DGIdb - NILOTINIB Drug Record

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:

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

Reported Cancer Type	Melanoma
Indication/Tumor Type	melanoma
Response Type	sensitive

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

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

Nilotinib	PubChem Drug Name
644241	PubChem Drug ID
Tasigna	Drug Trade Name

antagonist (inhibitory)
inhibitor (inhibitory)

NILOTINIB Drug Record

NILOTINIB chembl:CHEMBL255863 ApprovedAntineoplasticImmunotherapy

Alternate Names:

Drug Info:

Publications:

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

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 26191369

Sources: DTC

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

Interaction Types & Directionality: n/a

Interaction Info: Fusion protein BCR:ABL1

PMIDs: None found

Sources: PharmGKB FDA

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24898899 17611564

Sources: PharmGKB FDA

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18191450

Sources: CIViC

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

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 26703895

Sources: CIViC MyCancerGenomeClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24322003

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28720666

Sources: CIViC

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

Alternate Names: NILOTINIB Primary Drug Name

Drug Info: Drug Class antineoplastic agent Year of Approval 2007

Publications:

CancerCommons: NILOTINIB

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

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

Alternate Names:

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

Publications:

DTC: NILOTINIB

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

Alternate Names:

Drug Info:

DoCM: NILOTINIB

Alternate Names:

Drug Info:

PharmGKB: nilotinib

Alternate Names:

Drug Info:

CIViC: NILOTINIB

Alternate Names:

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

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
26191369

Sources:
DTC

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

Interaction Types & Directionality:

n/a

Interaction Info:

Fusion protein BCR:ABL1

PMIDs:
None found

Sources:
PharmGKB FDA

Interaction Types & Directionality:

n/a

PMIDs:
24898899 17611564

Sources:
PharmGKB FDA

Interaction Types & Directionality:

n/a

PMIDs:
18191450

Sources:
CIViC

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

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
26703895

Sources:
CIViC MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
24322003

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
28720666

Sources:
CIViC

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

Alternate Names:

NILOTINIB Primary Drug Name

Drug Info:

Drug Class antineoplastic agent

Year of Approval 2007

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

Alternate Names:

NILOTINIB Generic Name

TASIGNA Trade Name

Drug Info:

Drug Class Kinase Inhibitors

FDA Approval Chronic myelogenous leukemia (Philadelphia chromosome positive)

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval approved

Alternate Names:

CHEMBL255863 ChEMBL Drug ID

Publications:

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

Alternate Names:

D00STL TTD Drug ID