Chemistry:Stenoparib
Stenoparib, also known as 2X-121 and previously designated E7449, is an investigational new drug under evaluation for the treatment of advanced cancers, including ovarian cancer. It is an orally available small molecule that functions as a dual poly(ADP-ribose) polymerase (PARP) inhibitor (PARP1/2) and tankyrase inhibitor (tankyrase 1/2).[1][2] Stenoparib has not been approved by the U.S. Food and Drug Administration (FDA).[1]
Clinical development
Stenoparib has been evaluated in Phase 2 clinical trials for the treatment of COVID-19 and certain cancer types.[1] The drug has received FDA Fast Track designation, and development includes a companion diagnostic (Drug Response Predictor, DRP) intended to guide patient selection.
Pharmacology
Stenoparib combines two mechanisms of action: inhibition of PARP, which disrupts DNA repair in tumor cells, and inhibition of tankyrase, which interferes with Wnt/β-catenin signaling.[3]
Chemistry
2X-121 belongs to the class of quinazoline heterocycles with fused rings.[4]
References
- ↑ 1.0 1.1 1.2 "2x-121" (in en). PubChem. U.S. National Library of Medicine. https://pubchem.ncbi.nlm.nih.gov/compound/135565981.
- ↑ "Stenoparib (E7449) | 98.29%(HPLC) | PARP inhibitor" (in en). https://www.selleckchem.com/products/e7449.html.
- ↑ "E7449: A dual inhibitor of PARP1/2 and tankyrase1/2 inhibits growth of DNA repair deficient tumors and antagonizes Wnt signaling". Oncotarget 6 (38): 41307–41323. December 2015. doi:10.18632/oncotarget.5846. PMID 26513298.
- ↑ "2X-121" (in en). https://go.drugbank.com/drugs/DB16063.
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