Population Pharmacokinetics Modeling of Selpercatinib to Support Posology in Pediatric Patients With RET-Altered Metastatic Thyroid Cancer or Solid Tumors.

ABSTRACT: Selpercatinib is a first-in-class, highly selective, RET kinase inhibitor with CNS activity, approved for the treatment of RET-altered lung, thyroid, and other cancers. We report pharmacokinetic analyses to identify factors affecting selpercatinib steady-state exposure and support posology in pediatric patients. Population pharmacokinetic analyses using nonlinear mixed-effects modeling were performed on data from two ongoing, open-label, Phase 1/2 studies in adult and pediatric patients with advanced solid tumors. In LIBRETTO-001 (NCT03157128) patients (≥ 12 years) received oral selpercatinib from 20 mg once daily through 240 mg twice daily (BID) during phase 1 and 160 mg BID in phase 2. In LIBRETTO-121 (NCT03899792), patients (6 months-21 years) received doses based on body surface area (

SUBMITTER: Liu D 

PROVIDER: S-EPMC12625185 | biostudies-literature | 2025 Nov

REPOSITORIES: biostudies-literature