Dosage of Selpercatinib

1.Recommended Dosage

Take selpercatinib with or without food at approximately the same time every day.

Swallow tablets whole. Do not crush, chew, split, or dissolve tablets.If the patient misses a dose of selpercatinib by 4 or more hours or if vomiting occurs, resume dosing with the next scheduled dose.

2.Dosage Modification for Adverse Reactions

The recommended dose reductions for adverse reactions are provided in Table 1. 

Table 1: Recommended Dose Reductions for selpercatinib for Adverse Reactions

* Permanently discontinue selpercatinib if unable to tolerate 4.5 mg once daily for 14 days of each 21-day cycle. 

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

Table 2: Recommended Dosage Modifications for selpercatinib Adverse Reactions

*Severity as defined by National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE)
version 4.03.

3.Dosage Modification for Concomitant Use with Strong or Moderate
CYP3A Inhibitors

Avoid concomitant use of strong and moderate CYP3A inhibitors with selpercatinib. If concomitant use with a strong or moderate CYP3A inhibitor cannot be avoided:

Reduce selpercatinib dosage from 13.5 mg to 9 mg. 

Reduce selpercatinib dosage from 9 mg to 4.5 mg. 

If concomitant use of a strong or moderate CYP3A inhibitor is discontinued, increase the selpercatinib dosage (after 3 plasma half-lives of the CYP3A inhibitor) to the dosage that was used before starting the strong or moderate inhibitor.

4.Recommended Dosage for Severe Renal Impairment

The recommended dosage of selpercatinib for patients with severe renal impairment (eGFRestimated by Modification of Diet in Renal Disease [MDRD] 15 mL/min/1.73 m2 to 29 mL/min/1.73 m2) is 9 mg with the schedule (intermittent or continuous) designated for the indication.

5.Recommended Dosage for Severe Hepatic Impairment

The recommended dosage of selpercatinib for patients with severe hepatic impairment (total bilirubin > 3 × ULN with any AST) is 9 mg with the schedule (intermittent or continuous) designated for the indication.

from FDA，2024.06