GC-MS-based quantitative signatures of cytochrome P450-mediated steroid oxidation induced by rifampicin

Ju Yeon Moon, Se Mi Kang, Jeongae Lee, Joo Youn Cho, Myeong Hee Moon, In Jin Jang, Bong Chul Chung, Man Ho Choi

Research output: Contribution to journalArticlepeer-review

16 Citations (Scopus)


BACKGROUND: Drug-induced cytochrome P450 (CYP) activity affects endocrine function and drug clearance rates, leading to the development of unpredictable pathologic and toxicologic risks. METHODS: Urinary steroid profiling based on gas chromatography-mass spectrometry (GC-MS) was used for simultaneous quantification of CYP-mediated regioselective hydroxysteroids and their substrates, including 26 androgens, 9 estrogens, 5 progestins, and 7 corticoids. The quantitative data were visualized using a hierarchically clustered heat map to allow identification of CYP-mediated steroid signatures. Twelve healthy subjects were orally administered 600 mg of rifampicin a day for 7 days, and their CYP enzyme activity was evaluated. RESULTS: Using GC-MS, all 47 steroids were well separated with good peak shapes. This assay had good linearity (r > 0.994) in a dynamic range, and the interassay imprecision (% CV) and inaccuracy (% bias) were 3.0%-15.6% and 98.0%-109.2%, respectively. Administration of the CYP3A4 inducer rifampicin produced distinct differences in CYP3A4 and CYP11B1, CYP19A1, HSD11B, and HSD17B, which were indicated by their heat map-visualized steroid signatures. CONCLUSIONS: This CYP-mediated steroid signature profile allows simultaneous assessment of CYP1A, CYP1B, CYP2C, CYP3A, CYP11B, CYP17A, CYP19A, and CYP21A in urine samples. This method could therefore be a useful tool for assessing drug efficacy.

Original languageEnglish
Pages (from-to)473-484
Number of pages12
JournalTherapeutic Drug Monitoring
Issue number4
Publication statusPublished - 2013 Aug

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Pharmacology (medical)


Dive into the research topics of 'GC-MS-based quantitative signatures of cytochrome P450-mediated steroid oxidation induced by rifampicin'. Together they form a unique fingerprint.

Cite this