GSK1795091   Click here for help

GtoPdb Ligand ID: 11150

Synonyms: compound 4 [PMID: 18835160] | CRX-601 | CRX601 | GSK'091 | GSK-1795091
Compound class: Synthetic organic
Comment: GSK1795091 is a dendritic glycolipid TLR4 agonist with potential immunoadjuvant activity [2-3]. Structurally it is a mimetic of bacterial lipid A [1]. TLR4 plays a key role in the activation of the innate immune response. Activating TLR4 stimulates dendritic cells (DCs), monocytes and macrophages to increase production of pro-inflammatory cytokines (IFNγ, TNFα, interleukins (IL), IL-1 beta, -6 and -12). This mechanism produces a Th1 immune response that offers adjuvant potential in combination with tumour antigen vaccines, and a subsequent cytotoxic T-lymphocyte response against the targeted tumour cells. It also enhances the immune response to checkpoint inhibitor cancer therapies.
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 18
Hydrogen bond donors 6
Rotatable bonds 79
Topological polar surface area 264.75
Molecular weight 1445.13
XLogP 26.84
No. Lipinski's rules broken 4
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InChI InChI=1S/C81H157N2O16P/c1-7-13-19-25-31-37-40-46-52-58-69(93-61-55-49-43-34-28-22-16-10-4)64-74(85)82-72(80(88)89)68-96-81-77(83-75(86)65-70(59-53-47-41-38-32-26-20-14-8-2)94-62-56-50-44-35-29-23-17-11-5)79(78(73(67-84)97-81)99-100(90,91)92)98-76(87)66-71(60-54-48-42-39-33-27-21-15-9-3)95-63-57-51-45-36-30-24-18-12-6/h69-73,77-79,81,84H,7-68H2,1-6H3,(H,82,85)(H,83,86)(H,88,89)(H2,90,91,92)/t69-,70-,71-,72+,73-,77-,78-,79-,81-/m1/s1
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Summary of Clinical Use Click here for help
GSK1795091 was advanced to early stage cancer clinical trials. Clinical development was terminated in mid 2020.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT00001693 Phase I-II Multiple-Dose Safety and Efficacy Study of a Selective Inhibitor of Cyclooxygenase - 2 (SC-58635) in Hereditary Non-Polyposis Colorectal Cancer (HNPCC) Patients and Carriers Phase 1 Interventional National Institutes of Health Clinical Center (CC) In the 2nd quarter of 2020, GSK made the decision to terminate the GSK1795091 programme, following a review of their development pipeline.