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NILOTINIB Drug Record

  • Summary
  • Interactions
  • Claims
  • NILOTINIB chembl:CHEMBL255863 ApprovedAntineoplasticImmunotherapy

    Alternate Names:

    NILOTINIB
    AMN-107
    AMN107
    TASIGNA
    TASIGNA®
    AMN 107
    NILOTINIBUM
    pubchem.compound:644241
    drugbank:04868
    rxcui:662281
    chemidplus:641571-10-0
    chembl:CHEMBL255863

    Drug Info:

    Year of Approval 2007
    Drug Class antineoplastic agent
    FDA Approval Chronic myelogenous leukemia (Philadelphia chromosome positive)
    Drug Class Kinase Inhibitors
    FDA Approval approved
    Drug Class Small molecule
    Drug Indications antineoplastic agent
    Pharmaceutical Developer Novartis
    Source Reported Drug Name(s) Nilotinib/AMNN107 (approved for CML+)
    Drug Class Kit Inhibitor
    (11 More Sources)

    Publications:

    Cang et al., 2008, P-loop mutations and novel therapeutic approaches for imatinib failures in chronic myeloid leukemia., J Hematol Oncol
    Soverini et al., 2006, Presence or the emergence of a F317L BCR-ABL mutation may be associated with resistance to dasatinib in Philadelphia chromosome-positive leukemia., J. Clin. Oncol.
    Strhakova et al., 2011, Use of direct sequencing for detection of mutations in the BCR-ABL kinase domain in Slovak patients with chronic myeloid leukemia., Neoplasma
    Eskazan et al., 2011, Chronic myeloid leukemia patients with F317L BCR-ABL kinase domain mutation are resistant to dasatinib: is that true for all the patients?, Leuk. Res.
    MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
    Sharma et al., 2010, Mutations in ABL kinase domain are associated with inferior progression-free survival., Leuk. Lymphoma
    Chahardouli et al., 2013, Detection of BCR-ABL kinase domain mutations in patients with chronic myeloid leukemia on imatinib., Hematology
    Oyekunle et al., 2011, F317L BCR-ABL1 kinase domain mutation associated with a sustained major molecular response in a CML patient on dasatinib., Leuk. Res.
    Branford et al., 2003, Detection of BCR-ABL mutations in patients with CML treated with imatinib is virtually always accompanied by clinical resistance, and mutations in the ATP phosphate-binding loop (P-loop) are associated with a poor prognosis., Blood
    Branford et al., 2002, High frequency of point mutations clustered within the adenosine triphosphate-binding region of BCR/ABL in patients with chronic myeloid leukemia or Ph-positive acute lymphoblastic leukemia who develop imatinib (STI571) resistance., Blood
    Soverini et al., 2011, BCR-ABL kinase domain mutation analysis in chronic myeloid leukemia patients treated with tyrosine kinase inhibitors: recommendations from an expert panel on behalf of European LeukemiaNet., Blood
    Hughes et al., 2009, Impact of baseline BCR-ABL mutations on response to nilotinib in patients with chronic myeloid leukemia in chronic phase., J. Clin. Oncol.
    Pemovska T et al., 2015, Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation., Nature
    Bradeen HA et al., 2006, Comparison of imatinib mesylate, dasatinib (BMS-354825), and nilotinib (AMN107) in an N-ethyl-N-nitrosourea (ENU)-based mutagenesis screen: high efficacy of drug combinations., Blood
    Redaelli et al., 2009, Activity of bosutinib, dasatinib, and nilotinib against 18 imatinib-resistant BCR/ABL mutants., J. Clin. Oncol.
    An et al., 2010, BCR-ABL tyrosine kinase inhibitors in the treatment of Philadelphia chromosome positive chronic myeloid leukemia: a review., Leuk. Res.
    Maekawa et al., 2007, The Bcr-Abl tyrosine kinase inhibitor imatinib and promising new agents against Philadelphia chromosome-positive leukemias., Int. J. Clin. Oncol.
    Weisberg et al., 2006, AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL., Br. J. Cancer
    Kantarjian et al., 2007, 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
    Swords et al., 2009, Nilotinib: optimal therapy for patients with chronic myeloid leukemia and resistance or intolerance to imatinib., Drug Des Devel Ther
    Rosti et al., 2009, Nilotinib for the frontline treatment of Ph(+) chronic myeloid leukemia., Blood
    Zick et al., 2017, Treatment inferred from mutations identified using massive parallel sequencing leads to clinical benefit in some heavily pretreated cancer patients., Medicine (Baltimore)
    Deguchi Y et al., 2008, Comparison of imatinib, dasatinib, nilotinib and INNO-406 in imatinib-resistant cell lines., Leuk Res
    Cullinane et al., 2010, Preclinical evaluation of nilotinib efficacy in an imatinib-resistant KIT-driven tumor model., Mol. Cancer Ther.
    Guo et al., 2007, Sorafenib inhibits the imatinib-resistant KITT670I gatekeeper mutation in gastrointestinal stromal tumor., Clin. Cancer Res.
    Valent et al., 2015, Chronic mast cell leukemia (MCL) with KIT S476I: a rare entity defined by leukemic expansion of mature mast cells and absence of organ damage., Ann. Hematol.
    Carlino et al., 2014, Resistance to c-Kit inhibitors in melanoma: insights for future therapies., Oncoscience
    Todd et al., 2013, Secondary c-Kit mutations confer acquired resistance to RTK inhibitors in c-Kit mutant melanoma cells., Pigment Cell Melanoma Res
    Guo et al., 2017, Efficacy and safety of nilotinib in patients with KIT-mutated metastatic or inoperable melanoma: final results from the global, single-arm, phase II TEAM trial., Ann. Oncol.
    Delyon et al., 2017, STAT3 mediates Nilotinib response in KIT-altered Melanoma: a Phase II Multicenter Trial of the French Skin Cancer Network., J. Invest. Dermatol.
    Sawaki et al., 2011, Phase 2 study of nilotinib as third-line therapy for patients with gastrointestinal stromal tumor., Cancer
    Cauchi et al., 2012, Evaluation of nilotinib in advanced GIST previously treated with imatinib and sunitinib., Cancer Chemother. Pharmacol.
    Carvajal et al., 2015, Phase II Study of Nilotinib in Melanoma Harboring KIT Alterations Following Progression to Prior KIT Inhibition., Clin. Cancer Res.
    Cho et al., 2012, Nilotinib in patients with metastatic melanoma harboring KIT gene aberration., Invest New Drugs
    Antonescu et al., 2007, L576P KIT mutation in anal melanomas correlates with KIT protein expression and is sensitive to specific kinase inhibition., Int. J. Cancer
    Woodman et al., 2009, Activity of dasatinib against L576P KIT mutant melanoma: molecular, cellular, and clinical correlates., Mol. Cancer Ther.
    Shen et al., 2017, Inactivation of Receptor Tyrosine Kinases Reverts Aberrant DNA Methylation in Acute Myeloid Leukemia., Clin. Cancer Res.
    Lee SJ et al., 2015, Phase II Trial of Nilotinib in Patients With Metastatic Malignant Melanoma Harboring KIT Gene Aberration: A Multicenter Trial of Korean Cancer Study Group (UN10-06)., Oncologist
    Abumiya M et al., 2014, Influence of UGT1A1 6, 27, and 28 polymorphisms on nilotinib-induced hyperbilirubinemia in Japanese patients with chronic myeloid leukemia., Drug Metab Pharmacokinet
    Singer JB et al., 2007, UGT1A1 promoter polymorphism increases risk of nilotinib-induced hyperbilirubinemia., Leukemia
    Dewaele et al., 2008, 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.
    Ishibashi T et al., 2016, Ph-like ALL-related novel fusion kinase ATF7IP-PDGFRB exhibits high sensitivity to tyrosine kinase inhibitors in murine cells., Exp Hematol
    Hayes et al., 2016, Long-Term ERK Inhibition in KRAS-Mutant Pancreatic Cancer Is Associated with MYC Degradation and Senescence-like Growth Suppression., Cancer Cell
    Murray CW et al., 2015, Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors., ACS Med Chem Lett
    Skoglund K et al., 2014, Single-nucleotide polymorphisms of ABCG2 increase the efficacy of tyrosine kinase inhibitors in the K562 chronic myeloid leukemia cell line., Pharmacogenet Genomics
  • NILOTINIB   ABL1

    Interaction Score: 2.85

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name nilotinib , AMN-107,Tasigna
    Novel drug target Established target
    Variant Effect gain-of-function

    PMIDs:
    18828913 17114651 21895409 21605905 25157968 20367437 23676790 21489624 12623848 11964322 21562040 19652056 25686603 16772610 19075254 20537386 17929114 16721371 17715389 19920925 19822896 28514312 18191450


    Sources:
    MyCancerGenome TdgClinicalTrial JAX-CKB TEND DoCM COSMIC CIViC PharmGKB FDA OncoKB

  • NILOTINIB   DDR2

    Interaction Score: 2.25

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    26191369


    Sources:
    DTC

  • NILOTINIB   KIT

    Interaction Score: 1.84

    Interaction Types & Directionality:
    antagonist (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Reported Cancer Type Melanoma
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    20442311 17699867 25209843 25594040 23582185 28327988 28843487 21456006 22119758 25695690 22068222 17372901 19671763 28720666 26424760


    Sources:
    JAX-CKB COSMIC CIViC CancerCommons MyCancerGenomeClinicalTrial

  • NILOTINIB   BCR

    Interaction Score: 0.94

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Fusion protein BCR:ABL1

    PMIDs:
    None found


    Sources:
    PharmGKB FDA

  • NILOTINIB   UGT1A1

    Interaction Score: 0.61

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24898899 17611564


    Sources:
    PharmGKB FDA

  • NILOTINIB   LYN

    Interaction Score: 0.28

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18191450


    Sources:
    CIViC

  • NILOTINIB   PDGFRA

    Interaction Score: 0.26

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type Advanced Solid Tumor
    Response Type resistant
    Approval Status Preclinical - Cell culture

    PMIDs:
    18794084


    Sources:
    JAX-CKB MyCancerGenomeClinicalTrial

  • NILOTINIB   PDGFRB

    Interaction Score: 0.24

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    26703895


    Sources:
    CIViC MyCancerGenomeClinicalTrial

  • NILOTINIB   ABCG2

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24322003


    Sources:
    PharmGKB

  • NILOTINIB   FLT3

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28720666


    Sources:
    CIViC

  • NILOTINIB   KRAS

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Nilotinib + SCH772984
    Indication/Tumor Type pancreatic ductal adenocarcinoma
    Response Type sensitive

    PMIDs:
    26725216


    Sources:
    JAX-CKB

  • TEND: NILOTINIB

    • Version: 01-August-2011

    Alternate Names:
    NILOTINIB Primary Drug Name

    Drug Info:
    Drug Class antineoplastic agent
    Year of Approval 2007

    Publications:

  • CancerCommons: NILOTINIB

    • Version: 25-July-2013

    Alternate Names:
    Nilotinib PubChem Drug Name
    644241 PubChem Drug ID
    Tasigna Drug Trade Name

    Drug Info:
    Drug Class Kit Inhibitor
    Source Reported Drug Name(s) Nilotinib/AMNN107 (approved for CML+)
    Pharmaceutical Developer Novartis

    Publications:

  • MyCancerGenome: NILOTINIB

    • Version: 20-Jun-2017

    Alternate Names:
    NILOTINIB Generic Name
    TASIGNA Trade Name

    Drug Info:
    Drug Class Kinase Inhibitors
    FDA Approval Chronic myelogenous leukemia (Philadelphia chromosome positive)

    Publications:

  • TdgClinicalTrial: NILOTINIB

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications antineoplastic agent
    Drug Class Small molecule
    FDA Approval approved

    Publications:

  • DTC: NILOTINIB

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL255863 ChEMBL Drug ID

    Drug Info:

    Publications:
    Murray CW et al., 2015, Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors., ACS Med Chem Lett

  • JAX-CKB: Nilotinib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Hayes et al., 2016, Long-Term ERK Inhibition in KRAS-Mutant Pancreatic Cancer Is Associated with MYC Degradation and Senescence-like Growth Suppression., Cancer Cell
    Delyon et al., 2017, STAT3 mediates Nilotinib response in KIT-altered Melanoma: a Phase II Multicenter Trial of the French Skin Cancer Network., J. Invest. Dermatol.
    Cullinane et al., 2010, Preclinical evaluation of nilotinib efficacy in an imatinib-resistant KIT-driven tumor model., Mol. Cancer Ther.

  • DoCM: NILOTINIB

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Chahardouli et al., 2013, Detection of BCR-ABL kinase domain mutations in patients with chronic myeloid leukemia on imatinib., Hematology
    Branford et al., 2003, Detection of BCR-ABL mutations in patients with CML treated with imatinib is virtually always accompanied by clinical resistance, and mutations in the ATP phosphate-binding loop (P-loop) are associated with a poor prognosis., Blood
    Sharma et al., 2010, Mutations in ABL kinase domain are associated with inferior progression-free survival., Leuk. Lymphoma

  • PharmGKB: nilotinib

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Skoglund K et al., 2014, Single-nucleotide polymorphisms of ABCG2 increase the efficacy of tyrosine kinase inhibitors in the K562 chronic myeloid leukemia cell line., Pharmacogenet Genomics
    Singer JB et al., 2007, UGT1A1 promoter polymorphism increases risk of nilotinib-induced hyperbilirubinemia., Leukemia
    Abumiya M et al., 2014, Influence of UGT1A1 6, 27, and 28 polymorphisms on nilotinib-induced hyperbilirubinemia in Japanese patients with chronic myeloid leukemia., Drug Metab Pharmacokinet

  • CIViC: NILOTINIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Shen et al., 2017, Inactivation of Receptor Tyrosine Kinases Reverts Aberrant DNA Methylation in Acute Myeloid Leukemia., Clin. Cancer Res.
    Lee SJ et al., 2015, Phase II Trial of Nilotinib in Patients With Metastatic Malignant Melanoma Harboring KIT Gene Aberration: A Multicenter Trial of Korean Cancer Study Group (UN10-06)., Oncologist
    Antonescu et al., 2007, L576P KIT mutation in anal melanomas correlates with KIT protein expression and is sensitive to specific kinase inhibition., Int. J. Cancer

  • TTD: Nilotinib

    • Version: 2020.06.01

    Alternate Names:
    D00STL TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL255863

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • MyCancerGenomeClinicalTrial: NILOTINIB

    • Version: 30-February-2014

    Alternate Names:

    Drug Info:

    Publications:

  • OncoKB: Nilotinib

    • Version: 23-July-2020

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Nilotinib

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

  • COSMIC: Nilotinib

    • Version: 4-Sep-2020

    Alternate Names:

    Drug Info:

    Publications:

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A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21