Crystallographic structure of human fatty acid synthase (rainbow color, N-terminus = blue, C-terminus = red) inhibited by<unk>  (space-filling model; carbon = grey, oxygen = red, nitrogen = blue).<unk>  works by inhibiting gastric and pancreatic lipases, the enzymes that break down triglycerides in the intestine. When lipase activity is blocked, triglycerides from the diet are not hydrolyzed into absorbable free fatty acids, and instead are excreted unchanged. Only trace amounts of<unk>  are absorbed systemically; the primary effect is local lipase inhibition within the GI tract after an oral dose. The primary route of elimination is through the feces.<unk>  was also recently found to inhibit the thioesterase domain of fatty acid synthase (FAS), an enzyme involved in the proliferation of cancer cells but not normal cells. However, potential side effects of<unk> , such as inhibition of other cellular off-targets or poor bioavailability, might hamper its application as an effective antitumor agent. One profiling study undertook a chemical proteomics approach to look for new cellular targets of<unk> , including its off-targets.<unk>  also shows potential activity against the Trypanosoma brucei parasite. At the standard prescription dose of 120 mg three times daily, before meals,<unk>  prevents approximately 30% of dietary fat from being absorbed. Higher doses do not produce more potent effects.
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