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RM1490
- Development stage
- Preclinical
- Lead developer
- R2M Pharma
- Modality
- Small Molecules
- Administration
- Subcutaneous, Possibly Oral (based On Standard Routes For Small Molecule Maintenance Therapies; Not Directly Specified)
01
Overview
RM1490 is a **brain-penetrant, small molecule agonist of the µ-opioid receptor (MOR)**, designed for the maintenance treatment of opioid use disorder[1][2]. It is based on a nonmorphinan scaffold and demonstrates **approximately half the intrinsic MOR efficacy of buprenorphine**, situating its pharmacological activity between that of buprenorphine (partial agonist) and naltrexone (antagonist)[1]. RM1490 achieves high occupancy of CNS MOR, inhibiting the euphoric effects of opioids with **limited risk of abuse, dependence, and precipitated withdrawal**, and was more effective than buprenorphine at reversing fentanyl-induced respiratory depression without suppressing respiration in combination with diazepam[1]. It shows high potency (EC50 of 3.4 and 4.4 nM in GTPγS and cAMP assays)[2] and offers a behavioral and physiological profile suitable for OUD maintenance therapy[1].
- Brand names
- RM1490RM-1490RM 1490
- Other names
- RM 1490RM1490RM-1490
02
Targets
MOR (Mu opioid receptor)
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