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'Aprepitant' is a chemical compound that belongs to a class of drugs called substance P antagonists (SPA). It mediates its effect by acting on neurokinin 1 receptor.
Aprepitant is manufactured by Merck & Co. under the brand name 'Emend' for 'prevention' of acute and delayed chemotherapy-induced nausea and vomiting (CINV) and for 'prevention' of postoperative nausea and vomiting. It was approved by the FDA in 2003.
Aprepitant may also be useful in the treatment of cyclic vomiting syndrome but there are few studies to date.

Contents

Introduction

Structure and properties of aprepitant

Synthesis

Drug development

Mechanism of action

Other uses

Notes and references

External links

Introduction

Acute or delayed CINV is an unpleasant side effect experienced by over 80% of patients who undergo initial and repeated highly emetogenic cancer chemotherapy, for example Cisplatin in combination with other antiemetic agents. Throughout the 1990's a noticeable increase occurred in the number of diagnosed cancer patients undergoing chemotherapy and therefore experiencing CINV. As a result of this, towards the end of the decade initial research was conducted to try to develop a drug that eases the severity and decreasing the likelihood of CINV, and after several years of research Merck & Co. successfully developed a drug known as Emend.
The active substance of Emend is aprepitant, which is effective in helping to prevent CINV because it antagonizes the NK1 receptor. This receptor is located at the brain stem nuclei of the dorsal vagal complex and is a crucial part of the regulation of emesis (vomiting). This is due to the receptor binding with substance P, a peptide neurotransmitter.

Structure and properties of aprepitant

While the common name for the molecule above is aprepitant its chemical name is 5-