Drug intelligence / Profile preview

metformin + phentermine + topiramate

Development stage
Preclinical
Lead developer
VIVUS LLC
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of three drugs—metformin, phentermine, and topiramate—used together for weight management or metabolic indications. Metformin is a biguanide antihyperglycemic agent that decreases hepatic glucose production and improves insulin sensitivity. Phentermine is a sympathomimetic amine anorectic that suppresses appetite via central nervous system stimulation. Topiramate is an anticonvulsant with weight loss properties, thought to act through modulation of voltage-gated ion channels and enhancement of GABA activity in the brain. While the fixed-dose combination of phentermine plus topiramate (marketed as Qsymia) is approved for chronic weight management in obesity, there are no approved products combining all three agents into a single formulation; however, they may be used together off-label in clinical practice for patients with obesity and comorbidities such as type 2 diabetes[3][6][9]. The combination targets both appetite suppression (phentermine/topiramate) and glycemic control (metformin).

02

Targets

SERT (Sodium-dependent serotonin transporter)AMPK (Adenosine monophosphate–activated protein kinase)GABRR (GABA-A receptor subunit rho)NaV (Voltage-gated sodium channels)iGluR (Ionotropic receptor 76b (Ir76b))GSEC (Gamma-Secretase Complex)TAAR1 (Trace amine-associated receptor 1)NET (Norepinephrine Transporter)ND1 (Mitochondrial electron transport chain complex I)DAT (Dopamine plasma membrane transport protein)CA2 (Carbonic Anhydrase 2)

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