Clinical development of dabrafenib in BRAF mutant melanoma and other malignancies

Expert Opinion on Drug Metabolism and Toxicology

Volumn 9, Issue 7, 2013, Pages 893-899

  Gibney, Geoffrey T ^a   Zager, Jonathan S ^a  

^a H LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE   (United States)

Author keywords

BRAF inhibitor; Dabrafenib; GSK2118436; Melanoma

Indexed keywords

ARQ 736; B RAF KINASE; CHIR 265; DABRAFENIB; DACARBAZINE; LGX 818; SORAFENIB; TRAMETINIB; UNCLASSIFIED DRUG; VEMURAFENIB; XL 281;

ARTHRALGIA; ARTICLE; BRAIN HEMORRHAGE; BRAIN METASTASIS; CANCER SURVIVAL; COLORECTAL CANCER; CONVULSION; DISEASE ACTIVITY; DRUG BLOOD LEVEL; DRUG DOSE ESCALATION; DRUG DOSE REDUCTION; DRUG EFFICACY; DRUG HALF LIFE; DRUG MEGADOSE; DRUG METABOLISM; DRUG SAFETY; DRUG TOLERABILITY; DRUG WITHDRAWAL; FATIGUE; FEVER; GASTROINTESTINAL STROMAL TUMOR; GENE MUTATION; HAIRY CELL LEUKEMIA; HEADACHE; HOSPITAL PATIENT; HUMAN; HYPERKERATOSIS; IC 50; IN VITRO STUDY; KERATOACANTHOMA; KIDNEY CARCINOMA; LIVER CELL CARCINOMA; LUNG NON SMALL CELL CANCER; MAXIMUM PLASMA CONCENTRATION; MAXIMUM TOLERATED DOSE; MELANOMA; METASTATIC MELANOMA; MOLECULAR WEIGHT; MONOTHERAPY; NONHUMAN; OVARY CANCER; OVERALL SURVIVAL; PATIENT CARE; PERSONALIZED MEDICINE; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 2 CLINICAL TRIAL (TOPIC); PHASE 3 CLINICAL TRIAL (TOPIC); PROGRESSION FREE SURVIVAL; RANDOMIZED CONTROLLED TRIAL (TOPIC); RECOMMENDED DRUG DOSE; RECURRENT CANCER; SIGNAL TRANSDUCTION; SKIN CARCINOMA; SKIN PAPILLOMA; THYROID CARCINOMA; TREATMENT RESPONSE; TUMOR REGRESSION;

ANTINEOPLASTIC AGENTS; BRAIN NEOPLASMS; CLINICAL TRIALS AS TOPIC; DISEASE-FREE SURVIVAL; DRUG EVALUATION; HUMANS; IMIDAZOLES; INDOLES; MELANOMA; MUTATION; OXIMES; PROTO-ONCOGENE PROTEINS B-RAF; SULFONAMIDES;

EID: 84879231242     PISSN: 17425255     EISSN: 17447607     Source Type: Journal    
DOI: 10.1517/17425255.2013.794220     Document Type: Article

References (34)

1. Davies H, Bignell GR, Cox C, et al. Mutations of the BRAF gene in human cancer. Nature 2002;417:949-54 (Pubitemid 34716871)
2. Davies MA, Samuels Y. Analysis of the genome to personalize therapy for melanoma. Oncogene 2010;29:5545-55
3. Schnittger S, Bacher U, Haferlach T, et al. Development and validation of a real-time quantification assay to detect and monitor BRAFV600E mutations in hairy cell leukemia. Blood 2012;119:3151-4
4. Siegel R, Naishadham D, Jemal A. Cancer statistics. CA Cancer J Clin 2013;63(1):11-30
5. Avril MF, Aamdal S, Grob JJ, et al. Fotemustine compared with dacarbazine in patients with disseminated malignant melanoma: a phase III study. J Clin Oncol 2004;22:1118-25 (Pubitemid 41095046)
6. Hauschild A, Agarwala SS, Trefzer U, et al. Results of a phase III, randomized, placebo-controlled study of sorafenib in combination with carboplatin and paclitaxel as second-line treatment in patients with unresectable stage III or stage IV melanoma. J Clin Oncol 2009;27:2823-30
7. Middleton MR, Grob JJ, Aaronson N, et al. Randomized phase III study of temozolomide versus dacarbazine in the treatment of patients with advanced metastatic malignant melanoma. J Clin Oncol 2000;18:158-66 (Pubitemid 30036349)
8. Keilholz U, Conradt C, Legha SS, et al. Results of interleukin-2-based treatment in advanced melanoma: a case record-based analysis of 631 patients. J Clin Oncol 1998;16:2921-9 (Pubitemid 28417410)
9. Rosenberg SA, Yang JC, Topalian SL, et al. Treatment of 283 consecutive patients with metastatic melanoma or renal cell cancer using high-dose bolus interleukin. Jama 1994;271:907-13.
10. Schwartzentruber DJ, Lawson DH, Richards JM, et al. gp100 peptide vaccine and interleukin-2 in patients with advanced melanoma. N Engl J Med 2011;364:2119-27
11. Hodi FS, O'Day SJ, McDermott DF, et al. Improved survival with ipilimumab in patients with metastatic melanoma. N Engl J Med 2010;363:711-23
12. Robert C, Thomas L, Bondarenko I, et al. Ipilimumab plus dacarbazine for previously untreated metastatic melanoma. N Engl J Med 2011;364:2517-26
13. Flaherty KT, Puzanov I, Kim KB, et al. Inhibition of mutated, activated BRAF in metastatic melanoma. N Engl J Med 2010;363:809-19
14. Chapman PB, Hauschild A, Robert C, et al. Improved survival with vemurafenib in melanoma with BRAF V600E mutation. N Engl J Med 2011;364:2507-16.
15. Falchook GS, Long GV, Kurzrock R, 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.
16. Laquerre S, Arnone M, Moss K, 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:abstract B88
17. Bollag G, Hirth P, Tsai J, et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature 2010;467:596-9
18. Greger JG, Eastman SD, Zhang V, et al. Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations. Mol Cancer Ther 2012;11:909-20
19. Mao M, Tian F, Mariadason JM, et al. Resistance to BRAF inhibition in BRAF-mutant colon cancer can be overcome with PI3K inhibition or demethylating agents. Clin Cancer Res 2013;19:657-67
20. Colombino M, Capone M, Lissia A, et al. BRAF/NRAS mutation frequencies among primary tumors and metastases in patients with melanoma. J Clin Oncol 2012;30:2522-9
21. Ellerhorst JA, Greene VR, Ekmekcioglu S, et al. Clinical correlates of NRAS and BRAF mutations in primary human melanoma. Clin Cancer Res 2011;17:229-35
22. Klein O, Clements A, Menzies AM, et al. BRAF inhibitor activity in V600R metastatic melanoma. Eur J Cancer 2013;49:1073-9
23. Bahadoran P, Allegra M, Giacchero D, et al. Major clinical response to BRAF inhibitor in a patient with BRAF L597R mutated melanoma. Pigment Cell Melanoma Res 2012;25:842
24. Dahlman KB, Xia J, Hutchinson K, et al. BRAF(L597) mutations in melanoma are associated with sensitivity to MEK inhibitors. Cancer Discov 2012;2:791-7
25. Trefzer U, Minor D, Ribas A, et al. BREAK-2: a phase IIA trial of the selective BRAF kinase inhibitor GSK2118436 in patients with BRAF mutation-positive (V600E/K) metastatic melanoma. Pigment Cell Melanoma Res 2011;24:1020
26. Long GV, Trefzer U, Davies MA, et al. Dabrafenib in patients with Val600Glu or Val600Lys BRAF-mutant melanoma metastatic to the brain (BREAK-MB): a multicentre, open-label, phase 2 trial. Lancet Oncol 2012;13:1087-95.
27. Flaherty KT, Infante JR, Daud A, et al. Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations. N Engl J Med 2012;367:1694-703.
28. Flaherty KT, Robert C, Hersey P, et al. Improved survival with MEK inhibition in BRAF-mutated melanoma. N Engl J Med 2012;367:107-14
29. Hauschild A, Grob JJ, Demidov LV, et al. Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial. Lancet 2012;380:358-65.
30. Poulikakos PI, Zhang C, Bollag G, et al. RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF. Nature 2010;464:427-30
31. Andrews DW, Scott CB, Sperduto PW, et al. Whole brain radiation therapy with or without stereotactic radiosurgery boost for patients with one to three brain metastases: phase III results of the RTOG 9508 randomised trial. Lancet 2004;363:1665-72 (Pubitemid 38670323)
32. Callahan MK, Rampal R, Harding JJ, et al. Progression of RAS-mutant leukemia during RAF inhibitor treatment. N Engl J Med 2012;367:2316-21
33. Chapman P, Metz D, Sepulveda A, et al. Development of colonic adenomas and gastric polyps in BRAF mutant melanoma patients treated with vemurafenib. Pigment Cell Melanoma Res 2012;25:847
34. Zimmer L, Hillen U, Livingstone E, et al. Atypical melanocytic proliferations and new primary melanomas in patients with advanced melanoma undergoing selective BRAF inhibition. J Clin Oncol 2012;30:2375-83