Cotellic(cobimetinib)
Cotellic (cobimetinib) is a small molecule pharmaceutical. Cobimetinib was first approved as Cotellic on 2015-11-10. It is used to treat melanoma in the USA. It has been approved in Europe to treat melanoma. The pharmaceutical is active against dual specificity mitogen-activated protein kinase kinase 1 and dual specificity mitogen-activated protein kinase kinase 2. In addition, it is known to target dual specificity mitogen-activated protein kinase kinase 7.
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Commercial
Trade Name
FDA
EMA
Cotellic
Labels
FDA
EMA
Brand Name | Status | Last Update |
|---|---|---|
| cotellic | New Drug Application | 2024-11-18 |
Agency Specific
FDA
EMA
Expiration | Code | ||
|---|---|---|---|
COBIMETINIB FUMARATE, COTELLIC, GENENTECH INC | |||
| 2029-10-28 | ODE-416 | ||
| 2026-01-28 | PED | ||
| 2025-10-28 | I-902 | ||
| 2025-07-28 | M-278 | ||
HCPCS
No data
Clinical
Clinical Trials
121 clinical trials
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Indications Phases 4
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Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Melanoma | D008545 | — | — | 2 | 6 | 4 | — | 1 | 12 |
| Neoplasms | D009369 | — | C80 | 3 | 8 | 3 | — | — | 11 |
| Colorectal neoplasms | D015179 | — | — | 1 | 3 | 2 | — | — | 5 |
| Multiple myeloma | D009101 | — | C90.0 | 1 | 3 | 1 | — | — | 3 |
| Ovarian neoplasms | D010051 | EFO_0003893 | C56 | 1 | 2 | 1 | — | — | 3 |
| Non-small-cell lung carcinoma | D002289 | — | — | 1 | 3 | 2 | — | — | 3 |
| Adenocarcinoma | D000230 | — | — | 2 | 2 | 1 | — | — | 3 |
| Hematologic neoplasms | D019337 | — | — | — | 2 | 2 | — | — | 2 |
| Lung neoplasms | D008175 | — | C34.90 | — | 1 | 1 | — | — | 1 |
| Carcinoma | D002277 | — | C80.0 | — | 1 | 1 | — | — | 1 |
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Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Breast neoplasms | D001943 | EFO_0003869 | C50 | — | 2 | — | — | — | 2 |
| Non-hodgkin lymphoma | D008228 | — | C85.9 | — | 1 | — | — | — | 1 |
| Neoplasm metastasis | D009362 | EFO_0009708 | — | — | 1 | — | — | — | 1 |
| Unknown primary neoplasms | D009382 | — | — | — | 1 | — | — | — | 1 |
| Plasma cell neoplasms | D054219 | — | — | 1 | 1 | — | — | — | 1 |
| Esophageal neoplasms | D004938 | — | C15 | 1 | 1 | — | — | — | 1 |
| Pancreatic neoplasms | D010190 | EFO_0003860 | C25 | 1 | 1 | — | — | — | 1 |
| Triple negative breast neoplasms | D064726 | — | — | — | 1 | — | — | — | 1 |
Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Ovarian epithelial carcinoma | D000077216 | — | — | 1 | — | — | — | — | 1 |
| Leukemia | D007938 | — | C95 | 1 | — | — | — | — | 1 |
| Myeloid leukemia acute | D015470 | — | C92.0 | 1 | — | — | — | — | 1 |
| Myeloid leukemia | D007951 | — | C92 | 1 | — | — | — | — | 1 |
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | Cobimetinib |
| INN | cobimetinib |
| Description | Cobimetinib is a member of the class of N-acylazetidines obtained by selective formal condensation of the carboxy group of 3,4-difluoro-2-(2-fluoro-4-iodoanilino)benzoic acid with the secondary amino group from the azetidine ring of 3-[(2S)-piperidin-2-yl]azetidin-3-ol. An inhibitor of mitogen-activated protein kinase that is used (as its fumarate salt) in combination with vemurafenib for the treatment of patients with unresectable or metastatic melanoma. It has a role as an EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor and an antineoplastic agent. It is a member of piperidines, a N-acylazetidine, a tertiary alcohol, an aromatic amine, a secondary amino compound, a difluorobenzene and an organoiodine compound. It is a conjugate base of a cobimetinib(1+). |
| Classification | Small molecule |
| Drug class | tyrosine kinase inhibitors: tyrosine kinase inhibitors; MEK (MAPK kinase) inhibitors |
| Image (chem structure or protein) |  |
| Structure (InChI/SMILES or Protein Sequence) | O=C(c1ccc(F)c(F)c1Nc1ccc(I)cc1F)N1CC(O)([C@@H]2CCCCN2)C1 |
Identifiers
| PDB | — |
| CAS-ID | 934660-93-2 |
| RxCUI | — |
| ChEMBL ID | CHEMBL2146883 |
| ChEBI ID | — |
| PubChem CID | 16222096 |
| DrugBank | DB05239 |
| UNII ID | ER29L26N1X (ChemIDplus, GSRS) |
Target
Agency Approved
No data
Alternate
MAP2K7
MAP2K7
BRAF
BRAF
Organism
Homo sapiens
Gene name
MAP2K7
Gene synonyms
JNKK2, MEK7, MKK7, PRKMK7, SKK4
NCBI Gene ID
Protein name
dual specificity mitogen-activated protein kinase kinase 7
Protein synonyms
c-Jun N-terminal kinase kinase 2, JNK kinase 2, JNK-activating kinase 2, JNKK 2, MAP kinase kinase 7, MAPK/ERK kinase 7, MEK 7, SAPK kinase 4, SAPKK-4, SAPKK4, Stress-activated protein kinase kinase 4
Uniprot ID
Mouse ortholog
Map2k7 (26400)
dual specificity mitogen-activated protein kinase kinase 7 (Q8CE90)
Variants
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Financial
Estimated US medical usage
No data
Trends
PubMed Central
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Safety
Black-box Warning
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Adverse Events
Top Adverse Reactions
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3,981 adverse events reported
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