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selpercatinib (Retevmo)
Indications:
- adults with metastatic RET fusion-positive non-small cell lung cancer (NSCLC) [1]
- patients >= 12 years with advanced or metastatic RET-mutant medullary thyroid cancer
Dosage:
- < 50 kg: 120 mg PO BID
- > 50 kg: 160 mg PO BUD
Capsule 80 mg
Monitor:
- serum ALT serum AST prior to initiating RETEVMO, every 2 weeks during 1st 3 months, then monthly
- electrocardiogram for QTc prolongation & serum TSH at baseline, then periodically
Adverse effects:
- laboratory abnormalities
- increased serum AST & serum ALT
- hyperglycemia, hypoalbuminemia, hypocalcemia, hyponatremia
- increased serum creatinine, increased serum alkaline phosphatase
- leukopenia,, thrombocytopenia
- hypercholesterolemia
- xerostomia, diarrhea, constipation, hypertension, fatigue, edema, rash
Drug interactions:
- antacids
- avoid strong & moderate CYP3A inhibitors & inducers
- avoid CYP2C8 & CYP3A substrates
Mechanism of action:
- tyrosine kinase inhibitor
- inhibits wild-type RET & multiple mutated RET isoforms
- inhibits VEGFR1 & VEGFR3
- imhibits FGFR1, FGFR2, & FGFR3
Interactions
drug adverse effects of tyrosine kinase inhibitor(s)
General
small inhibitory antineoplastic agent (ib drug)
tyrosine kinase inhibitor
Database Correlations
PUBCHEM cid=134436906
References
- Larkin HD
Selpercatinib Receives Regular Approval for Non-Small Cell Lung Cancer.
JAMA. 2022;328(17):1679. Nov 1
PMID: 36318150
https://jamanetwork.com/journals/jama/fullarticle/2797894
- Highlights of prescribing information
RETEVMO (selpercatinib) capsules, for oral use
https://uspl.lilly.com/retevmo/retevmo.html#pi