605
Views
23
CrossRef citations to date
0
Altmetric
Review Article

Mechanism-based inactivation of CYP450 enzymes: a case study of lapatinib

, , &
Pages 21-28 | Received 11 Sep 2014, Accepted 20 Dec 2014, Published online: 02 Feb 2015

Keep up to date with the latest research on this topic with citation updates for this article.

Read on this site (2)

Miao Yan, Wenqun Li, Wen-Bo Li, Qi Huang, Jing Li, Hua-Lin Cai, Hui Gong, Bi-Kui Zhang & Yi-Kun Wang. (2023) Metabolic activation of tyrosine kinase inhibitors: recent advance and further clinical practice. Drug Metabolism Reviews 55:1-2, pages 94-106.
Read now
Chunyong He & Hong Wan. (2018) Drug metabolism and metabolite safety assessment in drug discovery and development. Expert Opinion on Drug Metabolism & Toxicology 14:10, pages 1071-1085.
Read now

Articles from other publishers (21)

Ni-hong Pang, Ren-ai Xu, Lian-guo Chen, Zhe Chen, Guo-xin Hu & Bo-wen Zhang. (2024) Inhibitory effects of the main metabolites of Apatinib on CYP450 isozymes in human and rat liver microsomes. Toxicology in Vitro 95, pages 105739.
Crossref
Lloyd Wei Tat Tang & Eric Chun Yong Chan. (2022) Metabolic activation of drugs by cytochrome P450 enzymes: Biochemical insights into mechanism-based inactivation by fibroblast growth factor receptor inhibitors and chemical approaches to attenuate reactive metabolite formation. Biochemical Pharmacology 206, pages 115336.
Crossref
Nancy H. C. Loos, Jos H. Beijnen & Alfred H. Schinkel. (2022) The Mechanism-Based Inactivation of CYP3A4 by Ritonavir: What Mechanism?. International Journal of Molecular Sciences 23:17, pages 9866.
Crossref
Lloyd Wei Tat Tang, Guoyi Wu & Eric Chun Yong Chan. (2022) Identification of Infigratinib as a Potent Reversible Inhibitor and Mechanism-Based Inactivator of CYP2J2: Nascent Evidence for a Potential In Vivo Metabolic Drug-Drug Interaction with Rivaroxaban. Journal of Pharmacology and Experimental Therapeutics 382:2, pages 123-134.
Crossref
Lloyd Wei Tat Tang, Jiaxin Fu, Siew Kwan Koh, Guoyi Wu, Lei Zhou & Eric Chun Yong Chan. (2022) Metabolic Activation of the Acrylamide Michael Acceptor Warhead in Futibatinib to an Epoxide Intermediate Engenders Covalent Inactivation of CYP3A. Drug Metabolism and Disposition 50:7, pages 931-941.
Crossref
Eda Dogan, Hale Guler Kara, Buket Kosova & Vildan Bozok Cetintas. 2022. Metastasis. Metastasis 163 180 .
Lloyd Wei Tat Tang, Wan Wei, Ravi Kumar Verma, Siew Kwan Koh, Lei Zhou, Hao Fan & Eric Chun Yong Chan. (2022) Direct and Sequential Bioactivation of Pemigatinib to Reactive Iminium Ion Intermediates Culminates in Mechanism-Based Inactivation of Cytochrome P450 3A. Drug Metabolism and Disposition 50:5, pages 529-540.
Crossref
Jacqueline Wen Hui Leow, Lloyd Wei Tat Tang & Eric Chun Yong Chan. 2022. Pharmacology and Toxicology of Cytochrome P450 – 60th Anniversary. Pharmacology and Toxicology of Cytochrome P450 – 60th Anniversary 131 176 .
Lloyd Wei Tat Tang, Jian Wei Teng, Ravi Kumar Verma, Siew Kwan Koh, Lei Zhou, Mei Lin Go, Hao Fan & Eric Chun Yong Chan. (2021) Infigratinib Is a Reversible Inhibitor and Mechanism-Based Inactivator of Cytochrome P450 3A4. Drug Metabolism and Disposition 49:9, pages 856-868.
Crossref
Lloyd Wei Tat Tang, Jian Wei Teng, Siew Kwan Koh, Lei Zhou, Mei Lin Go & Eric Chun Yong Chan. (2021) Mechanism-Based Inactivation of Cytochrome P450 3A4 and 3A5 by the Fibroblast Growth Factor Receptor Inhibitor Erdafitinib. Chemical Research in Toxicology 34:7, pages 1800-1813.
Crossref
Lloyd Wei Tat Tang, Ravi Kumar Verma, Hao Fan & Eric Chun Yong Chan. (2021) Mechanism-Based Inactivation of Cytochrome P450 3A4 by Benzbromarone. Molecular Pharmacology 99:4, pages 266-276.
Crossref
Michael Mohutsky & Stephen D. Hall. 2021. Enzyme Kinetics in Drug Metabolism. Enzyme Kinetics in Drug Metabolism 51 88 .
Tingting Jiang, Ting Cheng, Jing Li, Mengyue Zhou, Rong Tan, Xiaojing Yang, Yang Wang, Weiwei Li & Jiang Zheng. (2020) Bergaptol, a mechanism-based inactivator of CYP2C9. Medicinal Chemistry Research 29:7, pages 1230-1237.
Crossref
Jie Jack Li. 2020. Medicinal Chemistry for Practitioners. Medicinal Chemistry for Practitioners 305 379 .
Jie Jack Li. 2020. Medicinal Chemistry for Practitioners. Medicinal Chemistry for Practitioners 1 96 .
Hong Huang, Xue Bai & Lijun Yang. (2020) Intriguing generative metabolism discovery of reactive metabolite nitroso of lapatinib and relevant structural modification. International Journal of Quantum Chemistry 120:12.
Crossref
Jennifer E. Bissada, Vivian Truong, Arsany A. Abouda, Kahari J. Wines, Rachel D. Crouch & Klarissa D. Jackson. (2019) Interindividual Variation in CYP3A Activity Influences Lapatinib Bioactivation. Drug Metabolism and Disposition 47:11, pages 1257-1269.
Crossref
Marie‐Noëlle Paludetto, Florent Puisset, Etienne Chatelut & Cécile Arellano. (2019) Identifying the reactive metabolites of tyrosine kinase inhibitors in a comprehensive approach: Implications for drug‐drug interactions and hepatotoxicity. Medicinal Research Reviews 39:6, pages 2105-2152.
Crossref
Anne M. Filppula, Tiffany M. Mustonen & Janne T. Backman. (2018) In Vitro Screening of Six Protein Kinase Inhibitors for Time-Dependent Inhibition of CYP2C8 and CYP3A4: Possible Implications with regard to Drug-Drug Interactions. Basic & Clinical Pharmacology & Toxicology 123:6, pages 739-748.
Crossref
Juanita S. Lopez & Udai Banerji. (2016) Combine and conquer: challenges for targeted therapy combinations in early phase trials. Nature Reviews Clinical Oncology 14:1, pages 57-66.
Crossref
J. K. Towles, R. N. Clark, M. D. Wahlin, V. Uttamsingh, A. E. Rettie & K. D. Jackson. (2016) Cytochrome P450 3A4 and CYP3A5-Catalyzed Bioactivation of Lapatinib. Drug Metabolism and Disposition 44:10, pages 1584-1597.
Crossref

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.