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. 2020 Jan 31;25(3):627. doi: 10.3390/molecules25030627

Table 2.

TLR4-targeting ligands currently in clinical trials.

Compound Class Disease Model Activity Phase Identifier/Status
Eritoran Glycolipid Insulin sensitivity Antagonist II NCT02321111/Completed 3
GLA-SE 1 Glycolipid Stage III & IV soft tissue sarcoma Agonist I NCT02180698/Completed
GLA (Mart-1 Antigen) Glycolipid Stage IIA, IIB, IIC, IIIA, IIIB, IIIC & IV melanoma Agonist I NCT02320305/Active
GLA-SE Glycolipid Metastatic colorectal cancer Agonist I NCT03982121/Active
GSK1795091 Glycolipid Cancer, neoplasms agonist I NCT02798978/Completed
NI-0101 Antibody Rheumatoid arthritis antagonist II NCT03241108/Completed
G100 Glycolipid Follicular low-grade non-Hodgkin’s lymphoma Agonist I NCT02501473/Active
CX-01 Polysaccharide Myelodysplastic syndrome, AML 2 Antagonist I NCT02995655/Completed
GLA-SE Glycolipid Merkel cell carcinoma Agonist I NCT02035657/Completed
G100 Glycolipid Lymphoma Agonist II NCT03742804/Not yet recruiting
GLA-SE Glycolipid Schistosomiasis Agonist II NCT03041766/Completed
GLA Glycolipid Hookworm infection Agonist I NCT01717950/Completed
JKB-121 Small molecule Nonalcoholic steatohepatitis Antagonist II NCT02442687/Completed
Ibudilast Small molecule Methamphetamine use disorder Antagonist II NCT01860807/Completed

1 GLA: glucopyranosyl lipid A; 2 AML: acute myeloid leukemia; 3 NCT: national clinical trial.