capmatinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| tyrosine kinase inhibitors | 5392 | 1029712-80-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.80 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 20, 2022 | EMA | NOVARTIS EUROPHARM LIMITED | |
| May 6, 2020 | FDA | NOVARTIS PHARM | |
| June 29, 2020 | PMDA | Novartis Pharma K.K. |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Malignant neoplasm progression | 175.55 | 48.89 | 56 | 676 | 82065 | 63406225 |
| Oedema peripheral | 94.59 | 48.89 | 45 | 687 | 189466 | 63298824 |
| Death | 80.79 | 48.89 | 51 | 681 | 374330 | 63113960 |
| Non-small cell lung cancer | 56.16 | 48.89 | 12 | 720 | 3583 | 63484707 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Oedema peripheral | 176.20 | 41.97 | 68 | 528 | 119744 | 34836591 |
| Malignant neoplasm progression | 125.25 | 41.97 | 49 | 547 | 87997 | 34868338 |
| Death | 75.52 | 41.97 | 58 | 538 | 397991 | 34558344 |
| Oedema | 66.50 | 41.97 | 26 | 570 | 45715 | 34910620 |
| Non-small cell lung cancer | 60.98 | 41.97 | 14 | 582 | 3926 | 34952409 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Malignant neoplasm progression | 197.55 | 40.04 | 70 | 883 | 135920 | 79607515 |
| Oedema peripheral | 133.44 | 40.04 | 63 | 890 | 252225 | 79491210 |
| Non-small cell lung cancer | 103.03 | 40.04 | 22 | 931 | 6338 | 79737097 |
| Death | 74.76 | 40.04 | 58 | 895 | 566456 | 79176979 |
| Oedema | 45.40 | 40.04 | 24 | 929 | 119556 | 79623879 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| 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|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| D10696 | KEGG_DRUG |
| TY34L4F9OZ | UNII |
| 1865733-40-9 | SECONDARY_CAS_RN |
| C4053698 | UMLSCUI |
| CHEMBL3188267 | ChEMBL_ID |
| 25145656 | PUBCHEM_CID |
| DB11791 | DRUGBANK_ID |
| CHEMBL3989937 | ChEMBL_ID |
| 7904 | IUPHAR_LIGAND_ID |
| 018358 | NDDF |
| 018359 | NDDF |
| 874907006 | SNOMEDCT_US |
| 876837000 | SNOMEDCT_US |
| 4039388 | VANDF |
| 2362165 | RXNORM |
| 334138 | MMSL |
| 38424 | MMSL |
| d09556 | MMSL |
| C000613976 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9948 | INN_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| TABRECTA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0709 | TABLET, FILM COATED | 150 mg | ORAL | NDA | 30 sections |
| TABRECTA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0709 | TABLET, FILM COATED | 150 mg | ORAL | NDA | 30 sections |
| TABRECTA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0709 | TABLET, FILM COATED | 150 mg | ORAL | NDA | 30 sections |
| TABRECTA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0716 | TABLET, FILM COATED | 200 mg | ORAL | NDA | 30 sections |
| TABRECTA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0716 | TABLET, FILM COATED | 200 mg | ORAL | NDA | 30 sections |
| TABRECTA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0716 | TABLET, FILM COATED | 200 mg | ORAL | NDA | 30 sections |