Asundexian

Asundexian
Legal status
Legal status	Investigational;
Identifiers
	IUPAC name 4-[[(2S)-2-[4-[5-Chloro-2-[4-(trifluoromethyl)triazol-1-yl]phenyl]-5-methoxy-2-oxopyridin-1-yl]butanoyl]amino]-2-fluorobenzamide;
CAS Number	2064121-65-7;
PubChem CID	135206011;
ChemSpider	115009501;
UNII	LA585UM8DE;
Chemical and physical data
Formula	C26H21ClF4N6O4
Molar mass	592.94 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC[C@@H](C(=O)NC1=CC(=C(C=C1)C(=O)N)F)N2C=C(C(=CC2=O)C3=C(C=CC(=C3)Cl)N4C=C(N=N4)C(F)(F)F)OC;
	InChI InChI=1S/C26H21ClF4N6O4/c1-3-19(25(40)33-14-5-6-15(24(32)39)18(28)9-14)36-11-21(41-2)17(10-23(36)38)16-8-13(27)4-7-20(16)37-12-22(34-35-37)26(29,30)31/h4-12,19H,3H2,1-2H3,(H2,32,39)(H,33,40)/t19-/m0/s1; Key:XYWIPYBIIRTJMM-IBGZPJMESA-N;

Asundexian is a Factor XIa inhibitor developed by Bayer to prevent stroke.^[1]^[2]^[3]^[4]

References

↑ Piccini, Jonathan P; Caso, Valeria; Connolly, Stuart J; et al. (April 2022). "Safety of the oral factor XIa inhibitor asundexian compared with apixaban in patients with atrial fibrillation (PACIFIC-AF): a multicentre, randomised, double-blind, double-dummy, dose-finding phase 2 study". The Lancet. 399 (10333): 1383–1390. doi:10.1016/S0140-6736(22)00456-1. hdl:11379/560377. PMID 35385695.
↑ Rao, Sunil V.; Kirsch, Bodo; Bhatt, Deepak L.; et al. (18 October 2022). "A Multicenter, Phase 2, Randomized, Placebo-Controlled, Double-Blind, Parallel-Group, Dose-Finding Trial of the Oral Factor XIa Inhibitor Asundexian to Prevent Adverse Cardiovascular Outcomes After Acute Myocardial Infarction". Circulation. 146 (16): 1196–1206. doi:10.1161/CIRCULATIONAHA.122.061612. PMID 36030390. S2CID 251882310.
↑ Heitmeier, Stefan; Visser, Mayken; Tersteegen, Adrian; Dietze‐Torres, Julia; Glunz, Julia; Gerdes, Christoph; Laux, Volker; Stampfuss, Jan; Roehrig, Susanne (June 2022). "Pharmacological profile of asundexian, a novel, orally bioavailable inhibitor of factor XIa". Journal of Thrombosis and Haemostasis. 20 (6): 1400–1411. doi:10.1111/jth.15700. PMC 9313898. PMID 35289054.
↑ Shoamanesh, Ashkan; Mundl, Hardi; Smith, Eric E; Masjuan, Jaime; Milanov, Ivan; Hirano, Teruyuki; Agafina, Alina; Campbell, Bruce; Caso, Valeria; Mas, Jean-Louis; Dong, Qiang; Turcani, Peter; Christensen, Hanne; Ferro, Jose M; Veltkamp, Roland; Mikulik, Robert; De Marchis, Gian Marco; Robinson, Thompson; Lemmens, Robin; Stepien, Adam; Greisenegger, Stefan; Roine, Risto; Csiba, Laszlo; Khatri, Pooja; Coutinho, Jonathan; Lindgren, Arne G; Demchuk, Andrew M; Colorado, Pablo; Kirsch, Bodo; Neumann, Christoph; Heenan, Laura; Xu, Lizhen; Connolly, Stuart J; Hart, Robert G (September 2022). "Factor XIa inhibition with asundexian after acute non-cardioembolic ischaemic stroke (PACIFIC-Stroke): an international, randomised, double-blind, placebo-controlled, phase 2b trial". The Lancet. 400 (10357): 997–1007. doi:10.1016/S0140-6736(22)01588-4. PMID 36063821. S2CID 252035902.

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[1] Piccini, Jonathan P; Caso, Valeria; Connolly, Stuart J; et al. (April 2022). "Safety of the oral factor XIa inhibitor asundexian compared with apixaban in patients with atrial fibrillation (PACIFIC-AF): a multicentre, randomised, double-blind, double-dummy, dose-finding phase 2 study". The Lancet. 399 (10333): 1383–1390. doi:10.1016/S0140-6736(22)00456-1. hdl:11379/560377. PMID 35385695.

[2] Rao, Sunil V.; Kirsch, Bodo; Bhatt, Deepak L.; et al. (18 October 2022). "A Multicenter, Phase 2, Randomized, Placebo-Controlled, Double-Blind, Parallel-Group, Dose-Finding Trial of the Oral Factor XIa Inhibitor Asundexian to Prevent Adverse Cardiovascular Outcomes After Acute Myocardial Infarction". Circulation. 146 (16): 1196–1206. doi:10.1161/CIRCULATIONAHA.122.061612. PMID 36030390. S2CID 251882310.

[3] Heitmeier, Stefan; Visser, Mayken; Tersteegen, Adrian; Dietze‐Torres, Julia; Glunz, Julia; Gerdes, Christoph; Laux, Volker; Stampfuss, Jan; Roehrig, Susanne (June 2022). "Pharmacological profile of asundexian, a novel, orally bioavailable inhibitor of factor XIa". Journal of Thrombosis and Haemostasis. 20 (6): 1400–1411. doi:10.1111/jth.15700. PMC 9313898. PMID 35289054.

[4] Shoamanesh, Ashkan; Mundl, Hardi; Smith, Eric E; Masjuan, Jaime; Milanov, Ivan; Hirano, Teruyuki; Agafina, Alina; Campbell, Bruce; Caso, Valeria; Mas, Jean-Louis; Dong, Qiang; Turcani, Peter; Christensen, Hanne; Ferro, Jose M; Veltkamp, Roland; Mikulik, Robert; De Marchis, Gian Marco; Robinson, Thompson; Lemmens, Robin; Stepien, Adam; Greisenegger, Stefan; Roine, Risto; Csiba, Laszlo; Khatri, Pooja; Coutinho, Jonathan; Lindgren, Arne G; Demchuk, Andrew M; Colorado, Pablo; Kirsch, Bodo; Neumann, Christoph; Heenan, Laura; Xu, Lizhen; Connolly, Stuart J; Hart, Robert G (September 2022). "Factor XIa inhibition with asundexian after acute non-cardioembolic ischaemic stroke (PACIFIC-Stroke): an international, randomised, double-blind, placebo-controlled, phase 2b trial". The Lancet. 400 (10357): 997–1007. doi:10.1016/S0140-6736(22)01588-4. PMID 36063821. S2CID 252035902.

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