Drug intelligence / Profile preview

naloxone + lofexidine

Development stage
Unknown
Lead developer
Endo International
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular, Subcutaneous, Intranasal
01

Overview

Naloxone + lofexidine is a combination of two drugs, naloxone and lofexidine, each with distinct mechanisms of action. Naloxone is an opioid receptor antagonist that rapidly reverses the effects of opioids by competitively inhibiting μ-opioid receptors, making it essential in the management of opioid overdose[4]. Lofexidine is a centrally acting alpha-2A-adrenergic receptor agonist used to mitigate symptoms associated with acute opioid withdrawal; it reduces autonomic symptoms such as chills, sweating, stomach cramps, and muscle pain without being an opioid itself[2][3][5]. While both drugs are individually approved for specific indications related to opioid use and withdrawal management, there is no evidence or approval for a fixed-dose combination product containing both naloxone and lofexidine. Each drug may be used separately or as part of broader protocols in managing different aspects of opioid dependence or withdrawal.

02

Targets

DOR (Opioid Receptor Delta 1)KOR (Kappa opioid receptor)ADRA2A (α2A)ADRA1A (α1A)MOR (Mu opioid receptor)

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