losmapimod
Small moleculeexperimental
Losmapimod (GW856553X) is an investigational drug that reached stage III clinical trials for multiple medical conditions, but did not prove efficacy. It was most recently in development by Fulcrum Therapeutics for the treatment of facioscapulohumeral muscular dystrophy (FSHD). Losmapimod selectively inhibits enzymes p38α/β mitogen-activated protein kinases (MAPKs), which are modulators of DUX4 expression and mediators of inflammation. — Wikipedia
Clinical trial activity
28 trials · 6 clinical orgs · 0 marketing orgs
Phase 1
7
Phase 2
21
Phase 3
3
Phase 4
0
Earliest trial started Nov 1, 2005 (NCT00256919)
Timeline
Indications
Studied for
- Acute Coronary Syndrome · Phase 3
- Arthritis, Rheumatoid · Phase 2
- Atherosclerosis · Phase 2
- Cardiovascular Diseases · Phase 1
- COVID-19 · Phase 3
- Dyslipidemias · Phase 2
- Glomerulosclerosis, Focal Segmental · Phase 2
- Healthy Volunteers · Phase 2
- Major Depressive Disorder · Phase 2
- Muscular Dystrophies · Phase 3
- Neuralgia · Phase 2
- Pulmonary Disease, Chronic Obstructive · Phase 2
Mechanism of action
- MAP kinase p38 betaINHIBITOR
MAPK11 inhibitor
- MAP kinase p38 alphaINHIBITOR
MAPK14 inhibitor
Chemistry & pharmacology
Loading structure…
SMILES
Cc1c(F)cc(C(=O)NC2CC2)cc1-c1ccc(C(=O)NCC(C)(C)C)cn1- Mol. weight
- 383.47 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaLosmapimod ↗
- ChEMBLCHEMBL1088752 ↗
Also known as
- 6-(5-((cyclopropylamino)carbonyl)-3-fluoro-2-methylphenyl)-n-(2,2-dimethylprpyl)-3-pyridinecarboxamide
- gs856553
- gs856553
- gskahab
- gskahab
- gsk-ahab
- gw856553
- gw856553
- gw856553
- gw856553
- gw856553x
- gw856553x
- gw856553x
- losmapimod
- losmapimod
- losmapimod
- losmapimod
- losmapimod
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05397470 | Phase 3 | Jun 16, 2022 | Fulcrum Therapeutics |
| NCT05002231 | Phase 1 | Aug 19, 2021 | Fulcrum Therapeutics |
| NCT04511819 | Phase 3 | Aug 28, 2020 | Fulcrum Therapeutics |
| NCT04264442 | Phase 2 | Feb 29, 2020 | Fulcrum Therapeutics |
| NCT04004000 | Phase 2 | Jul 31, 2019 | Fulcrum Therapeutics |
| NCT04003974 | Phase 2 | Jul 31, 2019 | Fulcrum Therapeutics |
| NCT02299375 | Phase 2 | Dec 1, 2014 | GlaxoSmithKline |
| NCT02000440 | Phase 2 | Jul 1, 2014 | GlaxoSmithKline |
| NCT02145468 | Phase 3 | Jun 3, 2014 | GlaxoSmithKline, The TIMI Study Group |
| NCT01756495 | Phase 1 | Jan 10, 2013 | GlaxoSmithKline |
| NCT01648192 | Phase 1 | Jul 1, 2012 | GlaxoSmithKline |
| NCT01541852 | Phase 2 | Jun 1, 2012 | GlaxoSmithKline, Technology Strategy Board, United Kingdom, University of Cambridge, University of London |
| NCT01218126 | Phase 2 | Nov 1, 2010 | GlaxoSmithKline |
| NCT01039961 | Phase 1 | Feb 2, 2010 | GlaxoSmithKline |
| NCT01110057 | Phase 2 | Jan 7, 2010 | GlaxoSmithKline |
| NCT00910962 | Phase 2 | Oct 1, 2009 | GlaxoSmithKline |
| NCT00976560 | Phase 2 | Sep 25, 2009 | GlaxoSmithKline |
| NCT00969059 | Phase 2 | Aug 1, 2009 | GlaxoSmithKline |
| NCT00633022 | Phase 2 | Jun 1, 2008 | GlaxoSmithKline |
| NCT00642148 | Phase 2 | Feb 14, 2008 | GlaxoSmithKline |
Showing 20 of 28 trials
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Organizations
Research & Development (6)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| GlaxoSmithKline | For profit | 22 | 21 | 3 | 2005 |
| Fulcrum Therapeutics | For profit | 6 | 6 | 3 | 2019 |
| Technology Strategy Board, United Kingdom | Government | 1 | 0 | 1 | 2012 |
| The TIMI Study Group | Academic/Hospital | 1 | 0 | 1 | 2014 |
| University of Cambridge | Academic/Hospital | 1 | 1 | 1 | 2012 |
| University of London | Academic/Hospital | 1 | 0 | 1 | 2012 |
6 organizations
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