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MRTX849
MRTX849 is a small-molecule inhibitor that selectively targets KRAS G12C mutations, blocking oncogenic signaling in cancer cells.
MRTX849 is a small-molecule inhibitor that selectively targets KRAS G12C mutations, blocking oncogenic signaling in cancer cells. Used for Non-small cell lung cancer with KRAS G12C mutation, Colorectal cancer with KRAS G12C mutation, Pancreatic cancer with KRAS G12C mutation.
At a glance
| Generic name | MRTX849 |
|---|---|
| Also known as | adagrasib, Adagrasib, KRAZATI, KRAS G12C, adagrasib (KRAZATI) |
| Sponsor | Mirati Therapeutics Inc. |
| Drug class | KRAS G12C inhibitor |
| Target | KRAS G12C |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
MRTX849 binds covalently to the mutant KRAS G12C protein in its inactive GDP-bound state, preventing its activation and downstream signaling through the MAPK and PI3K pathways. This mechanism is selective for the G12C mutation, which occurs in approximately 10-15% of non-small cell lung cancers and other solid tumors. By locking KRAS in its inactive state, the drug inhibits tumor cell proliferation and survival.
Approved indications
- Non-small cell lung cancer with KRAS G12C mutation
- Colorectal cancer with KRAS G12C mutation
- Pancreatic cancer with KRAS G12C mutation
Common side effects
- Diarrhea
- Nausea
- Fatigue
- Vomiting
- Abdominal pain
- Rash
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)
- 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)
- A Phase 1 Study of MRTX0902 in Solid Tumors With Mutations in the KRAS MAPK Pathway (PHASE1)
- A Study of BMS-986488 as Monotherapy and Combination Therapy in Participants With Advanced Malignant Tumors (PHASE1)
- Phase Ib Trial of the KRAS G12C Inhibitor Adagrasib (MRTX849) in Combination With the PARP Inhibitor Olaparib in Patients With KRAS G12C Mutated Advanced Solid Tumors, With a Focus on Gynecological, Breast, Pancreatic and KEAP1 Mutated Non-small Cell Lung Cancers (PHASE1)
- Phase 1/2 Study of MRTX849 in Patients With Cancer Having a KRAS G12C Mutation KRYSTAL-1 (PHASE1, PHASE2)
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 |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- MRTX849 CI brief — competitive landscape report
- MRTX849 updates RSS · CI watch RSS
- Mirati Therapeutics Inc. portfolio CI