Advanced search
Publication Cover
Xenobiotica
the fate of foreign compounds in biological systems
Volume 38, 2008 - Issue 11
Submit an article Journal homepage
236
Views
17
CrossRef citations to date
0
Altmetric
Research Article

Assessing and minimizing time-dependent inhibition of cytochrome P450 3A in drug discovery: A case study with melanocortin-4 receptor agonists

W. Tang Department of Drug Metabolism and Pharmacokinetics, Merck Research Laboratories, Rahway, NJ, USACorrespondence[email protected]
,
R. A. Stearns Department of Drug Metabolism and Pharmacokinetics, Merck Research Laboratories, Rahway, NJ, USA
,
R. W. Wang Department of Drug Metabolism and Pharmacokinetics, Merck Research Laboratories, Rahway, NJ, USA
,
R. R. Miller Department of Drug Metabolism and Pharmacokinetics, Merck Research Laboratories, Rahway, NJ, USA
,
Q. Chen Department of Drug Metabolism and Pharmacokinetics, Merck Research Laboratories, Rahway, NJ, USA
,
J. Ngui Department of Drug Metabolism and Pharmacokinetics, Merck Research Laboratories, Rahway, NJ, USA
,
R. K. Bakshi Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ, USA
,
R. P. Nargund Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ, USA
,
D. C. Dean Department of Drug Metabolism and Pharmacokinetics, Merck Research Laboratories, Rahway, NJ, USA
&
T. A. Baillie Department of Drug Metabolism and Pharmacokinetics, Merck Research Laboratories, Rahway, NJ, USA
 show all
Pages 1437-1451 | Received 21 Jul 2008, Accepted 09 Sep 2008, Published online: 04 Nov 2008

Citations (17)

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

Subscribe to citation updates

Read on this site (2)

Wei Tang & Anthony Y.H. Lu. (2010) Metabolic bioactivation and drug-related adverse effects: current status and future directions from a pharmaceutical research perspective. Drug Metabolism Reviews 42:2, pages 225-249.
Read now
Zhi-Wei Zhou & Shu-Feng Zhou. (2009) Application of mechanism-based CYP inhibition for predicting drug–drug interactions. Expert Opinion on Drug Metabolism & Toxicology 5:6, pages 579-605.
Read now

Articles from other publishers (15)

Chunyong He, Yuchang Mao & Hong Wan. (2023) Preclinical evaluation of chemically reactive metabolites and mitigation of bioactivation in drug discovery. Drug Discovery Today 28:7, pages 103621.
Crossref
Jaclyn R. Patterson, Lamont R. Terrell, Carla A. Donatelli, Dennis A. Holt, Larry J. Jolivette, Ralph A. Rivero, Theresa J. Roethke, Arthur Shu, Patrick Stoy, Guosen Ye, Mark Youngman & Brian G. Lawhorn. (2020) Design and Optimization of an Acyclic Amine Series of TRPV4 Antagonists by Electronic Modulation of Hydrogen Bond Interactions. Journal of Medicinal Chemistry 63:23, pages 14867-14884.
Crossref
Shaoyi Sun & Jianmin Fu. (2018) Methyl-containing pharmaceuticals: Methylation in drug design. Bioorganic & Medicinal Chemistry Letters 28:20, pages 3283-3289.
Crossref
Bianca M. Liederer, Xingrong Liu, Simon Wong & Daniel R. Mudra. 2017. Translating Molecules into Medicines. Translating Molecules into Medicines 165 230 .
Thomas A. Baillie. 2015. New Horizons in Predictive Drug Metabolism and Pharmacokinetics. New Horizons in Predictive Drug Metabolism and Pharmacokinetics 202 226 .
Xing Liu, Yuanfu Lu, Xinfu Guan, Bingning Dong, Hemantkumar Chavan, Jin Wang, Yiqing Zhang, Partha Krishnamurthy & Feng Li. (2015) Metabolomics reveals the formation of aldehydes and iminium in gefitinib metabolism. Biochemical Pharmacology 97:1, pages 111-121.
Crossref
Feng Li, Jie Lu & Xiaochao Ma. (2014) CPY3A4-Mediated α -Hydroxyaldehyde Formation in Saquinavir Metabolism . Drug Metabolism and Disposition 42:2, pages 213-220.
Crossref
Amit S. Kalgutkar & Antonia F. Stepan. 2012. Analogue‐Based Drug Discovery III. Analogue‐Based Drug Discovery III 37 75 .
Suvi T. M. Orr, Sharon L. Ripp, T. Eric Ballard, Jaclyn L. Henderson, Dennis O. Scott, R. Scott Obach, Hao Sun & Amit S. Kalgutkar. (2012) Mechanism-Based Inactivation (MBI) of Cytochrome P450 Enzymes: Structure–Activity Relationships and Discovery Strategies To Mitigate Drug–Drug Interaction Risks. Journal of Medicinal Chemistry 55:11, pages 4896-4933.
Crossref
Kevin L. Salyers & Yang Xu. 2012. ADME‐Enabling Technologies in Drug Design and Development. ADME‐Enabling Technologies in Drug Design and Development 253 276 .
Alexander V. LyubimovThomas A. Baillie. 2011. Encyclopedia of Drug Metabolism and Interactions. Encyclopedia of Drug Metabolism and Interactions 1 24 .
Yukihiro Nishio, Hidenori Kimura, Naoyuki Sawada, Eiji Sugaru, Masakuni Horiguchi, Michiko Ono, Yudai Furuta, Mutsuko Sakai, Yumi Masui, Misato Otani, Takahiko Hashizuka, Yayoi Honda, Jiro Deguchi, Tsutomu Nakagawa & Hiroyuki Nakahira. (2011) 2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5-yl}methyl)-4-fluorobenzonitrile (DSR-12727): A potent, orally active dipeptidyl peptidase IV inhibitor without mechanism-based inactivation of CYP3A. Bioorganic & Medicinal Chemistry 19:18, pages 5490-5499.
Crossref
Cuyue Tang & Thomayant Prueksaritanont. (2010) Use of In Vivo Animal Models to Assess Pharmacokinetic Drug-Drug Interactions. Pharmaceutical Research 27:9, pages 1772-1787.
Crossref
Simon G. Wong, Peter W. Fan, Raju Subramanian, George R. Tonn, Kirk R. Henne, Michael G. Johnson, Michelle Tadano Lohr & Bradley K. Wong. (2010) Bioactivation of a Novel 2-Methylindole-Containing Dual Chemoattractant Receptor-Homologous Molecule Expressed on T-Helper Type-2 Cells/d-Prostanoid Receptor Antagonist Leads to Mechanism-Based CYP3A Inactivation: Glutathione Adduct Characterization and Prediction of In Vivo Drug-Drug Interaction. Drug Metabolism and Disposition 38:5, pages 841-850.
Crossref
Bernard P. Murray. 2009. Annual Reports in Medicinal Chemistry Volume 44. Annual Reports in Medicinal Chemistry Volume 44 535 553 .

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:

Order Reprints Request Corporate Permissions

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:

Request Academic Permissions

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.

Related research

People also read lists articles that other readers of this article have read.

Recommended articles lists articles that we recommend and is powered by our AI driven recommendation engine.

Cited by lists all citing articles based on Crossref citations.
Articles with the Crossref icon will open in a new tab.