Aprepitant - Initial Development

Initial Development

Acute or delayed CINV is an unpleasant side effect experienced by over 80% of patients undergoing initial and repeated highly emetogenic cancer chemotherapy, for example cisplatin. Throughout the 1990s a noticeable increase occurred in the number of diagnosed cancer patients undergoing chemotherapy and therefore experiencing CINV. As a result of this, toward the end of the decade, initial research was conducted to try to develop a drug that eases the severity and decreases 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 vomiting. This is due to the receptor binding with substance P, a peptide neurotransmitter.

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