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 Nilotinib

Nilotinib is an orally bioavailable aminopyrimidine-derivative Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity. Designed to overcome imatinib resistance, nilotinib binds to and stabilizes the inactive conformation of the kinase domain of the Abl protein of the Bcr-Abl fusion protein, resulting in the inhibition of the Bcr-Abl-mediated proliferation of Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) cells. This agent also inhibits the receptor tyrosine kinases platelet-derived growth factor receptor (PDGF-R) and c-kit, a receptor tyrosine kinase mutated and constitutively activated in most gastrointestinal stromal tumors (GISTs). With a binding mode that is energetically more favorable than that of imatinib, nilotinib has been shown to have an approximately 20-fold increased potency in kinase and proliferation assays compared to imatinib. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Nilotinib was approved as Tasigna in the USA and the EU for drug-resistant chronic myelogenous leukemia (CML). In June 2006, a Phase I clinical trial found nilotinib, also known by its clinical code AMN107, has a relatively favorable safety profile and shows activity in cases of CML resistant to treatment with imatinib (Gleevec), another tyrosine kinase inhibitor currently used as a first-line treatment. In that study 92% of patients (already resistant or unresponsive to Gleevec) achieved a normal white blood cell counts after five months of treatment. The drug carries a black box warning for possible heart complications.

Tasigna (nilotinib) belongs to a pharmacologic class of drugs known as kinase inhibitors.
Nilotinib drug substance, a monohydrate mono-hydrochloride, is a white to slightly yellowish to slightly greenish yellow powder with the anhydrous molecular formula and weight, respectively, of C28H22F3N7O•HCl • H2O and 565.98. The solubility of nilotinib in aqueous solutions decreases with increasing pH. Nilotinib is not optically active. The pKa1 was determined to be 2.1; pKa2 was estimated to be 5.4. The chemical name of nilotinib is 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5(trifluoromethyl)phenyl]-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-benzamide, monohydrochloride, monohydrate.  Tasigna (nilotinib) capsules, for oral use, contain 200 mg nilotinib base, anhydrous (as hydrochloride, monohydrate) with the following inactive ingredients: colloidal silicon dioxide, crospovidone, lactose monohydrate, magnesium stearate and polyoxamer 188. The capsules contain gelatin, iron oxide (red), iron oxide (yellow), and titanium dioxide.

Nilotinib is an inhibitor of the Bcr-Abl kinase. Nilotinib binds to and stabilizes the inactive conformation of the kinase domain of Abl protein. In vitro, nilotinib inhibited Bcr-Abl mediated proliferation of murine leukemic cell lines and human cell lines derived from Ph+ CML patients. Under the conditions of the assays, nilotinib was able to overcome imatinib resistance resulting from Bcr-Abl kinase mutations, in 32 out of 33 mutations tested. In vivo, nilotinib reduced the tumor size in a murine Bcr-Abl xenograft model. Nilotinib inhibited the autophosphorylation of the following kinases at IC50 values as indicated: Bcr-Abl (20-60 nM), PDGFR (69 nM), c-Kit (210 nM), CSR-1R (125-250 nM) and DDR (3.7 nM).

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145: Perini GF, Santos FP, Funke V, Ruiz J, Neto BH, Hamerschlak N. Nilotinib post-liver transplantation for acute hepatic failure related to imatinib. Leuk Res. 2009 Dec;33(12):e234-5. Epub 2009 Jul 25. PubMed PMID: 19632720.

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153: Ottmann OG, Pfeifer H. First-line treatment of Philadelphia chromosome-positive acute lymphoblastic leukaemia in adults. Curr Opin Oncol. 2009 Jun;21 Suppl 1:S43-6. Review. PubMed PMID: 19561414.

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156: Eccersley LR, Hoffbrand AV, Rustin MH, McNamara CJ. Paraneoplastic pemphigus associated with systemic mastocytosis. Am J Hematol. 2009 Dec;84(12):847-8. PubMed PMID: 19544477.

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171: Schmid-Wendtner MH, Wendtner CM. Intensified inflammatory reaction of actinic keratoses after single application of topical 5-fluorouracil in a patient treated with nilotinib for chronic myeloid leukemia. Dermatology. 2009;219(4):341-3. Epub 2009 May 22. PubMed PMID: 19468201.

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186: Ocheni S, Iwanski GB, Schafhausen P, Zander AR, Ayuk F, Klyuchnikov E, Zabelina T, Fiedler W, Schnittger S, Hochhaus A, Brümmendorf TH, Kröger N, Bacher U. Characterisation of extramedullary relapse in patients with chronic myeloid leukemia in advanced disease after allogeneic stem cell transplantation. Leuk Lymphoma. 2009 Apr;50(4):551-8. PubMed PMID: 19373652.

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192: Gamas P, Marchetti S, Puissant A, Grosso S, Jacquel A, Colosetti P, Pasquet JM, Mahon FX, Cassuto JP, Auberger P. Inhibition of imatinib-mediated apoptosis by the caspase-cleaved form of the tyrosine kinase Lyn in chronic myelogenous leukemia cells. Leukemia. 2009 Aug;23(8):1500-6. Epub 2009 Apr 2. PubMed PMID: 19340007.

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195: Mauro MJ. Tailoring tyrosine kinase inhibitor therapy in chronic myeloid leukemia. Cancer Control. 2009 Apr;16(2):108-21. Review. PubMed PMID: 19337197.

196: Tyler T. Once-daily dasatinib for treatment of patients with chronic myeloid leukemia. Ann Pharmacother. 2009 May;43(5):920-7. Epub 2009 Mar 31. Review. PubMed PMID: 19336654.

197: von Bubnoff N, Engh RA, Aberg E, Sänger J, Peschel C, Duyster J. FMS-like tyrosine kinase 3-internal tandem duplication tyrosine kinase inhibitors display a nonoverlapping profile of resistance mutations in vitro. Cancer Res. 2009 Apr 1;69(7):3032-41. Epub 2009 Mar 24. PubMed PMID: 19318574.

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199: Fava C, Kantarjian HM, Jabbour E, O'Brien S, Jain N, Rios MB, Garcia-Manero G, Ravandi F, Verstovsek S, Borthakur G, Shan J, Cortes J. Failure to achieve a complete hematologic response at the time of a major cytogenetic response with second-generation tyrosine kinase inhibitors is associated with a poor prognosis among patients with chronic myeloid leukemia in accelerated or blast phase. Blood. 2009 May 21;113(21):5058-63. Epub 2009 Mar 12. PubMed PMID: 19282457.

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202: Bixby DL, Talpaz M. Efficacy of various doses and schedules of second-generation tyrosine kinase inhibitors. Clin Lymphoma Myeloma. 2008 Mar;8 Suppl 3:S95-S106. Review. PubMed PMID: 19254887.

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217: Müller BA. Imatinib and its successors--how modern chemistry has changed drug development. Curr Pharm Des. 2009;15(2):120-33. Review. PubMed PMID: 19149608.

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221: Au WY, Caguioa PB, Chuah C, Hsu SC, Jootar S, Kim DW, Kweon IY, O'Neil WM, Saikia TK, Wang J. Chronic myeloid leukemia in Asia. Int J Hematol. 2009 Jan;89(1):14-23. Epub 2008 Dec 20. Review. PubMed PMID: 19101781.

222: Yanada M, Ohno R, Naoe T. Recent advances in the treatment of Philadelphia chromosome-positive acute lymphoblastic leukemia. Int J Hematol. 2009 Jan;89(1):3-13. Epub 2008 Dec 18. Review. PubMed PMID: 19093166.

223: Martinelli G, Soverini S, Iacobucci I, Baccarani M. Intermittent targeting as a tool to minimize toxicity of tyrosine kinase inhibitor therapy. Nat Clin Pract Oncol. 2009 Feb;6(2):68-9. Epub 2008 Dec 17. PubMed PMID: 19092801.

224: Cervantes F. [Chronic myeloid leukemia 2008]. Med Clin (Barc). 2008 Nov 15;131(17):658-9. Review. Spanish. PubMed PMID: 19087793.

225: Gora-Tybor J, Robak T. Targeted drugs in chronic myeloid leukemia. Curr Med Chem. 2008;15(29):3036-51. Review. PubMed PMID: 19075651.

226: Redaelli S, Piazza R, Rostagno R, Magistroni V, Perini P, Marega M, Gambacorti-Passerini C, Boschelli F. Activity of bosutinib, dasatinib, and nilotinib against 18 imatinib-resistant BCR/ABL mutants. J Clin Oncol. 2009 Jan 20;27(3):469-71. Epub 2008 Dec 15. PubMed PMID: 19075254.

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228: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2008 Sep;30(7):543-88. PubMed PMID: 18985183.

229: Jarkowski A, Sweeney RP. Nilotinib: a new tyrosine kinase inhibitor for the treatment of chronic myelogenous leukemia. Pharmacotherapy. 2008 Nov;28(11):1374-82. Review. PubMed PMID: 18956997.

230: Day E, Waters B, Spiegel K, Alnadaf T, Manley PW, Buchdunger E, Walker C, Jarai G. Inhibition of collagen-induced discoidin domain receptor 1 and 2 activation by imatinib, nilotinib and dasatinib. Eur J Pharmacol. 2008 Dec 3;599(1-3):44-53. Epub 2008 Oct 11. PubMed PMID: 18938156.

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232: Bewry NN, Nair RR, Emmons MF, Boulware D, Pinilla-Ibarz J, Hazlehurst LA. Stat3 contributes to resistance toward BCR-ABL inhibitors in a bone marrow microenvironment model of drug resistance. Mol Cancer Ther. 2008 Oct;7(10):3169-75. PubMed PMID: 18852120; PubMed Central PMCID: PMC2676735.

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234: Kubuki Y. [Management of chronic myeloid leukemia]. Rinsho Ketsueki. 2008 Oct;49(10):1401-10. Review. Japanese. PubMed PMID: 18833925.

235: Cang S, Liu D. P-loop mutations and novel therapeutic approaches for imatinib failures in chronic myeloid leukemia. J Hematol Oncol. 2008 Oct 1;1:15. Review. PubMed PMID: 18828913; PubMed Central PMCID: PMC2567340.

236: Zeidan A, Wang ES, Wetzler M. What is imatinib-resistant chronic myeloid leukemia? Identifying and managing loss of response. Clin Adv Hematol Oncol. 2008 Sep;6(9):673-83. PubMed PMID: 18827790.

237: Jabbour E, Kantarjian HM, Jones D, Reddy N, O'Brien S, Garcia-Manero G, Burger J, Cortes J. Characteristics and outcome of chronic myeloid leukemia patients with F317L BCR-ABL kinase domain mutation after therapy with tyrosine kinase inhibitors. Blood. 2008 Dec 15;112(13):4839-42. Epub 2008 Sep 25. PubMed PMID: 18818391.

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239: Dewaele B, Wasag B, Cools J, Sciot R, Prenen H, Vandenberghe P, Wozniak A, Schöffski P, Marynen P, Debiec-Rychter M. Activity of dasatinib, a dual SRC/ABL kinase inhibitor, and IPI-504, a heat shock protein 90 inhibitor, against gastrointestinal stromal tumor-associated PDGFRAD842V mutation. Clin Cancer Res. 2008 Sep 15;14(18):5749-58. PubMed PMID: 18794084.

240: Distler JH, Distler O. Intracellular tyrosine kinases as novel targets for anti-fibrotic therapy in systemic sclerosis. Rheumatology (Oxford). 2008 Oct;47 Suppl 5:v10-1. Review. PubMed PMID: 18784126.

241: Reichardt P. Novel approaches to imatinib- and sunitinib-resistant GIST. Curr Oncol Rep. 2008 Jul;10(4):344-9. Review. PubMed PMID: 18778561.

242: Dierks C, Beigi R, Guo GR, Zirlik K, Stegert MR, Manley P, Trussell C, Schmitt-Graeff A, Landwerlin K, Veelken H, Warmuth M. Expansion of Bcr-Abl-positive leukemic stem cells is dependent on Hedgehog pathway activation. Cancer Cell. 2008 Sep 9;14(3):238-49. PubMed PMID: 18772113.

243: Hazarika M, Jiang X, Liu Q, Lee SL, Ramchandani R, Garnett C, Orr MS, Sridhara R, Booth B, Leighton JK, Timmer W, Harapanhalli R, Dagher R, Justice R, Pazdur R. Tasigna for chronic and accelerated phase Philadelphia chromosome--positive chronic myelogenous leukemia resistant to or intolerant of imatinib. Clin Cancer Res. 2008 Sep 1;14(17):5325-31. PubMed PMID: 18765523.

244: Tanaka R, Kimura S. Abl tyrosine kinase inhibitors for overriding Bcr-Abl/T315I: from the second to third generation. Expert Rev Anticancer Ther. 2008 Sep;8(9):1387-98. Review. PubMed PMID: 18759691.

245: O'Connor LM, Langabeer S, McCann SR, Conneally E. Restoration of donor chimerism by nilotinib in a chronic myeloid leukaemia patient post mutation-associated imatinib mesylate resistance and allogeneic stem cell transplant failure. Bone Marrow Transplant. 2008 Dec;42(12):833-5. Epub 2008 Aug 18. PubMed PMID: 18711344.

246: Braconi C, Bracci R, Cellerino R. Molecular targets in Gastrointestinal Stromal Tumors (GIST) therapy. Curr Cancer Drug Targets. 2008 Aug;8(5):359-66. Review. PubMed PMID: 18690842.

247: Kantarjian H, Cortes J. BCR-ABL tyrosine kinase inhibitors in chronic myeloid leukemia: using guidelines to make rational treatment choices. J Natl Compr Canc Netw. 2008 Mar;6 Suppl 2:S37-42; quiz S43-S44. Review. PubMed PMID: 18397680.

248: Shah NP. Advanced CML: therapeutic options for patients in accelerated and blast phases. J Natl Compr Canc Netw. 2008 Mar;6 Suppl 2:S31-S36. Review. PubMed PMID: 18397679.

249: Cortes J, Kantarjian H. Beyond dose escalation: clinical options for relapse or resistance in chronic myelogenous leukemia. J Natl Compr Canc Netw. 2008 Mar;6 Suppl 2:S22-S30. Review. PubMed PMID: 18397678.

250: Noronha G, Cao J, Chow CP, Dneprovskaia E, Fine RM, Hood J, Kang X, Klebansky B, Lohse D, Mak CC, McPherson A, Palanki MS, Pathak VP, Renick J, Soll R, Zeng B. Inhibitors of ABL and the ABL-T315I mutation. Curr Top Med Chem. 2008;8(10):905-21. PubMed PMID: 18673174.

251: Ganapathipillai SS, Medová M, Aebersold DM, Manley PW, Berthou S, Streit B, Blank-Liss W, Greiner RH, Rothen-Rutishauser B, Zimmer Y. Coupling of mutated Met variants to DNA repair via Abl and Rad51. Cancer Res. 2008 Jul 15;68(14):5769-77. PubMed PMID: 18632630.

252: Quintás-Cardama A, Cortes J. Therapeutic options against BCR-ABL1 T315I-positive chronic myelogenous leukemia. Clin Cancer Res. 2008 Jul 15;14(14):4392-9. Review. PubMed PMID: 18628453.

253: Shimoni A, Leiba M, Schleuning M, Martineau G, Renaud M, Koren-Michowitz M, Ribakovski E, le Coutre P, Arnold R, Guilhot F, Nagler A. Prior treatment with the tyrosine kinase inhibitors dasatinib and nilotinib allows stem cell transplantation (SCT) in a less advanced disease phase and does not increase SCT Toxicity in patients with chronic myelogenous leukemia and philadelphia positive acute lymphoblastic leukemia. Leukemia. 2009 Jan;23(1):190-4. Epub 2008 Jul 3. PubMed PMID: 18596746.

254: Deininger MW. Nilotinib. Clin Cancer Res. 2008 Jul 1;14(13):4027-31. Review. PubMed PMID: 18593977.

255: Hussar DA. New drugs08, part 2. Nursing. 2008 Jul;38(7):41-8; quiz 49. PubMed PMID: 18580663.

256: Hasselbalch HC, Birgens H, Dufva IH, Dalseg AM, Brown Pde N, Jensen MK, Vangsted A. [Novel medical treatment modalities in hematology]. Ugeskr Laeger. 2008 Jun 9;170(24):2115-9. Review. Danish. PubMed PMID: 18565291.

257: Moral MA, Tomillero A. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2008 Mar;30(2):149-71. PubMed PMID: 18560631.

258: Jabbour E, El Ahdab S, Cortes J, Kantarjian H. Nilotinib: a novel Bcr-Abl tyrosine kinase inhibitor for the treatment of leukemias. Expert Opin Investig Drugs. 2008 Jul;17(7):1127-36. PubMed PMID: 18549348.

259: Walz C, Cross NC, Van Etten RA, Reiter A. Comparison of mutated ABL1 and JAK2 as oncogenes and drug targets in myeloproliferative disorders. Leukemia. 2008 Jul;22(7):1320-34. Epub 2008 Jun 5. PubMed PMID: 18528425.

260: Fabarius A, Giehl M, Rebacz B, Krämer A, Frank O, Haferlach C, Duesberg P, Hehlmann R, Seifarth W, Hochhaus A. Centrosome aberrations and G1 phase arrest after in vitro and in vivo treatment with the SRC/ABL inhibitor dasatinib. Haematologica. 2008 Aug;93(8):1145-54. Epub 2008 Jun 2. PubMed PMID: 18519516.

261: Padmanabhan S, Ravella S, Curiel T, Giles F. Current status of therapy for chronic myeloid leukemia: a review of drug development. Future Oncol. 2008 Jun;4(3):359-77. Review. PubMed PMID: 18518762.

262: Tam CS, Kantarjian H, Garcia-Manero G, Borthakur G, O'Brien S, Ravandi F, Shan J, Cortes J. Failure to achieve a major cytogenetic response by 12 months defines inadequate response in patients receiving nilotinib or dasatinib as second or subsequent line therapy for chronic myeloid leukemia. Blood. 2008 Aug 1;112(3):516-8. Epub 2008 May 20. PubMed PMID: 18492956.

263: O'Hare T, Eide CA, Deininger MW. New Bcr-Abl inhibitors in chronic myeloid leukemia: keeping resistance in check. Expert Opin Investig Drugs. 2008 Jun;17(6):865-78. Review. PubMed PMID: 18491988.

264: Agaram NP, Laquaglia MP, Ustun B, Guo T, Wong GC, Socci ND, Maki RG, DeMatteo RP, Besmer P, Antonescu CR. Molecular characterization of pediatric gastrointestinal stromal tumors. Clin Cancer Res. 2008 May 15;14(10):3204-15. PubMed PMID: 18483389.

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266: Tiribelli M, Sperotto A, Candoni A, Simeone E, Buttignol S, Fanin R. Nilotinib and donor lymphocyte infusion in the treatment of Philadelphia-positive acute lymphoblastic leukemia (Ph+ ALL) relapsing after allogeneic stem cell transplantation and resistant to imatinib. Leuk Res. 2009 Jan;33(1):174-7. Epub 2008 May 8. PubMed PMID: 18471874.

267: Quintás-Cardama A, Cortes J. Omacetaxine mepesuccinate--a semisynthetic formulation of the natural antitumoral alkaloid homoharringtonine, for chronic myelocytic leukemia and other myeloid malignancies. IDrugs. 2008 May;11(5):356-72. PubMed PMID: 18465678.

268: Giles FJ, DeAngelo DJ, Baccarani M, Deininger M, Guilhot F, Hughes T, Mauro M, Radich J, Ottmann O, Cortes J. Optimizing outcomes for patients with advanced disease in chronic myelogenous leukemia. Semin Oncol. 2008 Feb;35(1 Suppl 1):S1-17; quiz S18-20. Review. PubMed PMID: 18346528.

269: Neumann F, Markett J, Fenk R, Pooten M, Koch A, Bruennert D, Schimkus N, Wulfert M, Royer-Pokora B, Kronenwett R, Haas R, Gattermann N. Therapy adapted to molecular response in patients with chronic myelogenous leukaemia in first chronic phase: results of the Duesseldorf study. Hematol Oncol. 2008 Dec;26(4):213-8. PubMed PMID: 18449950.

270: Ramirez P, DiPersio JF. Therapy options in imatinib failures. Oncologist. 2008 Apr;13(4):424-34. Review. PubMed PMID: 18448557.

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338: Goldman JM. How I treat chronic myeloid leukemia in the imatinib era. Blood. 2007 Oct 15;110(8):2828-37. Epub 2007 Jul 12. Review. PubMed PMID: 17626839.

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354: von Mehren M. Beyond imatinib: second generation c-KIT inhibitors for the management of gastrointestinal stromal tumors. Clin Colorectal Cancer. 2006 Nov;6 Suppl 1:S30-4. Review. PubMed PMID: 17419150.

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361: Mughal TI, Goldman JM. Emerging strategies for the treatment of mutant Bcr-Abl T315I myeloid leukemia. Clin Lymphoma Myeloma. 2007 Mar;7 Suppl 2:S81-4. Review. PubMed PMID: 17382017.

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