Search
adagrasib (Krazati)
Indications:
- non-small cell lung carcinoma (NSCLC)
- locally advanced or metastatic NSCLC with KRAS G12C mutations
Dosage:
- 600 mg PO BID until disease progression or unacceptable toxicity
200 mg oral tablet
Laboratory:
- Agilent Resolution ctDx FIRST Assay (plasma)
- QIAGEN therascreen KRAS RGQ PCR kit (tissue)
* companion diagnostics for Krazati
* if no mutation is detected in a plasma specimen (Agilent), the tumor tissue should be tested (QIAGEN)
Adverse effects:
- common (>= 20%)
- diarrhea, nausea, fatigue, vomiting, musculoskeletal pain, hepatotoxicity, renal impairment, dyspnea, edema, decreased appetite, cough, pneumonia, dizziness, constipation, abdominal pain, QTc interval prolongation
- most common laboratory abnormalities (>= 25%)
- lymphopenia, anemia, thrombocytopenia
- hyponatremia, hypokalemia, hypomagnesemia, increased serum creatinine
- increased serum ALT & serum AST, decreased serum albumin, increased serum lipase
Mechanism of action:
- RAS GTPase family inhibitor
General
small inhibitory antineoplastic agent (ib drug)
Database Correlations
PUBCHEM cid=138611145
References
- Food and Drug Administration (FDA) December 12, 2022
FDA grants accelerated approval to adagrasib for KRAS G12C-mutated NSCLC.
https://www.fda.gov/drugs/resources-information-approved-drugs/fda-grants-accelerated-approval-adagrasib-kras-g12c-mutated-nsclc
- Janne PA, Riely GJ, Gadgeel SM et al
Adagrasib in Non-Small-Cell Lung Cancer Harboring a KRAS G12C Mutation
N Engl J Med 2022; 387:120-131
PMID: 35658005
https://www.nejm.org/doi/full/10.1056/nejmoa2204619
- HIGHLIGHTS OF PRESCRIBING INFORMATION
Krazati (adagrasib) tablets, for oral use
https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/216340s000lbl.pdf