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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Mitogen-activated protein kinase (MEK) inhibitors
cobimetinib
L01EE02
Adult Dosing
- 60 mg orally once daily for 21 consecutive days followed by 7 days off treatment (28-day cycle)
- Continue treatment until disease progression or unacceptable toxicity
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, in combination with vemurafenib
Mechanism of Action
- Reversible inhibitor of MEK1 and MEK2 kinases
- Prevents downstream MAPK/ERK pathway signaling in BRAF-mutated cancers, reducing cellular proliferation
Contraindications
- Known hypersensitivity to cobimetinib or any of its excipients
Adverse Reactions
- Diarrhea
- Photosensitivity reaction
- Nausea
- Pyrexia
- Vomiting
- Elevated creatine phosphokinase (CPK)
- Elevated ALT and AST
- Anemia
- Rash
- Serous retinopathy
Drug Interactions
- Strong or moderate CYP3A inhibitors may increase cobimetinib exposure and toxicity
- Strong or moderate CYP3A inducers may decrease cobimetinib exposure and reduce efficacy
- QT interval-prolonging drugs may increase the risk of QT prolongation when used with the cobimetinib/vemurafenib combination
Curated Content: Needs Vetting Before Put to Clinical Use