DOI: 10.3390/pharmaceutics18070773 ISSN: 1999-4923
RAS Inhibitors: Changing the Paradigm from the Undruggable
Federica Campana, Emanuela De Bellis, Floriana Porcaro, Gaetano Di Guida, Luigi Della Gravara, Alberto Servetto, Floriana Morgillo, Federica Papaccio, Amelia Filippelli, Carminia Maria Della Della Corte, Valeria ContiFor 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.