Australia)

^d UNIVERSITY OF CALIFORNIA SAN DIEGO   (United States)

^e PRINCE OF WALES HOSPITAL   (Australia)

^f UNIVERSITY OF ADELAIDE   (Australia)

^g Angeles Clinic and Research Institute   (United States)

^h SARAH CANNON RESEARCH INSTITUTE   (United States)

ⁱ UNIVERSITY OF WESTERN AUSTRALIA   (Australia)

^j NEW YORK UNIVERSITY SCHOOL OF MEDICINE   (United States)

^k UNIVERSITY OF NEW SOUTH WALES   (Australia)

^l GLAXOSMITHKLINE   (United States)

more..

Author keywords

[No Author keywords available]

Indexed keywords

B RAF KINASE; DABRAFENIB; FLUORODEOXYGLUCOSE; MITOGEN ACTIVATED PROTEIN KINASE; IMIDAZOLE DERIVATIVE; OXIME; PROTEIN KINASE INHIBITOR;

AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG DOSE COMPARISON; DRUG SAFETY; DRUG TOLERABILITY; ENZYME PHOSPHORYLATION; FAINTNESS; FEMALE; FEVER; GENE MUTATION; HUMAN; HYPONATREMIA; MAJOR CLINICAL STUDY; MALE; MELANOMA; PHARMACODYNAMICS; PHASE 1 CLINICAL TRIAL; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; SKIN CARCINOMA; ADULT; AGED; ANTAGONISTS AND INHIBITORS; CLINICAL TRIAL; DRUG ADMINISTRATION; GENETICS; MIDDLE AGED; MUTATION; PATHOLOGY; TREATMENT OUTCOME; VERY ELDERLY;

ADULT; AGED; AGED, 80 AND OVER; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG ADMINISTRATION SCHEDULE; FEMALE; HUMANS; IMIDAZOLES; MALE; MELANOMA; MIDDLE AGED; MUTATION; OXIMES; POSITRON-EMISSION TOMOGRAPHY; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS B-RAF; TREATMENT OUTCOME;

EID: 84917728415     PISSN: 10780432     EISSN: 15573265     Source Type: Journal    
DOI: 10.1158/1078-0432.CCR-14-0887     Document Type: Article

References (17)

1. Laquerre S, Arnone M, Moss K, Yang J, Fisher KE, Kane-Carson LS, et al. A selective raf kinase inhibitor induces cell death and tumor regression of human cancer cell lines encoding B-RafV600E mutation. Mol Cancer Ther 2009;8(Suppl 12):B88.
2. Hauschild A, Grob JJ, Demidov LV, Jouary T, Gutzmer R, Millward M, et al. Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial. Lancet 2012;380:358-65.
3. Simon R, Freidlin B, Rubinstein L, Arbuck SG, Collins J, Christian MC. Accelerated titration designs for phase I clinical trials in oncology. J Natl Cancer Inst 1997;89:1138-47.
4. Goodwin R, Giaccone G, Calvert H, Lobbezoo M, Eisenhauer EA. Targeted agents: how to select the winners in preclinical and early clinical studies? Eur J Cancer 2012;48:170-8.
5. Ivy SP, Siu LL, Garrett-Mayer E, Rubinstein L. Approaches to phase 1 clinical trial design focused on safety, efficiency, and selected patient populations: a report from the clinical trial design task force of the national cancer institute investigational drug steering committee. Clin Cancer Res 2010;16:1726-36.
6. Falchook GS, Long GV, Kurzrock R, Kim KB, Arkenau TH, Brown MP, et al. Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial. Lancet 2012;379:1893-901.
7. Common terminology criteria for adverse events (CTCAE) v3.0, 2011. [Accessed December 2, 2012]. Available from: http://ctep.cancer.gov/protocolDevelopment/electronic-applications/docs/ctcaev3.pdf.
8. Therasse P, Arbuck SG, Eisenhauer EA, Wanders J, Kaplan RS, Rubinstein L, 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.
9. Tran JQ, Kovacs SJ, McIntosh TS, Davis HM, Martin DE. Morning spot and 24-hour urinary 6 beta-hydroxycortisol to cortisol ratios: Intraindividual variability and correlation under basal conditions and conditions of CYP 3A4 induction. J Clin Pharmacol 1999;39:487-94.
10. Adjei AA. What is the right dose? the elusive optimal biologic dose in phase I clinical trials. J Clin Oncol 2006;24:4054-5.
11. Skipper HE, Schabel FM Jr, Wilcox WS. Experimental evaluation of potential anticancer agents. xiii. on the criteria and kinetics associated with "curability" of experimental leukemia. Cancer Chemother Rep 1964;35:1-111.
12. Skipper HE, Schabel FM Jr, Mellett LB, Montgomery JA, Wilkoff LJ, Lloyd HH, et al. Implications of biochemical, cytokinetic, pharmacologic, and toxicologic relationships in the design of optimal therapeutic schedules. Cancer Chemother Rep 1970;54:431-50.
13. Gordon MS, Margolin K, Talpaz M, Sledge GW Jr, Holmgren E, Benjamin R, et al. Phase I safety and pharmacokinetic study of recombinant human anti-vascular endothelial growth factor in patients with advanced cancer. J Clin Oncol 2001;19:843-50.
14. Slamon DJ. Final study report (FSR) for H0407g: A phase 1 safety and tolerance study of intravenous anti-p185 HER2 humanized monoclonal antibody (rhu MAb HER2) in patients with HER2 overexpressing tumors. Silver Spring, MD: US Food and Drug Administration; 1996.
15. Druker BJ, Talpaz M, Resta DJ, Peng B, Buchdunger E, Ford JM, et al. Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia. N Engl J Med 2001;344:1031-7.
16. Issa JP, Garcia-Manero G, Giles FJ, Mannari R, Thomas D, Faderl S, et al. Phase 1 study of low-dose prolonged exposure schedules of the hypomethylating agent 5-aza-20-deoxycytidine (decitabine) in hematopoietic malignancies. Blood 2004;103:1635-40.
17. Jain RK, Lee JJ, Hong D, Markman M, Gong J, Naing A, et al. Phase I oncology studies: evidence that in the era of targeted therapies patients on lower doses do not fare worse. Clin Cancer Res 2010;16:1289-97.