Galapagos’ R&D Roundtable showcases Toledo program

• Comprehensive preclinical package elucidates dual mode of action (MoA) and potential broad applicability of salt-inducible kinase (SIK) inhibitors in inflammation
• Innovative chemistry generated multiple series of SIK compounds with distinct selectivity profiles, aimed at a range of inflammatory & fibrotic conditions
• Phase 1 data with SIK2/3 selective GLPG3970 confirm dose-dependent dual MoA effect
• Data package supports comprehensive clinical development of GLPG3970 in multiple Proof of Concept trials

Mechelen, Belgium; 27 October 2020, 16.15 CET – Galapagos NV (Euronext & NASDAQ: GLPG) unveils the Toledo target family as a series of salt-inducible kinase inhibitors. Toledo exhibits a dual mode of action characterized by enhanced transcription of anti-inflammatory cytokines and inhibited transcription of pro-inflammatory cytokines. Today, Galapagos also presents new preclinical and healthy volunteer data, and details its broad program to discover and develop multiple series of Toledo compounds with different selectivity profiles, aimed at treating a broad range of autoimmune conditions with important unmet medical need.

“The discovery of the SIK family of targets in our dual layer assays a number of years ago goes hand in hand with the scientific literature pointing to a dual mode of action of SIKs in inflammatory conditions,” said Dr. Piet Wigerinck, Chief Scientific Officer at Galapagos. “Galapagos developed innovative chemistry to address a number of selectivity profiles, and we now also show promising preclinical activity in fibrotic models, further broadening the scope of the Toledo program to a second disease paradigm where we built up substantial scientific know-how over the years. In  the Phase 1 trial, we have shown a favorable PK profile and confirmed the dual mode of action, observing a dose-dependent effect in ex vivo healthy volunteers with GLPG3970.”

“We generated the data package to take our first Toledo compound, GLPG3970, confidently into multiple proof of concept studies running in parallel. Currently the CALOSOMA study in psoriasis, the SEA TURTLE study in ulcerative colitis, and the LADYBUG study in rheumatoid arthritis are actively recruiting patients, and we aim to initiate two additional Phase 2 studies in Sjögren’s and systemic lupus erythematosus early next year,” said Dr. Walid Abi-Saab, Chief Medical Officer at Galapagos. “Furthermore, we continue to take a programmatic approach, cross-learning from the different proof-of-concept studies and biomarkers in our comprehensive development plan. Building up our knowledge with rapid signal detection studies, we aim to understand as well as maximize the potential of our Toledo program to become a new paradigm in the treatment of inflammatory and fibrotic diseases. Our development strategy is aimed at optimizing the route of GLPG3970 to the market.”