WEMURAFENIB JAKO SELEKTYWNY INHIBITOR KINAZY SERONINOWO-TREONINOWEJ B-RAF STOSOWANY W LECZENIU CZERNIAKA

Krzysztof Kubica; Aleksander Mazurek

doi:10.56782/pps.117

Published : 2016-12-02

Vol. 14 No. 8 (2016)

VEMURAFENIB AS A SELECTIVE INHIBITOR OF THE SERINE/THREONINE-PROTEIN KINASE B-RAF, USED IN THE TREATMENT OF MELANOMA

Krzysztof Kubica

Aleksander Mazurek

DOI: https://doi.org/10.56782/pps.117

Abstract

Protein kinases are now the second most important group of proteins targeted in molecular-level anticancer therapies. Inhibiting the activity of protein kinases emerged as an important aspect of anticancer therapy. Vemurafenib is particularly effective in treating melanoma because its inhibitory activity is limited only to the B-RAF protein. It has relatively minor side effects. The biggest problem is an increasing resistance of tumor cells to this drug. The solution may involve combination therapies that will likely constitute the preferred future treatment of melanoma by inhibitors of protein kinases.

Keywords:

melanoma, protein kinases, protein kinase inhibitors, vemurafenib

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Kubica, K., & Mazurek, A. (2016). VEMURAFENIB AS A SELECTIVE INHIBITOR OF THE SERINE/THREONINE-PROTEIN KINASE B-RAF, USED IN THE TREATMENT OF MELANOMA. Prospects in Pharmaceutical Sciences, 14(8), 52–56. https://doi.org/10.56782/pps.117

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References

Linos E, Swetter SM, Cockburn MG, Colditz GA, Clarke CA. Increasing burden of melanoma in the United States. J Invest Dermatol 2009, 129(7), 1666–1674. DOI: https://doi.org/10.1038/jid.2008.423

Garbe C, Leiter U. Melanoma epidemiology and trends. Clin Dermatol 2009, 27(1), 3–9. DOI: https://doi.org/10.1016/j.clindermatol.2008.09.001

Erdmann F, Lortet-Tieulent J, Schüz J, Zeeb H, Greinert R, Breitbart EW, Bray F. International trends in the incidence of malignant melanoma 1953-2008--are recent generations at higher or lower risk? Int J Cancer 2013, 132(2), 385–400. DOI: https://doi.org/10.1002/ijc.27616

Bucheit AD, Davies MA. Emerging insights into resistance to BRAF inhibitors in melanoma. Biochem Pharmacol 2014, 87(3) ,381–389. DOI: https://doi.org/10.1016/j.bcp.2013.11.013

Cancer Facts and Figures 2016. American Cancer Society 2016.

Parkin DM, Bray F, Ferlay J, Pisani P. Estimating the world cancer burden: Globocan 2000. Int J Cancer 2001, 94(2), 153–156. DOI: https://doi.org/10.1002/ijc.1440

Friedman RJ, Rigel DS, Kopf AW. Early detection of malignant melanoma: The role of physician examination and self-examination of the skin. CA Cancer J Clin 1985, 35(3), 130–151. DOI: https://doi.org/10.3322/canjclin.35.3.130

Thompson JF, Scolyer RA, Kefford RF. Cutaneous melanoma. The Lancet 2005, 365(9460), 687–701. DOI: https://doi.org/10.1016/S0140-6736(05)17951-3

Ford D, Bliss JM, Swerdlow AJ, Armstrong BK, Franceschi S, Green A, Holly EA, Mack T, MacKie RM. Risk of cutaneous melanoma associated with a family history of the disease. The International Melanoma Analysis Group (IMAGE). Int J Cancer 1995, 62(4), 377–381. DOI: https://doi.org/10.1002/ijc.2910620403

Goldstein AM, Tucker MA. Genetic epidemiology of familial melanoma. Dermatol Clin 1995, 13(3), 605–612. DOI: https://doi.org/10.1016/S0733-8635(18)30066-4

Armstrong BK, Kricker A. The epidemiology of UV induced skin cancer. J Photochem Photobiol B 2001, 63(1–3), 8–18. DOI: https://doi.org/10.1016/S1011-1344(01)00198-1

Tucker MA, Goldstein AM. Melanoma etiology: where are we? Oncogene 2003, 22(20), 3042–3052. DOI: https://doi.org/10.1038/sj.onc.1206444

Viros A, Fridlyand J, Bauer J, Lasithiotakis K, Garbe C, Pinkel D, Bastin BC. Improving Melanoma Classification by Integrating Genetic and Morphologic Features. PLOS Med 2008, 5(6), e120. DOI: https://doi.org/10.1371/journal.pmed.0050120

Azoury SC, Lange JR. Epidemiology, risk factors, prevention, and early detection of melanoma. Surg Clin North Am 2014, 94(5), 945–962. DOI: https://doi.org/10.1016/j.suc.2014.07.013

Michael Binder, Scott Menzies. Computer aided instrumentation for the diagnosis of primary melanoma. CRC Press 2003, 234–240. DOI: https://doi.org/10.1201/b14732-20

Cook MG, Clarke TJ, Humphreys S, Fletcher A, McLaren KM, Smith NP, Stevens A, Theaker JM, Melia J. The evaluation of diagnostic and prognostic criteria and the terminology of thin cutaneous malignant melanoma by the CRC Melanoma Pathology Panel. Histopathology 1996, 28(6), 497–512. DOI: https://doi.org/10.1046/j.1365-2559.1996.d01-464.x

Krauss G. Biochemistry of Signal Transduction and Regulation. Wiley-VCH Verlag GmbH & Co. KGaA 2003. DOI: https://doi.org/10.1002/3527601864

Ubersax JA, Ferrell Jr JE. Mechanisms of specificity in protein phosphorylation. Nat Rev Mol Cell Biol 2007, 8(7), 530–541. DOI: https://doi.org/10.1038/nrm2203

Cohen P. Protein kinases--the major drug targets of the twenty-first century? Nat Rev Drug Discov 2002, 1(4), 309–315. DOI: https://doi.org/10.1038/nrd773

Zhang J, Yang PL, Gray NS. Targeting cancer with small molecule kinase inhibitors. Nat Rev Cancer 2009, 9(1), 28–39. DOI: https://doi.org/10.1038/nrc2559

Hidaka H, Kobayashi R. Pharmacology of Protein Kinase Inhibitors. Annu Rev Pharmacol Toxicol 1992, 32(1), 377–397. DOI: https://doi.org/10.1146/annurev.pa.32.040192.002113

Li R, Stafford JA, editors. Protein Inhibitor Drugs 2009. DOI: https://doi.org/10.1002/9780470524961

Bollag G, Tsai J, Zhang J, Zhang C, Ibrahim P, Nolop K, Hirth P. Vemurafenib: the first drug approved for BRAF-mutant cancer. Nat Rev Drug Discov 2012, 11(11), 873–886. DOI: https://doi.org/10.1038/nrd3847

Force T, Kuida K, Namchuk M, Parang K, Kyriakis JM. Inhibitors of Protein Kinase Signaling Pathways Emerging Therapies for Cardiovascular Disease. Circulation 2004, 109(10), 1196–1205. DOI: https://doi.org/10.1161/01.CIR.0000118538.21306.A9

Traxler P. Tyrosine kinases as targets in cancer therapy - successes and failures. Expert Opin Ther Targets 2003, 7(2), 215–234. DOI: https://doi.org/10.1517/14728222.7.2.215

Koseła H, Świtaj T, Rutkowski P. BRAF and MEK inhibitors in therapy of advanced melanoma. Oncol Clin Pract 2011, 7(5), 246–253.

Wan PTC, Garnett MJ, Roe SM, Lee S, Niculescu-Duvaz D, Good VM, Jones CM, Marshall C, Springer CJ, Barford D, Marais R. Mechanism of Activation of the RAF-ERK Signaling Pathway by Oncogenic Mutations of B-RAF. Cell 2004, 116(6), 855–867. DOI: https://doi.org/10.1016/S0092-8674(04)00215-6

Raman M, Chen W, Cobb MH. Differential regulation and properties of MAPKs. Oncogene 2007, 26(22), 3100–3112. DOI: https://doi.org/10.1038/sj.onc.1210392

Garnett MJ, Marais R. Guilty as charged: B-RAF is a human oncogene. Cancer Cell 2004, 6(4), 313–319. DOI: https://doi.org/10.1016/j.ccr.2004.09.022

Swaika A, Crozier JA, Joseph RW. Vemurafenib: an evidence-based review of its clinical utility in the treatment of metastatic melanoma. Drug Des Devel Ther 2014, 8, 775–787. DOI: https://doi.org/10.2147/DDDT.S31143

Wilhelm SM, Adnane L, Newell P, Villanueva A, Llovet JM, Lynch M. Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling. Mol Cancer Ther 2008, 7(10), 3129–3140. DOI: https://doi.org/10.1158/1535-7163.MCT-08-0013

Niezgoda A, Niezgoda P, Czajkowski R. Novel Approaches to Treatment of Advanced Melanoma: A Review on Targeted Therapy and Immunotherapy. BioMed Res Int BioMed Res Int 2015. DOI: https://doi.org/10.1155/2015/851387

Richman J, Martin-Liberal J, Diem S, Larkin J. BRAF and MEK inhibition for the treatment of advanced BRAF mutant melanoma. Expert Opin Pharmacother 2015, 16(9), 1285–1297. DOI: https://doi.org/10.1517/14656566.2015.1044971

da Rocha Dias S, Salmonson T, van Zwieten-Boot B, Jonsson B, Marchetti S, Schellens JHM, Giuliani R, Pignatti F. The European Medicines Agency review of vemurafenib (Zelboraf®) for the treatment of adult patients with BRAF V600 mutation-positive unresectable or metastatic melanoma: Summary of the scientific assessment of the Committee for Medicinal Products for Human Use. Eur J Cancer 2013, 49(7), 1654–1661. DOI: https://doi.org/10.1016/j.ejca.2013.01.015

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 A, Dreno B, Nolop K, Li J, Nelson B, Hou J, Lee RJ, Flaherty KT, McArthur GA. Improved Survival with Vemurafenib in Melanoma with BRAF V600E Mutation. N Engl J Med 2011, 364(26), 2507–2516. DOI: https://doi.org/10.1056/NEJMoa1103782

Sala E, Mologni L, Truffa S, Gaetano C, Bollag GE, Gambacorti-Passerini C. BRAF silencing by short hairpin RNA or chemical blockade by PLX4032 leads to different responses in melanoma and thyroid carcinoma cells. Mol Cancer Res MCR 2008, 6(5), 751–759. DOI: https://doi.org/10.1158/1541-7786.MCR-07-2001

Maverakis E, Cornelius LA, Bowen GM, Phan T, Patel FB, Fitzmaurice S, He Y, Burrall B, Duong C, Kloxin AM, Sultani H, Wilken R, Martinez SR, Patel F. Metastatic melanoma - a review of current and future treatment options. Acta Derm Venereol 2015, 95(5), 516–524. DOI: https://doi.org/10.2340/00015555-2035

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, Lebbe C, Jouary T, Schadendorf D, O`Day SJ, Kirkwood JM, Eggermont A, Dreno B, Sosman JA, Flaherty KT, Yin M, Caro I, Cheng S, Trunzer K, Hauschild A. Safety and efficacy of vemurafenib in BRAFV600E and BRAFV600K mutation-positive melanoma (BRIM-3): extended follow-up of a phase 3, randomised, open-label study. Lancet Oncol 2014, 15(3), 323–332. DOI: https://doi.org/10.1016/S1470-2045(14)70012-9

Ravnan MC, Matalka MS. Vemurafenib in Patients With BRAF V600E Mutation–Positive Advanced Melanoma. Clin Ther 2012, 34(7), 1474–1486. DOI: https://doi.org/10.1016/j.clinthera.2012.06.009

Hatzivassiliou G, Song K, Yen I, Brandhuber BJ, Anderson DJ, Alvarado R, Ludlam MJC, Stokoe D, Gloor SL, Vigers G, Morales T, Aliagas I, Liu B, Sideris S, Hoeflich KP, Jaiswal BS, Seshagiri S, Koeppen H, Belvin M, Friedman LS, Malek S. RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth. Nature 2010, 464(7287), 431–435. DOI: https://doi.org/10.1038/nature08833

Halaban R, Zhang W, Bacchiocchi A, Cheng E, Parisi F, Ariyan S, Krauthammer M, McCusker JP, Kluger Y, Sznol M. PLX4032, a selective BRAF(V600E) kinase inhibitor, activates the ERK pathway and enhances cell migration and proliferation of BRAF melanoma cells. Pigment Cell Melanoma Res 2010, 23(2), 190–200. DOI: https://doi.org/10.1111/j.1755-148X.2010.00685.x

Nazarian R, Shi H, Wang Q, Kong X, Koya RC, Lee H, Chen Z, Lee MK, Attar N, Sazegar H, Chodon T, Nelson SF, McArthur G, Sosman JA, Ribas A, Lo RS. Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation. Nature 2010, 468(7326), 973–977. DOI: https://doi.org/10.1038/nature09626

Straussman R, Morikawa T, Shee K, Barzily-Rokni M, Qian ZR, Du J, Davis A, Mongare MM, Gould J, Frederick DT, Cooper ZA, Chapman PB, Solit DB, Ribas A, Lo RS, Flaherty KT, Ogino S, Wargo JA, Golub TR. Tumour micro-environment elicits innate resistance to RAF inhibitors through HGF secretion. Nature 2012, 487(7408), 500–504. DOI: https://doi.org/10.1038/nature11183

Wilson TR, Fridlyand J, Yan Y, Penuel E, Burton L, Chan E, Peng J, Lin E, Wang Y, Sosman J, Ribas A, Li J, Moffatt J, Sutherin DP, Koeppen H, Merchant M, Neve R, Settleman J. Widespread potential for growth-factor-driven resistance to anticancer kinase inhibitors. Nature 2012, 487(7408), 505–509. DOI: https://doi.org/10.1038/nature11249

Hernandez-Davies JE, Tran TQ, Reid MA, Rosales KR, Lowman XH, Pan M, Moriceau G, Yang Y, Wu J, Lo RS, Kong M. Vemurafenib resistance reprograms melanoma cells towards glutamine dependence. J Transl Med 2015, 13:210. 1-11 DOI: https://doi.org/10.1186/s12967-015-0581-2

Garber K. Melanoma Drug Vindicates Targeted Approach. Science 2009, 326(5960), 1619–1619. DOI: https://doi.org/10.1126/science.326.5960.1619

Flaherty K, Puzanov I, Sosman J, Kim K, Ribas A, McArthur G, Lee RJ, Grippo JF, Nolop K, Chapman PB. Phase I study of PLX4032: Proof of concept for V600E BRAF mutation as a therapeutic target in human cancer. J Clin Oncol 2010, 28(1). suppl; abstr nr 9000. DOI: https://doi.org/10.1200/jco.2009.27.15_suppl.9000

Flaherty KT, Puzanov I, Kim KB, Ribas A, McArthur GA, Sosman JA, O`Dwyer PJ, Lee RJ, Grippo JF, Nolop K, Chapman PB. Inhibition of Mutated, Activated BRAF in Metastatic Melanoma. N Engl J Med 2010, 363(9), 809–819. DOI: https://doi.org/10.1056/NEJMoa1002011

Sosman JA, Kim KB, Schuchter L, Gonzalez R, Pavlick AC, Weber JS, McArthur GA, Hutson TE, Moschos S, Flaherty KT, Hersey P, Kefford R, Lawrence D, Puzanov I, Lewis KD, Amaravadi RK, Chmielowski B, Lawrence HJ, Shyr Y, Ye F, Li J, Nolop KB, Lee RJ, Joe AK, Ribas A. Survival in BRAF V600–Mutant Advanced Melanoma Treated with Vemurafenib. N Engl J Med 2012, 366(8), 707–714. DOI: https://doi.org/10.1056/NEJMoa1112302

Funck-Brentano E, Alvarez JC, Longvert C, Abe E, Beauchet A, Funck-Brentano C, Saiag P. Plasma vemurafenib concentrations in advanced BRAFV600mut melanoma patients: impact on tumour response and tolerance. Ann Oncol Off J Eur Soc Med Oncol ESMO 2015, 26(7), 1470–1475. DOI: https://doi.org/10.1093/annonc/mdv189

Kramkimel N, Sakji L, Schoemann A, Golmard J, Rosencher E, Theodore C, Goldwasser F. Severe skin rash during vemurafenib treatment: A predictive factor of early positive response in metastatic melanoma? J Clin Oncol 2014, 32(5). suppl; abstr nr 9092. DOI: https://doi.org/10.1200/jco.2014.32.15_suppl.9092

Ribas A, Zhang W, Chang I, Shirai K, Ernstoff MS, Daud A, Cowey CL, Daniels G, Seja E, O`Laco E, Glaspy JA, Chmielowski B, Hill T, Joe AK, Grippo JF The effects of a high-fat meal on single-dose vemurafenib pharmacokinetics. J Clin Pharmacol 2014, 54(4), 368–374. DOI: https://doi.org/10.1002/jcph.255

Boussemart L, Routier E, Mateus C, Opletalova K, Sebille G, Kamsu-Kom N, Thomas M, Vagner S, Favre M, Tomasic G, Wechsler J, Lacroix L, Robert C. Prospective study of cutaneous side-effects associated with the BRAF inhibitor vemurafenib: a study of 42 patients. Ann Oncol 2013, 24(6), 1691–1697. DOI: https://doi.org/10.1093/annonc/mdt015

Boyd KP, Vincent B, Andea A, Conry RM, Hughey LC. Nonmalignant cutaneous findings associated with vemurafenib use in patients with metastatic melanoma. J Am Acad Dermatol 2012, 67(6), 1375–1379. DOI: https://doi.org/10.1016/j.jaad.2012.06.045

Lacouture ME, Duvic M, Hauschild A, Prieto VG, Robert C, Schadendorf D, Kim CC, McCormack C, Myskowski PL, Spleiss O, Trunzer K, Su F, Nelson B, Nolop KB, Grippo JF, Lee RJ, Klimek MJ, Troy JL, Joe AK. Analysis of Dermatologic Events in Vemurafenib-Treated Patients With Melanoma. The Oncologist 2013, 18(3), 314–322. DOI: https://doi.org/10.1634/theoncologist.2012-0333

Jhaveri KD, Sakhiya V, Fishbane S. Nephrotoxicity of the braf inhibitors vemurafenib and dabrafenib. JAMA Oncol 2015, 1(8), 1133–1134. DOI: https://doi.org/10.1001/jamaoncol.2015.1713

Larkin J, Ascierto PA, Dréno B, Atkinson V, Liszkay G, Maio M, Mandala M, Demidov L, Stroyakovskiy D, Thomas L, de la Cruz L, Dutriaux C, Garbe C, Sovak MA, Chang I, Choong N, Hack SP, McArthur GA, Ribas A. Combined Vemurafenib and Cobimetinib in BRAF-Mutated Melanoma. N Engl J Med 2014, 371(20), 1867–1876. DOI: https://doi.org/10.1056/NEJMoa1408868

Krzysztof Kubica

krzysztof.pawel.kubica@gmail.com

Affiliation:

Zakład Chemii Leków, Wydział Farmaceutyczny z Oddziałem Medycyny Laboratoryjnej, Warszawski Uniwersytet Medyczny, Banacha 1, 02-097 Warszawa Poland

Bio Statement (e.g., department and rank)

autor korespondujący, tel: +48 505 430 166

Aleksander Mazurek

Affiliation:

Zakład Chemii Leków, Wydział Farmaceutyczny z Oddziałem Medycyny Laboratoryjnej, Warszawski Uniwersytet Medyczny, Banacha 1, 02-097 Warszawa Poland