Current Drug Targets

Francis J. Castellino
Kleiderer-Pezold Professor of Biochemistry
Director, W.M. Keck Center for Transgene Research
Dean Emeritus, College of Science
230 Raclin-Carmichael Hall, University of Notre Dame
Notre Dame, IN 46556


Tachykinin Receptors Antagonists: From Research to Clinic

Author(s): Laura Quartara, Maria Altamura.


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.

Keywords: Tachykinin, antagonist, clinical development, medicinal chemistry, emesis, irritable bowel syndrome, schizophrenia

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Article Details

Year: 2006
Page: [975 - 992]
Pages: 18
DOI: 10.2174/138945006778019381
Price: $58