Reaction Phenotyping: Current Industry Efforts to Identify Enzymes Responsible for Metabolizing Drug Candidates
Explore this paper's citation graph
Summary
A limited review of current approaches to reaction phenotyping studies used within the pharmaceutical industry is presented.
- Type
- article
- Published
- 2008-04-05
- Cited by
- 64
- References
- 51
- Access
- Open access
- OpenAlex
- https://openalex.org/W18446520
- Semantic Scholar
- https://api.semanticscholar.org/CorpusID:24539352
Keywords
Computer science
References
- Integrated cytochrome P450 reaction phenotyping: attempting to bridge the gap between cDNA-expressed cytochromes P450 and native human liver microsomes.
- Use of in vitro human metabolism studies in drug development. An industrial perspective.
- Glucuronidation of 3′-Azido-3′-Deoxythymidine (Zidovudine) by Human Liver Microsomes: Relevance to Clinical Pharmacokinetic Interactions with Atovaquone, Fluconazole, Methadone, and Valproic Acid
- Clinically important pharmacokinetic drug–drug interactions: role of cytochrome P450 enzymes
- Cytochrome P450 inhibitors. Evaluation of specificities in the in vitrometabolism of therapeutic agents by human liver microsomes.
- Dietary indole-3-carbinol inhibits FMO activity and the expression of flavin-containing monooxygenase form 1 in rat liver and intestine.
- Monoclonal antibodies specific and inhibitory to human cytochromes P450 2C8, 2C9, and 2C19.
- Pharmacokinetic Interaction between Ritonavir and Indinavir in Healthy Volunteers
- Interindividual variability in acetaminophen glucuronidation by human liver microsomes: identification of relevant acetaminophen UDP-glucuronosyltransferase isoforms.
- The in vitro interaction of dexmedetomidine with human liver microsomal cytochrome P4502D6 (CYP2D6).
- In vitro glucuronidation using human liver microsomes and the pore-forming peptide alamethicin.
- Verification of the selectivity of (+)N-3-benzylnirvanol as a CYP2C19 inhibitor.
- Genetic polymorphism of cytochrome P450s, CYP2C19, and CYP2C9 in a Japanese population.
- Interethnic differences in genetic polymorphism of debrisoquin and mephenytoin hydroxylation between Japanese and Caucasian populations
- Polymorphic Gene Regulation and Interindividual Variation of UDP-glucuronosyltransferase Activity in Human Small Intestine*
- UDP-glucuronosyltransferases and clinical drug-drug interactions.
- Interaction of sulfaphenazole derivatives with human liver cytochromes P450 2C: molecular origin of the specific inhibitory effects of sulfaphenazole on CYP 2C9 and consequences for the substrate binding site topology of CYP 2C9.
- Characterization of the inhibition of P4501A2 by furafylline.
- Mechanism of alamethicin insertion into lipid bilayers.
- Monospecific antipeptide antibodies against human hepatic UDP-glucuronosyltransferase 1A subfamily (UGT1A) isoforms.
Cited by
- A High-Throughput (HTS) Assay for Enzyme Reaction Phenotyping in Human Recombinant P450 Enzymes Using LC-MS/MS.
- Determination of metabolic profile of novel triethylamine containing thiophene S006-830 in rat, rabbit, dog and human liver microsomes.
- In Vitro Kinetic Characterization of Axitinib Metabolism
- Chemical inhibitors of CYP450 enzymes in liver microsomes: combining selectivity and unbound fractions to guide selection of appropriate concentration in phenotyping assays
- In vitro metabolism of a novel antithrombotic compound, S002-333, and its enantiomers: quantitative cytochrome P450 phenotyping, metabolic profiling and enzyme kinetic studies
- Assays and applications in warfarin metabolism: what we know, how we know it and what we need to know
- Reaction Phenotyping: Advances in the Experimental Strategies Used to Characterize the Contribution of Drug-Metabolizing Enzymes
- In vitro metabolism of piperaquine is primarily mediated by CYP3A4
- Metabolic activation of clopidogrel: in vitro data provide conflicting evidence for the contributions of CYP2C19 and PON1
- Are there differences in the catalytic activity per unit enzyme of recombinantly expressed and human liver microsomal cytochrome P450 2C9? A systematic investigation into inter‐system extrapolation factors
- Selective Mechanism-Based Inactivation of CYP3A4 by CYP3cide (PF-04981517) and Its Utility as an In Vitro Tool for Delineating the Relative Roles of CYP3A4 versus CYP3A5 in the Metabolism of Drugs
- Incorporating population variability and susceptible subpopulations into dosimetry for high-throughput toxicity testing.
- Preclinical Pharmacokinetics of a HepDirect Prodrug of a Novel Phosphonate-Containing Thyroid Hormone Receptor Agonist
- Software-aided cytochrome P450 reaction phenotyping and kinetic analysis in early drug discovery.
- Evaluation of a New Molecular Entity as a Victim of Metabolic Drug-Drug Interactions—an Industry Perspective
- In vitro identification of cytochrome P450 enzymes responsible for drug metabolism.
- Investigating the chemical space and metabolic bioactivation of natural products and cross-reactivity of chemical inhibitors in CYP450 phenotyping
- In vitro metabolism of the anti-inflammatory clerodane diterpenoid polyandric acid A and its hydrolysis product by human liver microsomes and recombinant cytochrome P450 and UDP-glucuronosyltransferase enzymes
- Improvement of the chemical inhibition phenotyping assay by cross-reactivity correction
- In vitro metabolism studies of natural products are crucial in the early development of medicines
Related papers
No related papers recorded.