Drug intelligence / Profile preview

RO 15-8081

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Oral
01

Overview

RO 15-8081 is a novel small molecule that acts as a **mixed serotonin (5-HT) and noradrenaline (norepinephrine) uptake inhibitor**, developed for its potential analgesic (pain-reducing) effects. It has shown potent antinociceptive properties in animal pain models, and in human studies, it has been found to elevate the threshold and tolerance to experimentally induced pain. In clinical trials, RO 15-8081 demonstrated analgesic efficacy for conditions such as osteoarthritis, particularly at higher doses, but its tolerability was limited by side effects such as dry mouth, insomnia, headache, constipation, nausea, dizziness, nervousness, and palpitations. The compound is a substituted cyclohexanol hydrochloride and was developed by Hoffmann-La Roche.

02

Targets

SERT (Sodium-dependent serotonin transporter)NET (Norepinephrine Transporter)

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