Tachykinin Receptors Antagonists: From Research to Clinic
In this chapter it is described how, starting from different approaches and through extensive medicinal chemistry studies, several discovery compounds were optimized and reached the development stage.
The first tachykinin receptor antagonist to reach the market in 2003 for chemotherapy-induced emesis has been aprepitant. Other clinical candidates (for central nervous system disorders: osanetant, talnetant and saredutant; for irritable bowel syndrome: nepadutant and saredutant) are in advanced clinical phase.
The clinical studies reported in the literature and the destiny of the clinical candidates, where available, will be reviewed.
The first tachykinin receptor antagonist to reach the market in 2003 for chemotherapy-induced emesis has been aprepitant. Other clinical candidates (for central nervous system disorders: osanetant, talnetant and saredutant; for irritable bowel syndrome: nepadutant and saredutant) are in advanced clinical phase.
The clinical studies reported in the literature and the destiny of the clinical candidates, where available, will be reviewed.
Keywords: Tachykinin; antagonist; clinical development; emesis; irritable bowel syndrome; medicinal chemistry; schizophrenia
Document Type: Research Article
Affiliations: Menarini Ricerche SpA, Via Sette Santi 3, Florence I-50131, Italy.
Publication date: 01 August 2006
- Current Drug Targets aims to cover the latest and most outstanding developments on the medicinal chemistry and pharmacology of molecular drug targets e.g. disease specific proteins, receptors, enzymes, genes. Each issue of the journal will be devoted to a single timely topic, with series of in-depth reviews, written by leaders in the field, covering a range of current topics on drug targets. These issues will be organized and led by a guest editor who is a recognized expert in the overall topic. As the discovery, identification, characterisation and validation of novel human drug targets for drug discovery continues to grow; this journal will be essential reading for all pharmaceutical scientists involved in drug discovery and development.
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