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ITI-333
- Development stage
- Phase 1
- Lead developer
- Intra-Cellular Therapies
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
ITI-333 is a novel, orally bioavailable small molecule developed by Intra-Cellular Therapies for the treatment of opioid use disorder, pain, and related psychiatric comorbidities. It acts as a partial agonist at the μ-opioid receptor (MOR) and as an antagonist at serotonin 5-HT2A, dopamine D1, and adrenergic α1A receptors. Preclinical studies demonstrated that ITI-333 produces analgesic effects dependent on μ-opioid receptor activation but with reduced abuse liability compared to full opioid agonists. The drug was designed to address both substance use disorders and associated symptoms such as anxiety and depression[1][2][3][4][5][6].
02
Targets
HTR2A (Serotonin receptor 5-HT2A)ADRA1A (α1A)DRD1 (Dopamine D1 Receptor)DRD2 (Dopamine D2 Receptor)MOR (Mu opioid receptor)
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