vidofludimus   Click here for help

GtoPdb Ligand ID: 9860

Synonyms: 4SC-101 | IMU-838 (vidofludimus calcium) | SC12267
PDB Ligand Immunopharmacology Ligand
Compound class: Synthetic organic
Comment: Vidofludimus (4SC-101) is a small molecule dihydroorotate dehydrogenase (DHOD) inhibitor that was developed for immunosuppressive potential [3]. It has an improved toxicity profile in comparison to the clinically used disease modifying anti-rheumatic drug (DMARD) leflunomide.
Since its initial development, vidofludimus has been superceded by IMU-838 which is an orally active polymorph of vidofludimus calcium (PubChem CID: 56944639) [5].SARS-CoV-2 and COVID-19: The target of vidofludimus, DHODH, plays a role in the metabolism of activated T cells and B cells to regulate the inflammatory response. It has been advanced to clinical trial in patients with severe COVID-19, to as attempt to block the release of pro-inflammatory cytokines and temper hyperinflammation in these patients.
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 4
Hydrogen bond donors 2
Rotatable bonds 6
Topological polar surface area 75.63
Molecular weight 355.12
XLogP 3.34
No. Lipinski's rules broken 0
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Canonical SMILES COc1cccc(c1)c1ccc(c(c1)F)NC(=O)C1=C(CCC1)C(=O)O
Isomeric SMILES COc1cccc(c1)c1ccc(c(c1)F)NC(=O)C1=C(CCC1)C(=O)O
InChI InChI=1S/C20H18FNO4/c1-26-14-5-2-4-12(10-14)13-8-9-18(17(21)11-13)22-19(23)15-6-3-7-16(15)20(24)25/h2,4-5,8-11H,3,6-7H2,1H3,(H,22,23)(H,24,25)
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Summary of Clinical Use Click here for help
Phase 2 clinical trials designed to determine the clinical efficacy of the original formulation, 4SC-101 in inflammatory bowel disease and rheumatoid arthritis have been completed. Published results from the IBD trial NCT00820365 are indicative of clinical efficacy in this indication [2]. Vidofludimus missed the primary endpoint in a Phase 2b RA trial. A new formulation of vidofludimus known as IMU-838 has replaced the original agent, and this is under active evaluation for clinical efficacy in ulcerative colitis, primary sclerosing cholangitis, multiple sclerosis [6] and COVID-19.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT04379271 A Study to Evaluate the Efficacy, Safety and Tolerability of IMU-838 as Addition to Investigator's Choice of Standard of Care Therapy, in Patients With Coronavirus Disease 19 (COVID-19) Phase 2/Phase 3 Interventional Immunic AG
NCT03722576 Vidofludimus Calcium for Primary Sclerosing Cholangitis Phase 2 Interventional Mayo Clinic
NCT03341962 Phase 2 Dose-finding IMU-838 for Ulcerative Colitis Phase 2 Interventional Immunic AG
NCT03846219 MRI Trial to exPlore the efficAcy and Safety of IMU-838 in Relapsing Remitting Multiple Sclerosis (EMPhASIS) Phase 2 Interventional Immunic AG Immunic have informally reported that IMU-838 (vidofludimus calcium, treatment for 6 months) has significant anti-demyelination efficacy in patients with RR MS (determined by MRI as a decrease in brain lesions). This trial includes the availability of an extension phase through which patients can choose to keep receiving treatment for up to nine and a half years.