Aprepitant

The history of neurokinins begins with substance P, discovered in 1931 by Ulf von Euler and John H. Gaddum.

While studying extracts from horse brain and intestine, they encountered an unidentified substance capable of producing intestinal smooth-muscle contraction and lowering blood pressure. They called the active preparation “substance P”, with the original "P" referring to their preparation.

A major breakthrough came in 1971, when Chang and Leeman isolated and determined the amino-acid sequence of substance P.

                                               Neurokinin Receptor Antagonist

Aprepitant was introduced clinically as an NK₁ antagonist for prevention of chemotherapy-induced nausea and vomiting. 

It represented the first major therapeutic success of the neurokinin antagonist field

Other Neurokinin 1 Receptor Antagonists

Snapshot