Stenoparib

Stenoparib
Clinical data
Other names	2X-121, E7449, E-7449
Identifiers
	IUPAC name 11-(1,3-dihydroisoindol-2-ylmethyl)-2,3,10,12-tetrazatricyclo[7.3.1.05,13]trideca-1,5(13),6,8,11-pentaen-4-one;
CAS Number	1140964-99-3;
PubChem CID	135565981;
DrugBank	DB16063;
ChemSpider	35308197;
UNII	9X5A2QIA7C;
ChEMBL	ChEMBL3644587;
Chemical and physical data
Formula	C18H15N5O
Molar mass	317.352 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES O=C1NN=C2NC(CN3CC4=C(C3)C=CC=C4)=NC3=C2C1=CC=C3;
	InChI InChI=1S/C18H15N5O/c24-18-13-6-3-7-14-16(13)17(21-22-18)20-15(19-14)10-23-8-11-4-1-2-5-12(11)9-23/h1-7H,8-10H2,(H,22,24)(H,19,20,21); Key:JLFSBHQQXIAQEC-UHFFFAOYSA-N;

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

Stenoparib belongs to the class of quinazoline heterocycles with fused rings.^[4]

References

1 2 3 "2x-121". PubChem. U.S. National Library of Medicine. Retrieved 2025-09-06.
↑ "Stenoparib (E7449) | 98.29%(HPLC) | PARP inhibitor". selleckchem.com. Retrieved 2025-09-06.
↑ McGonigle S, Chen Z, Wu J, Chang P, Kolber-Simonds D, Ackermann K, Twine NC, Shie JL, Miu JT, Huang KC, Moniz GA, Nomoto K (December 2015). "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. doi:10.18632/oncotarget.5846. PMC 4747407. PMID 26513298.
↑ "2X-121". go.drugbank.com. Retrieved 2025-09-06.

[:0-1] 1 2 3 "2x-121". PubChem. U.S. National Library of Medicine. Retrieved 2025-09-06.

[2] "Stenoparib (E7449) | 98.29%(HPLC) | PARP inhibitor". selleckchem.com. Retrieved 2025-09-06.

[McGonigle_2015-3] McGonigle S, Chen Z, Wu J, Chang P, Kolber-Simonds D, Ackermann K, Twine NC, Shie JL, Miu JT, Huang KC, Moniz GA, Nomoto K (December 2015). "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. doi:10.18632/oncotarget.5846. PMC 4747407. PMID 26513298.

[4] "2X-121". go.drugbank.com. Retrieved 2025-09-06.

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