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    DRUG:

    setidegrasib (ASP3082)

    i
    Other names: ASP3082, ASP 3082, ASP-3082
    Company:
    Astellas
    Drug class:
    KRAS G12D degrader
    3d
    3082-CL-0101: A Study of ASP3082 in Adults With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=681, Recruiting, Astellas Pharma Inc | Trial completion date: Dec 2027 --> Dec 2028 | Trial primary completion date: Dec 2027 --> Dec 2028
    Trial completion date • Trial primary completion date
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12D • KRAS G12
    |
    Keytruda (pembrolizumab) • Erbitux (cetuximab) • carboplatin • gemcitabine • 5-fluorouracil • albumin-bound paclitaxel • pemetrexed • leucovorin calcium • setidegrasib (ASP3082)
    8d
    UNLOCK ASP3082: Study Investigating ASP3082 in Patients With Metastatic/Locally Advanced Non-small-cell Lung Cancer (NSCLC) and Pancreatic Ductal Adenocarcinoma (PDAC), With Biomarker Analysis to Characterize Response/Resistance (clinicaltrials.gov)
    P2, N=60, Recruiting, Gustave Roussy, Cancer Campus, Grand Paris | Not yet recruiting --> Recruiting
    Enrollment open
    |
    EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • MET (MET proto-oncogene, receptor tyrosine kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • NTRK (Neurotrophic receptor tyrosine kinase)
    |
    KRAS mutation • EGFR mutation • BRAF mutation • KRAS G12D • RET fusion • RET mutation • ROS1 fusion • MET mutation • KRAS G12 • NTRK fusion
    |
    setidegrasib (ASP3082)
    10d
    Setidegrasib in Advanced Non-Small-Cell Lung Cancer and Pancreatic Cancer. (PubMed, N Engl J Med)
    Setidegrasib was associated with antitumor activity and a low incidence of treatment discontinuation due to adverse events in patients with previously treated advanced KRAS p.G12D-mutated NSCLC or pancreatic ductal adenocarcinoma. (Funded by Astellas Pharma; ClinicalTrials.gov number, NCT05382559.).
    Journal
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12D • KRAS G12
    |
    setidegrasib (ASP3082)
    15d
    UNLOCK ASP3082: Study Investigating ASP3082 in Patients With Metastatic/Locally Advanced Non-small-cell Lung Cancer (NSCLC) and Pancreatic Ductal Adenocarcinoma (PDAC), With Biomarker Analysis to Characterize Response/Resistance (clinicaltrials.gov)
    P2, N=60, Not yet recruiting, Gustave Roussy, Cancer Campus, Grand Paris
    New P2 trial
    |
    EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • MET (MET proto-oncogene, receptor tyrosine kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • NTRK (Neurotrophic receptor tyrosine kinase)
    |
    KRAS mutation • EGFR mutation • BRAF mutation • KRAS G12D • RET fusion • RET mutation • ROS1 fusion • MET mutation • KRAS G12 • NTRK fusion
    |
    setidegrasib (ASP3082)
    29d
    A Study to Evaluate the Effectiveness and Safety of Setidegrasib, Given With Either mFOLFIRINOX or NALIRIFOX Chemotherapies, in People With Pancreatic Cancer (clinicaltrials.gov)
    P3, N=614, Recruiting, Astellas Pharma Global Development, Inc. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12D • KRAS G12
    |
    5-fluorouracil • oxaliplatin • leucovorin calcium • setidegrasib (ASP3082) • Onivyde (nanoliposomal irinotecan) • levoleucovorin calcium
    30d
    A Study to Learn How Fluconazole, Carbamazepine and Itraconazole Affect How the Body Processes ASP3082 in Healthy Adults (clinicaltrials.gov)
    P1, N=54, Recruiting, Astellas Pharma Global Development, Inc. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    setidegrasib (ASP3082) • itraconazole
    1m
    3082-CL-0101: A Study of ASP3082 in Adults With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=681, Recruiting, Astellas Pharma Inc | Trial completion date: Oct 2026 --> Dec 2027 | Trial primary completion date: Oct 2026 --> Dec 2027
    Trial completion date • Trial primary completion date
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12D • KRAS G12
    |
    Keytruda (pembrolizumab) • Erbitux (cetuximab) • carboplatin • gemcitabine • 5-fluorouracil • albumin-bound paclitaxel • pemetrexed • leucovorin calcium • setidegrasib (ASP3082)
    2ms
    CSET 2025/4116: Phase 2, Multicenter, Open label, Platform Study investigating ASP3082 in patients with Metastatic/Locally Advanced Non-Small-Cell Lung Cancer (NSCLC) and Pancreatic Ductal Adenocarcinoma (PDAC), with biomarker analysis to characterize response/resistance (UNLOCK ASP3082) (2025-522533-54-00)
    P1/2, N=60, Not yet recruiting, Institut Gustave Roussy
    New P1/2 trial
    |
    EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • MET (MET proto-oncogene, receptor tyrosine kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • NTRK (Neurotrophic receptor tyrosine kinase)
    |
    KRAS mutation • EGFR mutation • BRAF mutation • KRAS G12D • RET fusion • RET mutation • ROS1 fusion • MET mutation • KRAS G12 • NTRK fusion
    |
    setidegrasib (ASP3082)
    2ms
    A Study to Confirm the Safety of ASP3082, and if it Delays Tumor Growth in People With Pancreatic Cancer, When Given With Either mFOLFIRINOX or NALIRIFOX Chemotherapies (clinicaltrials.gov)
    P3, N=614, Not yet recruiting, Astellas Pharma Global Development, Inc.
    New P3 trial
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12D • KRAS G12
    |
    5-fluorouracil • oxaliplatin • leucovorin calcium • setidegrasib (ASP3082) • Onivyde (nanoliposomal irinotecan) • levoleucovorin calcium
    2ms
    A Study to Learn How Fluconazole, Carbamazepine and Itraconazole Affect How the Body Processes ASP3082 in Healthy Adults (clinicaltrials.gov)
    P1, N=54, Not yet recruiting, Astellas Pharma Global Development, Inc.
    New P1 trial
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    setidegrasib (ASP3082) • itraconazole
    7ms
    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)
    almost2years
    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)