Source: FDA, National Drug Code (US) Revision Year: 2020
AYVAKIT is indicated for the treatment of adults with unresectable or metastatic GIST harboring a platelet-derived growth factor receptor alpha (PDGFRA) exon 18 mutation, including PDGFRA D842V mutations [see Dosage and Administration (2.1)].
Select patients for treatment with AYVAKIT based on the presence of a PDGFRA exon 18 mutation [see Clinical Studies (14.1)]. An FDA-approved test for the detection of exon 18 mutations is not currently available.
The recommended dosage of AYVAKIT is 300 mg orally once daily on an empty stomach, at least 1 hour before and 2 hours after a meal [see Clinical Pharmacology (12.3)]. Continue treatment until disease progression or unacceptable toxicity. Do not make up for a missed dose within 8 hours of the next scheduled dose.
Do not take an additional dose if vomiting occurs after AYVAKIT, but continue with the next scheduled dose.
The recommended dose reductions and dosage modifications for adverse reactions are provided in Table 1 and Table 2.
Table 1. Recommended Dose Reductions for AYVAKIT for Adverse Reactions:
| Dose Reduction | Recommended Dosage |
|---|---|
| First | 200 mg once daily |
| Second | 100 mg once daily |
* Permanently discontinue AYVAKIT in patients who are unable to tolerate a dose of 100 mg once daily.
Table 2. Recommended Dosage Modifications for AYVAKIT for Adverse Reactions:
| Adverse Reaction | Severity*] | Dosage Modification |
|---|---|---|
| Intracranial Hemorrhage [see Warnings and Precautions (5.1)] | Grade 1 or Grade 2 | First Occurrence: Withhold AYVAKIT until resolution. Resume at reduced dose. Subsequent Occurrence: Permanently discontinue. |
| Grade 3 or Grade 4 | Permanently discontinue AYVAKIT. | |
| Central Nervous System Effects [see Warnings and Precautions (5.2)] | Grade 1 | Continue AYVAKIT at same dose or withhold until improvement to baseline or resolution. Resume at same dose or reduced dose. |
| Grade 2 or Grade 3 | Withhold AYVAKIT until improvement to baseline, Grade 1, or resolution. Resume at same dose or reduced dose. | |
| Grade 4 | Permanently discontinue AYVAKIT. | |
| Other [see Adverse Reactions (6.1)] | Grade 3 or Grade 4 | Withhold AYVAKIT until improvement to less than or equal to Grade 2. Resume at same dose or reduced dose, as clinically appropriate. |
* Severity as defined by the National Cancer Institute Common Terminology Criteria for Adverse Events version 5.0
Avoid concomitant use of AYVAKIT with strong or moderate CYP3A inhibitors. If concomitant use with a moderate CYP3A inhibitor cannot be avoided, reduce the starting dose of AYVAKIT from 300 mg orally once daily to 100 mg orally once daily [see Drug Interactions (7.1)].
Store at 20°C to 25°C (68°F to 77°F); excursions are permitted from 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature].
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