The sodium-glucose co-transporters (SGLTs) 1 and 2 play an important role in glucose and sodium transport in the kidneys and gastrointestinal tract. SGLT1 is expressed in the small intestine, where is needed for glucose and galactose absorption. Inhibition of SGLT1 results in glucose and galactose malabsorption[1]. Licogliflozin is a combined inhibitor of SGLT1 and SGLT2 and is hypothesized to further enhance the effects on renal sodium and glucose handling via inhibition of both cotransporter subtypes in the proximal renal tubule. Licogliflozin demonstrated significant weight loss (~6%) versus placebo, with favorable changes in metabolic parameters and incretin hormones. Dual inhibition of SGLT1/2 with licogliflozin in the gut and kidneys is an attractive strategy for treating obesity and diabetes[2]. Oral absorption of licogliflozin was rapid (tmax < 1 h) with absorption estimated at 87%, 100% and 77% in rats, dogs and humans, respectively. Excretion of licogliflozin-related radioactivity was rapid and nearly complete following oral administration with total radioactivity recovery ranging from 73% in dogs, 92.5% in humans, to 100% in rats. Elimination of licogliflozin was predominantly via metabolism with the majority of the radioactivity dose (∼54-74%) excreted as metabolites across species[3].
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