RAF-Inhibitoren

Andrulis M, Lehners N, Capper D, Penzel R, Heining C, Huellein J, Zenz T, von Deimling A, Schirmacher P, Ho AD, Goldschmidt H, Neben K, Raab MS (2013) Targeting the BRAF V600E mutation in multiple myeloma. Cancer Discov 3:862–869 CrossRefPubMed

Ascierto PA, Minor D, Ribas A, Lebbe C, O’Hagan A, Arya N, Guckert M, Schadendorf D, Kefford RF, Grob JJ, Hamid O, Amaravadi R, Simeone E, Wilhelm T, Kim KB, Long GV, Martin AM, Mazumdar J, Goodman VL, Trefzer U (2013) Phase II trial (BREAK-2) of the BRAF inhibitor dabrafenib (GSK2118436) in patients with metastatic melanoma. J Clin Oncol. 31(26):3205–3211

Badalian-Very G, Vergilio JA, Degar BA, MacConaill LE, Brandner B, Calicchio ML, Kuo FC, Ligon AH, Stevenson KE, Kehoe SM, Garraway LA, Hahn WC, Meyerson M, Fleming MD, Rollins BJ (2010) Recurrent BRAF mutations in Langerhans cell histiocytosis. Blood 116:1919–1923 CrossRefPubMedPubMedCentral

Brose MS, Cabanillas ME, Cohen EE, Wirth LJ, Riehl T, Yue H, Sherman SI, Sherman EJ (2016) Vemurafenib in patients with BRAF(V600E)-positive metastatic or unresectable papillary thyroid cancer refractory to radioactive iodine: a non-randomised, multicentre, open-label, phase 2 trial. Lancet Oncol 17:1272–1282 CrossRefPubMedPubMedCentral

Boussemart L, Girault I, Malka-Mahieu H, Mateus C, Routier E, Rubington M, Kamsu-Kom N, Thomas M, Tomasic G, Agoussi S, Breckler M, Laporte M, Lacroix L, Eggermont AM, Cavalcanti A, Grange F, Adam J, Vagner S, Robert C (2016) Secondary tumors arising in patients undergoing BRAF inhibitor therapy exhibit increased BRAF-CRAF heterodimerization. Cancer Res 76:1476–1484 CrossRefPubMed

Chapman PB, Hauschild A, Robert C, Haanen JB, Ascierto P, Larkin J, Dummer R, Garbe C, Testori A, Maio M, Hogg D, Lorigan P, Lebbe C, Jouary T, Schadendorf D, Ribas A, O’Day SJ, Sosman JA, Kirkwood JM, Eggermont AM, Dreno B, Nolop K, Li J, Nelson B, Hou J, Lee RJ, Flaherty KT, McArthur GA, BRIM-3 Study Group (2011) Improved survival with vemurafenib in melanoma with BRAF V600E mutation. N Engl J Med 364:2507–2516 CrossRefPubMedPubMedCentral

Diamond EL, Durham BH, Haroche J, Yao Z, Ma J, Parikh SA, Wang Z, Choi J, Kim E, Cohen-Aubart F, Lee SC, Gao Y, Micol JB, Campbell P, Walsh MP, Sylvester B, Dolgalev I, Aminova O, Heguy A, Zappile P, Nakitandwe J, Ganzel C, Dalton JD, Ellison DW, Estrada-Veras J, Lacouture M, Gahl WA, Stephens PJ, Miller VA, Ross JS, Ali SM, Briggs SR, Fasan O, Block J, Héritier S, Donadieu J, Solit DB, Hyman DM, Baselga J, Janku F, Taylor BS, Park CY, Amoura Z, Dogan A, Emile JF, Rosen N, Gruber TA, Abdel-Wahab O (2016) Diverse and targetable kinase alterations drive histiocytic neoplasms. Cancer Discov 6:154–165 CrossRefPubMed

Dietrich S, Glimm H, Andrulis M, von Kalle C, Ho AD, Zenz T (2012) BRAF inhibition in refractory hairy-cell leukemia. N Engl J Med 366:2038–2040 CrossRefPubMed

Dietrich S, Pircher A, Endris V, Peyrade F, Wendtner CM, Follows GA, Hüllein J, Jethwa A, Ellert E, Walther T, Liu X, Dyer MJ, Elter T, Brummer T, Zeiser R, Hermann M, Herold M, Weichert W, Dearden C, Haferlach T, Seiffert M, Hallek M, von Kalle C, Ho AD, Gaehler A, Andrulis M, Steurer M, Zenz T (2016) BRAF inhibition in hairy cell leukemia with low-dose vemurafenib. Blood 127:2847–2855 CrossRefPubMed

Ferreri AJ, Illerhaus G, Zucca E, Cavalli F, International Extranodal Lymphoma Study Group (2010) Flows and flaws in primary central nervous system lymphoma. Nat Rev Clin Oncol 7. doi: 10.​1038/​nrclinonc.​2010.​9-c1 PubMed

Long GV, Flaherty KT, Stroyakovskiy D, Gogas H, Levchenko E, de Braud F, Larkin J, Garbe C, Jouary T, Hauschild A, Chiarion-Sileni V, Lebbe C, Mandalà M, Millward M, Arance A, Bondarenko I, Haanen JBAG, Hansson J, Utikal J, Ferraresi V, Mohr P, Probachai V, Schadendorf D, Nathan P, Robert C, Ribas A, Davies MA, Lane SR, Legos JJ, Mookerjee B, Grob JJ (2015) Dabrafenib plus trametinib versus dabrafenib monotherapy in patients with metastatic BRAF V600E/K–mutant melanoma: long-term survival and safety analysis of a phase 3 study. Lancet. 386(9992):444–451. doi: 10.​1016/​S0140-6736(15)60898-4

Follows GA, Sims H, Bloxham DM, Zenz T, Hopper MA, Liu H, Bench A, Wright P, Van’t Veer MB, Scott MA (2013) Rapid response of biallelic BRAF V600E mutated hairy cell leukaemia to low dose vemurafenib. Br J Haematol 161:150–153 CrossRefPubMed

Haroche J, Charlotte F, Arnaud L, von Deimling A, Hélias-Rodzewicz Z, Hervier B, Cohen-Aubart F, Launay D, Lesot A, Mokhtari K, Canioni D, Galmiche L, Rose C, Schmalzing M, Croockewit S, Kambouchner M, Copin MC, Fraitag S, Sahm F, Brousse N, Amoura Z, Donadieu J, Emile JF (2012) High prevalence of BRAF V600E mutations in Erdheim-Chester disease but not in other non-Langerhans cell histiocytoses. Blood 120:2700–2703 CrossRefPubMed

Hecht M, Zimmer L, Loquai C, Weishaupt C, Gutzmer R, Schuster B, Gleisner S, Schulze B, Goldinger SM, Berking C, Forschner A, Clemens P, Grabenbauer G, Müller-Brenne T, Bauch J, Eich HT, Grabbe S, Schadendorf D, Schuler G, Keikavoussi P, Semrau S, Fietkau R, Distel LV, Heinzerling L (2015) Radiosensitization by BRAF inhibitor therapy-mechanism and frequency of toxicity in melanoma patients. Ann Oncol 26:1238–1244 CrossRefPubMed

Köhler M, Röring M, Schorch B, Heilmann K, Stickel N, Fiala GJ, Schmitt LC, Braun S, Ehrenfeld S, Uhl FM, Kaltenbacher T, Weinberg F, Herzog S, Zeiser R, Schamel WW, Jumaa H, Brummer T (2016) Activation loop phosphorylation regulates B‑Raf in vivo and transformation by B‑Raf mutants. EMBO J 35:143–161 CrossRefPubMed

Kordes M, Röring M, Heining C, Braun S, Hutter B, Richter D, Geörg C, Scholl C, Gröschel S, Roth W, Rosenwald A, Geissinger E, von Kalle C, Jäger D, Brors B, Weichert W, Grüllich C, Glimm H, Brummer T, Fröhling S (2016) Cooperation of BRAF(F595L) and mutant HRAS in histiocytic sarcoma provides new insights into oncogenic BRAF signaling. Leukemia 30:937–946 CrossRefPubMed

Larkin J, Ascierto PA, Dréno B, Atkinson V, Liszkay G, Maio M, Mandalà M, Demidov L, Stroyakovskiy D, Thomas L, de la Cruz-Merino L, Dutriaux C, Garbe C, Sovak MA, Chang I, Choong N, Hack SP, McArthur GA, Ribas A (2014) Combined vemurafenib and cobimetinib in BRAF-mutated melanoma. N Engl J Med 371:1867–1876 CrossRefPubMed

Lavoie H, Therrien M (2015) Regulation of RAF protein kinases in ERK signalling. Nat Rev Mol Cell Biol 16:281–298 CrossRefPubMed

Long GV, Stroyakovskiy D, Gogas H, Levchenko E, de Braud F, Larkin J, Garbe C, Jouary T, Hauschild A, Grob JJ, Chiarion Sileni V, Lebbe C, Mandalà M, Millward M, Arance A, Bondarenko I, Haanen JB, Hansson J, Utikal J, Ferraresi V, Kovalenko N, Mohr P, Probachai V, Schadendorf D, Nathan P, Robert C, Ribas A, DeMarini DJ, Irani JG, Casey M, Ouellet D, Martin AM, Le N, Patel K, Flaherty K (2014) Combined BRAF and MEK inhibition versus BRAF inhibition alone in melanoma. N Engl J Med 371:1877–1888 CrossRefPubMed

Long GV, Stroyakovskiy D, Gogas H, Levchenko E, de Braud F, Larkin J, Garbe CJouary T, Hauschild A, Grob JJ, Chiarion-Sileni V, Lebbe C, Mandalà M, Millward M, Arance A, Bondarenko I, Haanen JB, Hansson J, Utikal J, Ferraresi V, Kovalenko N, Mohr P, Probachai V, Schadendorf D, Nathan P, Robert C, Ribas A, DeMarini DJ, Irani JG, Swann S, Legos JJ, Jin F, Mookerjee B, Flaherty K (2015) Dabrafenib and trametinib versus dabrafenib and placebo for Val600 BRAF-mutant melanoma: a multicentre, double-blind, phase 3 randomised controlled trial. Lancet 386:444–451 CrossRefPubMed

Manousaridis I, Mavridou S, Goerdt S, Leverkus M, Utikal J (2013) Cutaneous side effects of inhibitors of the RAS/RAF/MEK/ERK signalling pathway and their management. J Eur Acad Dermatol Venereol 27:11–18 CrossRefPubMed

McArthur GA, Chapman PB, Robert C, Larkin J, Haanen JB, Dummer R, Ribas A, Hogg D, Hamid O, Ascierto PA, Garbe C, Testori A, Maio M, Lorigan P, Lebbé C, Jouary T, Schadendorf D, O’Day SJ, Kirkwood JM, Eggermont AM, Dréno B, Sosman JA, Flaherty KT, Yin M, Caro I, Cheng S, Trunzer K, Hauschild A (2014) Safety and efficacy of vemurafenib in BRAF(V600E) and BRAF(V600K) mutation-positive melanoma (BRIM-3): extended follow-up of a phase 3, randomised, open-label study. Lancet Oncol 15:323–332 CrossRefPubMedPubMedCentral

Orouji E, Ziegler B, Umansky V, Gebhardt C, Utikal J (2014) Leukocyte count restoration under dabrafenib treatment in a melanoma patient with vemurafenib-induced leukopenia: case report. Medicine (Baltimore) 93:e161 CrossRef

Röring M, Herr R, Fiala GJ, Heilmann K, Braun S, Eisenhardt AE, Halbach S, Capper D, von Deimling A, Schamel WW, Saunders DN, Brummer T (2012) Distinct requirement for an intact dimer interface in wild-type, V600E and kinase-dead B‑Raf signalling. EMBO J 31:2629–2647 CrossRefPubMedPubMedCentral

Roesch A, Paschen A, Landsberg J, Helfrich I, Becker JC, Schadendorf D (2016) Phenotypic tumour cell plasticity as a resistance mechanism and therapeutic target in melanoma. Eur J Cancer 59:109–112 CrossRefPubMed

Rosove MH, Peddi PF, Glaspy JA (2013) BRAF V600E inhibition in anaplastic thyroid cancer. N Engl J Med 368:684–685 CrossRefPubMed

Ross JS, Wang K, Chmielecki J, Gay L, Johnson A, Chudnovsky J, Yelensky R, Lipson D, Ali SM, Elvin JA, Vergilio JA, Roels S, Miller VA, Nakamura BN, Gray A, Wong MK, Stephens PJ (2016) The distribution of BRAF gene fusions in solid tumors and response to targeted therapy. Int J Cancer 138:881–890 CrossRefPubMed

Samatar AA, Poulikakos PI (2014) Targeting RAS-ERK signalling in cancer: promises and challenges. Nat Rev Drug Discov 13:928–942 CrossRefPubMed

Schilling B, Sondermann W, Zhao F, Griewank KG, Livingstone E, Sucker A, Zelba H, Weide B, Trefzer U, Wilhelm T, Loquai C, Berking C, Hassel J, Kähler KC, Utikal J, Al Ghazal P, Gutzmer R, Goldinger SM, Zimmer L, Paschen A, Hillen U, Schadendorf D, De CO (2014) Differential influence of vemurafenib and dabrafenib on patients’ lymphocytes despite similar clinical efficacy in melanoma. Ann Oncol 25:747–753 CrossRefPubMedPubMedCentral

Stadler S, Weina K, Gebhardt C, Utikal J (2015) New therapeutic options for advanced non-resectable malignant melanoma. Adv Med Sci. 60(1):83–88

Sullivan RJ, Weber JS, Patel SP, Dummer R, Miller WH, Cosgrove D, Carlino MS, Tan DS, Lebbe C, Cipani T, Élez E, Maacke H, Nikolopoulos P, Aout M, De Parseval LA, Ascierto PA (2015) A phase Ib/II study of BRAF inhibitor (BRAFi) encorafenib (ENCO) plus MEK inhibitor (MEKi) binimetinib (BINI) in cutaneous melanoma patients naive to BRAFi treatment. J Clin Oncol 33:suppl; abstr 9007

Tiacci E, Trifonov V, Schiavoni G, Holmes A, Kern W, Martelli MP, Pucciarini A, Bigerna B, Pacini R, Wells VA, Sportoletti P, Pettirossi V, Mannucci R, Elliott O, Liso A, Ambrosetti A, Pulsoni A, Forconi F, Trentin L, Semenzato G, Inghirami G, Capponi M, Di Raimondo F, Patti C, Arcaini L, Musto P, Pileri S, Haferlach C, Schnittger S, Pizzolo G, Foà R, Farinelli L, Haferlach T, Pasqualucci L, Rabadan R, Falini B (2011) BRAF mutations in hairy-cell leukemia. N Engl J Med 364:2305–2315 CrossRefPubMedPubMedCentral

Tiacci E, Park JH, De Carolis L, Chung SS, Broccoli A, Scott S, Zaja F, Devlin S, Pulsoni A, Chung YR, Cimminiello M, Kim E, Rossi D, Stone RM, Motta G, Saven A, Varettoni M, Altman JK, Anastasia A, Grever MR, Ambrosetti A, Rai KR, Fraticelli V, Lacouture ME, Carella AM, Levine RL, Leoni P, Rambaldi A, Falzetti F, Ascani S, Capponi M, Martelli MP, Park CY, Pileri SA, Rosen N, Foà R, Berger MF, Zinzani PL, Abdel-Wahab O, Falini B, Tallman MS (2015) Targeting mutant BRAF in relapsed or refractory hairy-cell leukemia. N Engl J Med 373:1733–1747 CrossRefPubMedPubMedCentral

Yao Z, Torres NM, Tao A, Gao Y, Luo L, Li Q, de Stanchina E, Abdel-Wahab O, Solit DB, Poulikakos PI, Rosen N (2015) BRAF mutants evade ERK-dependent feedback by different mechanisms that determine their sensitivity to pharmacologic inhibition. Cancer Cell 28:370–383 CrossRefPubMedPubMedCentral

Yaktapour N, Meiss F, Mastroianni J, Zenz T, Andrlova H, Mathew NR, Claus R, Hutter B, Fröhling S, Brors B, Pfeifer D, Pantic M, Bartsch I, Spehl TS, Meyer PT, Duyster J, Zirlik K, Brummer T, Zeiser R (2014) BRAF inhibitor-associated ERK activation drives development of chronic lymphocytic leukemia. J Clin Invest 124:5074–5084 CrossRefPubMedPubMedCentral

Zhang C, Spevak W, Zhang Y, Burton EA, Ma Y, Habets G, Zhang J, Lin J, Ewing T, Matusow B, Tsang G, Marimuthu A, Cho H, Wu G, Wang W, Fong D, Nguyen H, Shi S, Womack P, Nespi M, Shellooe R, Carias H, Powell B, Light E, Sanftner L, Walters J, Tsai J, West BL, Visor G, Rezaei H, Lin PS, Nolop K, Ibrahim PN, Hirth P, Bollag G (2015) RAF inhibitors that evade paradoxical MAPK pathway activation. Nature 526:583–586 CrossRefPubMed