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Clinical Pharmacokinetics of Irinotecan
  • G. Chabot
  • Biology, Medicine
    Clinical pharmacokinetics
  • 1 October 1997
TLDR
Irinotecan, and its more potent metabolite SN-38 (7-ethyl-10-hydroxy-camptothecin), interfere with mammalian DNA topoisomerase I and cancer cell death appears to result from DNA strand breaks caused by the formation of cleavable complexes.
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Retinoic acid metabolism and mechanism of action: a review.
TLDR
Therapy of cancer with retinoids is still in its infancy, but the use of new analogues with improved pharmacological properties, along with combination with other drugs, could undoubtedly improve the management of several cancers in the future.
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Activation of Retinoic Acid Receptor-dependent Transcription by All-trans-retinoic Acid Metabolites and Isomers*
TLDR
ATRA metabolites can bind to and activate the three RARs with variable relative affinity but with similar efficacy, suggesting that ATRA metabolites may activate several signaling pathways and probably play an important role in cellular physiology and cancer therapy.
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Expression and inducibility of cytochrome P450 3A9 (CYP3A9) and other members of the CYP3A subfamily in rat liver.
TLDR
The data show that rat CYP3A genes are variably expressed depending on age, sex, or inducer type, and the results presented for CYp3A23 are those anticipated for CYP2A1, which may be an allelic variant of CYP 3A23 not detected in these experiments.
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Identification of human cytochrome P450s involved in the formation of all-trans-retinoic acid principal metabolites.
TLDR
Several human P450s involved in atRA metabolism have been identified, and the expression of which was shown to direct at RA metabolism toward the formation of specific metabolites, including 4-OH-RA and 4-oxo-RA.
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Population pharmacokinetics and pharmacodynamics of irinotecan (CPT-11) and active metabolite SN-38 during phase I trials.
TLDR
Although CPT-11 pharmacokinetic parameters presented an important interpatient variability, both Cpt-11 maximum concentrations (Cmax) and the C PT-11 area under the plasma concentration versus time curves (AUC) increased proportionally and linearly with dosage.
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Main drug-metabolizing enzyme systems in human breast tumors and peritumoral tissues.
TLDR
Several differences were observed between human breast tumors and peritumoral tissues for many conjugating enzymes (GST-mu, GST-pi, and UDP-glucuronosyltransferase) and hydrolytic enzymes (sulfatase and beta- glucuronidase) which could play a role in the relative drug sensitivity or insensitivity of human breast cancer tissues to chemotherapeutic agents.
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CPT-11-induced cholinergic effects in cancer patients.
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Human cytochrome P450s involved in the metabolism of 9-cis- and 13-cis-retinoic acids.
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Phase I and pharmacologic studies of the camptothecin analog irinotecan administered every 3 weeks in cancer patients.
TLDR
The MTD of CPT-11 administered as a 30-minute IV infusion every 3 weeks is 600 mg/m2, with granulocytopenia being dose-limiting, and the activity of this agent in 5-FU-refractory colorectal carcinoma makes it unique and mandates expedited phase II testing.
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