Drug intelligence / Profile preview

otaplimastat + alteplase

Development stage
Phase 3
Lead developer
Shinpoong Pharma
Modality
Small Molecules, Recombinant Proteins and Enzymes
Administration
Intravenous
01

Overview

**Otaplimastat + alteplase** is an investigational combination therapy aimed at the treatment of **acute ischemic stroke**. Alteplase is a recombinant tissue plasminogen activator (rtPA), approved for thrombolytic therapy, that binds to fibrin in thrombi and converts plasminogen to plasmin, promoting clot dissolution. Otaplimastat (SP-8203) is a small molecule with a quinazoline-2,4-dione scaffold developed as a neuroprotectant; it functions primarily by inhibiting matrix metalloproteinases (MMPs) via upregulation of tissue inhibitor of metalloproteinase-1 (TIMP1), thereby reducing edema, hemorrhagic transformation, and neurotoxicity associated with delayed alteplase treatment. Preclinical and early clinical studies suggest that otaplimastat may extend the therapeutic window of alteplase and mitigate its adverse effects such as intracerebral hemorrhage and blood-brain barrier disruption[2][3].

Brand names
Cathflo
Other names
recombinant tissue plasminogen activatorrtPAtPA
02

Targets

Fibrin (Factor Ia)PLG (Plasminogen)FGA (Fibrinogen alpha chain)FGG (Fibrinogen gamma chain)MMP12 (Macrophage Metalloelastase)NMDAR (Glutamate receptor ionotropic, NMDA)

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