selpercatinib (Retevmo)

Indications

• adults with metastatic RET fusion-positive non-small cell lung cancer (NSCLC)
• 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 adverse effects of tyrosine kinase inhibitor(s)

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

More general terms

• small inhibitory antineoplastic agent (ib drug)
• tyrosine kinase inhibitor

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=134436906