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    DRUG:

    setidegrasib (ASP3082)

    i
    Other names: ASP3082, ASP 3082, ASP-3082
    Company:
    Astellas
    Drug class:
    KRAS G12D degrader
    4ms
    Discovery of KRAS(G12D) selective degrader ASP3082. (PubMed, Commun Chem)
    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.
    Journal
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12D • KRAS G12
    |
    setidegrasib (ASP3082)
    over1year
    A Study of ASP3082 in Adults With Previously Treated Solid Tumors (clinicaltrials.gov)
    P1, N=541, Recruiting, Astellas Pharma Inc | N=356 --> 541
    Enrollment change • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12D • KRAS G12
    |
    Erbitux (cetuximab) • setidegrasib (ASP3082)
    over2years
    A Study of ASP3082 in Adults With Previously Treated Solid Tumors (clinicaltrials.gov)
    P1, N=356, Recruiting, Astellas Pharma Inc | Trial completion date: Jun 2026 --> Oct 2026 | Trial primary completion date: Jun 2026 --> Oct 2026
    Trial completion date • Trial primary completion date • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12D • KRAS G12
    |
    Erbitux (cetuximab) • setidegrasib (ASP3082)
    over2years
    A Study of ASP3082 in Adults With Previously Treated Solid Tumors (clinicaltrials.gov)
    P1, N=356, Recruiting, Astellas Pharma Inc | N=260 --> 356
    Enrollment change • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12D • KRAS G12
    |
    Erbitux (cetuximab) • setidegrasib (ASP3082)
    almost3years
    Novel KRAS G12D degrader ASP3082 demonstrates in vivo, dose-dependent KRAS degradation, KRAS pathway inhibition, and antitumor efficacy in multiple KRAS G12D-mutated cancer models (AACR 2023)
    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).
    Preclinical
    |
    KRAS (KRAS proto-oncogene GTPase) • CASP3 (Caspase 3)
    |
    KRAS mutation • KRAS G12D
    |
    setidegrasib (ASP3082)
    3years
    Trial in progress: A phase 1, first-in-human, open-label, multicenter, dose-escalation and dose-expansion study of ASP3082 in patients with previously treated advanced solid tumors and KRAS G12D mutations. (ASCO-GI 2023)
    Enrollment in Cohort 1 is complete, and enrollment to Cohort 2 began in September 2022. Clinical trial information: NCT05382559.
    Clinical • P1 data • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12D • KRAS wild-type • RAS wild-type • KRAS G12
    |
    setidegrasib (ASP3082)
    3years
    A Study of ASP3082 in Adults With Previously Treated Solid Tumors (clinicaltrials.gov)
    P1, N=240, Recruiting, Astellas Pharma Inc | N=136 --> 240
    Enrollment change • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12D • KRAS G12
    |
    Erbitux (cetuximab) • setidegrasib (ASP3082)
    over3years
    ASP3082, a First-in-class novel KRAS G12D degrader, exhibits remarkable anti-tumor activity in KRAS G12D mutated cancer models (AACR-NCI-EORTC 2022)
    ASP3082 is a potential therapeutic agent for patients with tumors harboring the KRAS G12D mutation. Currently, Phase I clinical trial is underway (NCT05382559).
    Preclinical
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12D • KRAS wild-type • RAS wild-type • KRAS G12
    |
    setidegrasib (ASP3082)
    over3years
    A Study of ASP3082 in Adults With Previously Treated Solid Tumors (clinicaltrials.gov)
    P1, N=136, Recruiting, Astellas Pharma Inc | Not yet recruiting --> Recruiting
    Enrollment open
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12D • KRAS G12
    |
    setidegrasib (ASP3082)
    over3years
    A Study of ASP3082 in Adults With Previously Treated Solid Tumors (clinicaltrials.gov)
    P1, N=136, Not yet recruiting, Astellas Pharma Inc
    New P1 trial
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12D • KRAS G12
    |
    setidegrasib (ASP3082)