Vipoglanstat

Vipoglanstat is an inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1; IC₅₀ = ≤0.5 nM in isolated human whole blood).¹ It reduces LPS-induced increases in the influx of neutrophils and levels of cytokines in bronchoalveolar lavage fluid (BALF), as well as the expression of PTGES, the gene encoding mPGES-1, Cox2, and Icam1 in the lung parenchyma, in a human PTGES knock-in mouse model of acute lung injury when administered at a dose of 30 mg/kg.² Vipoglanstat (30 mg/kg) also reduces the lung injury score and expression of PTGES and Nos2, the gene encoding inducible nitric oxide synthase (iNOS), as well as increases survival, in a human PTGES knock-in mouse model of sepsis induced by cecal ligation and puncture. It reduces status epilepticus-induced increases in brain capillary mPGES-1 and P-glycoprotein levels in a human PTGES knock-in mouse model of kainic acid-induced status epilepticus when administered at doses of 10, 30, and 100 mg/kg.³

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1. Tornling, G., Edenius, C., Pauling, J.D., et al. A phase 2 trial investigating the efficacy and safety of the mPGES-1 inhibitor vipoglanstat in systemic sclerosis-related Raynaud’s. Rheumatology (Oxford) (2024).

2. Gurusamy, M., Nasseri, S., Rampa, D.R., et al. Inhibition of microsomal prostaglandin E synthase-1 ameliorates acute lung injury in mice. J. Transl. Med. 19(1), 340 (2021).

3. Soldner, E.L.B., Hartz, A.M.S., Akanuma, S.I., et al. Inhibition of human microsomal PGE₂ synthase-1 reduces seizure-induced increases of P-glycoprotein expression and activity at the blood-brain barrier. The FASEB Journal 33(12), 13966-13981 (2019).