Metabolism of aminoglutethimide in humans: quantification and clinical relevance of induced metabolism
1985

Metabolism of Aminoglutethimide in Humans

Sample size: 80 publication Evidence: moderate

Author Information

Author(s): P.E. Goss, M. Jarman, L.J. Griggs

Primary Institution: Institute of Cancer Research

Hypothesis

The study aims to quantify hydroxylaminoglutethimide (HxAG) and confirm that its induction is AG-induced and increases with the duration of therapy.

Conclusion

The metabolism of aminoglutethimide to HxAG is an induced, major metabolic pathway that increases with time on therapy.

Supporting Evidence

  • HxAG was not detectable on Day 1 but was abundant in the Day 14 extract.
  • The ratio of HxAG to AG increased with time, indicating induced metabolism.
  • All spot urine samples from patients on treatment were positive for HxAG.

Takeaway

This study shows that a drug called aminoglutethimide changes how the body processes it over time, which can affect how well it works.

Methodology

Quantification of HxAG, AG, and N-AcAG using high performance liquid chromatography (HPLC) and a colorimetric assay.

Limitations

The study faced challenges due to the instability of HxAG at room temperature, which affected the accuracy of measurements.

Participant Demographics

Participants included 50 post-menopausal women with metastatic breast cancer and 30 male and female out-patients.

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