Retevmo Dosage

Generic name: selpercatinib 40mg
Dosage form: capsule
Drug class: Multikinase inhibitors

Medically reviewed by Drugs.com. Last updated on Sep 27, 2024.

Patient Selection

Select patients for treatment with RETEVMO based on the presence of a RET gene fusion (NSCLC, thyroid cancer, or other solid tumors) or specific RET gene mutation (MTC) in tumor specimens. Information on FDA-approved test(s) for the detection of RET gene fusions and RET gene mutations is available at: http://www.fda.gov/CompanionDiagnostics. An FDA-approved companion diagnostic test for the detection of RET gene fusions and RET gene mutations in plasma is not available.

Important Administration Instructions

RETEVMO may be taken with or without food unless coadministered with a proton pump inhibitor (PPI).

Recommended Dosage

The recommended dosage of RETEVMO is shown in Table 1:

Table 1: Recommended RETEVMO Dosage
Population	RETEVMO Dosage
Adult and adolescent patients 12 years of age or older based on body weight
Less than 50 kg	120 mg twice daily
50 kg or greater	160 mg twice daily
Pediatric patients 2 to less than 12 years of age based on body surface area
0.33 to 0.65 m2	40 mg three times daily
0.66 to 1.08 m2	80 mg twice daily
1.09 to 1.52 m2	120 mg twice daily
≥1.53 m2	160 mg twice daily
Dosing pediatric patients with body surface area less than 0.33 m2 is not recommended

Continue treatment with RETEVMO until disease progression or unacceptable toxicity.

Swallow the capsules whole. Do not crush or chew the capsules. Do not administer to pediatric patients who are unable to swallow a capsule.

Swallow the tablets whole. Do not crush or chew the tablets.

Do not take a missed dose unless it is more than 6 hours until next scheduled dose.

If vomiting occurs after RETEVMO administration, do not take an additional dose and continue to the next scheduled time for the next dose.

Dosage Modifications for Concomitant Use of Acid-Reducing Agents

Avoid concomitant use of a PPI, a histamine-2 (H2) receptor antagonist, or a locally-acting antacid with RETEVMO. If concomitant use cannot be avoided:

Take RETEVMO with food when coadministered with a PPI.
Take RETEVMO 2 hours before or 10 hours after administration of an H2 receptor antagonist.
Take RETEVMO 2 hours before or 2 hours after administration of a locally-acting antacid.

Dosage Modifications for Adverse Reactions

The recommended dose reductions for adverse reactions are provided in Table 2.

Table 2: Recommended RETEVMO Dose Reductions for Adverse Reactions
Current RETEVMO Dosage	Dose Reduction
Current RETEVMO Dosage	First	Second	Third
40 mg three times daily	40 mg twice daily	40 mg once daily	permanently discontinue
80 mg twice daily	40 mg twice daily	40 mg once daily	permanently discontinue
120 mg twice daily	80 mg twice daily	40 mg twice daily	40 mg once daily
160 mg twice daily	120 mg twice daily	80 mg twice daily	40 mg twice daily
Permanently discontinue RETEVMO in patients unable to tolerate three dose reductions.

The recommended dosage modifications for adverse reactions are provided in Table 3.

Table 3: Recommended RETEVMO Dosage Modifications for Adverse Reactions
Adverse Reaction	Severity	Dosage Modification
Hepatotoxicity	Grade 3 or Grade 4	Withhold RETEVMO and monitor AST/ALT once weekly until resolution to Grade 1 or baseline. Resume at reduced dose by 2 dose levels and monitor AST and ALT once weekly until 4 weeks after reaching dose taken prior to the onset of Grade 3 or 4 increased AST or ALT. Increase dose by 1 dose level after a minimum of 2 weeks without recurrence and then increase to dose taken prior to the onset of Grade 3 or 4 increased AST or ALT after a minimum of 4 weeks without recurrence.
Interstitial Lung Disease/ Pneumonitis	Grade 2	Withhold RETEVMO until resolution. Resume at a reduced dose. Discontinue RETEVMO for recurrent ILD/pneumonitis.
Interstitial Lung Disease/ Pneumonitis	Grade 3 or Grade 4	Discontinue RETEVMO for confirmed ILD/pneumonitis.
Hypertension	Grade 3	Withhold RETEVMO for Grade 3 hypertension that persists despite optimal antihypertensive therapy. Resume at a reduced dose when hypertension is controlled.
Hypertension	Grade 4	Discontinue RETEVMO.
QT Interval Prolongation	Grade 3	Withhold RETEVMO until recovery to baseline or Grade 0 or 1. Resume at a reduced dose or permanently discontinue RETEVMO.
QT Interval Prolongation	Grade 4	Discontinue RETEVMO.
Hemorrhagic Events	Grade 3 or Grade 4	Withhold RETEVMO until recovery to baseline or Grade 0 or 1. Discontinue RETEVMO for severe or life-threatening hemorrhagic events.
Hypersensitivity Reactions	All Grades	Withhold RETEVMO until resolution of the event. Initiate corticosteroids. Resume at a reduced dose by 3 dose levels while continuing corticosteroids. Increase dose by 1 dose level each week until the dose taken prior to the onset of hypersensitivity is reached, then taper corticosteroids.
Hypothyroidism	Grade 3 or Grade 4	Withhold RETEVMO until resolution to Grade 1 or baseline. Discontinue RETEVMO based on severity.
Other Adverse Reactions	Grade 3 or Grade 4	Withhold RETEVMO until recovery to baseline or Grade 0 or 1. Resume at a reduced dose.

Dosage Modifications for Concomitant Use of Strong and Moderate CYP3A Inhibitors

Avoid concomitant use of strong and moderate CYP3A inhibitors with RETEVMO. If concomitant use of a strong or moderate CYP3A inhibitor cannot be avoided, reduce the RETEVMO dose as recommended in Table 4. After the inhibitor has been discontinued for 3 to 5 elimination half-lives, resume RETEVMO at the dose taken prior to initiating the CYP3A inhibitor.

Table 4: Recommended RETEVMO Dosage for Concomitant Use of Strong and Moderate CYP3A Inhibitors
Current RETEVMO Dosage	Recommended RETEVMO Dosage
	Moderate CYP3A Inhibitor	Strong CYP3A Inhibitor
40 mg orally three times daily	40 mg orally once daily	40 mg orally once daily
80 mg orally twice daily	40 mg orally twice daily	40 mg orally twice daily
120 mg orally twice daily	80 mg orally twice daily	40 mg orally twice daily
160 mg orally twice daily	120 mg orally twice daily	80 mg orally twice daily

Dosage Modification for Severe Hepatic Impairment

Reduce the recommended dosage of RETEVMO for patients with severe hepatic impairment as recommended in Table 5.

Table 5: Recommended RETEVMO Dosage for Severe Hepatic Impairment
Current RETEVMO Dosage	Recommended RETEVMO Dosage
40 mg orally three times daily	40 mg orally twice daily
80 mg orally twice daily	40 mg orally twice daily
120 mg orally twice daily	80 mg orally twice daily
160 mg orally twice daily	80 mg orally twice daily