DGIdb - CERITINIB Drug Record

CERITINIB chembl:CHEMBL2403108 ApprovedAntineoplastic

Alternate Names:

LDK378
ZYKADIA
NVP-LDK-378-NX
CERITINIB
LDK-378
NVP-LDK378-NX
ZYKADIA®
N-{2-[(5-CHLORO-2-{[2-ISOPROPOXY-5-METHYL-4-(PIPERIDIN-4-YL)PHENYL]AMINO}PYRIMIDIN-4-YL)AMINO]PHENYL}PROPANE-2-SULFONAMIDE
CÉRITINIB
COMPOUND 15B [PMID 23742252]
pubchem.compound:57379345
rxcui:1535457
drugbank:09063
chembl:CHEMBL2403108
chemidplus:1032900-25-6

Drug Info:

FDA Approval	Non-small cell lung cancer (with ALK fusion)
Drug Class	Kinase Inhibitor
Pharmaceutical Developer	Novartis
Source Reported Drug Name(s)	LDK378
Drug Class	ALK Inhibitor
Drug Class	Kinase Inhibitors

(12 More Sources)

Publications:

Chen J et al., 2013, LDK378: a promising anaplastic lymphoma kinase (ALK) inhibitor., J Med Chem
Landi L et al., 2016, Ceritinib for the treatment of patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer., Expert Rev Clin Pharmacol
Kanaan Z et al., 2015, Novel targeted therapies for resistant ALK-rearranged non-small-cell lung cancer: ceritinib and beyond., Onco Targets Ther
Marsilje et al., 2013, Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials., J. Med. Chem.
Galkin et al., 2007, Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK., Proc. Natl. Acad. Sci. U.S.A.
Shaw et al., 2014, Ceritinib in ALK-rearranged non-small-cell lung cancer., N. Engl. J. Med.
Morán et al., 2013, Targeting EML4-ALK driven non-small cell lung cancer (NSCLC)., Transl Lung Cancer Res
Amin et al., 2016, TKI sensitivity patterns of novel kinase-domain mutations suggest therapeutic opportunities for patients with resistant ALK+ tumors., Oncotarget
Kodityal et al., 2016, A novel acquired ALK F1245C mutation confers resistance to crizotinib in ALK-positive NSCLC but is sensitive to ceritinib., Lung Cancer
Crystal et al., 2014, Patient-derived models of acquired resistance can identify effective drug combinations for cancer., Science
Johung et al., 2016, Extended Survival and Prognostic Factors for Patients With ALK-Rearranged Non-Small-Cell Lung Cancer and Brain Metastasis., J. Clin. Oncol.
Soria et al., 2017, First-line ceritinib versus platinum-based chemotherapy in advanced ALK-rearranged non-small-cell lung cancer (ASCEND-4): a randomised, open-label, phase 3 study., Lancet
Crinò et al., 2016, Multicenter Phase II Study of Whole-Body and Intracranial Activity With Ceritinib in Patients With ALK-Rearranged Non-Small-Cell Lung Cancer Previously Treated With Chemotherapy and Crizotinib: Results From ASCEND-2., J. Clin. Oncol.
Gainor et al., 2015, Progression-Free and Overall Survival in ALK-Positive NSCLC Patients Treated with Sequential Crizotinib and Ceritinib., Clin. Cancer Res.
Friboulet et al., 2014, The ALK inhibitor ceritinib overcomes crizotinib resistance in non-small cell lung cancer., Cancer Discov
Shaw et al., 2016, Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F., N. Engl. J. Med.
Gainor et al., 2016, Molecular Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in ALK-Rearranged Lung Cancer., Cancer Discov
Ceccon et al., 2015, Treatment Efficacy and Resistance Mechanisms Using the Second-Generation ALK Inhibitor AP26113 in Human NPM-ALK-Positive Anaplastic Large Cell Lymphoma., Mol. Cancer Res.
Zhang et al., 2016, The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models., Clin. Cancer Res.
Mologni et al., 2015, NPM/ALK mutants resistant to ASP3026 display variable sensitivity to alternative ALK inhibitors but succumb to the novel compound PF-06463922., Oncotarget
Katayama et al., 2014, Two novel ALK mutations mediate acquired resistance to the next-generation ALK inhibitor alectinib., Clin. Cancer Res.
Sakamoto et al., 2011, CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant., Cancer Cell
Choi et al., 2010, EML4-ALK mutations in lung cancer that confer resistance to ALK inhibitors., N. Engl. J. Med.
Chen et al., 2014, Co-clinical trials demonstrate superiority of crizotinib to chemotherapy in ALK-rearranged non-small cell lung cancer and predict strategies to overcome resistance., Clin. Cancer Res.
Kim et al., 2013, Heterogeneity of genetic changes associated with acquired crizotinib resistance in ALK-rearranged lung cancer., J Thorac Oncol
Doebele et al., 2012, Mechanisms of resistance to crizotinib in patients with ALK gene rearranged non-small cell lung cancer., Clin. Cancer Res.
Katayama et al., 2012, Mechanisms of acquired crizotinib resistance in ALK-rearranged lung Cancers., Sci Transl Med
Mansfield et al., 2016, Chromoplectic TPM3-ALK rearrangement in a patient with inflammatory myofibroblastic tumor who responded to ceritinib after progression on crizotinib., Ann. Oncol.
Yakirevich et al., 2016, Oncogenic ALK Fusion in Rare and Aggressive Subtype of Colorectal Adenocarcinoma as a Potential Therapeutic Target., Clin. Cancer Res.
Amatu et al., 2015, Novel CAD-ALK gene rearrangement is drugable by entrectinib in colorectal cancer., Br. J. Cancer
Ou et al., 2015, I1171 missense mutation (particularly I1171N) is a common resistance mutation in ALK-positive NSCLC patients who have progressive disease while on alectinib and is sensitive to ceritinib., Lung Cancer
Kim et al., 2016, Activity and safety of ceritinib in patients with ALK-rearranged non-small-cell lung cancer (ASCEND-1): updated results from the multicentre, open-label, phase 1 trial., Lancet Oncol.
Yoda S et al., 2018, Sequential ALK Inhibitors Can Select for Lorlatinib-Resistant Compound <i>ALK</i> Mutations in ALK-Positive Lung Cancer., Cancer Discov
Shaw AT et al., 2017, Ceritinib versus chemotherapy in patients with ALK-rearranged non-small-cell lung cancer previously given chemotherapy and crizotinib (ASCEND-5): a randomised, controlled, open-label, phase 3 trial., Lancet Oncol
Lovly et al., 2014, Rationale for co-targeting IGF-1R and ALK in ALK fusion-positive lung cancer., Nat. Med.
Davare et al., 2015, Structural insight into selectivity and resistance profiles of ROS1 tyrosine kinase inhibitors., Proc. Natl. Acad. Sci. U.S.A.
Lim et al., 2017, Open-Label, Multicenter, Phase II Study of Ceritinib in Patients With Non-Small-Cell Lung Cancer Harboring ROS1 Rearrangement., J. Clin. Oncol.
Katayama R et al., 2015, P-glycoprotein Mediates Ceritinib Resistance in Anaplastic Lymphoma Kinase-rearranged Non-small Cell Lung Cancer., EBioMedicine

CERITINIB EML4

Interaction Score: 5.06

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type resistant

Approval Status Preclinical

PMIDs:
26775591 25173427 24675041 27780853 25228534 27009859 27432227 26698910

Sources:
JAX-CKB
CERITINIB ALK

Interaction Score: 4.79

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Notes Specifically targets ALK translocations

Reported Cancer Type Lung

combination therapy Saracatinib + Ceritinib

PMIDs:
26582431 25945060 23742252 17185414 24670165 25806224 27009859 26775591 25394791 26438117 28126333 27432917 25724526 24675041 26698910 27432227 25421750 27780853 25749034 25228534 21575866 20979473 24327273 23344087 22235099 22277784 27742657 26933125 26633560 25736571 26973324 29650534 28602779

Sources:
TALC MyCancerGenome JAX-CKB ChemblInteractions DoCM COSMIC CIViC CancerCommons MyCancerGenomeClinicalTrial PharmGKB TTD FDA OncoKB
CERITINIB NPM1

Interaction Score: 1.61

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type anaplastic large cell lymphoma

Response Type resistant

Approval Status Preclinical

PMIDs:
27009859 25749034 25421750

Sources:
JAX-CKB
CERITINIB TSSK1B

Interaction Score: 1.41

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
23837797

Sources:
DTC
CERITINIB ROS1

Interaction Score: 0.8

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

Approval Status Phase II

PMIDs:
26372962 28520527

Sources:
JAX-CKB CIViC
CERITINIB IGF1R

Interaction Score: 0.3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
23837797

Sources:
DTC
CERITINIB MAP2K1

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Ceritinib + Selumetinib

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

PMIDs:
25394791

Sources:
JAX-CKB
CERITINIB SRC

Interaction Score: 0.2

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type resistant

Approval Status Preclinical

PMIDs:
25394791

Sources:
JAX-CKB
CERITINIB INSR

Interaction Score: 0.19

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
23837797

Sources:
DTC
CERITINIB ABCB1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26870817

Sources:
CIViC
CERITINIB CYP3A4

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23837797

Sources:
DTC

MyCancerGenome: CERITINIB
- Version: 20-Jun-2017
Alternate Names:

ZYKADIA Trade Name

Drug Info:

Drug Class Kinase Inhibitor

FDA Approval Non-small cell lung cancer (with ALK fusion)

Publications:
CancerCommons: LDK378
- Version: 25-July-2013
Alternate Names:

LDK378 Drug Trade Name

LDK378 Drug Development Name

Drug Info:

Drug Class ALK Inhibitor

Source Reported Drug Name(s) LDK378

Pharmaceutical Developer Novartis

Publications:
MyCancerGenome: LDK378
- Version: 20-Jun-2017
Alternate Names:

LDK378 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Publications:
DTC: CERITINIB
- Version: 02-September-2020
Alternate Names:

CHEMBL2403108 ChEMBL Drug ID

Drug Info:

Publications:

Chen J et al., 2013, LDK378: a promising anaplastic lymphoma kinase (ALK) inhibitor., J Med Chem

DoCM: CERITINIB

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Katayama et al., 2012, Mechanisms of acquired crizotinib resistance in ALK-rearranged lung Cancers., Sci Transl Med

Doebele et al., 2012, Mechanisms of resistance to crizotinib in patients with ALK gene rearranged non-small cell lung cancer., Clin. Cancer Res.

Chen et al., 2014, Co-clinical trials demonstrate superiority of crizotinib to chemotherapy in ALK-rearranged non-small cell lung cancer and predict strategies to overcome resistance., Clin. Cancer Res.

JAX-CKB: Ceritinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Amin et al., 2016, TKI sensitivity patterns of novel kinase-domain mutations suggest therapeutic opportunities for patients with resistant ALK+ tumors., Oncotarget

Mologni et al., 2015, NPM/ALK mutants resistant to ASP3026 display variable sensitivity to alternative ALK inhibitors but succumb to the novel compound PF-06463922., Oncotarget

Ceccon et al., 2015, Treatment Efficacy and Resistance Mechanisms Using the Second-Generation ALK Inhibitor AP26113 in Human NPM-ALK-Positive Anaplastic Large Cell Lymphoma., Mol. Cancer Res.

PharmGKB: ceritinib

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Landi L et al., 2016, Ceritinib for the treatment of patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer., Expert Rev Clin Pharmacol

Kanaan Z et al., 2015, Novel targeted therapies for resistant ALK-rearranged non-small-cell lung cancer: ceritinib and beyond., Onco Targets Ther

CIViC: CERITINIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Kodityal et al., 2016, A novel acquired ALK F1245C mutation confers resistance to crizotinib in ALK-positive NSCLC but is sensitive to ceritinib., Lung Cancer

Yakirevich et al., 2016, Oncogenic ALK Fusion in Rare and Aggressive Subtype of Colorectal Adenocarcinoma as a Potential Therapeutic Target., Clin. Cancer Res.

Ou et al., 2015, I1171 missense mutation (particularly I1171N) is a common resistance mutation in ALK-positive NSCLC patients who have progressive disease while on alectinib and is sensitive to ceritinib., Lung Cancer

TTD: Ceritinib
- Version: 2020.06.01
Alternate Names:

D04LVK TTD Drug ID

Drug Info:

Publications:
TALC: LDK378
- Version: 12-May-2016
Alternate Names:

LDK378 Primary Drug Name

LDK378 Drug Synonym

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL2403108
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL2403108
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
MyCancerGenomeClinicalTrial: 1032900-25-6
- Version: 30-February-2014
Alternate Names:

Drug Info:

Publications:
OncoKB: Ceritinib
- Version: 23-July-2020
Alternate Names:

Drug Info:

Publications:
FDA: Ceritinib
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:
COSMIC: Ceritinib
- Version: 4-Sep-2020
Alternate Names:

Drug Info:

Publications:

Indication/Tumor Type	Advanced Solid Tumor
Response Type	resistant
Approval Status	Preclinical

Notes	Specifically targets ALK translocations
Reported Cancer Type	Lung
combination therapy	Saracatinib + Ceritinib

Indication/Tumor Type	anaplastic large cell lymphoma
Response Type	resistant
Approval Status	Preclinical

Indication/Tumor Type	non-small cell lung carcinoma
Response Type	sensitive
Approval Status	Phase II

combination therapy	Ceritinib + Selumetinib
Indication/Tumor Type	non-small cell lung carcinoma
Response Type	sensitive

antagonist (inhibitory)
inhibitor (inhibitory)

LDK378	Drug Trade Name
LDK378	Drug Development Name

CERITINIB Drug Record

CERITINIB chembl:CHEMBL2403108 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

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

PMIDs: 26775591 25173427 24675041 27780853 25228534 27009859 27432227 26698910

Sources: JAX-CKB

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

Interaction Info: Notes Specifically targets ALK translocations Reported Cancer Type Lung combination therapy Saracatinib + Ceritinib

Sources: TALC MyCancerGenome JAX-CKB ChemblInteractions DoCM COSMIC CIViC CancerCommons MyCancerGenomeClinicalTrial PharmGKB TTD FDA OncoKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type anaplastic large cell lymphoma Response Type resistant Approval Status Preclinical

PMIDs: 27009859 25749034 25421750

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 23837797

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type non-small cell lung carcinoma Response Type sensitive Approval Status Phase II

PMIDs: 26372962 28520527

Sources: JAX-CKB CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 23837797

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Ceritinib + Selumetinib Indication/Tumor Type non-small cell lung carcinoma Response Type sensitive

PMIDs: 25394791

Sources: JAX-CKB

Interaction Types & Directionality: n/a

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

PMIDs: 25394791

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 23837797

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26870817

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23837797

Sources: DTC

MyCancerGenome: CERITINIB

Alternate Names: ZYKADIA Trade Name

Drug Info: Drug Class Kinase Inhibitor FDA Approval Non-small cell lung cancer (with ALK fusion)

Publications:

CancerCommons: LDK378

Alternate Names: LDK378 Drug Trade Name LDK378 Drug Development Name

Drug Info: Drug Class ALK Inhibitor Source Reported Drug Name(s) LDK378 Pharmaceutical Developer Novartis

Publications:

MyCancerGenome: LDK378

Alternate Names: LDK378 Development Name

Drug Info: Drug Class Kinase Inhibitors

Publications:

DTC: CERITINIB

Alternate Names: CHEMBL2403108 ChEMBL Drug ID

Drug Info:

Publications: Chen J et al., 2013, LDK378: a promising anaplastic lymphoma kinase (ALK) inhibitor., J Med Chem

DoCM: CERITINIB

Alternate Names:

Drug Info:

JAX-CKB: Ceritinib

Alternate Names:

Drug Info:

PharmGKB: ceritinib

Alternate Names:

Drug Info:

CIViC: CERITINIB

Alternate Names:

Drug Info:

TTD: Ceritinib

Alternate Names: D04LVK TTD Drug ID

Drug Info:

Publications:

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type resistant

Approval Status Preclinical

PMIDs:
26775591 25173427 24675041 27780853 25228534 27009859 27432227 26698910

Sources:
JAX-CKB

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Notes Specifically targets ALK translocations

Reported Cancer Type Lung

combination therapy Saracatinib + Ceritinib

Sources:
TALC MyCancerGenome JAX-CKB ChemblInteractions DoCM COSMIC CIViC CancerCommons MyCancerGenomeClinicalTrial PharmGKB TTD FDA OncoKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type anaplastic large cell lymphoma

Response Type resistant

Approval Status Preclinical

PMIDs:
27009859 25749034 25421750

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
23837797

Sources:
DTC

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

Approval Status Phase II

PMIDs:
26372962 28520527

Sources:
JAX-CKB CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
23837797

Sources:
DTC

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Ceritinib + Selumetinib

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

PMIDs:
25394791

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type resistant

Approval Status Preclinical

PMIDs:
25394791

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
23837797

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
26870817

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
23837797

Sources:
DTC

Alternate Names:

ZYKADIA Trade Name

Drug Info:

Drug Class Kinase Inhibitor

FDA Approval Non-small cell lung cancer (with ALK fusion)

Alternate Names:

LDK378 Drug Trade Name

LDK378 Drug Development Name

Drug Info:

Drug Class ALK Inhibitor

Source Reported Drug Name(s) LDK378

Pharmaceutical Developer Novartis

Alternate Names:

LDK378 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Alternate Names:

CHEMBL2403108 ChEMBL Drug ID

Publications:

Chen J et al., 2013, LDK378: a promising anaplastic lymphoma kinase (ALK) inhibitor., J Med Chem

Alternate Names:

D04LVK TTD Drug ID

Alternate Names:

LDK378 Primary Drug Name

LDK378 Drug Synonym