Pralsetinib: A Drug Review

Abstract

REarranged during Transfection (RET) is a transforming proto-oncogene that codes for the tyrosine kinase receptor. Pralsetinib is an orally bioavailable, selective inhibitor of mutant forms and fusions involving the RET proto-oncogene. Following administration, pralsetinib limits the upregulation or dysregulation of RET gene mutations. This drug review aimed to explore the pharmacokinetics, pharmacodynamics, clinical indications, contraindications, dosing regimen, dose modifications, adverse drug events, and storage and administration of pralsetinib. This review was curated after exhaustive literature screening of all existing documents available on Google Scholar, PubMed, ScienceDirect, Dimensions, and EBSCO Host, as well as by browsing the Web sites of the U.S. Food and Drug Administration (FDA), drug manuals, and conference presentations, using keywords, such as “Pralsetinib,” “RET fusion,” and “Gavreto.” Additional supporting data were obtained from various abstracts and conference proceedings. Presently, pralsetinib has been granted FDA approval for use in non–small cell lung cancer (NSCLC), metastatic RET fusion-positive NSCLC, and metastatic RET-mutant medullary thyroid cancer.

Keywords

pralsetinib - Gavreto - RET fusion - tyrosine kinase receptor - thyroid - cancer

^* These authors contributed equally.

Publication History

Article published online:
19 December 2024

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