Orlistat
Orlistat. Irreversibly inhibits pancreatic + gastric lipases via covalent serine modification → blocks hydrolysis of dietary triglycerides → ~30% of ingested fat…
Irreversibly inhibits pancreatic + gastric lipases via covalent serine modification → blocks hydrolysis of dietary triglycerides → ~30% of ingested fat passes unabsorbed. Modest weight loss 3–6% at 1 year. Largely unabsorbed systemically — acts locally in gut lumen.
PK: STRIPPED. THE CITATION IS AN ARGUMENT THAT THIS RECORD SHOULD NOT EXIST. It screened twenty-five phase-1 studies plus two radiolabel mass-balance studies and concluded that "systemic absorption of orlistat is negligible", with "almost the entire dose ... recovered from fecal samples; little was found in plasma and urine" — and it states NO half-life, NO volume and NO bioavailability number, so both stored values were class 1. A plasma curve is the wrong object for a drug whose entire pharmacology is luminal lipase inhibition, and with no volume authored the solver was rendering one against an arbitrary thirty-five litres anyway.
Related compounds
- Vitamin D3 — caution
Sources: PMID:8626884