Skip to main content

Pralsetinib Dosage

Medically reviewed by Drugs.com. Last updated on Oct 19, 2020.

Applies to the following strengths: 100 mg

Usual Adult Dose for Non-Small Cell Lung Cancer

400 mg orally once daily until disease progression or unacceptable toxicity

Use: For the treatment of adult patients with metastatic RET fusion-positive non-small cell lung cancer (NSCLC) as detected by an approved test.

Renal Dose Adjustments

Mild (CrCl 60 to less than 90 mL/min) to moderate (CrCl 30 to less than 60 mL/min) renal impairment: No adjustment recommended.
Severe (CrCl 15 to less than 30 mL/min) or end-stage (CrCl less than 15 mL/min) renal impairment: Data not available

Liver Dose Adjustments

Mild (total bilirubin less than or equal to upper limit of normal [ULN] and AST greater than ULN OR total bilirubin greater than 1 to 1.5 x ULN and any AST hepatic impairment: No adjustment recommended.
-Moderate (total bilirubin greater than 1.5 to 3 x ULN and any AST OR severe (total bilirubin greater than 3 x ULN and any AST): Data not available

Dose Adjustments

DOSE REDUCTIONS FOR ADVERSE REACTIONS:
-First dose reduction: 300 mg orally once daily
-Second dose reduction: 200 mg orally once daily
-Third dose reduction: 100 mg orally once daily
-Discontinue therapy in patients unable to tolerate 100 mg orally once daily.

DOSE MODIFICATIONS FOR ADVERSE REACTIONS:
ILD/PNEUMONITIS:
-Grade 1 or 2: Withhold therapy until resolution; resume at reduced dose.
-Grade 3 or 4 or recurrent: Permanently discontinue therapy.
HYPERTENSION:
-Grade 3: Withhold therapy for Grade 3 hypertension that persists despite antihypertensives; resume at reduced dose when controlled.
-Grade 4: Permanently discontinue therapy.
HEPATOTOXICITY:
-Grade 3 or 4: Withhold therapy until recovery to Grade 1, or 0, or baseline; resume at reduced dose.
-Grade 3 or higher recurring: Discontinue therapy.
HEMORRHAGIC EVENTS:
-Grade 3 or 4: Withhold therapy until recovery to Grade 1, or 0, or baseline; resume at reduced dose.
-Severe or life-threatening hemorrhagic events: Discontinue therapy.
OTHER ADVERSE REACTIONS:
-Grade 3 or 4: Withhold therapy until improvement to Grade 2 or less; resume at reduced dose.
-Recurrent Grade 4: Permanently discontinue therapy.

DOSE MODIFICATION FOR USE WITH COMBINED P-GLYCOPROTEIN (P-GP) AND STRONG CYP450 3A INHIBITORS:
-Avoid coadministration of this drug with combined P-gp and strong CYP450 3A inhibitors. If coadministration cannot be avoided, reduce the dose of this drug. After the inhibitor has been discontinued for 3 to 5 elimination half-lives, resume this drug at the previous dose.

DOSE MODIFICATIONS FOR COADMINISTRATION WITH COMBINED P-GP AND STRONG CYP450 3A INHIBITORS:
-Current dose is 400 mg once daily: Reduce to 200 mg once daily.
-Current dose is 400 mg once daily: Reduce to 200 mg once daily.
-Current dose is 200 mg once daily: Reduce to 100 mg once daily.

DOSE MODIFICATION FOR COADMINISTRATION WITH STRONG CYP450 3A INDUCERS:
-Avoid coadministration of this drug with strong CYP450 3A inducers.
-If coadministration with a strong CYP450 3A inducer cannot be avoided, increase the starting dose of this drug to double the current dose starting on Day 7 of coadministration. After the inducer has been discontinued for at least 14 days, resume this drug at the previous dose.

Precautions

CONTRAINDICATIONS:
-None

Safety and efficacy have not been established in patients younger than 18 years.

Consult WARNINGS section for additional precautions.

Dialysis

Data not available

Other Comments

Administration advice:
-Select patients for treatment with this drug based on the presence of a RET gene fusion.
-This drug should be taken on an empty stomach (at least 2 hours before or 1 hour after food intake).
-If a dose is missed, it can be taken as soon as possible on the same day; resume the regular daily dose schedule for the next day.
-If vomiting occurs after taking this drug do not take an additional dose.

Storage requirements:
Store at 20C to 25C (68F to 77F); excursions permitted from 15C to 30C (59F to 86F).

Patient advice:
-Advise the patient to read the approved patient labeling (Patient Information).

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.