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sr-123781a
- Development stage
- Discontinued
- Lead developer
- Sanofi
- Modality
- Microbiome-Derived Products → Microbiome Therapeutics, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
- Administration
- Intravenous, Subcutaneous
01
Overview
SR-123781A is a synthetic hexadecasaccharide and heparin mimetic that acts as an anticoagulant by inhibiting both Factor IIa (thrombin) and Factor Xa. It was developed through convergent synthesis from glucose, incorporating an antithrombin binding domain, a thrombin binding domain, and a neutral methylated hexasaccharide sequence. SR-123781A binds with high affinity to human antithrombin (AT), catalyzing its inhibitory effects on factor Xa and thrombin, thereby preventing clot formation. Unlike standard heparins, it does not activate platelets in the presence of plasma from patients with heparin-induced thrombocytopenia. The drug demonstrated potent antithrombotic activity in preclinical models with a favorable safety profile compared to traditional anticoagulants. It was under investigation for the prevention and treatment of thrombosis, venous thromboembolism (VTE), and acute coronary syndromes but development has been discontinued[1][2][5][7].
- Other names
- UNII-V952P6826MUNII-V-952P6826MUNII-V 952P6826M
02
Targets
F2 (Thrombin)ATIII (Antithrombin III)F10 (Factor Xa)
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