repotrectinib (Augtyro)

Indications

• treatment of adult patients with locally advanced or metastatic ROS1-positive non-small cell lung cancer

Dosage

• 160 mg PO QD for 14 days
  • increase to 160 mg PO BID, with or without food.

Capsules: 40 mg

Adverse effects

• > 20%
  • dizziness, dysgeusia, peripheral neuropathy, constipation, dyspnea, ataxia, fatigue, cognitive disorders, muscle weakness

Drug interactions

• strong & moderate CYP3A inhibitors: avoid concurrent use
• P-glucoprotein inhibitors: avoid concurrent use
• strong & moderate CYP3A inducers: avoid concurrent use
• hormonal contraceptives: avoid concurrent use

Mechanism of action

• inhibits ROS1 & tropomyosin receptor tyrosine kinases TRKA, TRKB, & TRKC

More general terms

• small inhibitory antineoplastic agent (ib drug)

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=135565923