Pyridoglutethimide [3-ethyl-3-(4-pyridyl)-piperidine-2,6-dione], an analogue of aminoglutethimide: Metabolism and pharmacokinetics

Abstract Pyridoglutethimide [3-ethyl-3-(4-pyridyl)piperidine-2,6-dione] has been developed as an analogue of aminoglutethimide [3-(4-aminophenyl)-3-ethyl-piperidine-2,6-dione] possessing specific aromatase activity with potency comparable to aminoglutethimide. This study investigates the pharmacokinetics of pyridoglutethimide in the rat and the rabbit: the plasma half-life is 6 hr in the rat and 16.4 hr in the rabbit. The sole metabolite found in urine (rat) and plasma (rat and rabbit) is pyridoglutethimide N -oxide.