Vipoglanstat selectively and safely inhibits mPGES-1

Gesynta Pharma develops vipoglanstat (GS-248) – a drug candidate with a unique ability to effectively inhibit the enzyme mPGES-1, which has been proven to play a key role in endometriosis.

mPGES-1 is part of the complex arachidonic acid cascade, where both physiological and pathogenic processes are regulated. It stimulates production of prostaglandin E2 (PGE2), a potent biological messenger that has a pronounced impact on inflammation as well as inflammatory pain. It is well documented that endometriotic lesions contain high levels of mPGES-1, which in turn causes an increase in PGE2 levels in the abdominal cavity of the patient.

Development of vipoglanstat

Vipoglanstat has proven preclinical proof-of-concept in an advanced disease model of endometriosis. The results show that the drug candidate markedly reduces the number of endometriotic lesions and has a positive effect on parameters measuring pain and well-being. Its effect on the endometriotic lesions points toward the disease-modifying capability of vipoglanstat.

Vipoglanstat has previously been evaluated in clinical studies in healthy subjects as well as in patients suffering from chronic inflammatory disease. The results show that vipoglanstat can be administered in a patient-friendly way and reaches therapeutic levels in the blood in a short period of time. Importantly, treatment with vipoglanstat has been shown to completely inhibit mPGES-1 in patients with chronic inflammation. No serious side effects were observed during four weeks of treatment and the drug candidate was well-tolerated by the patients.

The compelling results from the preclinical proof-of-concept study of vipoglanstat provide strong support for its analgesic and disease-modifying capacity. Together with data from previous clinical studies regarding the drug candidate's safety profile, pharmacokinetic properties, and ability to inhibit the target enzyme mPGES-1, this constitutes a solid scientific foundation for the continued development of Vipoglanstat as an effective non-hormonal treatment for endometriosis. A clinical phase II study in patients with endometriosis is now being prepared.

Intellectual property

Vipoglanstat is protected by composition of matter patents in the most important markets – the United States, Europe, China, Japan – as well as in a number of other countries. In addition to the already approved patents, a patent application was submitted in 2022 covering the use of vipoglanstat in endometriosis, which may strengthen and extend the already granted IP protection.

Projects in other indications: GS-073

Gesynta Pharma is developing GS-073, part of the next generation of mPGES-1 inhibitors. The company has developed complete preclinical safety documentation and a study protocol for the GS-073 project. The drug candidate is expected to enter clinical phase I in 2023 in an undisclosed disease area.