Osanetant is a clinical-stage, selective, non-peptide tachykinin NK3 receptor antagonist. NK3R is the main receptor for neurokinin B (“NKB”), a tachykinin peptide primarily found in the arcuate nucleus (ARC) of the hypothalamus. In December 2018, we entered into an exclusive license agreement with Sanofi to acquire worldwide rights to osanetant.
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 325 healthy subjects and 665 schizophrenic patients with clinical and laboratory safety data from 21 completed Phase 1 and Phase 2 studies. No major safety concerns were identified from these studies after single-dose and repeated-dose administration of up to 400mg once daily for up to 21 days, and 200mg once daily for up to six weeks. 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 various patient populations with induced Vasomotor Symptoms (iVMS), including iVMS following treatment for Hormone Receptor (+) breast cancer and prostate cancer, and for BRCA1/2 breast cancer following bilateral salpingo-oophorectomy. We are targeting submission of an osanetant IND in the second quarter of 2021 subject to discussions with the FDA. We plan to initiate a Phase 1/2 pharmacokinetic/pharmocodynamic and safety trial evaluating osanetant in patients with medically and/or surgically induced vasomotor symptoms (iVMS) in the second half of 2021, subject to additional capital.
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