Foselutoclax
CAS 2271269-01-1
MF C53H59ClF3N6O10PS3 MW 1159.7 g/mol
(10R)-14-chloro-25-methyl-7,7-dioxo-10-[(phenylsulfanyl)methyl]-134-(phosphonooxy)-21-(propan-2-yl)-83-(trifluoromethanesulfonyl)-21H-7λ6-thia-6,9-diaza-4(1,4)-piperazina-13(1)-piperidina-2(2,3)-pyrrola-1(1),3(1,3),5,8(1,4)-tetrabenzenatridecaphane-24-carboxylic acid
5-(4-chlorophenyl)-2-methyl-4-[3-[4-[4-[[4-[[(2R)-1-phenylsulfanyl-4-(4-phosphonooxypiperidin-1-yl)butan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylamino]phenyl]piperazin-1-yl]phenyl]-1-propan-2-ylpyrrole-3-carboxylic acid
B-cell lymphoma 2 (Bcl-2) inhibitor, antineoplastic, VT53CL5GES, UBX 1325
Foselutoclax is an investigational new drug that is being evaluated for the treatment of age-related eye diseases, particularly diabetic macular edema (DME) and wet age-related macular degeneration (AMD). Developed by Unity Biotechnology, this senolytic compound acts as a potent inhibitor of Bcl-xL, a protein that senescent cells rely on for survival.[1] Foselutoclax is designed to selectively eliminate senescent cells in the retina, potentially addressing the underlying causes of vision loss in these conditions.[2]
- Assess the Efficacy and Safety of Repeat Intravitreal Injections of Foselutoclax (UBX1325) in Patients With DME (ASPIRE)CTID: NCT06011798Phase: Phase 2Status: CompletedDate: 2025-08-05
- Safety, Tolerability and Evidence of Activity Study of UBX1325 in Patients With Diabetic Macular Edema (BEHOLD)CTID: NCT04857996Phase: Phase 2Status: CompletedDate: 2024-05-16
- Safety and Tolerability Study of UBX1325 in Patients With Diabetic Macular Edema or Neovascular Age-Related Macular DegenerationCTID: NCT04537884Phase: Phase 1Status: CompletedDate: 2022-03-10
REF
- Therapeutic targeting of cellular senescence in diabetic macular edema: preclinical and phase 1 trial resultsPublication Name: Nature MedicinePublication Date: 2024-02PMID: 38321220DOI: 10.1038/s41591-024-02802-4
- Senolytics in the treatment of diabetic retinopathyPublication Name: Frontiers in PharmacologyPublication Date: 2022-08-26PMCID: PMC9462063PMID: 36091769DOI: 10.3389/fphar.2022.896907
- Senolytic drugs: from discovery to translationPublication Name: Journal of Internal MedicinePublication Date: 2020-08-04PMCID: PMC7405395PMID: 32686219DOI: 10.1111/joim.13141
- bcl-x, a bcl-2-related gene that functions as a dominant regulator of apoptotic cell deathPublication Name: CellPublication Date: 1993-08-27PMID: 8358789DOI: 10.1016/0092-8674(93)90508-n
PAT
Treatment of Lung Diseases Using Pharmaceutical Agents that Eliminate Senescent Cells
Publication Number: US-2020354336-A9
Priority Date: 2017-08-11
- Senescent Cells and for Treating CancerPublication Number: US-2022017485-A1Priority Date: 2018-06-13
- Acyl sulfonamides that are bcl family antagonists for use in clinical management of conditions caused or mediated by senescent cells and for treating cancerPublication Number: EP-4335516-A2Priority Date: 2018-06-13
- Methods of Inhibiting Pathological AngiogenesisPublication Number: US-2020253991-A1Priority Date: 2017-10-31
- Methods of inhibiting pathological angiogenesisPublication Number: US-11129838-B2Priority Date: 2017-10-31Grant Date: 2021-09-28
- Treatment of Lung Diseases Using Pharmaceutical Agents that Eliminate Senescent CellsPublication Number: US-2020199103-A1Priority Date: 2017-08-11
SYN
https://patentscope.wipo.int/search/en/detail.jsf?docId=US279621490&_cid=P21-MGPXU3-15237-1
SYN
https://patentscope.wipo.int/search/en/detail.jsf?docId=US421382898&_cid=P21-MGPXWE-19244-1
A crystalline solid meglumine salt of of (R)-5-(4-chlorophenyl)-1-isopropyl-2-methyl-4-(3-(4-(4-((4-((1-(phenylthio)-4-(4-((phosphonooxy)methyl)piperidin-1-yl)butan-2-yl)amino)-3-((trifluoromethyl)sulfonyl)phenyl)sulfonamido)phenyl)piperazin-1-yl)phenyl)-1H-pyrrole-3-carboxylic acid, the compound of Formula I:
SYN
https://patentscope.wipo.int/search/en/detail.jsf?docId=US348024244&_cid=P21-MGPXWE-19244-1
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| Clinical data | |
|---|---|
| Other names | UBX1325 |
| Identifiers | |
| IUPAC name | |
| CAS Number | 2271269-01-1 |
| PubChem CID | 147562879 |
| IUPHAR/BPS | 13366 |
| ChemSpider | 115277082 |
| UNII | VT53CL5GES |
| Chemical and physical data | |
| Formula | C53H59ClF3N6O10PS3 |
| Molar mass | 1159.69 g·mol−1 |
| 3D model (JSmol) | Interactive image |
| SMILES | |
| InChI | |
References
- Crago SM (22 June 2023). “Design for Phase 2B ASPIRE Study of UBX1325 for DME announced by UNITY”. Modern Retina. Archived from the original on 13 August 2024.
- Macha N, Yu M, Sapieha P, Klier S, Ghosh A, White L, et al. (September 2024). “Multifocal Electroretinography Changes after UBX1325 (Foselutoclax) Treatment in Neovascular Age-Related Macular Degeneration”. Journal of Clinical Medicine. 13 (18): 5540. doi:10.3390/jcm13185540. PMC 11433175. PMID 39337030.
//////////foselutoclax, antineoplastic, VT53CL5GES, UBX 1325