Ideal orally administrated hPL inhibitors for preventing and treating obesity or obesity-associated complications should meet the following three requirements, good safety profile (28), high efficacy (29), high local exposure to the gastrointestinal tract, and very low exposure into the circulatory system which could minimize the influence on the endogenous metabolism in the liver or other deep organs (30, 31). The gene discussed is LGALS1; the disease is Obesity.