Drug intelligence / Profile preview

sibutramine + orlistat

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

Overview

Sibutramine + orlistat is a combination of two pharmacological agents used for the management of obesity. Sibutramine acts as a norepinephrine and serotonin reuptake inhibitor, thereby reducing appetite and increasing satiety. Orlistat is a gastrointestinal lipase inhibitor that reduces the absorption of dietary fats by inhibiting gastric and pancreatic lipases. The rationale for combining these drugs lies in their complementary mechanisms—sibutramine targets central appetite regulation, while orlistat acts peripherally to decrease fat absorption. Clinical studies have shown that this combination can lead to weight loss in obese patients; however, evidence suggests that the combination does not provide significant additional benefit over sibutramine monotherapy in terms of weight reduction[1][4][5]. Both drugs are associated with their own side effect profiles, including gastrointestinal disturbances (orlistat) and cardiovascular/central nervous system effects (sibutramine)[1][5].

02

Targets

LIPF (Gastric lipase)SERT (Sodium-dependent serotonin transporter)NET (Norepinephrine Transporter)PNLIP (Pancreatic triacylglycerol lipase)

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