China
Africa
Explore chapters and articles related to this topic
Peptide Structure and Analysis
Published in Marco Chinol, Giovanni Paganelli, Radionuclide Peptide Cancer Therapy, 2016
Carlo Pedone, Giancarlo Morelli, Diego Tesauro, Michele Saviano
An example of a new compound with reduced flexibility obtained by cyclization is the cyclo(Met-Asp-Trp-Phe-Dap-Leu)cyclo(2β-5β) (Fig. 5) (8), a selective and potent Tachykinin NK2 receptor antagonist. Now a glycosilated peptide analogue, NEPADUTANT (MENARINI Group) is in phase IIa trials in Belgium and Sweden for the potential treatment of asthma and irritable bowel syndrome.
Neurokinin receptor antagonism: a patent review (2014-present)
Published in Expert Opinion on Therapeutic Patents, 2020
To date, in humans, no NK-2R or NK-3R antagonist has been approved to be administered. NK-2R antagonists (e.g. saredutant, nepadutant, ibodutant) have been tested for the treatment of major depressive disorder, asthma, gastrointestinal disorders, and diarrhea, whereas NK-3R antagonists (e.g. osanetant, talnetant) were used to treat depression, panic disorder, and schizophrenia (Figure 2) [2]. These trials were abandoned due to the lack of efficacy. The species used in preclinical studies could explain the ineffective action of NK receptor antagonists observed in some human trials, since in experimental animals, modifications in the amino acid sequence of the NK receptor have been reported and hence these alterations could modify the intensity action of the antagonist [3,23]. Another explanation could be the low doses of the NK receptor antagonists generally used in clinical trials and hence it seems that increasing the dose of the NK receptor antagonist and the number of days administered (compared to the standard clinical practice: day 1 (125 mg); day 2 (80 mg) and day 3 (80 mg)) [21], therapeutic effects could be observed (e.g. antipruritic or antitumor actions).