Drug candidates with a unique mechanism of action

Gesynta Pharma’s drug candidates utilize a unique mechanism of action to reduce inflammation while simultaneously increasing blood flow through vasodilation. 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 leads to increased vasodilation

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, while a simultaneous shunting mechanism leads to increased levels of the vasoprotective mediator prostacyclin. Prostacyclin is primarily produced in the walls of blood vessels and is one of the body’s most potent vasodilating mediators. Gesynta Pharma’s drug candidates leverage on their unique mechanism to decrease the inflammatory PGE2 and increase the vasoprotective prostacyclin.

Read more about microvascular dysfunction, mPGES-1 and PGE2 here.

GS-248 potently inhibits mPGES-1

GS-248 is Gesynta Pharma’s most advanced drug candidate, currently in clinical development as a potential treatment of systemic sclerosis. Recent 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-daily oral dose is sufficient to maintain the therapeutic effect over 24 hours, which enables a convenient and patient-friendly administration.

Gesynta Pharma is currently conducting a placebo-controlled clinical study in order to document the safety and efficacy profile of GS-248 during a four-week-treatment in circa 80 patients. The participants have been diagnosed with systemic sclerosis and exhibit recurrent Raynaud’s phenomenon. The study is primarily tracking patients’ symptoms, including the frequency of Raynaud attacks, but also documenting digital blood flow as well as inflammatory biomarkers. The study, which is conducted in four European countries, is coordinated by the University of Manchester Centre for Musculoskeletal Research. Initial study results are expected in 2022. The results will contribute with important insights not only for the continued development of GS-248 in systemic sclerosis, but also for its potential development in other inflammatory diseases.

Provided a satisfactory outcome of the current study, Gesynta will move forward with a clinical Phase IIb study to further document the efficacy of GS-248 in reducing the incidence of Raynaud’s phenomenon as well as digital ulcers in patients with systemic sclerosis. Following a satisfactory Phase IIb study, the company will seek the optimum solution to bring GS-248 to regulatory approval and launch. This can be done by the company alone, or together with a strategic partner.

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. The company is continuously exploring drug development in medical conditions associated with microvascular dysfunction, including complex chronic inflammatory diseases and conditions with manifested cardiovascular complications. 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 2022. It is currently in the final stages of preclinical development. This project will be addressing an indication with high unmet need, which is separate from systemic sclerosis.


The drug candidate GS-659, which is sprung from Gesynta Pharma’s drug development platform, is currently in preclinical development phase. Project updates will be announced in due course.

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. Treatments of systemic sclerosis are classified by regulatory authorities as orphan drugs. GS-248 has been granted Orphan Drug Designation in the US by the FDA for the treatment of systemic sclerosis. The designation may provide increased opportunities for long-term market exclusivity as well as advantages in the regulatory market approval process

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.

Systemic sclerosis is an autoimmune disease hallmarked by chronic inflammation in the body’s smallest blood vessels.

Raynaud’s phenomenon affects most systemic sclerosis patients. It is often the first sign of the disease.

Half of systemic sclerosis patients develop difficult-to-heal digital ulcers, hampering many everyday activities.

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