Drug candidates with a unique mechanism of action

Gesynta Pharma’s drug candidates utilize a unique mechanism of action to reduce inflammation and pain. By targeting a key enzyme present in local inflammations, our drug candidates decrease the inflammatory process with a substantially higher precision than currently available treatments. Read more about our drug candidates and how they work below.

Inhibition of mPGES-1 – a novel anti-inflammatory treatment paradigm

Gesynta Pharma’s drug candidates have a unique ability to selectively inhibit microsomal prostaglandin E synthase (mPGES-1), the enzyme that promotes production of the harmful inflammatory mediator prostaglandin E2 (PGE2). By targeting mPGES-1, the levels of PGE2 decrease, leading to anti-inflammatory and pain-relieving effects, while preserving the production of the vasoprotective mediator prostacyclin.

GS-248 potently inhibits mPGES-1

GS-248 is Gesynta Pharma’s most advanced drug candidate, currently in Phase II. Clinical phase I data in healthy individuals show that GS-248 potently inhibits the production of PGE2 in a tolerable and safe manner, while increasing the observed levels of protective and vasodilatory prostacyclin by two to three times. The study data also show that a once- or twice-daily oral dose is sufficient to maintain the therapeutic effect over 24 hours, which enables a convenient and patient-friendly administration.

The objectives of the recently concluded explorative Phase II study included investigating the safety profile of GS-248, its ability to inhibit mPGES-1, as well as its effect on Raynaud’s phenomenon and peripheral blood flow in systemic sclerosis patients. The study was conducted at clinical centers in four European countries. No significant effects were seen after treatment with GS-248 compared to placebo in terms of symptomatic relief in patients with systemic sclerosis.

For the first time in patients, the Phase II study confirmed the tolerability and safety profile, pharmacokinetics, and unique ability of GS-248 to inhibit mPGES-1 and thus modify prostaglandin profile. Collectively, the data strengthens the rationale to progress the development of the drug for endometriosis.

Explore the results from our clinical Phase I study of GS-248, presented at EULAR in 2020: Inhibition of microsomal prostaglandin E synthase-1 (mPGES-1) by GS-248 reduces prostaglandin E2 biosynthesis while increasing prostacyclin in human subjects

Projects in other indications

Gesynta Pharma’s pipeline contains additional anti-inflammatory and vasoprotective compounds, which are based on the same unique mechanism of action as GS-248, but with different properties. Therefore, novel drugs candidates may be tailored with attributes suitable for specific indications. Gesynta Pharma’s broad project portfolio constitutes an attractive foundation which provides opportunities to establish high-quality collaborations, as well as a strong leverage in negotiations with potential licensees.


Gesynta Pharma’s drug candidate GS-073 is expected to enter clinical phase I in 2023. It is currently in the final stages of preclinical development.

Intellectual property

Gesynta Pharma has been granted patents for GS-248 in the United States, Europe, China, Japan and several additional important markets until 2031 (excluding potential patent extensions). Extended market exclusivity may be obtained for seven years after authorization in the United States and ten years in Europe.

Learn more about Gesynta Pharma

Gesynta Pharma bases its R&D on groundbreaking research from the Karolinska Institutet.

Our executive team and board of directors hold vast experience in drug development, commercialization and company scale-up.

Endometriosis is a chronic, inflammatory, estrogen-dependent disease affecting millions of women worldwide.

Our lead drug candidate GS-248 is currently under evaluation in a phase 2 study.