Drug intelligence / Profile preview

ERAS-007 + sotorasib

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

Overview

**ERAS-007 + sotorasib** is a combination therapy consisting of two small molecule inhibitors targeting key nodes in the MAPK pathway for the treatment of KRAS G12C-mutated solid tumors, primarily non-small-cell lung cancer (NSCLC). **Sotorasib** is a covalent inhibitor of the KRAS G12C oncoprotein, binding irreversibly to a unique cysteine residue and locking KRAS in its inactive GDP-bound state, thereby inhibiting downstream oncogenic signaling. **ERAS-007** is an oral inhibitor of ERK1/2 (extracellular signal-regulated kinases 1 and 2), the terminal kinases in the MAPK signaling cascade. Preclinical studies and early-phase clinical trials support that co-inhibition of KRAS G12C and ERK1/2 may overcome resistance mechanisms and provide enhanced antitumor activity compared to monotherapy. This combination is under clinical investigation for KRAS G12C-mutated advanced solid tumors, especially NSCLC and colorectal cancer.

02

Targets

MAPK3 (Mitogen-activated protein kinase 1)KRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)

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