ReviewEuropean journal of drug metabolism and pharmacokinetics2011
Chemical inhibitors of cytochrome P450 isoforms in human liver microsomes: a re-evaluation of P450 isoform selectivity.
Review in European journal of drug metabolism and pharmacokinetics, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 42 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
42 citing papers in PubMed, 136 citations in OpenAlex.
- In vitro and in vivo human metabolism and pharmacokinetics of S- and R-praziquantel.Pharmacology research & perspectives · 2020Trial
- Synthesis of aryl-fused bicyclo[3.1.1]heptanes and validation as naphthyl bioisosteres.Nature chemistry · 2026Article
- Article
- Ionic Liquid 1-Octyl-3-Methylimidazolium (M8OI) Is Mono-Oxygenated by CYP3A4 and CYP3A5 in Adult Human Liver.Journal of xenobiotics · 2024Article
- A Review of CYP-Mediated Drug Interactions: Mechanisms and In Vitro Drug-Drug Interaction Assessment.Biomolecules · 2024Review
- Next-generation of BBQ analogues that selectively target breast cancer.Frontiers in chemistry · 2024Article
- A Novel Cytochrome P450 2E1 Inhibitor Q11 Is Effective on Lung Cancer via Regulation of the Inflammatory Microenvironment.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2023Article
- The role of cytochrome P450 3A4-mediated metabolism in sorafenib and lapatinib hepatotoxicity.Livers · 2023Article
- A Physiologically-Based Pharmacokinetic Model for Cannabidiol in Healthy Adults, Hepatically-Impaired Adults, and Children.Drug metabolism and disposition: the biological fate of chemicals · 2023Article
- Characterizing and Quantifying Extrahepatic Metabolism of (-)-ΔDrug metabolism and disposition: the biological fate of chemicals · 2022Article
- Towards the Elucidation of the Pharmacokinetics of Voriconazole: A Quantitative Characterization of Its Metabolism.Pharmaceutics · 2022Article
- Biological Activity and Stability of Aeruginosamides from Cyanobacteria.Marine drugs · 2022Article
- CYP2C9 and 3A4 play opposing roles in bioactivation and detoxification of diphenylamine NSAIDs.Biochemical pharmacology · 2021Article
- Meloxicam methyl group determines enzyme specificity for thiazole bioactivation compared to sudoxicam.Toxicology letters · 2021Article
- Effects of Avitinib on CYP450 Enzyme Activity in vitro and in vivo in Rats.Drug design, development and therapy · 2021Article
- In vitro evaluation of the metabolic enzymes and drug interaction potential of triapine.Cancer chemotherapy and pharmacology · 2020Article
- Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death.Journal of medicinal chemistry · 2020Article
- Strong and Selective Inhibitory Effects of the Biflavonoid Selamariscina A against CYP2C8 and CYP2C9 Enzyme Activities in Human Liver Microsomes.Pharmaceutics · 2020Article
- Impact of cytochrome P450 variation on meperidineXenobiotica; the fate of foreign compounds in biological systems · 2020Article
- Structural Insights into the Interaction of Cytochrome P450 3A4 with Suicide Substrates: Mibefradil, Azamulin and 6',7'-Dihydroxybergamottin.International journal of molecular sciences · 2019Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The majority of marketed small-molecule drugs undergo metabolism by hepatic Cytochrome P450 (CYP) enzymes (Rendic 2002). Since these enzymes metabolize a structurally diverse number of drugs, metabolism-based drug-drug interactions (DDIs) can potentially occur when multiple drugs are coadministered to patients. Thus, a careful in vitro assessment of the contribution of various CYP isoforms to the total metabolism is important for predicting whether such DDIs might take place. One method of CYP phenotyping involves the use of potent and selective chemical inhibitors in human liver microsomal incubations in the presence of a test compound. The selectivity of such inhibitors plays a critical role in deciphering the involvement of specific CYP isoforms. Here, we review published data on the potency and selectivity of chemical inhibitors of the major human hepatic CYP isoforms. The most selective inhibitors available are furafylline (in co-incubation and pre-incubation conditions) for CYP1A2, 2-phenyl-2-(1-piperidinyl)propane (PPP) for CYP2B6, montelukast for CYP2C8, sulfaphenazole for CYP2C9, (-)-N-3-benzyl-phenobarbital for CYP2C19 and quinidine for CYP2D6. As for CYP2A6, tranylcypromine is the most widely used inhibitor, but on the basis of initial studies, either 3-(pyridin-3-yl)-1H-pyrazol-5-yl)methanamine (PPM) and 3-(2-methyl-1H-imidazol-1-yl)pyridine (MIP) can replace tranylcypromine as the most selective CYP2A6 inhibitor. For CYP3A4, ketoconazole is widely used in phenotyping studies, although azamulin is a far more selective CYP3A inhibitor. Most of the phenotyping studies do not include CYP2E1, mostly because of the limited number of new drug candidates that are metabolized by this enzyme. Among the inhibitors for this enzyme, 4-methylpyrazole appears to be selective.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.