Role of cytochrome P450 2C8 in drug metabolism and interactions
Abstract During the last 10-15 years, cytochrome P450 (CYP) 2C8 has emerged as an
important drug-metabolizing enzyme. CYP2C8 is highly expressed in human liver and is …
important drug-metabolizing enzyme. CYP2C8 is highly expressed in human liver and is …
Kinase inhibitor pharmacokinetics: comprehensive summary and roadmap for addressing inter-individual variability in exposure
Introduction: Small molecule protein kinase inhibitors (KIs) are a class of drugs with complex
and unconventional physiochemical and pharmacokinetic characteristics. Cytochrome P450 …
and unconventional physiochemical and pharmacokinetic characteristics. Cytochrome P450 …
Pharmacokinetic drug‐drug interactions of tyrosine kinase inhibitors: A focus on cytochrome P450, transporters, and acid suppression therapy
C Gay, D Toulet, P Le Corre - Hematological oncology, 2017 - Wiley Online Library
The extensive use of tyrosine kinase inhibitors (TKI's) in hematology and oncology has
shown that these drugs have a significant potential for drug‐drug interactions. Since these …
shown that these drugs have a significant potential for drug‐drug interactions. Since these …
CYP2D6 and CYP2C8 pharmacogenetics and pharmacological interactions to predict imatinib plasmatic exposure in GIST patients
C Dalle Fratte, S Gagno, R Roncato… - British Journal of …, 2023 - Wiley Online Library
Aims Patients on treatment with oral fixed dose imatinib are frequently under‐or
overexposed to the drug. We investigated the association between the gene activity score …
overexposed to the drug. We investigated the association between the gene activity score …
Cytochromes P450 2C8 and 3A catalyze the metabolic activation of the tyrosine kinase inhibitor masitinib
BD Latham, DS Oskin, RD Crouch… - Chemical research in …, 2022 - ACS Publications
Masitinib is a small molecule tyrosine kinase inhibitor under investigation for the treatment of
amyotrophic lateral sclerosis, mastocytosis, and COVID-19. Hepatotoxicity has been …
amyotrophic lateral sclerosis, mastocytosis, and COVID-19. Hepatotoxicity has been …
CYP2C8 Genotype Significantly Alters Imatinib Metabolism in Chronic Myeloid Leukaemia Patients
DT Barratt, HK Cox, A Menelaou, DT Yeung… - Clinical …, 2017 - Springer
Objective The aims of this study were to determine the effects of the CYP2C8* 3 and* 4
polymorphisms on imatinib metabolism and plasma imatinib concentrations in chronic …
polymorphisms on imatinib metabolism and plasma imatinib concentrations in chronic …
[HTML][HTML] Role of pharmacogenetics in personalised imatinib dosing
DT Barratt, AA Somogyi - Translational Cancer Research, 2017 - tcr.amegroups.org
Imatinib is the original tyrosine kinase inhibitor specifically designed and clinically used for
the molecularly targeted treatment of chronic myeloid leukaemia (CML). It remains one of the …
the molecularly targeted treatment of chronic myeloid leukaemia (CML). It remains one of the …
[HTML][HTML] The application of virtual therapeutic drug monitoring to assess the pharmacokinetics of imatinib in a Chinese Cancer population group
H Yu, RKS Badhan - Journal of Pharmaceutical Sciences, 2023 - Elsevier
Purpose Imatinib is used in gastrointestinal stromal tumours (GIST) and chronic myeloid
leukaemia (CML). Oncology patients demonstrate altered physiology compared to healthy …
leukaemia (CML). Oncology patients demonstrate altered physiology compared to healthy …
Advances in drug metabolism and pharmacogenetics research in Australia
Metabolism facilitates the elimination, detoxification and excretion in urine or bile (as
biotransformation products) of a myriad of structurally diverse drugs and other chemicals …
biotransformation products) of a myriad of structurally diverse drugs and other chemicals …
Influence of CYP2C8*3 and ABCG2 C421A genetic polymorphisms on trough concentration and molecular response of imatinib in Egyptian patients with chronic …
SA Mangoura, MH Abdel-Raheem, HA Eltyb… - Cancer Chemotherapy …, 2025 - Springer
Purpose The treatment landscape for chronic myeloid leukemia (CML) has been
revolutionized by the introduction of imatinib, a tyrosine kinase inhibitor, which has …
revolutionized by the introduction of imatinib, a tyrosine kinase inhibitor, which has …