The only once-daily RET inhibitor1

Stomach Patients should take GAVRETO on an empty stomach (no food intake for at least 2 hours before and at least 1 hour after taking GAVRETO).

Continue treatment until disease progression or until unacceptable toxicity.

If a dose of GAVRETO is missed, it can be taken as soon as possible on the same day. Resume the regular daily dose schedule for GAVRETO the next day.

Advise patients not to take an additional dose if vomiting occurs after taking GAVRETO but to continue with the next dose as scheduled.

Select patients for treatment with GAVRETO based on the presence of a RET gene fusion or RET gene mutation.

Recommended dosage reductions and modifications for adverse reactions

GAVRETO is available in 100-mg capsules, giving you the opportunity to modify dosage based on individual patient needs

Adverse Reactions Severity* Dosage Modification
ILD/Pneumonitis Grade 1 or 2 Withhold GAVRETO until resolution.
Resume by reducing the dose (see dose reduction table).
Permanently discontinue GAVRETO for recurrent ILD/pneumonitis.
Grade 3 or 4 Permanently discontinue for confirmed ILD/pneumonitis.
Hypertension Grade 3 Withhold GAVRETO for Grade 3 hypertension that persists despite optimal antihypertensive therapy. Resume at a reduced dose when hypertension is controlled.
Grade 4 Discontinue GAVRETO.
Hepatotoxicity Grade 3 or Grade 4 Withhold GAVRETO and monitor AST/ALT once weekly until resolution to Grade 1 or baseline.
Resume at reduced dose.
If hepatotoxicity recurs at Grade 3 or higher, discontinue GAVRETO.
Hemorrhagic Events Grade 3 or Grade 4 Withhold GAVRETO until recovery to baseline or Grade 0 or 1.
Discontinue GAVRETO for severe or life-threatening hemorrhagic events.
Other Adverse Reactions Grade 3 or 4 Withhold GAVRETO until improvement to ≤ Grade 2.
Resume at reduced dose.
Permanently discontinue for recurrent Grade 4 adverse reactions.
* Adverse reactions graded by the National Cancer Institute Common Terminology Criteria for Adverse Events (NCI-CTCAE) version 4.03.
Dose Reduction Recommended Dosage
First 300 mg once daily
Second 200 mg once daily
Final 100 mg once daily

Permanently discontinue GAVRETO in patients who are unable to tolerate 100 mg taken orally once daily.

Recommended Dosage Modifications for GAVRETO for Coadministration with Combined P-gp and Strong CYP3A Inhibitors

Current GAVRETO Dosage Recommended GAVRETO Dosage
400 mg orally
once daily
200 mg orally once daily
300 mg orally
once daily
200 mg orally once daily
200 mg orally
once daily
100 mg orally once daily

Avoid coadministration of GAVRETO with known combined P-gp and strong CYP3A inhibitors. If coadministration with a combined P-gp and strong CYP3A inhibitor cannot be avoided, reduce the current dose of GAVRETO as recommended in the table directly above. After the inhibitor has been discontinued for 3 to 5 elimination half-lives, resume GAVRETO at the dose taken prior to initiating the combined P-gp and strong CYP3A inhibitor.

Avoid coadministration of GAVRETO with strong CYP3A inducers. If coadministration with a strong CYP3A inducer cannot be avoided, increase the starting dose of GAVRETO to double the current GAVRETO dosage starting on Day 7 of coadministration of GAVRETO with the strong CYP3A inducer. After the inducer has been discontinued for at least 14 days, resume GAVRETO at the dose taken prior to initiating the strong CYP3A inducer.

ILD=interstitial lung disease; P-gp=P-glycoprotein.