NKB/NK3R is implicated in a variety of human functions and affects the hypothalamus-pituitary-gonadal axis, which plays a critical part in the development and regulation of a number of the body’s systems, such as the reproductive and immune systems. Clinical proof of concept studies with other NK3R antagonists have demonstrated rapid and clinically-meaningful improvement in vasomotor symptoms and polycystic ovarian syndrome.
Osanetant was originally developed by Sanofi for the treatment of symptoms associated with schizophrenia. Osanetant was studied in healthy subjects and schizophrenic patients with clinical and laboratory safety data from 21 completed Phase 1 and Phase 2 studies in a total of 1,586 people, of whom 665 patients were treated with osanetant. Osanetant is orally bioavailable and readily crosses the blood-brain barrier. We believe that several disorders involving the hypothalamus-pituitary-gonadal axis could benefit from treatment with an NK3R antagonist.
We plan to evaluate osanetant in rare and life-threatening neuroendocrine disorders initially in Phase 1/2 studies, evaluating pharmacokinetics, pharmacodynamics and safety.
- Emonds-Alt, X; et al. SR 142801, the first potent non-peptide antagonist of the tachykinin NK3 receptor”. Life Sciences. 1995, 56(1): PL27–32. doi:10.1016/0024-3205(94)00413-M. PMID 7830490.
- Kamali, F. Osanetant Sanofi-Synthélabo. Current Opinion in Investigational Drugs. 2001, 2(7): 950–6. PMID 11757797.
- Quartara L, Altamura M. Tachykinin receptors antagonists: from research to clinic. Current Drug Targets. 2006, 7 (8): 975–92. doi:10.2174/138945006778019381. PMID 16918326. Retrieved 2011-04-14.