Chen, Yakun
Tang, Yong
Nie, Jeffrey Z.
Zhang, Yuanqin
Nie, Daotai http://orcid.org/0000-0001-5239-5663
Funding for this research was provided by:
National Cancer Institute (1R15CA133776-01A1)
Article History
Received: 31 January 2021
Accepted: 1 September 2021
First Online: 15 September 2021
Declarations
:
: On behalf of all authors, the corresponding author states that there is no conflict of interest.
: Megestrol acetate specifically induces the expression of cytochrome P450 3A4 (CYP3A4) in human hepatocytes through binding to human PXR and recruitment of cofactors. But it has minimal effects on the expression of other drug metabolizing enzymes and efflux transporters. The study suggests a potential interaction of megestrol acetate with other drugs that are substrates of CYP3A4, as well as the utility of this compound to induce CYP3A4 specifically for pharmacological studies.