Drug intelligence / Profile preview

metformin + naltrexone

Development stage
Preclinical
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-AgelessRx-COVID-19metformin-AgelessRx-COVID19metformin-AgelessRx-COVID 19Metformin and Low Dose NaltrexoneMetformin and LDNMetformin and Low Dose Naltrexone (LDN)
02

Targets

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

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