Drug intelligence / Profile preview

ERAS-007 + ERAS-601

Development stage
Unknown
Lead developer
Erasca
Modality
Small Molecules
Administration
Oral
01

Overview

**ERAS-007 + ERAS-601** is a combination of two investigational oral small molecules targeting the RAS/MAPK pathway in solid tumors. ERAS-007 is a highly selective inhibitor of ERK1/2 (extracellular signal-regulated kinases 1 and 2), which are terminal effectors in the MAPK pathway regulating cell proliferation, differentiation, and survival. ERAS-601 is a selective inhibitor of SHP2, a key signal transduction node connecting receptor tyrosine kinases (RTKs) to downstream RAS/MAPK pathway. The rationale for combination therapy (termed MAPKlamp) is to simultaneously block convergent and divergent nodes of the pathway to overcome resistance, suppress compensatory signaling, and deliver more durable anti-cancer effects, particularly in cancers harboring RAS, BRAF, or MAPK pathway alterations. The combination is being developed by Erasca, primarily for various advanced solid tumors. Early clinical data (Phase 1b) indicate favorable safety profiles and early signals of efficacy, especially in BRAF-driven and RAS/MAPK-altered tumors, including patients with class 2 and 3 BRAF mutations, which lack approved targeted therapies[1][3][4][6][7].

Other names
MAPKlamp
02

Targets

MAPK3 (Mitogen-activated protein kinase 1)PTPN11 (Tyrosine-protein phosphatase non-receptor type 11)

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