• Alias: AB1010
    • Selectively inhibits both the wild-type and mutated forms of KIT, PDGFR, and FGFR3
    • Currently under investigation in phase 3 clinical trials for MM, GIST, KIT–positive melanoma, and colorectal and pancreatic cancers
    • Recommended phase 3 dose: 12 mg/kg PO daily in two divided doses
    • Half-life: â™24 hours
    • Metabolism: Affected by the isoenzymes of CYP3A4, CYP2D6, and CYP2C9
    • Common side effects: Asthenia, peripheral edema, rash (pruritus), muscle spasms, abdominal pain, liver dysfunction, nausea/vomiting, diarrhea, hyponatremia, renal insufficiency
    (Soria et al., 2009)
    Other topics in Targeted and Immunotherapy Agents