Last reviewed · How we verify
Cotellic (cobimetinib)
Cotellic works by blocking the activity of two proteins, BRAF and MEK, which are involved in the growth and spread of cancer cells.
Cobimetinib (Cotellic), marketed by Roche, is approved for the treatment of unresectable or metastatic melanoma, competing in a crowded MEK inhibitor market. A key strength of Cotellic is its dual mechanism of action, inhibiting both BRAF and MEK, which may offer a more comprehensive approach to managing cancer cell growth and spread. The primary risk is the strong competition from other same-class drugs, such as trametinib, binimetinib, and selumetinib, all of which have later patent expiries, potentially eroding Cotellic's market share over time.
At a glance
| Generic name | cobimetinib |
|---|---|
| Sponsor | Roche |
| Drug class | Kinase Inhibitor |
| Target | Dual specificity mitogen-activated protein kinase kinase 1 |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2015 |
| Annual revenue | 200 |
Mechanism of action
Cobimetinib is reversible inhibitor of mitogen-activated protein kinase (MAPK)/extracellular signal regulated kinase (MEK1) and MEK2. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway, which promotes cellular proliferation. BRAF V600E and mutations result in constitutive activation of the BRAF pathway which includes MEK1 and MEK2. In mice implanted with tumor cell lines expressing BRAF V600E, cobimetinib inhibited tumor cell growth.Cobimetinib and vemurafenib target two different kinases in the RAS/RAF/MEK/ERK pathway. Compared to either drug alone, coadministration of cobimetinib and vemurafenib resulted in increased apoptosis in vitro and reduced tumor growth in mouse implantation models of tumor cell lines harboring BRAF V600E mutations. Cobimetinib also prevented vemurafenib-mediated growth enhancement of wild-type BRAF tumor cell line in an in vivo mouse implantation model.
Approved indications
- Unresectable or Metastatic Melanoma
- Histiocytic Neoplasms
Common side effects
- Diarrhea
- Photosensitivity reaction
- Nausea
- Pyrexia
- Vomiting
- Increased GGT
- Increased CPK
- Hypophosphatemia
- Increased ALT
- Lymphopenia
- Increased AST
- Increased alkaline phosphatase
Key clinical trials
- Canadian Profiling and Targeted Agent Utilization Trial (CAPTUR) (PHASE2)
- Testing the Combination of APG-1252 (Pelcitoclax) and Cobimetinib in Recurrent Ovarian and Endometrial Cancers (PHASE1)
- TAPUR: Testing the Use of Food and Drug Administration (FDA) Approved Drugs That Target a Specific Abnormality in a Tumor Gene in People With Advanced Stage Cancer (PHASE2)
- A Study Evaluating the Efficacy and Safety of Biomarker-Driven Therapies in Patients With Persistent or Recurrent Rare Epithelial Ovarian Tumors (PHASE2)
- A Study to Evaluate the Efficacy and Safety of Multiple Targeted Therapies as Treatments for Participants With Non-Small Cell Lung Cancer (NSCLC) (PHASE2,PHASE3)
- A Study of Multiple Therapies in Biomarker-selected Participants With Resectable Stages IB-III Non-small Cell Lung Cancer (NSCLC) (PHASE2)
- Comprehensive Analysis of Chemotherapy and Targeted Therapy Outcomes in Recurrent Malignant Gliomas
- Belvarafenib in Combination With Cobimetinib in Patients With Locally Advanced or Metastatic NRAS-Mutant Melanoma (PHASE2)
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
| SEC EDGAR | Revenue + earnings |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Cotellic CI brief — competitive landscape report
- Cotellic updates RSS · CI watch RSS
- Roche portfolio CI