Drug intelligence / Profile preview

metformin + naltrexone

Development stage
Phase 3
Modality
Small Molecules
Administration
Oral
01

Overview

Metformin + naltrexone is a combination of two pharmaceutical drugs, metformin and naltrexone, used off-label and in compounded formulations for weight management and metabolic health. - **Metformin** is a biguanide class drug that lowers blood glucose by decreasing hepatic glucose production, reducing intestinal absorption of glucose, and improving insulin sensitivity. It is primarily used for type 2 diabetes mellitus. - **Naltrexone** is an opioid receptor antagonist, blocking mu-opioid receptors in the central nervous system. It is approved for opioid addiction and alcohol dependence; in weight-loss settings, it is hypothesized to reduce food cravings and regulate appetite via modulation of reward mechanisms. - The combination is designed to act on multiple metabolic and neurobiological pathways, targeting insulin resistance, appetite regulation, and reward-driven eating behavior. - The combination does not have FDA approval as a standardized pharmaceutical product but is available through compounded prescriptions, sometimes alongside bupropion. - Mechanism: The combination targets central appetite regulation and peripheral metabolism to assist weight reduction and metabolic improvement[6][9].

Other names
Metformin and Low Dose NaltrexoneMetformin and LDNMetformin and Low Dose Naltrexone (LDN)
02

Targets

AMPK (Adenosine monophosphate–activated protein kinase)DOR (Opioid Receptor Delta 1)KOR (Kappa opioid receptor)MOR (Mu opioid receptor)TLR4 (Toll-like receptor 4)INSR (Insulin receptor)

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