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| Trade names | Krazati |
| Other names | MRTX-849 |
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| Routes of administration |
By mouth |
| Drug class | Antineoplastic agents |
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| Identifiers | |
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| CAS Number | |
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| KEGG | |
| ECHA InfoCard | 100.329.928 |
| Chemical and physical data | |
| Formula | C32H35ClFN7O2 |
| Molar mass | 604.13 g·mol−1 |
| 3D model (JSmol) | |
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Adagrasib, sold under the brand name Krazati, is an anticancer medication used to treat non-small cell lung cancer. Adagrasib is an inhibitor of the RAS GTPase family. It is taken by mouth. It is being developed by Mirati Therapeutics.
The most common adverse reactions include diarrhea, nausea, fatigue, vomiting, musculoskeletal pain, hepatotoxicity, renal impairment, dyspnea, edema, decreased appetite, cough, pneumonia, dizziness, constipation, abdominal pain, and QTc interval prolongation. The most common laboratory abnormalities include decreased lymphocytes, increased aspartate aminotransferase, decreased sodium, decreased hemoglobin, increased creatinine, decreased albumin, increased alanine aminotransferase, increased lipase, decreased platelets, decreased magnesium, and decreased potassium.
It was approved for medical use in the United States in December 2022.
Medical uses
Adagrasib is indicated for the treatment of adults with KRAS G12C-mutated locally advanced or metastatic non-small cell lung cancer (NSCLC), as determined by an FDA approved test, who have received at least one prior systemic therapy.
History
Approval by the US Food and Drug Administration (FDA) was based on KRYSTAL-1, a multicenter, single-arm, open-label clinical trial (NCT03785249) which included participants with locally advanced or metastatic non-small cell lung cancer with KRAS G12C mutations. Efficacy was evaluated in 112 participants whose disease has progressed on or after platinum-based chemotherapy and an immune checkpoint inhibitor, given either concurrently or sequentially.
The FDA granted the application for adagrasib fast-track, breakthrough therapy, and orphan drug designations.
Research
It is undergoing clinical trials.
External links
- "Adagrasib". Drug Information Portal. U.S. National Library of Medicine.
- Clinical trial number NCT03785249 for "Phase 1/2 Study of MRTX849 in Patients With Cancer Having a KRAS G12C Mutation KRYSTAL-1" at ClinicalTrials.gov