• Aliases: STI-571, CGP-57148B, Glivec
    • Inhibitor of BCR-ABL as well as KIT and PDGFR
    • FDA approved for Ph+ ALL, KIT (CD117)+ GIST, Ph+ CML, mastocytosis, HES, MDS/MPD with PDGFR gene rearrangement
    • Recommended dose: 400 or 600 mg daily
    • Half-life: Parent drug â™18 hours
    • Metabolism: Major CYP3A4 substrate
    • Common side effects: Edema/fluid retention (periorbital edema), nausea/vomiting, diarrhea, myelosuppression, hemorrhage, musculoskeletal pain (arthralgia), fatigue, rash (pruritus), muscle cramps, liver dysfunction (transaminitis, increased bilirubin)
    • Clinical pearls: Monitor thyroid function tests; while treating patients, hypothyroidism may occur.
    Other topics in Targeted and Immunotherapy Agents