NCT02321111: Eritoran1

The Role of TLR4 on Lipid-Induced Insulin Resistance

Completed Phase 2 Results posted Last updated 16 September 2019

What this trial tests

Phase 2 trial testing Eritoran in Insulin Sensitivity in 10 participants. Completed in 1 September 2018.

Timeline

1 January 2015

Primary endpoint
1 September 2018

1 September 2018

Quick facts

Lead sponsor	The University of Texas Health Science Center at San Antonio
Phase	Phase 2
Status	Completed
Study type	INTERVENTIONAL
Allocation	randomized
Design	crossover
Masking	quadruple
Primary purpose	treatment
Enrollment	10
Start date	1 January 2015
Primary completion	1 September 2018
Estimated completion	1 September 2018
Sites	1 location across United States

Drugs / interventions tested

• Eritoran — full drug profile →
• D5W (5% Dextrose in water) — full drug profile →

Conditions studied

• Insulin Sensitivity — all drugs for Insulin Sensitivity →

Sponsor

The University of Texas Health Science Center at San Antonio

Who can join

Adults 18 to 65, any sex, with Insulin Sensitivity. Healthy volunteers can join.

What's being measured

Primary outcomes are the specific endpoints the trial is designed to prove or disprove.

• Effect of Eritoran on Muscle Insulin Sensitivity
  Time frame: 72 hours
  Muscle insulin sensitivity = muscle insulin sensitivity is determined by euglycemic hyperinsulinemic clamp procedure. M value (mg glucose / kg of body weight / minute) calculated from the clamp is measured. Higher M value indicates better insulin sensitivity. There is no established reference range.
• Effect of Eritoran on Hepatic Insulin Sensitivity
  Time frame: 72 hours
  Hepatic insulin sensitivity = is determined by euglycemic hyperinsulinemic clamp procedure. Endogenous glucose production or EGP (mg/kg/min) calculated from the clamp is measured. Lower EGP indicates better hepatic insulin sensitivity. There is no established reference range.

Sponsor's own description

The purpose of this study is to determine whether pharmacologic inhibition of Toll-like receptor 4 (TLR4) with eritoran for injection (E5564) prevents lipid-induced insulin resistance in lean, normal glucose tolerant (NGT) subjects.

Publications & conference data

8 peer-reviewed publications reference this trial (live from Europe PMC):

1. Pattern recognition receptors in health and diseases.
   Li D, Wu M. · · 2021 · cited 1148× · PMID 34344870 · DOI 10.1038/s41392-021-00687-0
2. Recent clinical trends in Toll-like receptor targeting therapeutics.
   Anwar MA, Shah M, Kim J, Choi S. · · 2019 · cited 209× · PMID 30450666 · DOI 10.1002/med.21553
3. TLR4-Targeting Therapeutics: Structural Basis and Computer-Aided Drug Discovery Approaches.
   Ain QU, Batool M, Choi S. · · 2020 · cited 84× · PMID 32023919 · DOI 10.3390/molecules25030627
4. Pattern recognition receptors: function, regulation and therapeutic potential.
   Chen R, Zou J, Chen J, Zhong X, et al · · 2025 · cited 53× · PMID 40640149 · DOI 10.1038/s41392-025-02264-1
5. Targeting toll-like receptor 4 signalling pathways: can therapeutics pay the toll for hypertension?
   Nunes KP, de Oliveira AA, Mowry FE, Biancardi VC. · · 2019 · cited 46× · PMID 29981161 · DOI 10.1111/bph.14438
6. Pattern Recognition Receptor-Mediated Chronic Inflammation in the Development and Progression of Obesity-Related Metabolic Diseases.
   Yu L, Li Y, Du C, Zhao W, et al · · 2019 · cited 33× · PMID 31582899 · DOI 10.1155/2019/5271295
7. Effect of acute TLR4 inhibition on insulin resistance in humans.
   Liang H, Sathavarodom N, Colmenares C, Gelfond J, et al · · 2022 · cited 15× · PMID 36066991 · DOI 10.1172/jci162291
8. Toll-like receptors in innate immunity and inflammation: from fundamental biology to clinic insights.
   Qian C, Cao X, Hoffmann JA. · · 2026 · PMID 42052154 · DOI 10.1007/s44466-026-00040-6