메뉴 건너뛰기




Volumn 68, Issue 4, 2008, Pages 449-459

Nilotinib

Author keywords

Adis Drug Profiles; Chronic myeloid leukaemia; Nilotinib, general; Research and development

Indexed keywords

BCR ABL PROTEIN; DASATINIB; IMATINIB; KETOCONAZOLE; MIDAZOLAM; NILOTINIB; PROTEIN TYROSINE KINASE;

EID: 40349091842     PISSN: 00126667     EISSN: 00126667     Source Type: Journal    
DOI: 10.2165/00003495-200868040-00005     Document Type: Review
Times cited : (29)

References (36)
  • 3
    • 0033614446 scopus 로고    scopus 로고
    • Chronic myeloid leukemia
    • Apr 29;
    • Sawyers CL. Chronic myeloid leukemia. N Engl J Med 1999 Apr 29; 340 (17): 1330-40
    • (1999) N Engl J Med , vol.340 , Issue.17 , pp. 1330-1340
    • Sawyers, C.L.1
  • 4
    • 33745114173 scopus 로고    scopus 로고
    • AMN107 (nilotinib): A novel and selective inhibitor of BCR-ABL
    • Jun 19;
    • Weisberg E, Manley P, Mestan J, et al. AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL. Br J Cancer 2006 Jun 19; 94 (12): 1765-9
    • (2006) Br J Cancer , vol.94 , Issue.12 , pp. 1765-1769
    • Weisberg, E.1    Manley, P.2    Mestan, J.3
  • 5
    • 13844251975 scopus 로고    scopus 로고
    • Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl
    • Feb;
    • Weisberg E, Manley PW, Breitenstein W, et al. Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl. Cancer Cell 2005 Feb; 7 (2): 129-41
    • (2005) Cancer Cell , vol.7 , Issue.2 , pp. 129-141
    • Weisberg, E.1    Manley, P.W.2    Breitenstein, W.3
  • 6
    • 0041466445 scopus 로고    scopus 로고
    • Specific targeted therapy of chronic myelogenous leukemia with imatinib
    • Deininger MWN, Druker BJ. Specific targeted therapy of chronic myelogenous leukemia with imatinib. Pharmacol Rev 2003; 55 (3): 401-23
    • (2003) Pharmacol Rev , vol.55 , Issue.3 , pp. 401-423
    • Deininger, M.W.N.1    Druker, B.J.2
  • 7
    • 33845444046 scopus 로고    scopus 로고
    • Five-year follow-up of patients receiving imatinib for chronic myeloid leukemia
    • Dec 7;
    • Druker BJ, Guilhot F, O'Brien SG, et al. Five-year follow-up of patients receiving imatinib for chronic myeloid leukemia. N Engl J Med 2006 Dec 7; 355 (23): 2408-17
    • (2006) N Engl J Med , vol.355 , Issue.23 , pp. 2408-2417
    • Druker, B.J.1    Guilhot, F.2    O'Brien, S.G.3
  • 8
    • 33847057304 scopus 로고    scopus 로고
    • Imatinib: A review of its use in chronic myeloid leukaemia
    • Moen MD, McKeage K, Plosker GL, et al. Imatinib: a review of its use in chronic myeloid leukaemia. Drugs 2007; 67 (2): 299-320
    • (2007) Drugs , vol.67 , Issue.2 , pp. 299-320
    • Moen, M.D.1    McKeage, K.2    Plosker, G.L.3
  • 9
    • 16844372957 scopus 로고    scopus 로고
    • Four years of follow-up of 1027 patients with late chronic phase (L-CP), accelerated phase (AP), or blast crisis (BC) chronic myeloid leukemia (CML) treated with imatinib in three large phase II trials [abstract no. 23]
    • Nov 16;
    • Silver RT, Talpaz M, Sawyers CL, et al. Four years of follow-up of 1027 patients with late chronic phase (L-CP), accelerated phase (AP), or blast crisis (BC) chronic myeloid leukemia (CML) treated with imatinib in three large phase II trials [abstract no. 23]. Blood 2004 Nov 16; 104 (11 Pt 1): 11a
    • (2004) Blood , vol.104 , Issue.11 PART 1
    • Silver, R.T.1    Talpaz, M.2    Sawyers, C.L.3
  • 10
    • 31344472945 scopus 로고    scopus 로고
    • Novel targeted therapies to overcome imatinib mesylate resistance in chronic myeloid leukemia (CML)
    • Feb;
    • Walz C, Sattler M. Novel targeted therapies to overcome imatinib mesylate resistance in chronic myeloid leukemia (CML). Crit Rev Oncol Hematol 2006 Feb; 57 (2): 145-64
    • (2006) Crit Rev Oncol Hematol , vol.57 , Issue.2 , pp. 145-164
    • Walz, C.1    Sattler, M.2
  • 11
    • 33745081606 scopus 로고    scopus 로고
    • Circumventing resistance to kinase-inhibitor therapy
    • Jun 15;
    • Druker BJ. Circumventing resistance to kinase-inhibitor therapy. N Engl J Med 2006 Jun 15; 354 (24): 2594-6
    • (2006) N Engl J Med , vol.354 , Issue.24 , pp. 2594-2596
    • Druker, B.J.1
  • 12
    • 21144451094 scopus 로고    scopus 로고
    • In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants
    • Jun 1;
    • O'Hare T, Walters DK, Stoffregen EP, et al. In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants. Cancer Res 2005 Jun 1; 65 (11): 4500-5
    • (2005) Cancer Res , vol.65 , Issue.11 , pp. 4500-4505
    • O'Hare, T.1    Walters, D.K.2    Stoffregen, E.P.3
  • 13
    • 0034161460 scopus 로고    scopus 로고
    • Induction of resistance to the Abelson inhibitor STI571 in human leukemic cells through gene amplification
    • Mar 1;
    • le Coutre P, Tassi E, Varella-Garcia M, et al. Induction of resistance to the Abelson inhibitor STI571 in human leukemic cells through gene amplification. Blood 2000 Mar 1; 95 (5): 1758-66
    • (2000) Blood , vol.95 , Issue.5 , pp. 1758-1766
    • le Coutre, P.1    Tassi, E.2    Varella-Garcia, M.3
  • 14
    • 0036850514 scopus 로고    scopus 로고
    • Molecular and chromosomal mechanisms of resistance to imatinib (STI571) therapy
    • Hochhaus A, Kreil S, Corbin AS, et al. Molecular and chromosomal mechanisms of resistance to imatinib (STI571) therapy. Leukemia 2002; 16: 2190-6
    • (2002) Leukemia , vol.16 , pp. 2190-2196
    • Hochhaus, A.1    Kreil, S.2    Corbin, A.S.3
  • 15
    • 34248204301 scopus 로고    scopus 로고
    • Jabbour E, Cortes J, Kantarjian H. Dasatinib for the treatment of Philadelphia chromosome-positive leukaemias [published erratum appears in Expert Opin Investig Drugs 2007 Jul; 16 (7): 1135]. Expert Opin Investig Drugs 2007 May; 16 (5): 679-87
    • Jabbour E, Cortes J, Kantarjian H. Dasatinib for the treatment of Philadelphia chromosome-positive leukaemias [published erratum appears in Expert Opin Investig Drugs 2007 Jul; 16 (7): 1135]. Expert Opin Investig Drugs 2007 May; 16 (5): 679-87
  • 16
    • 33745102555 scopus 로고    scopus 로고
    • Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias
    • Jun 15;
    • Talpaz M, Shah NP, Kantarjian H, et al. Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias. N Engl J Med 2006 Jun 15; 354 (24): 2531-41
    • (2006) N Engl J Med , vol.354 , Issue.24 , pp. 2531-2541
    • Talpaz, M.1    Shah, N.P.2    Kantarjian, H.3
  • 17
    • 33947280081 scopus 로고    scopus 로고
    • Dasatinib induces notable hematologic and cytogenetic responses in chronic phase chronic myeloid leukemia after failure of imatinib therapy
    • Mar 15;
    • Hochhaus A, Kantarjian HM, Baccarani M, et al. Dasatinib induces notable hematologic and cytogenetic responses in chronic phase chronic myeloid leukemia after failure of imatinib therapy. Blood 2007 Mar 15; 109 (6): 2303-9
    • (2007) Blood , vol.109 , Issue.6 , pp. 2303-2309
    • Hochhaus, A.1    Kantarjian, H.M.2    Baccarani, M.3
  • 18
    • 34248324467 scopus 로고    scopus 로고
    • Dasatinib induces significant hematologic and cytogenetic responses in patients with imatinib-resistant or -intolerant chronic myeloid leukemia in accelerated phase
    • May 15;
    • Guilhot F, Apperley J, Kim D-W, et al. Dasatinib induces significant hematologic and cytogenetic responses in patients with imatinib-resistant or -intolerant chronic myeloid leukemia in accelerated phase. Blood 2007 May 15; 109 (10): 4143-50
    • (2007) Blood , vol.109 , Issue.10 , pp. 4143-4150
    • Guilhot, F.1    Apperley, J.2    Kim, D.-W.3
  • 19
    • 33947356135 scopus 로고    scopus 로고
    • Dasatinib induces complete hematologic and cytogenetic responses in patients with imatinib-resistant or -intolerant chronic myeloid leukemia in blast crisis
    • Apr 15;
    • Cortes J, Rousselot P, Kim D-W, et al. Dasatinib induces complete hematologic and cytogenetic responses in patients with imatinib-resistant or -intolerant chronic myeloid leukemia in blast crisis. Blood 2007 Apr 15; 109 (8): 3207-13
    • (2007) Blood , vol.109 , Issue.8 , pp. 3207-3213
    • Cortes, J.1    Rousselot, P.2    Kim, D.-W.3
  • 20
    • 24644464172 scopus 로고    scopus 로고
    • AMN107, a novel aminopyrimidine inhibitor of p190 Bcr-Abl activation and of in vitro proliferation of Philadelphia-positive acute lymphoblastic leukemia cells
    • Sep 15;
    • Verstovsek S, Golemovic M, Kantarjian H, et al. AMN107, a novel aminopyrimidine inhibitor of p190 Bcr-Abl activation and of in vitro proliferation of Philadelphia-positive acute lymphoblastic leukemia cells. Cancer 2005 Sep 15; 104 (6): 1230-6
    • (2005) Cancer , vol.104 , Issue.6 , pp. 1230-1236
    • Verstovsek, S.1    Golemovic, M.2    Kantarjian, H.3
  • 21
    • 24644435728 scopus 로고    scopus 로고
    • AMN107, a novel aminopyrimidine inhibitor of Bcr-Abl, has in vitro activity against imatinib-resistant chronic myeloid leukemia
    • Jul 1;
    • Golemovic M, Verstovsek S, Giles F, et al. AMN107, a novel aminopyrimidine inhibitor of Bcr-Abl, has in vitro activity against imatinib-resistant chronic myeloid leukemia. Clin Cancer Res 2005 Jul 1; 11 (13): 4941-7
    • (2005) Clin Cancer Res , vol.11 , Issue.13 , pp. 4941-4947
    • Golemovic, M.1    Verstovsek, S.2    Giles, F.3
  • 22
    • 33745089491 scopus 로고    scopus 로고
    • AMN107: Inhibitory profile against non-mutated and mutated forms of the Bcr-Abl tyrosine kinase
    • abstract no. 5985, Presented at the, Apr 16-20; Anaheim CA
    • Manley PW, Mestan J, Cowan-Jacob S, et al. AMN107: inhibitory profile against non-mutated and mutated forms of the Bcr-Abl tyrosine kinase [abstract no. 5985]. Presented at the 96th Annual Meeting of the American Association for Cancer Research; 2005 Apr 16-20; Anaheim (CA)
    • (2005) 96th Annual Meeting of the American Association for Cancer Research
    • Manley, P.W.1    Mestan, J.2    Cowan-Jacob, S.3
  • 23
    • 40349088801 scopus 로고    scopus 로고
    • Response dynamics to nilotinib depend on the type of BCR-ABL mutations in patients with chronic myelogenous leukemia (CML) after imatinib failure [abstract no. 7024]
    • Jun 1-5; Chicago IL
    • Mueller MC, Branford S, Radich J, et al. Response dynamics to nilotinib depend on the type of BCR-ABL mutations in patients with chronic myelogenous leukemia (CML) after imatinib failure [abstract no. 7024]. Plus poster presented at the 43rd Annual Meeting of the American Society of Clinical Oncology; 2007 Jun 1-5; Chicago (IL)
    • (2007) Plus poster presented at the 43rd Annual Meeting of the American Society of Clinical Oncology
    • Mueller, M.C.1    Branford, S.2    Radich, J.3
  • 24
    • 33745086350 scopus 로고    scopus 로고
    • Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL
    • Jun 15;
    • Kantarjian H, Giles F, Wunderle L, et al. Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL. N Engl J Med 2006 Jun 15; 354 (24): 2542-51
    • (2006) N Engl J Med , vol.354 , Issue.24 , pp. 2542-2551
    • Kantarjian, H.1    Giles, F.2    Wunderle, L.3
  • 25
    • 40349087099 scopus 로고    scopus 로고
    • Kagan M, Tran P, Fischer V, et al. Safety, pharmacokinetics, metabolism, and mass balance of [14C]-AMN107, a novel aminopyrimidine inhibitor of Bcr-Abl tyrosine kinase, in healthy subjects [abstract no. 4887]. Blood 2005 Nov 16; 106 (11 Pt 2): 302b
    • Kagan M, Tran P, Fischer V, et al. Safety, pharmacokinetics, metabolism, and mass balance of [14C]-AMN107, a novel aminopyrimidine inhibitor of Bcr-Abl tyrosine kinase, in healthy subjects [abstract no. 4887]. Blood 2005 Nov 16; 106 (11 Pt 2): 302b
  • 26
    • 57749174353 scopus 로고    scopus 로고
    • Clinical pharmacokinetics (PK) of AMN107, a novel inhibitor of Bcr-Abl, in healthy subjects and patients with imatinib resistant or intolerant chronic myelogenous leukemia (CML) or relapsed/refractory Ph+ acute lymphocytic leukemia (Ph+ ALL) [abstract no. 3095]
    • Jun 20; , 144s
    • Tanaka C, Smith T, Kantarjian H, et al. Clinical pharmacokinetics (PK) of AMN107, a novel inhibitor of Bcr-Abl, in healthy subjects and patients with imatinib resistant or intolerant chronic myelogenous leukemia (CML) or relapsed/refractory Ph+ acute lymphocytic leukemia (Ph+ ALL) [abstract no. 3095]. J Clin Oncol 2006 Jun 20; (18 Pt 1 Suppl. 24): 144s
    • (2006) J Clin Oncol , Issue.18 PART 1 SUPPL. 24
    • Tanaka, C.1    Smith, T.2    Kantarjian, H.3
  • 27
    • 40349085592 scopus 로고    scopus 로고
    • Novartis Pharmaceuticals Corporation:, US prescribing information [online, Available from URL:, Accessed 2007 Nov 29
    • Novartis Pharmaceuticals Corporation: East Hanover (NJ). Tasigna® (nilotinib capsules): US prescribing information [online]. Available from URL: http://www.fda.gov/ [Accessed 2007 Nov 29]
    • Tasigna® (nilotinib capsules)
    • East Hanover, N.J.1
  • 28
    • 36348968931 scopus 로고    scopus 로고
    • Nilotinib (formerly AMN107), a highly selective Bcr-Abl tyrosine kinase inhibitor, is effective in patients with Philadelphia chromosome-positive chronic myelogenous leukemia in chronic phase following imatinib resistance and intolerance
    • Nov 15;
    • Kantarjian HM, Giles F, Gattermann N, et al. Nilotinib (formerly AMN107), a highly selective Bcr-Abl tyrosine kinase inhibitor, is effective in patients with Philadelphia chromosome-positive chronic myelogenous leukemia in chronic phase following imatinib resistance and intolerance. Blood 2007 Nov 15; 110 (10): 3540-6
    • (2007) Blood , vol.110 , Issue.10 , pp. 3540-3546
    • Kantarjian, H.M.1    Giles, F.2    Gattermann, N.3
  • 29
    • 41349083969 scopus 로고    scopus 로고
    • le Coutre P, Ottmann OG, Giles F, et al. Nilotinib (formerly AMN107), a highly selective BCR-ABL tyrosine kinase inhib-itor, is active in patients with imatinib-resistant or -intolerant accelerated phase chronic myelogenous leukemia. Blood 2008 Feb 15; 111 (4): 1834-9
    • le Coutre P, Ottmann OG, Giles F, et al. Nilotinib (formerly AMN107), a highly selective BCR-ABL tyrosine kinase inhib-itor, is active in patients with imatinib-resistant or -intolerant accelerated phase chronic myelogenous leukemia. Blood 2008 Feb 15; 111 (4): 1834-9
  • 30
    • 37349112422 scopus 로고    scopus 로고
    • Nilotinib monotherapy in patients with imatinib-resistant or -intolerant Ph+ chronic myelogenous leukemia (CML) in blast crisis (BC) or relapsed/refractory Ph+ acute lymphoblastic leukemia (ALL)
    • abstract no. 0556, Jun 7-10; Vienna
    • Ottmann O, Larson R, Kantarjian H, et al. Nilotinib monotherapy in patients with imatinib-resistant or -intolerant Ph+ chronic myelogenous leukemia (CML) in blast crisis (BC) or relapsed/refractory Ph+ acute lymphoblastic leukemia (ALL) [abstract no. 0556]. Plus poster presented at the 12th Congress of the European Hematology Association (EHA); 2007 Jun 7-10; Vienna
    • (2007) Plus poster presented at the 12th Congress of the European Hematology Association (EHA)
    • Ottmann, O.1    Larson, R.2    Kantarjian, H.3
  • 31
    • 40349087097 scopus 로고    scopus 로고
    • Nilotinib therapy after dasatinib failure in patients with imatinib-resistant or -intoler-ant chronic phase and accelerated phase Philadelphia-positive chronic myelogenous leukemia
    • abstract no. 0554, Jun 7-10; Vienna
    • Giles F, le Coutre P, Bhalla K, et al. Nilotinib therapy after dasatinib failure in patients with imatinib-resistant or -intoler-ant chronic phase and accelerated phase Philadelphia-positive chronic myelogenous leukemia [abstract no. 0554]. Plus poster presented at the 12th Congress of the European Hematology Association (EHA); 2007 Jun 7-10; Vienna
    • (2007) Plus poster presented at the 12th Congress of the European Hematology Association (EHA)
    • Giles, F.1    le Coutre, P.2    Bhalla, K.3
  • 32
    • 40349098026 scopus 로고    scopus 로고
    • A phase II study of nilotinib administered to patients with imatinib resistant or intolerant chronic myelogenous leukemia (CML) in chronic phase (CP), accelerated phase (AP) or blast crisis (BC) who also failed dasatinib
    • abstract no. 7038, Jun 1-5; Chicago IL
    • Giles FJ, le Coutre P, Bhalla K, et al. A phase II study of nilotinib administered to patients with imatinib resistant or intolerant chronic myelogenous leukemia (CML) in chronic phase (CP), accelerated phase (AP) or blast crisis (BC) who also failed dasatinib [abstract no. 7038]. Plus poster presented at the 43rd Annual Meeting of the American Society of Clinical Oncology; 2007 Jun 1-5; Chicago (IL)
    • (2007) Plus poster presented at the 43rd Annual Meeting of the American Society of Clinical Oncology
    • Giles, F.J.1    le Coutre, P.2    Bhalla, K.3
  • 33
    • 0037092980 scopus 로고    scopus 로고
    • Imatinib mesylate (STI571) therapy for Philadelphia chromosome-positive chronic myelogenous leukemia in blast phase
    • May 15;
    • Kantarjian HM, Cortes J, O'Brien S, et al. Imatinib mesylate (STI571) therapy for Philadelphia chromosome-positive chronic myelogenous leukemia in blast phase. Blood 2002 May 15; 99 (10): 3547-53
    • (2002) Blood , vol.99 , Issue.10 , pp. 3547-3553
    • Kantarjian, H.M.1    Cortes, J.2    O'Brien, S.3
  • 34
    • 0037186915 scopus 로고    scopus 로고
    • Hematologic and cytogenetic responses to imatinib mesylate in chronic myelogenous leukemia
    • Feb 28;
    • Kantarjian H, Sawyers C, Hochhaus A, et al. Hematologic and cytogenetic responses to imatinib mesylate in chronic myelogenous leukemia. N Engl J Med 2002 Feb 28; 346 (9): 645-52
    • (2002) N Engl J Med , vol.346 , Issue.9 , pp. 645-652
    • Kantarjian, H.1    Sawyers, C.2    Hochhaus, A.3
  • 35
    • 35648936586 scopus 로고    scopus 로고
    • UGT1A1 promoter polymorphism increases risk of nilotinib-induced hyperbilirubinemia
    • Nov;
    • Singer JB, Shou Y, Giles F, et al. UGT1A1 promoter polymorphism increases risk of nilotinib-induced hyperbilirubinemia. Leukemia 2007 Nov; 21 (11): 2311-5
    • (2007) Leukemia , vol.21 , Issue.11 , pp. 2311-2315
    • Singer, J.B.1    Shou, Y.2    Giles, F.3
  • 36
    • 40349088802 scopus 로고    scopus 로고
    • Princeton (NJ)
    • US prescribing information, online, Available from URL:, Accessed 2007 Dec 6
    • Bristol-Myers Squibb: Princeton (NJ). Sprycel® (dasatinib): US prescribing information. [online]. Available from URL: http://www.fda.gov [Accessed 2007 Dec 6]
    • Sprycel® (dasatinib)
    • Bristol-Myers Squibb1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.