capmatinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5392 1029712-80-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • capmatinib
  • capmatinib hydrochloride
  • capmatinib hydrochloride hydrate
  • tabrecta
  • NVP-INC280-NX
  • INC280
  • INCB-028060
Capmatinib is a kinase inhibitor indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have a mutation that leads to mesenchymal-epithelial transition (MET) exon 14 skipping as detected by an FDA-approved test.
  • Molecular weight: 412.43
  • Formula: C23H17FN6O
  • CLOGP: 2.27
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 1
  • TPSA: 85.07
  • ALOGS: -4.89
  • ROTB: 4

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.80 g O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
May 6, 2020 FDA NOVARTIS PHARM
June 29, 2020 PMDA Novartis Pharma K.K.

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Malignant neoplasm progression 85.52 54.49 27 302 68097 50536698
Oedema peripheral 56.73 54.49 25 304 157936 50446859

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Oedema peripheral 97.67 61.93 36 239 103521 29470731
Malignant neoplasm progression 85.62 61.93 30 245 73829 29500423

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Malignant neoplasm progression 100.64 44.66 35 406 112836 64385455
Oedema peripheral 69.81 44.66 32 409 210285 64288006
Death 59.57 44.66 38 403 482667 64015624

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EX17 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Other protein kinase inhibitors
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000182138 Cytochrome P450 1A2 Inhibitors
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000190113 Breast Cancer Resistance Protein Inhibitors
FDA MoA N0000191423 Multidrug and Toxin Extrusion Transporter 1 Inhibitors
FDA MoA N0000193929 Mesenchymal Epithelial Transition Inhibitors
FDA MoA N0000193932 Multidrug and Toxin Extrusion Transporter 2 K Inhibitors

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Metastatic non-small cell lung cancer indication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 150MG BASE TABRECTA NOVARTIS PHARM N213591 May 6, 2020 RX TABLET ORAL 8901123 May 20, 2029 USE FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH A MESENCHYMAL-EPITHELIAL TRANSITION (MET) EXON 14 SKIPPING MUTATION
EQ 200MG BASE TABRECTA NOVARTIS PHARM N213591 May 6, 2020 RX TABLET ORAL 8901123 May 20, 2029 USE FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH A MESENCHYMAL-EPITHELIAL TRANSITION (MET) EXON 14 SKIPPING MUTATION

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 150MG BASE TABRECTA NOVARTIS PHARM N213591 May 6, 2020 RX TABLET ORAL May 6, 2025 NEW CHEMICAL ENTITY
EQ 200MG BASE TABRECTA NOVARTIS PHARM N213591 May 6, 2020 RX TABLET ORAL May 6, 2025 NEW CHEMICAL ENTITY
EQ 150MG BASE TABRECTA NOVARTIS PHARM N213591 May 6, 2020 RX TABLET ORAL May 6, 2027 INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE A MUTATION THAT LEADS TO MESENCHYMAL-EPITHELIAL TRANSITION (MET) EXON 14 SKIPPING AS DETECTED BY AN FDA-APPROVED TEST
EQ 200MG BASE TABRECTA NOVARTIS PHARM N213591 May 6, 2020 RX TABLET ORAL May 6, 2027 INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE A MUTATION THAT LEADS TO MESENCHYMAL-EPITHELIAL TRANSITION (MET) EXON 14 SKIPPING AS DETECTED BY AN FDA-APPROVED TEST

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Hepatocyte growth factor receptor Kinase INHIBITOR IC50 9.88 SCIENTIFIC LITERATURE DRUG LABEL
Cyclin-dependent kinase-like 5 Kinase Kd 5.69 CHEMBL

External reference:

IDSource
D10696 KEGG_DRUG
TY34L4F9OZ UNII
C4053698 UMLSCUI
CHEMBL3188267 ChEMBL_ID
25145656 PUBCHEM_CID
DB11791 DRUGBANK_ID
CHEMBL3989937 ChEMBL_ID
7904 IUPHAR_LIGAND_ID
2362165 RXNORM
334138 MMSL
38424 MMSL
d09556 MMSL
874907006 SNOMEDCT_US
876837000 SNOMEDCT_US
4039388 VANDF
018358 NDDF
018359 NDDF
C000613976 MESH_SUPPLEMENTAL_RECORD_UI
9948 INN_ID
1865733-40-9 SECONDARY_CAS_RN

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
TABRECTA HUMAN PRESCRIPTION DRUG LABEL 1 0078-0709 TABLET, FILM COATED 150 mg ORAL NDA 29 sections
TABRECTA HUMAN PRESCRIPTION DRUG LABEL 1 0078-0716 TABLET, FILM COATED 200 mg ORAL NDA 29 sections