Office of Technology Transfer – University of Michigan

Mixed Disulfide Conjugates of Thienopyridines as Antiplatelet Agents

Technology #5574

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Researchers
Haoming Zhang
Managed By
Tiefei Dong
Senior Licensing Specialist, Life Sciences 734-763-5332
Patent Protection
US Patent Pending
US Patent 9,718,778

Current thienopyridines have side effects due to single-nucleotide polymorphism (SNP) of individuals and need 2-3 days to reach therapeutic concentration: Thienopyridinyl compounds are widely used as antiplatelet agents to prevent heart attack and stroke. In this category, clopidogrel (Plavix), ticlopidine (Ticlid) and prasugrel (Effient) are three commonly used prodrugs. These agents have to be activated by oxidization of polymorphic cytochromes P450 enzymes. This extra step leads to slow on-set of therapeutic effect and several adverse effects including neutropenia and thrombotic thrombocytopenic purpura.

Disulfide conjugates of thienopyridines have been developed to address this problem

These mixed conjugates are capable of releasing the active antiplatelet components in the presence of endogenous glutathione, and do not require bioactivation by P450s. Thus these conjugates can provide a therapy that is effective faster after administration and potentially with fewer side effects.

Applications and Advantages

  • First line or second line antiplatelet agents to prevent atherothrombotic events in cardiovascular, cerebrovascular and peripheral vascular disease.
  • Potentially reduce the side effects due to SNP.
  • Potentially need less time to reach to therapeutic concentration.