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Erlotinib treatment induces cytochrome P450 3A activity in non-small cell lung cancer patients

Artikel i vetenskaplig tidskrift
Författare A. Svedberg
S. Vikingsson
A. Vikstrom
N. Hornstra
M. Kentson
E. Branden
H. Koyi
Bengt Bergman
H. Green
Publicerad i British Journal of Clinical Pharmacology
Volym 85
Nummer/häfte 8
Sidor 1704-1709
ISSN 0306-5251
Publiceringsår 2019
Publicerad vid Institutionen för medicin
Sidor 1704-1709
Språk en
Länkar dx.doi.org/10.1111/bcp.13953
Ämnesord CYP3A activity, erlotinib, non-small cell lung cancer, quinine, Tarceva, receptor tyrosine kinase, in-vitro, quinine 3-hydroxylation, cyp3a, inhibitor, 4-beta-hydroxycholesterol, metabolism, midazolam, pharmacokinetics, induction, Pharmacology & Pharmacy
Ämneskategorier Farmaceutisk vetenskap

Sammanfattning

Aims Erlotinib is a tyrosine kinase inhibitor used in the treatment of non-small cell lung cancer highly metabolized by the cytochrome P450 (CYP) 3A. Hence, CYP3A4 activity might be a useful predictor of erlotinib pharmacokinetics in personalized medicine. The effect of erlotinib on CYP3A activity was therefore studied in non-small cell lung cancer patients. Methods The study included 32 patients scheduled for erlotinib monotherapy. CYP3A activity was assessed using quinine as a probe before and during erlotinib treatment. Plasma from blood samples drawn 16 hours post quinine administration were analysed using HPLC with fluorescence detection to determine the quinine/3-OH-quinine ratio. Results Matched samples, available from 13 patients, showed an induction of CYP3A activity (P = 0.003, Wilcoxon's signed rank test) after 2 months of treatment. The quinine/3-OH-quinine ratio decreased from 20.2 (+/- 13.4) at baseline to 11.0 (+/- 4.34). Single-point samples, available from 19 patients, supported the decrease in ratio (P = 0.007, Mann-Whitney U-test). Generally, females had a higher CYP3A activity both at baseline and after two months of treatment. Statistical analysis by gender also showed significant increase in CYP3A activity (males, n = 10, P = 0.001, and females, n = 22, P = 0.001). Conclusions An induction of CYP3A activity was observed after 2 months of erlotinib treatment which was also seen when subdividing based on gender. It could be important to take this into consideration for patients co-administering other CYP3A-metabolizing drugs during erlotinib treatment and also makes it difficult to use baseline CYP3A activity to predict erlotinib pharmacokinetics.

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