Creating a new generation of small molecule protease inhibitors

Overview

KalVista’s drug discovery capabilities leverage the expertise of its R&D team, which has spent more than two decades successfully discovering and developing small molecule protease inhibitors. Combined with world-leading expertise in the role of plasma kallikrein in disease, KalVista has developed a structurally diverse pipeline of novel, potent, and highly selective plasma kallikrein inhibitors.

Research and Development

Plasma kallikrein as a drug target

Plasma kallikrein is a protease that is an important component of the body’s inflammatory response. It circulates as an inactive enzyme (plasma prekallikrein) that, upon activation at the site of vascular injury, initiates a cascade that results in increased levels of the potent vasoactive peptide bradykinin, which in turn leads to dilation of blood vessels, increased vascular permeability, edema, and inflammation. Under normal circumstances plasma kallikrein activity is regulated by an endogenous inhibitor, C1-inhibitor. However, in some diseases, the plasma kallikrein activity is allowed to increase unchecked and results in damaging inflammation.

Eye examination

Excessive activity of the plasma kallikrein system has been shown to contribute to hereditary angioedema and is also strongly implicated in diabetic macular edema, cerebral hemorrhage, and other edematous and inflammatory disorders.