PS433540

Status : investigational

Description

PS433540 is the first and only dual-acting angiotensin and endothelin receptor antagonist (DARA) in development. The study showed all doses of PS433540 compared with placebo produced a statistically significant inhibition of the expected angiotensin (AII) induced increase in blood pressure.

Used

This drug Controls blood pressure in hypertensive patients.

Mechanism Of Action

The compound, which possesses two clinically validated mechanisms of action in a single molecule, works by selectively blocking the action of two potent vasoconstrictor and mitogenic agents, angiotensin II (AII) and endothelin 1 (ET1), at their respective receptors. PS433540 is highly selective (10,000-fold) for the AII receptor sub-type 1 and the ET receptor sub-type A. As such, PS433540 combines the properties of an angiotensin receptor blocker (ARB) and an endothelin receptor antagonist (ERA) in the same molecule.

Chemical Classification

Calculated Property

kind Value Source

Affected organism

Humans and other mammals

Target within organism

  • Angiotensinogen : in Human
  • Endothelin-1 receptor : in Human