RAS Inhibitors: Changing the Paradigm from the Undruggable

Pharmaceutics 2026 Open access

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Authors: Federica Campana, Emanuela De Bellis, Floriana Porcaro, Gaetano Di Guida, Luigi Della Gravara, Alberto Servetto, Floriana Morgillo, Federica Papaccio, Amelia Filippelli, Carminia Maria Della Corte, Valeria Conti
DOI: 10.3390/pharmaceutics18070773
Cited by: 1
References: 100

Abstract

For decades RAS mutations represented a chimera for drug developers, as all efforts put into attempting to pharmacologically inhibit them failed. Finally, in recent years, the advent of the KRAS G12C inhibitors sotorasib and adagrasib pushed the development of several new drugs; therefore, the landscape of RAS inhibitors evolved and now includes several compounds with different mechanisms of action. In this review we provide an updated summary of RAS inhibitor drugs, detailing their mechanism of action, pharmacokinetics and toxicity profile as well as efficacy studies.

Fields of Study & Subjects

Protein Kinase Regulation and GTPase Signaling Sphingolipid Metabolism and Signaling Receptor Mechanisms and Signaling

Publication details

Journal / source
Pharmaceutics
Publisher
MDPI AG
Volume
18
Issue
7
Pages
773–773
Publication date
24 June 2026
Language
EN