Drug intelligence / Profile preview

ERAS-10

Development stage
Discontinued
Lead developer
Erasca
Modality
Molecular Glues → Targeted Protein Degraders (TPDs) → Small Molecules
Administration
Oral
01

Overview

ERAS-10 is a RAS-selective molecular glue being developed by Erasca for the treatment of RAS-mutant solid tumors. It is designed to specifically target the active, GTP-bound state of RAS proteins, which are common drivers in various cancers. The drug's mechanism of action involves facilitating the formation of a ternary complex between RAS-GTP and the endogenous intracellular chaperone protein Peptidyl-prolyl cis-trans isomerase A (also known as Cyclophilin A or CypA). This recruitment sterically blocks the interaction between RAS and its downstream effectors, such as RAF, thereby inhibiting the MAPK (mitogen-activated protein kinase) signaling pathway. By targeting the "on" state of RAS, ERAS-10 aims to provide potent and selective inhibition of oncogenic signaling. In mid-2024, Erasca announced a strategic prioritization of its pipeline, deprioritizing ERAS-10 to focus on other lead assets such as naporafenib and ERAS-0015.

Other names
RAS-selective molecular glue
02

Targets

HRAS (H-Ras protein)

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