Cometriq(cabozantinib)
Cabometyx, Cometriq (cabozantinib) is a small molecule pharmaceutical. Cabozantinib was first approved as Cometriq on 2012-11-29. It is used to treat renal cell carcinoma in the USA. It has been approved in Europe to treat hepatocellular carcinoma, renal cell carcinoma, and thyroid neoplasms. The pharmaceutical is active against hepatocyte growth factor receptor and vascular endothelial growth factor receptor 2. In addition, it is known to target proto-oncogene tyrosine-protein kinase receptor Ret.
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Commercial
Therapeutic Areas
Trade Name
FDA
EMA
Cabometyx, Cometriq
Drug Products
FDA
EMA
Indications
FDA
EMA
Indication | Ontology | MeSH | ICD-10 |
|---|---|---|---|
| renal cell carcinoma | EFO_0000376 | D002292 | — |
Agency Specific
FDA
EMA
Expiration | Code | ||
|---|---|---|---|
CABOZANTINIB S-MALATE, CABOMETYX, EXELIXIS INC | |||
| 2028-09-17 | ODE-375 | ||
| 2026-01-14 | ODE-227 | ||
| 2024-09-17 | I-873 | ||
| 2024-01-22 | I-854 | ||
Patent Expiration
Patent | Expires | Flag | FDA Information |
|---|---|---|---|
| Cabozantinib S-Malate, Cabometyx, Exelixis Inc | |||
| 9724342 | 2033-07-09 | DP | |
| 11298349 | 2032-02-10 | DP | |
| 10034873 | 2031-07-18 | U-2488 | |
| 10039757 | 2031-07-18 | U-1480 | |
| 8877776 | 2030-10-08 | DS, DP | U-1617, U-3225 |
| 11091439 | 2030-01-15 | DP | |
| 11091440 | 2030-01-15 | DP | |
| 11098015 | 2030-01-15 | U-1220, U-1480, U-1617, U-2488, U-3225 | |
| 7579473 | 2026-08-14 | DS, DP | |
| 8497284 | 2024-09-24 | U-1220, U-1480, U-2488 | |
| Cabozantinib S-Malate, Cometriq, Exelixis | |||
| 9717720 | 2032-02-10 | DP | |
HCPCS
No data
Clinical
Clinical Trials
268 clinical trials
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Indications Phases 4
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Carcinoma | D002277 | — | C80.0 | 22 | 67 | 11 | 1 | 20 | 115 |
| Neoplasms | D009369 | — | C80 | 17 | 24 | 3 | 1 | — | 43 |
| Hepatocellular carcinoma | D006528 | — | C22.0 | 6 | 20 | 2 | 1 | 2 | 28 |
| Liver neoplasms | D008113 | EFO_1001513 | C22.0 | 5 | 17 | 2 | 1 | 2 | 24 |
| Thyroid neoplasms | D013964 | EFO_0003841 | — | 5 | 9 | 5 | 1 | 3 | 22 |
| Thyroid diseases | D013959 | HP_0000820 | E00-E07 | 3 | 7 | 5 | 1 | 3 | 19 |
| Neuroendocrine carcinoma | D018278 | — | — | 2 | 4 | 2 | 1 | 1 | 10 |
| Papillary thyroid cancer | D000077273 | — | — | 1 | 3 | 2 | 1 | 1 | 8 |
Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Renal cell carcinoma | D002292 | EFO_0000376 | — | 19 | 38 | 8 | — | 23 | 84 |
| Prostatic neoplasms | D011471 | — | C61 | 7 | 14 | 3 | — | 1 | 24 |
| Non-small-cell lung carcinoma | D002289 | — | — | 8 | 14 | 1 | — | — | 20 |
| Kidney neoplasms | D007680 | EFO_0003865 | C64 | 2 | 9 | 2 | — | 5 | 18 |
| Adenocarcinoma | D000230 | — | — | 3 | 11 | 1 | — | — | 14 |
| Neuroendocrine tumors | D018358 | EFO_1001901 | D3A.8 | 2 | 11 | 1 | — | 1 | 14 |
| Lung neoplasms | D008175 | HP_0100526 | C34.90 | 4 | 11 | 1 | — | — | 14 |
| Castration-resistant prostatic neoplasms | D064129 | — | — | 4 | 6 | 2 | — | — | 11 |
| Osteosarcoma | D012516 | — | — | 2 | 6 | 1 | — | — | 8 |
| Urinary bladder neoplasms | D001749 | — | C67 | 1 | 5 | 1 | — | — | 7 |
Show 14 more
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Recurrence | D012008 | — | — | 5 | 13 | — | — | 1 | 18 |
| Sarcoma | D012509 | — | — | 4 | 10 | — | — | — | 13 |
| Neoplasm metastasis | D009362 | EFO_0009708 | — | 5 | 7 | — | — | — | 12 |
| Urologic neoplasms | D014571 | — | C64-C68 | 4 | 7 | — | — | — | 10 |
| Colorectal neoplasms | D015179 | — | — | 6 | 5 | — | — | 1 | 10 |
| Melanoma | D008545 | — | — | 4 | 6 | — | — | 1 | 10 |
| Breast neoplasms | D001943 | EFO_0003869 | C50 | 3 | 4 | — | — | — | 7 |
| Medullary carcinoma | D018276 | — | — | 3 | 3 | — | — | 1 | 7 |
| Squamous cell carcinoma | D002294 | — | — | 2 | 5 | — | — | — | 7 |
| Brain neoplasms | D001932 | EFO_0003833 | C71 | 1 | 5 | — | — | — | 6 |
Show 82 more
Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Leukemia | D007938 | — | C95 | 2 | — | — | — | 1 | 3 |
| Myeloid leukemia acute | D015470 | — | C92.0 | 2 | — | — | — | 1 | 3 |
| Myeloid leukemia | D007951 | — | C92 | 2 | — | — | — | 1 | 3 |
| Precursor cell lymphoblastic leukemia-lymphoma | D054198 | — | — | 1 | — | — | — | 1 | 2 |
| Lymphoid leukemia | D007945 | — | C91 | 1 | — | — | — | 1 | 2 |
| Lymphoma | D008223 | — | C85.9 | 2 | — | — | — | — | 2 |
| Infections | D007239 | EFO_0000544 | — | 2 | — | — | — | — | 2 |
| Hiv infections | D015658 | EFO_0000764 | B20 | 2 | — | — | — | — | 2 |
| Acquired immunodeficiency syndrome | D000163 | EFO_0000765 | B20 | 2 | — | — | — | — | 2 |
| Ovarian epithelial carcinoma | D000077216 | — | — | 2 | — | — | — | — | 2 |
Show 32 more
Indications Without Phase
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Acute disease | D000208 | — | — | — | — | — | — | 1 | 1 |
| Drug-related side effects and adverse reactions | D064420 | — | T88.7 | — | — | — | — | 1 | 1 |
| Chronic kidney failure | D007676 | EFO_0003884 | N18.9 | — | — | — | — | 1 | 1 |
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | Cabozantinib |
| INN | cabozantinib |
| Description | Cabozantinib is a dicarboxylic acid diamide that is N-phenyl-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide in which the hydrogen at position 4 on the phenyl ring is substituted by a (6,7-dimethoxyquinolin-4-yl)oxy group. A multi-tyrosine kinase inhibitor, used (as its malate salt) for the treatment of progressive, metastatic, medullary thyroid cancer. It has a role as a tyrosine kinase inhibitor and an antineoplastic agent. It is a member of quinolines, an organofluorine compound, an aromatic ether and a dicarboxylic acid diamide. |
| Classification | Small molecule |
| Drug class | tyrosine kinase inhibitors |
| Image (chem structure or protein) |  |
| Structure (InChI/SMILES or Protein Sequence) | COc1cc2nccc(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3)c2cc1OC |
Identifiers
| PDB | — |
| CAS-ID | 849217-68-1 |
| RxCUI | — |
| ChEMBL ID | CHEMBL2105717 |
| ChEBI ID | 72317 |
| PubChem CID | 25102847 |
| DrugBank | DB08875 |
| UNII ID | 1C39JW444G (ChemIDplus, GSRS) |
Target
Agency Approved
No data
Alternate
RET
RET
Organism
Homo sapiens
Gene name
RET
Gene synonyms
CDHF12, CDHR16, PTC, RET51
NCBI Gene ID
Protein name
proto-oncogene tyrosine-protein kinase receptor Ret
Protein synonyms
Cadherin family member 12, cadherin-related family member 16, Proto-oncogene c-Ret, rearranged during transfection, ret proto-oncogene (multiple endocrine neoplasia and medullary thyroid carcinoma 1, Hirschsprung disease), RET receptor tyrosine kinase
Uniprot ID
Mouse ortholog
Ret (19713)
proto-oncogene tyrosine-protein kinase receptor Ret (P35546)
Variants
No data
Financial
Estimated US medical usage
No data
Trends
PubMed Central
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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36,689 adverse events reported
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