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Idiopathic pulmonary fibrosis

Galapagos is committed to establishing itself as a valued scientific partner in the race to combat idiopathic pulmonary fibrosis (IPF). We have a growing pipeline of new molecules with distinct modes of action which are moving rapidly in clinical development.


Ziritaxestat (GLPG1690)
Our most advanced molecule ziritaxestat is an oral, once daily autotaxin inhibitor currently in Phase 3 studies. We work together with our collaboration partner Gilead on the clinical development of ziritaxestat.

In December 2018, we dosed the first patient in ISABELA, a worldwide Phase 3 program to evaluate ziritexestat in IPF patients. The ISABELA program is intended to support both New Drug Application (NDA) and Market Authorization Application (MAA) submissions for ziritaxestat in respectively the US and EU. Read more at www.isabelastudies.com.

In the FLORA Phase 2a study with ziritaxestat in IPF patients, Galapagos reported a halt in disease progression, target engagement, and favorable safety and tolerability.

Ziritaxestat has been granted orphan status in IPF and systemic schlerosis (SSc) in Europe and the US. 

We reported achievement of the primary endpoint in the Phase 2 NOVESA trial with ziritaxestat in SSc patients in September 2020.


In July 2018, we announced the design for the PINTA Phase 2 trial with GLPG1205 in IPF, and recruitment was completed in January 2020. GLPG1205 is a GPR84 inhibitor discovered by and fully proprietary to us. GLPG1205 showed a reduction in signs and symptoms in IPF animal models and has shown favorable tolerability in healthy volunteers and in ulcerative colitis patients in previous trials. We expect to report topline results from PINTA in the second half of 2020.


Lung diseases like IPF are associated with an increased chitinase activity, which strongly correlates with disease stage, progression and prognosis. Chitinases (predominantly CHIT1) are involved in macrophage activation. Inhibition of chitinase activity translates into a potential therapeutic benefit, as shown in a range of preclinical models. GLPG4716 has shown robust anti-fibrotic activity in multiple animal models, when compared with the standard of care.

GLPG4716 (formerly OATD-01 inlicensed from OncoArendi) is a novel, small molecule CHIT1/AMCase inhibitor targeting a key pathway in tissue remodeling. It has shown compelling translational data, a favorable profile in animal studies at expected therapeutic doses and it has successfully completed Phase 1 studies in healthy volunteers. Galapagos aims to bring GLPG4716 to a Phase 2 clinical trial for the treatment of IPF and possibly other diseases with a fibrotic component.


Related publications

Rationale, Design and Objectives of Two Phase III, Randomized, Placebo-Controlled Studies of GLPG1690, a Novel Autotaxin Inhibitor, in Idiopathic Pulmonary Fibrosis (ISABELA 1 and 2), ATS 2019

A randomized, placebo-controlled, double blind Phase IIaclinical trial to assess the safety, tolerability, pharmacokinetics and pharmacodynamics of 12 weeks of treatment of an autotaxininhibitor (GLPG1690) in individuals with Idiopathic Pulmonary Fibrosis, ATS 2018

Assessment of the effects of GLPG1690 in idiopathic pulmonary disease (IPF) patients using functional respiratory imaging (FRI), ATS 2018

Pharmacodynamics and Pharmacokinetics of the Autotaxin Inhibitor GLPG1690 in the FLORA Trial: A Randomized, Placebo-Controlled, Double Blind Phase IIa Clinical Trial of 12 Weeks in Individuals, ATS 2018

Safety, tolerability, pharmacokinetics, and pharmacodynamics of GLPG1690, a novel autotaxin inhibitor, to treat idiopathic pulmonary fibrosis (FLORA): a phase 2a randomised placebo-controlled trial, The Lancet Respiratory Medicine, May 2018 

Autotaxin Inhibitor GLPG1690 Affects TGFβ-induced Production of the Pro-Fibrotic Mediators CTGF, IL-6 and ET-1 in Fibroblasts, ATS 2017

Discovery of GLPG1690, a First-in-Class Autotaxin Inhibitor Undergoing Clinical Evaluation for the Treatment of Idiopathic Pulmonary Fibrosis, Journal of Medical Chemistry, April 2017

Strong reversal of the lung fibrosis disease signature by autotaxin inhibitor GLPG1690 in a mouse model for IPF, ERS 2016

 Favorable human safety, PK/PD of the autotaxin inhibitor GLPG1690, a potential new treatment in IPF, ATS 2016

 Pharmacological profile and efficacy of GLPG1690, a novel autotaxin inhibitor for the treatment of IPF, ATS 2016

Discovery of GLPG1690: a first-in-class autotaxininhibitor in clinical development for the treatment of IPF at 251st American Chemical Society National Meeting 2016

Poster on pre-clinical data with GLPG1690 at ERS 2015

Oral presentation on pre-clinical data with GLPG1690 at ERS 2015

 Human safety, pharmacokinetics and pharmacodynamics of the GPR84 antagonist GLPG1205, ECCO 2015