Product Description
A maleimide-based, small molecule inhibitor of glycogen synthase kinase-3 (GSK-3; serine/threonine-protein kinase GSK3) with potential antineoplastic activity. Upon intravenous administration, elraglusib binds to and competitively inhibits GSK-3, which may lead to downregulation of nuclear factor kappa B (NF-kappaB) and decreased expression of NF-kappaB target genes including cyclin D1, B-cell lymphoma 2 (Bcl-2), anti-apoptotic protein XIAP, and B-cell lymphoma extra-large (Bcl-XL). This may inhibit NF-kappaB-mediated survival and chemoresistance in certain tumor types. GSK-3, a constitutively active serine/threonine kinase that plays a role in numerous pathways involved in protein synthesis, cellular proliferation, differentiation, and metabolism, is aberrantly overexpressed in certain tumor types and may promote tumor cell survival and resistance to chemotherapy and radiotherapy. (Sourced from: https://www.cancer.gov/publications/dictionaries/cancer-drug/def/elraglusib)
Mechanisms of Action: GSK3B Inhibitor
Novel Mechanism: Yes
Modality: Small Molecule
Route of Administration: Intravenous
FDA Designation: Fast Track - Pancreatic CancerOrphan Drug - Pancreatic CancerOrphan Drug - Sarcoma *
Approval Status: Not Approved
Approved Countries: None
Approved Indications: None
Known Adverse Events: None
Company: Actuate Therapeutics
Company Location: Western America
Company Founding Year: 2015
Additional Commercial Interests: None
Clinical Description
Countries in Clinic: Belgium, Canada, France, Netherlands, Portugal, Spain, United States
Active Clinical Trial Count: 4
Recent & Upcoming Milestones
- Clinical Outcomes Reported - Actuate Therapeutics presented P2 Pancreatic Cancer results on 2026-01-12 for Elraglusib
- Clinical Outcomes Reported - Actuate Therapeutics presented P1 Sarcoma results on 2026-01-06 for Elraglusib
Highest Development Phases
Phase 2: Acute Lymphoid Leukemia|Adenocarcinoma|Bone Cancer|Breast Cancer|Colorectal Cancer|Glioma|Kidney Cancer|Lung Cancer|Lymphoma, Non-Hodgkin|Oncology Hematological Unspecified|Oncology Solid Tumor Unspecified|Pancreatic Cancer|Precursor Cell Lymphoblastic Leukemia-Lymphoma|Precursor T-Cell Lymphoblastic Leukemia-Lymphoma|Renal Cell Carcinoma|Sarcoma|T-Cell Leukemia
Phase 1: Hereditary Sensory and Autonomic Neuropathies
Trial ID |
Trial |
Phase |
Trial Status |
Disease |
Primary Completion Date |
Probability of Success |
Latest Trial Update Date |
Data Updated |
|---|---|---|---|---|---|---|---|---|
NCT06896188 |
RiLEY | P1 |
Recruiting |
Pancreatic Cancer|Adenocarcinoma|Hereditary Sensory and Autonomic Neuropathies |
2027-09-30 |
12% |
2025-09-30 |
Primary Completion Date|Primary Endpoints|Start Date|Treatments|Trial Status |
2024-518409-16-00 |
1801 | P2 |
Active, not recruiting |
Pancreatic Cancer |
2025-12-31 |
2025-05-02 |
Treatments |
|
NCT03678883 |
NCT03678883 | P2 |
Active, not recruiting |
Pancreatic Cancer|T-Cell Leukemia|Precursor Cell Lymphoblastic Leukemia-Lymphoma|Bone Cancer|Adenocarcinoma|Glioma|Colorectal Cancer|Lung Cancer|Renal Cell Carcinoma|Lymphoma, Non-Hodgkin|Precursor T-Cell Lymphoblastic Leukemia-Lymphoma|Breast Cancer|Acute Lymphoid Leukemia|Sarcoma|Kidney Cancer |
2025-01-01 |
60% |
2024-11-27 |
Primary Endpoints |
2018-003739-32 |
Actuate 1801: Phase 1/2 of 9-ING-41 in Refractory Malignancies | P2 |
Completed |
Oncology Solid Tumor Unspecified|Oncology Hematological Unspecified |
2023-02-28 |
2025-05-06 |
Treatments|Trial Status |