Gabexatum
Gabexatum Uses, Dosage, Side Effects, Food Interaction and all others data.
Gabexatum is a synthetic serine protease inhibitor which has been used as an anticoagulant. It also known to decrease production of inflammatory cytokines. Gabexatum has been investigated for use in cancer, ischemia-reperfusion injury, and pancreatitis.
Gabexatum bind and inhibits serine proteases in the coagulation cascade to prevent blood clotting. It also prevents proteolytic destruction of IkappaB resulting in suppression of the nuclear factor kappa-B signalling pathway. Ultimately this decreases the production of inflammatory cytokines such as tumor necrosis factor alpha which are produced as a result of NFkappaB activation.
Trade Name | Gabexatum |
Generic | Gabexate |
Gabexate Other Names | Gabexate, Gabexato, Gabexatum |
Type | |
Formula | C16H23N3O4 |
Weight | Average: 321.377 Monoisotopic: 321.168856233 |
Groups | Investigational |
Therapeutic Class | |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Gabexatum is a protease inhibitor indicated in the treatment of acute pancreatitis.
No approved indication.
Gabexatum is also used to associated treatment for these conditions: Acute Pancreatitis (AP)
How Gabexatum works
Gabexatum inhibits kallikrein, plasmin, and thrombin by binding to their active sites. The inhibition of these components of the coagulation cascade ultimately prevents the formation of fibrin which must be present and polymerized to form a clot. Gabexatum decreases the production of inflammatory cytokines by attenuating NFkappaB and c-Jun N-terminal kinase (JNK) pathway activity. The exact mechanism for this is unknown but it is thought that gabexate prevents the proteolyytic destruction of IkappaB which deactivates NFkappaB and interferes with activator protein 1 binding to DNA.
Toxicity
LD50 of 6480mg/kg observed in rats.
Food Interaction
- Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
Innovators Monograph
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