4-Hydroxy Tolbutamide is the main product of the first-generation sulfonylurea hypoglycemic drug Tolbutamide metabolized by CYP2C9 in the human body [1]. 4-Hydroxy Tolbutamide has a certain effect of promoting insulin release, but the efficacy is weak [2]. 4-Hydroxy Tolbutamide is mainly used for pharmacokinetic research and metabolic enzyme activity detection [3].
References:
[1]. Hansen LL, Brøsen K. Quantitative determination of tolbutamide and its metabolites in human plasma and urine by high-performance liquid chromatography and UV detection. Therapeutic drug monitoring. 1999 Dec 1; 21(6): 664.
[2]. Choi MR, Kwon MH, Cho YY, et al. Pharmacokinetics of tolbutamide and its metabolite 4‐hydroxy tolbutamide in poloxamer 407‐induced hyperlipidemic rats. Biopharmaceutics & drug disposition. 2014 Jul; 35(5): 264-274.
[3]. Jetter A, Kinzig-Schippers M, Skott A, et al. Cytochrome P 450 2C9 phenotyping using low-dose tolbutamide. European journal of clinical pharmacology. 2004 May;60: 165-171.
4-Hydroxy Tolbutamide是第一代磺酰脲类降血糖药甲苯磺丁脲在人体内经CYP2C9代谢的主要产物 [1]。4-Hydroxy Tolbutamide具有一定的促进胰岛素释放作用，但药效较弱 [2]。4-Hydroxy Tolbutamide主要用于药代动力学研究和代谢酶活性检测 [3]。