Drug intelligence / Profile preview

lofexidine + buprenorphine

Development stage
Phase 2
Lead developer
US WorldMeds
Modality
Small Molecules
Administration
Oral
01

Overview

Lofexidine + buprenorphine is a **combination of two pharmaceutical agents**: lofexidine, an alpha-2 adrenergic receptor agonist approved for mitigation of opioid withdrawal symptoms, and buprenorphine, a partial opioid agonist approved for opioid use disorder (OUD) maintenance and withdrawal management. The combination is being studied, especially as adjunct therapy, for the treatment of opioid withdrawal and opioid use disorder, sometimes with the goal of also improving post-traumatic stress disorder (PTSD) symptoms. Lofexidine acts by stimulating alpha-2A and alpha-2C adrenoreceptors, resulting in reduced sympathetic outflow and mitigation of withdrawal symptoms without opioid receptor activation. Buprenorphine works primarily as a partial agonist at the mu-opioid receptor, reducing withdrawal symptoms and cravings associated with opioid cessation while lowering potential for misuse compared to full agonists. The combination is not an approved product but is under clinical investigation as an adjunct or parallel therapy in opioid use disorder and PTSD.

Other names
Lofexidine Combined With Buprenorphine
02

Targets

HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))HTR1D (5-hydroxytryptamine receptor 1D)HTR2C (5-hydroxytryptamine 2C receptor)HTR7 (5-hydroxytryptamine receptor 7)ADRA1A (α1A)ADRA2A (α2A)ADRA2C (α2C)MOR (Mu opioid receptor)

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