vipoglanstat (GS-248) / Orexo, Gesynta Pharma - LARVOL DELTA

A Study to Investigate Safety of GS-248 and Efficacy on Raynauds' Phenomenon in Systemic Sclerosis (clinicaltrials.gov) - P2 | N=94 | Completed | Sponsor: Gesynta Pharma AB | N=69 ➔ 94

Enrollment change • Cardiovascular • Immunology • Rheumatology • Scleroderma • Systemic Sclerosis

Vipoglanstat, a novel non-hormonal treatment in development for endometriosis targeting selective mPGES-1 inhibition (SEUD 2024) - No abstract available

Endometriosis • Gynecology • Women's Health

Orexo : partner Gesynta Pharma has announced phase II study results from the OX-MPI (GS-248) project (Market Screener) - P2 | N=69 | NCT04744207 | Sponsor: Gesynta Pharma AB | "Orexo's partner Gesynta Pharma, who owns all the rights to OX-MPI (GS-248), has recently announced the results from the exploratory phase II study in patients with systemic sclerosis. According to Gesynta Pharma, OX-MPI (GS-248) was tolerated well by patients and showed a good safety profile. A potent systemic inhibition of the target enzyme mPGES-1 was also displayed. However, no significant effects on the patients' symptoms could be demonstrated."

P2 data • Immunology • Systemic Sclerosis

"Ready for the First Time Disclosure of Clinical Candidate BI01029539 / GS-248, a mPGES1 Inhibitor @Boehringer #EFMCISMC22" (@EuroMedChem)

Clinical

A Study to Investigate Safety of GS-248 and Efficacy on Raynauds' Phenomenon in Systemic Sclerosis (clinicaltrials.gov) - P2 | N=69 | Completed | Sponsor: Gesynta Pharma AB | Active, not recruiting ➔ Completed

Trial completion • Cardiovascular • Fibrosis • Immunology • Rheumatology • Scleroderma • Systemic Sclerosis

A Study to Investigate Safety of GS-248 and Efficacy on Raynauds' Phenomenon in Systemic Sclerosis (clinicaltrials.gov) - P2 | N=80 | Active, not recruiting | Sponsor: Gesynta Pharma AB | Recruiting ➔ Active, not recruiting

Enrollment closed • Cardiovascular • Fibrosis • Immunology • Rheumatology • Scleroderma • Systemic Sclerosis

Orexo´s partner Gesynta Pharma granted Orphan Drug Designation by the FDA for OX-MPI (GS-248) for the treatment of systemic sclerosis (PRNewswire) - "Orexo AB...announces today that the company´s partner Gesynta Pharma AB which owns all the rights to OX-MPI (GS248), a drug candidate for the treatment of systemic sclerosis, has been granted Orphan Drug Designation in the US by the Food and Drug Administration (FDA)....The drug candidate is currently being evaluated in a clinical phase 2 trial and data is expected in late 2022."

Orphan drug • P2 data • Immunology • Systemic Sclerosis

A Study to Investigate Safety of GS-248 and Efficacy on Raynauds' Phenomenon in Systemic Sclerosis (clinicaltrials.gov) - P2 | N=80 | Recruiting | Sponsor: Gesynta Pharma AB | Trial completion date: Feb 2022 ➔ Jun 2022 | Trial primary completion date: Feb 2022 ➔ Jun 2022

Trial completion date • Trial primary completion date • Cardiovascular • Fibrosis • Immunology • Rheumatology • Scleroderma • Systemic Sclerosis

A Study to Investigate Safety of GS-248 and Efficacy on Raynauds' Phenomenon in Systemic Sclerosis (clinicaltrials.gov) - P2; N=80; Recruiting; Sponsor: Gesynta Pharma AB; Trial completion date: Jun 2021 ➔ Dec 2021; Trial primary completion date: Jun 2021 ➔ Dec 2021

Clinical • Trial completion date • Trial primary completion date • Cardiovascular • Fibrosis • Immunology • Rheumatology • Scleroderma • Systemic Sclerosis

Inhibition of microsomal prostaglandin E synthase-1 ameliorates acute lung injury in mice. (PubMed, J Transl Med) - "BI 1029539 ameliorates leukocyte infiltration and lung injury resulting from both endotoxin-induced and sepsis-induced lung injury."

Journal • Preclinical • Acute Lung Injury • Infectious Disease • Respiratory Diseases • Septic Shock • IL1B • MPO

Gesynta Pharma announces significant progress across development program for first-in-class drug candidate GS-248 (Gesynta Pharma Press Release) - "Gesynta Pharma AB today announced that an IND (Investigational New Drug Application) has been submitted to the U.S. Food & Drug Administration for its oral drug candidate GS-248 in patients with systemic sclerosis. Concurrently, more than half of the patients in the ongoing Phase II study in four countries across Europe have been recruited. The study investigates the safety of GS-248 and its efficacy on Raynaud’s phenomenon and peripheral vascular blood flow. Top-line data is expected in Q1/2022."

Enrollment status • IND • P2 data • Immunology • Systemic Sclerosis

"Gesynta Pharma rapporterar betydande framsteg i utvecklingsprogrammet för läkemedelskandidaten GS-248 https://t.co/i8L8RCaYAS" (@CisionNews)

A Study to Investigate Safety of GS-248 and Efficacy on Raynauds' Phenomenon in Systemic Sclerosis (clinicaltrials.gov) - P2; N=80; Recruiting; Sponsor: Gesynta Pharma AB

Clinical • New P2 trial • Fibrosis • Immunology • Rheumatoid Arthritis • Scleroderma • Systemic Sclerosis

"Gesynta Pharma inleder fas II-studie med sin läkemedelskandidat GS-248 i patienter med systemisk skleros https://t.co/sOM4px0Fmu" (@CisionNews)

Clinical

A Study in Healthy Subjects to Evaluate Pharmacokinetics and Food Effect After Dosing of GS-248 (clinicaltrials.gov) - P1; N=14; Completed; Sponsor: Gesynta Pharma AB

Clinical • New P1 trial

Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of GS-248 (clinicaltrials.gov) - P1; N=72; Completed; Sponsor: Gesynta Pharma AB; Recruiting ➔ Completed; Trial completion date: Jun 2020 ➔ Dec 2019; Trial primary completion date: Jun 2020 ➔ Dec 2019

Clinical • Trial completion • Trial completion date • Trial primary completion date • Fibrosis • Immunology • Scleroderma • Systemic Sclerosis

Gesynta raises SEK 190 million in round led by Hadean Ventures to accelerate development of first-in-class mPGES-1 inhibitor GS-248 for systemic sclerosis (Gesynta Pharma Press Release) - "Gesynta Pharma AB...today announced that it has successfully raised SEK 190 million in one of the largest private biotech placements of the year in the Nordics....The investment enables Gesynta to fund continued development of lead candidate GS-248 in systemic sclerosis patients. Following a successful Phase I study recently reported at EULAR2020...now scheduled to enter a multi-centre Phase IIa study in Q4, 2020."

Financing • New P2a trial • Immunology • Systemic Sclerosis

[VIRTUAL] INHIBITION OF MICROSOMAL PROSTAGLANDIN E SYNTHASE-1 (MPGES-1) BY GS-248 REDUCES PROSTAGLANDIN E2 BIOSYNTHESIS WHILE INCREASING PROSTACYCLIN IN HUMAN SUBJECTS (EULAR 2020) - "GS-248 at investigated oral doses was safe and well tolerated. There was a sustained inhibition of LPS induced PGE 2 formation in whole blood. In urine, there was a metabolite shift showing reduced PGE 2 and increased PGI 2 , while celecoxib reduced both PGE 2 and PGI 2 metabolites."

Clinical • Immunology • Scleroderma • Systemic Sclerosis

Inhibition of human microsomal PGE2 synthase-1 reduces seizure-induced increases of P-glycoprotein expression and activity at the blood-brain barrier. (PubMed, FASEB J) - "We show that BI1029539, an mPGES-1 inhibitor, prevented up-regulation of P-gp expression and transport activity in capillaries exposed to glutamate and in capillaries from humanized mPGES-1 mice after SE. Our data provide key signaling steps underlying seizure-induced P-gp up-regulation and suggest that mPGES-1 inhibitors could potentially prevent P-gp up-regulation in epilepsy.-Soldner, E. L. B., Hartz, A. M. S., Akanuma, S.-I., Pekcec, A., Doods, H., Kryscio, R. J., Hosoya, K.-I., Bauer, B. Inhibition of human microsomal PGE2 synthase-1 reduces seizure-induced increases of P-glycoprotein expression and activity at the blood-brain barrier."

Journal • CNS Disorders • Epilepsy