Importance of Prodrug-activating Enzymes in Drug Development and Precision Pharmacotherapy
Monday April 04, 2022
3:30 pm
-
5:00 pm
Central Time (CT)
113 C
DDD
DMDD
TCP
Chair :
Hao-Jie Zhu
University of Michigan
This session will discuss how genetic variants and tissue-specific expression of drug-metabolizing enzymes could affect the activation, pharmacokinetics, and therapeutic efficacy of various prodrugs with a focus on antiviral and anticancer medications. The session will stimulate the discussion regarding how to use genetic variants and tissue-specific proteomics information of drug-metabolizing enzymes to improve the design and delivery of prodrugs and enhance the efficacy and safety of prodrug pharmacotherapy.
Speakers
Namandjé Bumpus
- Johns Hopkins University
Pharmacogenetics of Kinases and Its Impact on the Activation of Nucleotide Reverse Transcriptase Inhibitor Prodrugs
Nucleotide reverse transcriptase inhibitors, such as tenofovir and emtricitabine, are key components of HIV treatment and HIV Pre-exposure Prophylaxis. These drugs are prodrugs and require phosphorylation by kinases within host cells in order to become activated. This talk will discuss the impact of genetic variation in kinases including adenylate and creatine kinases on the activation of clinically important nucleotide reverse transcriptase inhibitors.
Longqin Hu
- Rutgers University
Design of Anticancer Prodrugs for Site-specific Activation in Tumor Tissues through Bioreduction and Proteolysis
Many anticancer agents in current clinical use lack the desired tumor selectivity and are associated with systemic side effects. Prodrug design is one approach that could potentially improve the target-selectivity of anticancer agents. This talk will discuss the design of anticancer prodrugs for site-specific activation in tumor tissues through bioreduction and proteolysis
Hao-Jie Zhu
- University of Michigan
Proteomics of Drug-metabolizing Enzymes and Its Implications in the Development of Anti-COVID-19 Prodrugs
Anti-COVID-19 prodrugs (e.g., remdesivir) are activated by specific drug-metabolizing enzymes. This talk, co-presented by Drs Hao-Jie Zhu and Joy Feng, will discuss the proteomics of the activating enzymes in various organs related to the pharmacokinetics and pharmacodynamics of anti-COVID-19 prodrugs and the strategy of using the information to improve the design of anti-COVID-19 prodrugs.
Joy Feng
- Gilead
Proteomics of Drug-metabolizing Enzymes and Its Implications in the Development of Anti-COVID-19 Prodrugs
Anti-COVID-19 prodrugs (e.g., remdesivir) are activated by specific drug-metabolizing enzymes. This talk, co-presented by Drs Hao-Jie Zhu and Joy Feng, will discuss the proteomics of the activating enzymes in various organs related to the pharmacokinetics and pharmacodynamics of anti-COVID-19 prodrugs and the strategy of using the information to improve the design of anti-COVID-19 prodrugs.
Bing Yang
- University of Tennessee Health Science Center
Abstract #2772 - Ethanol Inhibits the Metabolism of the Multiple Sclerosis Drug Dimethyl Fumarate to its Active Metabolite and Decreases Brain Exposure