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.

Adult:

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.

Children:

Not established.

Warnings/Precautions:

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).

Pharmacologic Class:

Tyrosine kinase inhibitor.

Interactions:

See Adults. Potentiated by strong or moderate CYP3A inhibitors (eg, itraconazole, fluconazole). Antagonized by strong or moderate CYP3A inducers (eg, rifampin, efavirenz).

Adverse Reactions:

Edema, nausea, fatigue/asthenia, cognitive impairment, vomiting, decreased appetite, diarrhea, increased lacrimation, abdominal pain, rash, constipation, dizziness, hair color changes.

Generic Availability:

NO

How Supplied:

Tabs—30

Pricing for AYVAKIT

100mg tablet (Qty: 30)
Appx. price $32650
GoodRx