Colorectal and other GI cancers:
Indications for AYVAKIT:
Treatment of adults with unresectable or metastatic gastrointestinal stromal tumor (GIST) harboring a platelet-derived growth factor receptor alpha (PDGFRA) exon 18 mutation, including PDGFRA D842V mutations.
Give on an empty stomach (at least 1hr before and 2hrs after a meal). 300mg once daily; continue until disease progression or unacceptable toxicity. Avoid concomitant use with strong or moderate CYP3A inhibitors; if use with moderate CYP3A inhibitor is unavoidable, reduce dose to 100mg once daily. Dose modifications: see full labeling.
Risk of intracranial hemorrhage, CNS effects (eg, cognitive impairment, dizziness, sleep disorders, others); if occurs, withhold dose and then resume at reduced (or at same) dose upon resolution, or permanently discontinue based on severity. Severe renal impairment (CrCl 15–29mL/min) or ESRD (CrCl <15mL/min). Severe hepatic impairment. Embryo-fetal toxicity. Advise females and males of reproductive potential to use effective contraception during and for 6 weeks after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 2 weeks after the last dose).
Tyrosine kinase inhibitor.
See Adults. Potentiated by strong or moderate CYP3A inhibitors (eg, itraconazole, fluconazole). Antagonized by strong or moderate CYP3A inducers (eg, rifampin, efavirenz).
Edema, nausea, fatigue/asthenia, cognitive impairment, vomiting, decreased appetite, diarrhea, increased lacrimation, abdominal pain, rash, constipation, dizziness, hair color changes.