Pharmacological properties of 7-ethyl-10-hydroxy-camptothecin derivatives:research advances / 国际药学研究杂志

ABSTRACT

7-Ethyl-10-hydroxycamptothecin (SN-38) is a prominent anticancer agent, but it is insoluble in water and the most pharmaceutically acceptable solvents, the lactone ring of SN-38 shows reversible pH-dependent hydrolysis and forms to the open lactone in alkaline condition. All of these factors limit its application in clinic, and a variety of chemical modification studies have been reported to improve the efficient use of SN-38 by improving its solubility in water and pharmaceutical solvents, stabilizing the lactone form, and altering the pharmacological properties. This paper reviews the pharmacological properties of commercial SN-38 derivatives in clinical trials or preclinical studies and their research progress.