Lenampicillin (hydrochloride)

Lenampicillin hydrochloride (KBT 1585 hydrochloride) is an orally active prodrug of Ampicillin and is an effective beta-lactam antibacterial agent that inhibits bacterial penicillin-binding proteins (transpeptidase). Lenampicillin hydrochloride has improved absorption and decreased side effects compares to Ampicillin and is applied in the investigation of the suppurative skin and soft tissue infection ^{[1] [2] [3]}. IC50 & Target: IC50: bacterial penicillin-binding proteins (transpeptidase) In Vivo: Lenampicillin hydrochloride (KBT-1585) (oral adminstration; 0-1000 mg/kg) does not lead to death in dogs, and maximum dose of in this acute toxicity study is recorded because of causing emesis^[2].
Lenampicillin hydrochloride (LAPC) are identified for it main metabolites in rat and dogs. The main metabolite in peripheral plasma is 2,3-butanediol in rats and dog, On the other hand, high levels of acetoin is found in portal plasma for early period after dosing of LAPC. These results shows that the biotransformation of promoiety in LAPC to acetoin carried out mainly in intestinal tissues, but acetoin is converted to 2,3-butanediol in liver^[3].