Drug intelligence / Profile preview

topiramate + naltrexone

Development stage
Preclinical
Lead developer
Johnson & Johnson
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

Topiramate + naltrexone is a combination of two small molecule drugs, each with distinct mechanisms of action, used primarily in the management of substance use disorders—especially alcohol use disorder (AUD)—and under investigation for weight loss and eating disorders. Naltrexone is an opioid receptor antagonist that blocks the effects of endogenous and exogenous opioids, thereby reducing cravings and reward associated with alcohol or opioid consumption. Topiramate is an anticonvulsant that modulates neuronal excitability through multiple mechanisms, including enhancement of GABAergic activity and inhibition of glutamatergic neurotransmission; it also has effects on voltage-gated sodium channels and carbonic anhydrase inhibition. When used together, these agents may have additive or synergistic effects in reducing alcohol consumption and cravings. The combination has also been explored for potential benefits in weight loss protocols due to their individual impacts on appetite regulation and reward pathways[1][2][5].

02

Targets

NaV (Voltage-gated sodium channels)iGluR (Ionotropic receptor 76b (Ir76b))CA (Carbonic anhydrase)MOR (Mu opioid receptor)DOR (Opioid Receptor Delta 1)GABRR (GABA-A receptor subunit rho)KOR (Kappa opioid receptor)

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