1. Clear MOA
(1) Orexins bind and activate their associated G protein-coupled OX1Rs and OX2Rs and act on sleep-wake regulation.
(2) Antagonism of the orexin system increases NREM and REM sleep, decreases anxiety- and panic-like behaviors, and inhibits the reinforcing and motivational properties of addictive drugs.
(3) Inhibition of ACC enzymes pharmacologically provides an attractive approach to treating NAFLD/NASH by decreasing hepatic lipid synthesis while simultaneously increasing fatty acid oxidation.
(4) OX1Rs and OX2Rs play differential roles in the regulation of REM sleep and NREM sleep. NREM sleep is mainly regulated by OX2Rs.
2. High selective dual inhibition.
The antagonistic effect of the asset on OX2R is better than that on OX1R.
3. Treat insomnia: Significantly increases NREM time, decreases NREM latency and wakefulness time without affecting REM time in rats and cynomolgus monkeys.
4. After 12h administration (light on), the asset has no effect on NREM or wakefulness, showing slight residual effect of the next day.
5. Good safety:
(1) There is no significant correlation between the incidence of AEs and the dose.
(2) No SAEs, no TEAE leading to early withdrawal from the test or death.
6. High incidence
1. Asset type: High selective OX1R/OX2R dual inhibitor treating insomnia
2. Indication: Insomnia
3. Modality: Small molecular, orally QD, first class new medicine
4. Research phase: Phase Ⅰ completed, IP has been granted in the US, CN, etc
5. Cooperation demands: License-out or co-development the global right
6. Research progress:
(1) The asset has completed phase 1 trial.
(2) Slight residual effect of the next day
(3) Good efficacy without affecting REM time.
Explore our catalog of therapeutic antibody solutions to find the right products for you! We are dedicated to delivering solutions designed to help you drive innovation and push the boundaries of what therapeutic antibodies can be.
Organoid Toolbox is a collection of organoid solutions including ready-to-use organoids, organoid differentiation kits, and a variety of services to accelerate the progress of your drug development project.
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