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RZLT7824
- Development stage
- Preclinical
- Lead developer
- Rezolute
- Modality
- Small Molecules
- Administration
- Intraperitoneal
01
Overview
RZLT7824 is a small-molecule inhibitor of plasma kallikrein (PKa) developed by Rezolute. It selectively inhibits human plasma kallikrein with an IC50 of 13 nM and mouse plasma kallikrein with an IC50 of 5 nM, showing high selectivity over other serine proteases such as factor XIIa, factor XIa, factor Xa, thrombin (FIIa), and plasmin. RZLT7824 has been investigated in preclinical models of experimental cerebral malaria (ECM) to reduce vasogenic brain edema, preserve neurological function, and improve survival, particularly when used as an adjuvant therapy alongside the antiparasitic drug artesunate.
02
Targets
BDKRB1 (Bradykinin Receptor B1)Bradykinin B2 receptorKNG1 (High-molecular-weight kininogen)KLKB1 (Plasma kallikrein)
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