Pharmacokinetic Study of CPT-11, Raltegravir and Midazolam With Characterisation of UGT1A1 Genotype

Summary

The objectives of this study are: To correlate pharmacokinetic parameters of raltegravir and midazolam with irinotecan (CPT-11) and its metabolite SN-38. To correlate the genotype of UGT1A1 of patients receiving CPT-11 chemotherapy with irinotecan and raltegravir pharmacokinetic parameters. To model pharmacokinetic and pharmacodynamic behaviour of CPT-11 in the study population.

Timeline

Start

2010-04

Primary completion

2012-02

Completion

2012-02

Publications

• Background Atsumi R, Suzuki W, Hakusui H. Identification of the metabolites of irinotecan, a new derivative of camptothecin, in rat bile and its biliary excretion. Xenobiotica. 1991 Sep;21(9):1159-69. doi: 10.3109/00498259109039556.
• Background Gupta E, Mick R, Ramirez J, Wang X, Lestingi TM, Vokes EE, Ratain MJ. Pharmacokinetic and pharmacodynamic evaluation of the topoisomerase inhibitor irinotecan in cancer patients. J Clin Oncol. 1997 Apr;15(4):1502-10. doi: 10.1200/JCO.1997.15.4.1502.
• Lee LS, Seng KY, Wang LZ, Yong WP, Hee KH, Soh TI, Wong A, Cheong PF, Soong R, Sapari NS, Soo R, Fan L, Lee SC, Goh BC. Phenotyping of UGT1A1 Activity Using Raltegravir Predicts Pharmacokinetics and Toxicity of Irinotecan in FOLFIRI. PLoS One. 2016 Jan 25;11(1):e0147681. doi: 10.1371/journal.pone.0147681. eCollection 2016.

Drugs

Indications