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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › OTHER ANTINEOPLASTIC AGENTS › Other antineoplastic agents
adagrasib
L01XX77
Adult Dosing
- 600 mg orally twice daily with or without food
- Continue until disease progression or unacceptable toxicity
Pediatric Dosing
- Safety and efficacy not established in pediatric patients
Indications
- Non-small cell lung cancer (NSCLC) with KRAS G12C mutation, previously treated with at least one systemic therapy
- Colorectal cancer (CRC) with KRAS G12C mutation, previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy
Mechanism of Action
- Covalent and irreversible inhibitor of the KRAS G12C protein
- Locks KRAS G12C in its inactive GDP-bound state, preventing downstream signaling and cell proliferation
Contraindications
- Severe hypersensitivity to adagrasib or any of its excipients
Adverse Reactions
- Nausea and diarrhea
- Vomiting and fatigue
- Musculoskeletal pain
- Hepatotoxicity (elevated ALT/AST)
- QT interval prolongation
- Interstitial lung disease (ILD) / pneumonitis
Drug Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole): increase adagrasib exposure; avoid concurrent use
- Strong or moderate CYP3A4 inducers (e.g., rifampin): decrease adagrasib efficacy; avoid concurrent use
- CYP3A4 substrates: adagrasib may alter exposure of sensitive substrates
- QT-prolonging drugs: concurrent use increases risk of Torsades de Pointes
Curated Content: Needs Vetting Before Put to Clinical Use