ASP3082 effectively induces KRAS(G12D) protein degradation with remarkable selectivity, demonstrates highly efficacious and durable pharmacological activity, and induces tumor regression in multiple KRAS(G12D)-mutated cancer xenograft models. Our results suggest that ASP3082 is a potential therapeutic agent for KRAS(G12D)-mutated cancer, and is now under clinical investigation.

P1/2, N=159, Recruiting, Arvinas Inc.

RP03707 effectively inhibits tumor cell growth in multiple KRASG12D cell lines. It also exhibits prolonged PK/PD effects and excellent efficacy in mouse CDX models bearing KRASG12D tumors, highlighting its potential for the treatment of KRASG12D-driven tumors in clinical settings.

P1, N=541, Recruiting, Astellas Pharma Inc | N=356 --> 541

P1, N=356, Recruiting, Astellas Pharma Inc | Trial completion date: Jun 2026 --> Oct 2026 | Trial primary completion date: Jun 2026 --> Oct 2026

P1, N=356, Recruiting, Astellas Pharma Inc | N=260 --> 356

ASP3082 is a potential therapeutic agent for patients with tumors harboring the KRAS G12D mutation. Currently, a phase 1 clinical trial is underway in patients with previously treated, locally advanced or metastatic solid tumors with KRAS G12D mutation (NCT05382559).

Enrollment in Cohort 1 is complete, and enrollment to Cohort 2 began in September 2022. Clinical trial information: NCT05382559.

P1, N=240, Recruiting, Astellas Pharma Inc | N=136 --> 240

ASP3082 is a potential therapeutic agent for patients with tumors harboring the KRAS G12D mutation. Currently, Phase I clinical trial is underway (NCT05382559).