Last reviewed 2026-04-20 · How we verify

Krazati (ADAGRASIB)

Krazati works by binding to and inhibiting the GTPase activity of the KRAS G12C protein, preventing it from sending signals that promote cancer cell growth.

Krazati (ADAGRASIB) is a small molecule therapy originally developed by Mirati Therapeutics, Inc. and currently owned by Bristol. It targets the GTPase KRas, a protein involved in cell signaling, and is specifically approved for treating KRAS G12C-mutated locally advanced or metastatic non-small cell lung cancer. Krazati was FDA-approved in 2022 and has a half-life of 23 hours. It is a patented, proprietary medication with no generic manufacturers available.

At a glance

Mechanism of action

Adagrasib is an irreversible inhibitor of KRAS G12C that covalently binds to the mutant cysteine in KRAS G12C and locks the mutant KRAS protein in its inactive state that prevents downstream signaling without affecting wild-type KRAS protein. Adagrasib inhibits tumor cell growth and viability in cells harboring KRAS G12C mutations and results in tumor regression in KRAS G12C-mutated tumor xenograft models with minimal off-target activity.

Approved indications

• KRAS G12C-mutated locally advanced or metastatic non-small cell lung cancer

Common side effects

• Pneumonia
• Dyspnea
• Renal impairment
• Sepsis
• Hypoxia
• Pleural effusion
• Respiratory failure
• Anemia
• Cardiac failure
• Hyponatremia
• Hypotension
• Muscular weakness

Key clinical trials

• Trial of Two Adagrasib Dosing Regimens in NSCLC With KRAS G12C Mutation (KRYSTAL 21) (PHASE2)
• Immunotherapy Biomarkers to Predict First-line PD(L)1-based Immunotherapy Response and Selection of Second-line Treatment in Stage IIIB-IV Non-small Cell Lung Cancer, IMMUNO-BIOMAP Trial (PHASE2)
• Phase 2 Trial of Adagrasib Monotherapy and in Combination With Pembrolizumab and a Phase 3 Trial of Adagrasib in Combination in Patients With a KRAS G12C Mutation KRYSTAL-7 (PHASE2,PHASE3)
• A Study of Adagrasib Plus Pembrolizumab Plus Chemotherapy vs. Placebo Plus Pembrolizumab Plus Chemotherapy in Participants With Previously Untreated Non-squamous Non-small Cell Lung Cancer With KRAS G12C Mutation (KRYSTAL-4) (PHASE3)
• A Multicenter Phase 1b/2 Study of Adagrasib, Cetuximab, and Cemiplimab for Metastatic Colorectal Cancer Harboring KRAS G12C Mutations (PHASE1,PHASE2)
• Genetic Testing in Guiding Treatment for Patients With Brain Metastases (PHASE2)
• Phase I Trial of Adagrasib (MRTX849) in Combination With Cetuximab and Irinotecan in Patients With Colorectal Cancer (PHASE1)
• ASCEND-CRC: Profiling and Targeting Dynamic Tumor Resistance in Patients With Metastatic Colorectal Cancer (EARLY_PHASE1)

Patents

Primary sources

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