Gesynta Pharma reports positive Phase I results with its lead candidate GS-248 for microvascular disease.
Results from the completed First-in-Human clinical study with GS-248 for the treatment of microvascular disease have been presented at the EULAR 2020 E-Congress.
Following these results, Gesynta now intends to commence a Phase II study in patients with Systemic Sclerosis.
“The results obtained from the Phase I study are very promising for the development of new treatments for microvascular diseases, for which there is a large unmet medical need. The confirmation of strong effects on biomarkers of inflammation and vascular protection in humans demonstrates the potential of GS-248 as a unique treatment of microvascular dysfunction in Systemic Sclerosis and other chronic inflammatory conditions. We now intend to initiate a multicenter Phase IIa study with enrolment commencing in Q4, 2020,” says Patric Stenberg, CEO of Gesynta Pharma.
GS-248 is a potent and selective inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1) and preclinical studies have demonstrated that inhibition of mPGES-1 provides a combination of anti-inflammatory, vasodilatory and platelet inhibitory effects.
The Phase I study was designed to assess the safety, tolerability, pharmacokinetics and pharmacodynamics of single oral doses up to 300 mg and multiple once daily doses up to 180 mg for 10 days in healthy male and female subjects. The study demonstrated that GS-248 was safe and well tolerated with a pharmacokinetic profile supporting once daily dosing and with potent and durable effects on relevant anti-inflammatory (PGE2 decrease) and vasoprotective (prostacyclin increase) biomarkers. The biomarker response supports an effective shunting from PGE2 to prostacyclin synthesis. More details can be found via this link.
Photo of the Gesynta Pharma team