This week in therapeutics

Indication

Target/marker/pathway

Summary

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Cardiovascular disease

Arterial thrombosis; thrombosis

Purinergic receptor P2Y G protein-coupled 1 (P2RY1; P2Y1)

In vitro and rat studies have identified P2Y1 antagonists that could help treat thrombosis. Chemical synthesis, SAR and in vitro testing of ortho-anilino diaryl urea analogs identified several inhibitors of P2Y1 that blocked platelet aggregation ex vivo in human plasma at low nanomolar IC50 values. In rat models of arterial thrombosis and venous thrombosis, one compound decreased thrombus formation and increased blood flow compared with vehicle. Future work could include optimizing the bioavailability and other pharmacokinetic parameters of the lead compound.

SciBX 6(47); doi:10.1038/scibx.2013.1348
Published online Dec. 12, 2013

Patent and licensing status unavailable

Qiao, J.X. et al. J. Med. Chem.; published online Oct. 28, 2013;
doi:10.1021/jm4013906
Contact: Jennifer X. Qiao, Bristol-Myers Squibb Co., Pennington, N.J.
e-mail:
jennifer.qiao@bms.com