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Setidegrasib (ASP3082)

First-in-human KRAS G12D targeted protein degrader

First-in-human phase 1 trial of setidegrasib, a first-in-class KRAS G12D targeted protein degrader, in advanced PDAC and NSCLC.

Background

KRAS G12D is the most common KRAS variant in pancreatic cancer but has historically been undruggable. Setidegrasib (ASP3082) is a first-in-class targeted protein degrader designed to eliminate KRAS G12D protein rather than merely inhibit it.

Results

In this first-in-human phase 1 study, among 21 patients with metastatic PDAC receiving the 600 mg dose, 24% achieved an objective response.

In NSCLC (n=45), the objective response rate was 36% with a median PFS of 8.3 months.