Gavreto Dosage

Generic name: PRALSETINIB 100mg
Dosage form: capsule
Drug class: Multikinase inhibitors

Medically reviewed by Drugs.com. Last updated on Mar 31, 2024.

Patient Selection

Select patients for treatment with GAVRETO based on the presence of a RET gene fusion (NSCLC or thyroid cancer) [see Clinical Studies (14)].

Information on FDA-approved tests for RET gene fusion (NSCLC) is available at http://www.fda.gov/CompanionDiagnostics.

An FDA-approved test for the detection of RET gene fusion (thyroid cancer) is not currently available.

Recommended Dosage

The recommended dosage of GAVRETO is 400 mg orally once daily on an empty stomach (no food intake for at least 2 hours before and at least 1 hour after taking GAVRETO) [see Clinical Pharmacology (12.3)]. 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.

Do not take an additional dose if vomiting occurs after GAVRETO but continue with the next dose as scheduled.

Dosage Modifications for Adverse Reactions

The recommended dose reductions and dosage modifications for adverse reactions are provided in Table 1 and Table 2.

Table 1: Recommended Dose Reductions for GAVRETO for Adverse Reactions
Dose Reduction	Recommended Dosage
First	300 mg once daily
Second	200 mg once daily
Third	100 mg once daily

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

The recommended dosage modifications for adverse reactions are provided in Table 2.

Table 2: Recommended Dosage Modifications for GAVRETO for Adverse Reactions
Adverse Reaction	Severity*	Dosage Modification
* Adverse reactions graded by the National Cancer Institute Common Terminology Criteria for Adverse Events (NCI-CTCAE) version 4.03
ILD/Pneumonitis [see Warnings and Precautions (5.1)]	Grade 1 or 2	Withhold GAVRETO until resolution. Resume by reducing the dose as shown in Table 1.
	Grade 1 or 2	Permanently discontinue GAVRETO for recurrent ILD/pneumonitis.
	Grade 3 or 4	Permanently discontinue for confirmed ILD/pneumonitis.
Hypertension [see Warnings and Precautions (5.2)]	Grade 3	Withhold GAVRETO for Grade 3 hypertension that persists despite optimal antihypertensive therapy. Resume at a reduced dose when hypertension is controlled.
Hypertension [see Warnings and Precautions (5.2)]	Grade 4	Discontinue GAVRETO.
Hepatotoxicity [see Warnings and Precautions (5.3)]	Grade 3 or 4	Withhold GAVRETO and monitor AST/ALT once weekly until resolution to Grade 1 or baseline.
		Resume at reduced dose (Table 1).
		For recurrent events at Grade 3 or higher, discontinue GAVRETO.
Hemorrhagic Events [see Warnings and Precautions (5.4)]	Grade 3 or 4	Withhold GAVRETO until recovery to baseline or Grade 0 or 1.
Hemorrhagic Events [see Warnings and Precautions (5.4)]	Grade 3 or 4	Discontinue GAVRETO for severe or life-threatening hemorrhagic events.
Other Adverse Reactions [see Adverse Reactions (6.1)]	Grade 3 or 4	Withhold GAVRETO until improvement to ≤ Grade 2. Resume at reduced dose (Table 1).
Other Adverse Reactions [see Adverse Reactions (6.1)]	Grade 3 or 4	Permanently discontinue for recurrent Grade 4 adverse reactions.

Dose Modification for Use withCYP3A and/or P-glycoprotein (P-gp) Inhibitors

Avoid coadministration of GAVRETO with any of the following:

Strong CYP3A inhibitors
Moderate CYP3A inhibitors
P-gp inhibitors
Combined P-gp and strong CYP3A inhibitors
Combined P-gp and moderate CYP3A inhibitors

If coadministration with any of the above inhibitors cannot be avoided, reduce the current dose of GAVRETO as recommended in Table 3. After the inhibitor has been discontinued for 3 to 5 elimination half-lives, resume GAVRETO at the dose taken prior to initiating the inhibitor [see Drug Interactions (7.1), Clinical Pharmacology (12.3)].

Table 3: Recommended Dosage Modifications for GAVRETO for Coadministration with CYP3A and/or P-gp Inhibitors
Current GAVRETO Dosage	Recommended GAVRETO Dosage when Coadministered with:
	Combined P-gp and Strong CYP3A Inhibitors	Strong CYP3A Inhibitors; Moderate CYP3A Inhibitors; P-gp Inhibitors; Combined P-gp and Moderate CYP3A Inhibitors
400 mg orally once daily	200 mg orally once daily	300 mg orally once daily
300 mg orally once daily	200 mg orally once daily	200 mg orally once daily
200 mg orally once daily	100 mg orally once daily	100 mg orally once daily

Dose Modification for Use with CYP3A Inducers

Avoid coadministration of GAVRETO with any of the following:

Strong CYP3A inducers
Moderate CYP3A inducers

If coadministration with any of the above inducers cannot be avoided, increase the starting dose of GAVRETO as recommended in Table 4 starting on Day 7 of coadministration of GAVRETO with the inducer. After the inducer has been discontinued for at least 14 days, resume GAVRETO at the dose taken prior to initiating the inducer [see Drug Interactions (7.1), Clinical Pharmacology (12.3)].

Table 4: Recommended Dosage Modifications for GAVRETO for Coadministration with CYP3A Inducers
Current GAVRETO Dosage	Recommended GAVRETO Dosage when Coadministered with:
	Strong CYP3A Inducers	Moderate CYP3A Inducers
400 mg orally once daily	800 mg orally once daily	600 mg orally once daily
300 mg orally once daily	600 mg orally once daily	500 mg orally once daily
200 mg orally once daily	400 mg orally once daily	300 mg orally once daily