azeliragon
RAGE, also called AGER, is a 35 kilodalton transmembrane receptor of the immunoglobulin super family which was first characterized in 1992 by Neeper et al. Its name comes from its ability to bind advanced glycation end-products (AGEs), which include chiefly glycoproteins, the glycans of which have been modified non-enzymatically through the Maillard reaction. In view of its inflammatory function in innate immunity and its ability to detect a class of ligands through a common structural motif, RAGE is often referred to as a pattern recognition receptor. RAGE also has at least one other agonistic ligand: high mobility group protein B1 (HMGB1). HMGB1 is an intracellular DNA-binding protein important in chromatin remodeling which can be released by necrotic cells passively, and by active secretion from macrophages, natural killer cells, and dendritic cells. — Wikipedia
Clinical trial activity
15 trials · 14 clinical orgs · 0 marketing orgs
Earliest trial started Oct 1, 2005 (NCT00141661)
Timeline
Indications
Studied for
Mechanism of action
Advanced glycosylation end product-specific receptor antagonist
AGER inhibitor
Chemistry & pharmacology
SMILES
CCCCc1nc(-c2ccc(OCCCN(CC)CC)cc2)cn1-c1ccc(Oc2ccc(Cl)cc2)cc1- Mol. weight
- 532.13 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaRAGE (receptor) ↗
- ChEMBLCHEMBL3989929 ↗
Also known as
- azeliragon
- azeliragon
- azeliragon
- pf-04494700
- pf-04494700
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06831526 | Early Phase 1 (Phase 1) | May 31, 2025 | Cantex Pharmaceuticals, Washington University in St. Louis |
| NCT06724926 | Phase 1 | Jan 31, 2025 | New York University |
| NCT05773664 | Phase 1 | Dec 15, 2023 | City of Hope National Medical Center, National Cancer Institute (NCI) |
| NCT05986851 | Phase 2 | Sep 12, 2023 | Cantex Pharmaceuticals, Medpace, Inc. |
| NCT05789589 | Phase 1/Phase 2 (Phase 2) | Aug 16, 2023 | Baptist Health, Cantex Pharmaceuticals, Miami Cancer Institute |
| NCT05766748 | Phase 1/Phase 2 (Phase 2) | Jun 1, 2023 | Cantex Pharmaceuticals |
| NCT05815485 | Phase 2/Phase 3 (Phase 3) | May 4, 2023 | University of Michigan |
| NCT05635734 | Phase 1/Phase 2 (Phase 2) | Dec 31, 2022 | Cantex Pharmaceuticals, Universidad Complutense de Madrid |
| NCT05256745 | Phase 1/Phase 2 (Phase 2) | Nov 30, 2022 | Georgetown University |
| NCT03980730 | Phase 2/Phase 3 (Phase 3) | Jun 27, 2019 | vTv Therapeutics |
| NCT02916056 | Phase 3 | Dec 1, 2016 | vTv Therapeutics |
| NCT02080364 | Phase 3 | Apr 1, 2015 | vTv Therapeutics |
| NCT00566397 | Phase 2 | Dec 1, 2007 | National Institute on Aging (NIA), Pfizer |
| NCT00287183 | Phase 2 | Feb 1, 2006 | Pfizer |
| NCT00141661 | Phase 2 | Oct 1, 2005 | Pfizer, vTv Therapeutics |
Organizations
Research & Development (14)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Cantex Pharmaceuticals | For profit | 5 | 3 | 2 | 2022 |
| vTv Therapeutics | For profit | 4 | 3 | 2 | 2005 |
| Pfizer | For profit | 3 | 3 | 1 | 2005 |
| Baptist Health | Academic/Hospital | 1 | 1 | 1 | 2023 |
| City of Hope National Medical Center | Academic/Hospital | 1 | 1 | 1 | 2023 |
| Georgetown University | Academic/Hospital | 1 | 1 | 1 | 2022 |
| Medpace, Inc. | For profit | 1 | 0 | 1 | 2023 |
| Miami Cancer Institute | Academic/Hospital | 1 | 0 | 1 | 2023 |
| National Cancer Institute (NCI) | Government | 1 | 0 | 1 | 2023 |
| National Institute on Aging (NIA) | Government | 1 | 0 | 1 | 2007 |
| New York University | Academic/Hospital | 1 | 1 | 1 | 2025 |
| Universidad Complutense de Madrid | Academic/Hospital | 1 | 0 | 1 | 2022 |
| University of Michigan | Academic/Hospital | 1 | 1 | 1 | 2023 |
| Washington University in St. Louis | Academic/Hospital | 1 | 1 | 1 | 2025 |