Drug intelligence / Profile preview

sibutramine + orlistat + diethylpropion

Development stage
Discontinued
Lead developer
Abbott
Modality
Small Molecules
Administration
Oral
01

Overview

This drug is a **combination of sibutramine, orlistat, and diethylpropion**, each of which is a small molecule pharmaceutical used individually for the treatment of obesity and weight loss. - **Sibutramine** is a centrally acting serotonin-norepinephrine reuptake inhibitor that functions as an appetite suppressant. It enhances satiety and may increase thermogenesis by inhibiting the reuptake of serotonin and norepinephrine in the central nervous system[1]. - **Orlistat** is a lipase inhibitor that acts in the gastrointestinal tract to block the absorption of dietary fats. It works by inhibiting gastric and pancreatic lipases, reducing fat absorption by approximately 30% and increasing fecal fat excretion[1]. - **Diethylpropion** is a sympathomimetic amine anorectic agent structurally related to amphetamines. It exerts its effect as a noradrenergic appetite suppressant through stimulation of the central nervous system[4]. All three drugs have been individually approved for obesity treatment, though **sibutramine has been withdrawn from the market in many countries due to cardiovascular risks**[6]. Orlistat and diethylpropion remain in use, though the combination of all three agents together does not appear to be an approved or clinically validated therapy and is not discussed in combination in the available medical literature. Studies on combinations of sibutramine with orlistat showed no significant additional benefit over sibutramine alone[1][2][3].

Brand names
MeridiaXenicalAlliTenuateReductilTepanil
Other names
Intensive Medical Combination Therapy for ObesityLOSS trial drug combination
02

Targets

CEL (Carboxyl ester lipase)SERT (Sodium-dependent serotonin transporter)PNLIP (Pancreatic triacylglycerol lipase)DAT (Dopamine plasma membrane transport protein)LIPF (Gastric lipase)NET (Norepinephrine Transporter)

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