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Journal articles on the topic 'CYP2C8*5'

Author: Grafiati

Published: 3 June 2025

Last updated: 31 July 2025

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1

Niwa, Toshiro, and Yurie Imagawa. "Substrate Specificity of Human Cytochrome P450 (CYP) 2C Subfamily and Effect of Azole Antifungal Agents on CYP2C8." Journal of Pharmacy & Pharmaceutical Sciences 19, no. 4 (2016): 423. http://dx.doi.org/10.18433/j31s53.

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PURPOSE: The metabolic activities of aminopyrine N-demethylation and tolbutamide methylhydroxylation by the human hepatic cytochrome P450 (P450 or CYP) 2C subfamily were compared and the effects of azole antifungal agent on the drug-metabolizing activity of CYP2C8 were investigated. METHODS: Aminopyrine N-demethylation and tolbutamide methylhydroxylation by CYP2C8, CYP2C9, and CYP2C19 were determined by the previous reported methods. The effects of five azole antifungal agents, fluconazole, itraconazole, ketoconazole, miconazole, and voriconazole, on the aminopyrine N-demethylation activity by

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Chamboko, Chiratidzo R., Wayde Veldman, Rolland Bantar Tata, Birgit Schoeberl, and Özlem Tastan Bishop. "Human Cytochrome P450 1, 2, 3 Families as Pharmacogenes with Emphases on Their Antimalarial and Antituberculosis Drugs and Prevalent African Alleles." International Journal of Molecular Sciences 24, no. 4 (2023): 3383. http://dx.doi.org/10.3390/ijms24043383.

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Precision medicine gives individuals tailored medical treatment, with the genotype determining the therapeutic strategy, the appropriate dosage, and the likelihood of benefit or toxicity. Cytochrome P450 (CYP) enzyme families 1, 2, and 3 play a pivotal role in eliminating most drugs. Factors that affect CYP function and expression have a major impact on treatment outcomes. Therefore, polymorphisms of these enzymes result in alleles with diverse enzymatic activity and drug metabolism phenotypes. Africa has the highest CYP genetic diversity and also the highest burden of malaria and tuberculosis

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3

Zobdeh, Farzin, Ivan I. Eremenko, Mikail A. Akan, et al. "Pharmacogenetics and Pain Treatment with a Focus on Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) and Antidepressants: A Systematic Review." Pharmaceutics 14, no. 6 (2022): 1190. http://dx.doi.org/10.3390/pharmaceutics14061190.

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Background: This systematic review summarizes the impact of pharmacogenetics on the effect and safety of non-steroidal anti-inflammatory drugs (NSAIDs) and antidepressants when used for pain treatment. Methods: A systematic literature search was performed according to the preferred reporting items for systematic reviews and meta-analysis (PRISMA) guidelines regarding the human in vivo efficacy and safety of NSAIDs and antidepressants in pain treatment that take pharmacogenetic parameters into consideration. Studies were collected from PubMed, Scopus, and Web of Science up to the cutoff date 18

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Seo, Hyung-Ju, Seung-Bae Ji, Sin-Eun Kim, et al. "Inhibitory Effects of Schisandra Lignans on Cytochrome P450s and Uridine 5′-Diphospho-Glucuronosyl Transferases in Human Liver Microsomes." Pharmaceutics 13, no. 3 (2021): 371. http://dx.doi.org/10.3390/pharmaceutics13030371.

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Schisandra chinensis has been widely used as a traditional herbal medicine to treat chronic coughs, fatigue, night sweats, and insomnia. Numerous bioactive components including lignans have been identified in this plant. Lignans with a dibenzocyclooctadiene moiety have been known to possess anti-cancer, anti-inflammatory, and hepatoprotective activity. Fragmentary studies have reported the ability of some lignans to modulate some cytochrome P450 (P450) enzymes. Herein, we investigated the drug interaction potential of six dibenzocyclooctadiene lignans (schisandrin, gomisin A, B, C, and N, and

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5

Charles, Brown, Larbie Christopher, and Selorm Yao Amuzu Dominic. "Prevalence of the Genetic Mutation CYP2C8*5 in Selected Ethnic Groups in Southern Ghana." International Journal of Biochemistry Research & Review 12, no. 3 (2016): 1–9. https://doi.org/10.9734/IJBCRR/2016/25680.

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Aim: The study determined prevalence of clinically relevant CYP2C8*5 polymorphism in 80 unrelated individuals, from selected ethnic groups in Southern Ghana. Medical history on adverse drug reactions of the subjects and level of dependencyon drugs metabolized by CYP2C8 enzyme was obtained by questionnaire. Allele Specific-PCR analyses were used to genotype CYP2C8*5 alleles in the study subjects. Results: Allelic frequency for CYP2C8*5was 83.75% which was statistically significant (p<0.05). There was no significant difference (p> 0.05) in the prevalence of CYP2C8*5allele within the ethnic

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6

Park, So-Young, Phi-Hung Nguyen, Gahyun Kim, et al. "Strong and Selective Inhibitory Effects of the Biflavonoid Selamariscina A against CYP2C8 and CYP2C9 Enzyme Activities in Human Liver Microsomes." Pharmaceutics 12, no. 4 (2020): 343. http://dx.doi.org/10.3390/pharmaceutics12040343.

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Like flavonoids, biflavonoids, dimeric flavonoids, and polyphenolic plant secondary metabolites have antioxidant, antibacterial, antiviral, anti-inflammatory, and anti-cancer properties. However, there is limited data on their effects on cytochrome P450 (P450) and uridine 5′-diphosphoglucuronosyl transferase (UGT) enzyme activities. In this study we evaluate the inhibitory potential of five biflavonoids against nine P450 activities (P450s1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A) in human liver microsomes (HLMs) using cocktail incubation and liquid chromatography-tandem mass spectrometry

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7

Park, Eun Jeong, Ria Park, Ji-Hyeon Jeon, et al. "Inhibitory Effect of AB-PINACA, Indazole Carboxamide Synthetic Cannabinoid, on Human Major Drug-Metabolizing Enzymes and Transporters." Pharmaceutics 12, no. 11 (2020): 1036. http://dx.doi.org/10.3390/pharmaceutics12111036.

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Indazole carboxamide synthetic cannabinoid, AB-PINACA, has been placed into Schedule I of the Controlled Substances Act by the US Drug Enforcement Administration since 2015. Despite the possibility of AB-PINACA exposure in drug abusers, the interactions between AB-PINACA and drug-metabolizing enzymes and transporters that play crucial roles in the pharmacokinetics and efficacy of various substrate drugs have not been investigated. This study was performed to investigate the inhibitory effects of AB-PINACA on eight clinically important human major cytochrome P450s (CYPs) and six uridine 5′-diph

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8

Denisenko, N. P., Sh P. Abdullaev, K. A. Akmalova, et al. "Structure of the distribution of genetic determinants of the efficacy and safety of non-steroidal anti-inflammatory drugs in the Russian population: focus on CYP2C8, PTGS1 and PTGS2." Modern Rheumatology Journal 16, no. 1 (2022): 60–67. http://dx.doi.org/10.14412/1996-7012-2022-1-60-67.

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The efficacy and safety of non-steroidal anti-inflammatory drugs (NSAIDs) may be determined by the polymorphic nature of the CYP2C8, PTGS1 and PTGS2 genes.Objective: to analyze the nature of the distribution of CYP2C8*3 (rs10509681), CYP2C8*3 (rs11572080), PTGS1 (rs10306135), PTGS1 (rs12353214) and PTGS2 (rs20417) among residents of the North Caucasus.Patients and methods. The study involved 676 volunteers from Russian, Balkar, Kabardian and Ossetian ethnic groups. Carriage of polymorphic markers CYP2C8, PTGS1 and PTGS2 was determined using real-time polymerase chain reaction.Results and discu

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Crosby, Samantha V., Izzeldin Y. Ahmed, Laura R. Osborn, et al. "Similar 5F-APINACA Metabolism between CD-1 Mouse and Human Liver Microsomes Involves Different P450 Cytochromes." Metabolites 12, no. 8 (2022): 773. http://dx.doi.org/10.3390/metabo12080773.

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In 2019, synthetic cannabinoids accounted for more than one-third of new drugs of abuse worldwide; however, assessment of associated health risks is not ethical for controlled and often illegal substances, making CD-1 mouse exposure studies the gold standard. Interpretation of those findings then depends on the similarity of mouse and human metabolic pathways. Herein, we report the first comparative analysis of steady-state metabolism of N-(1-adamantyl)-1-(5-pentyl)-1H-indazole-3-carboxamide (5F-APINACA/5F-AKB48) in CD-1 mice and humans using hepatic microsomes. Regardless of species, 5F-APINA

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Ximenes, Rosana Christine Cavalcanti, Bashir Ahmed, Vahid Nikoui, Khuseyn Egamnazarov, and Muhammad Imran Khan. "Polymorphisms in CYP2C8 gene in Pakistani population and their frequencies in various ethnic groups." Molecular Medicine Communications 1, no. 1 (2021): 03–16. http://dx.doi.org/10.55627/mmc.001.01.0016.

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Cytochrome P4502C8 represents 7% of the hepatic cytochrome system and metabolizes around 5% of drugs in phase I processes. It also plays a significant role in the metabolism of endogenous compounds. More than 20 single nucleotide polymorphisms (SNPs) have been reported, mainly in exon 3, 5, and 8. Some of the SNP’s lead to decreased enzyme activity and may have impact on drug metabolism. This research study aims to determine the frequencies of the most common SNPs of the CYP2C8 gene (CYP2C8*2, *3, *4) in the Pakistani population. A cross-sectional study consisting of 391 healthy humans was con

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Choi, Won-Gu, Ria Park, Dong Kyun Kim, Yongho Shin, Yong-Yeon Cho, and Hye Suk Lee. "Mertansine Inhibits mRNA Expression and Enzyme Activities of Cytochrome P450s and Uridine 5′-Diphospho-Glucuronosyltransferases in Human Hepatocytes and Liver Microsomes." Pharmaceutics 12, no. 3 (2020): 220. http://dx.doi.org/10.3390/pharmaceutics12030220.

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Mertansine, a tubulin inhibitor, is used as the cytotoxic component of antibody–drug conjugates (ADCs) for cancer therapy. The effects of mertansine on uridine 5′-diphospho-glucuronosyltransferase (UGT) activities in human liver microsomes and its effects on the mRNA expression of cytochrome P450s (CYPs) and UGTs in human hepatocytes were evaluated to assess the potential for drug–drug interactions (DDIs). Mertansine potently inhibited UGT1A1-catalyzed SN-38 glucuronidation, UGT1A3-catalyzed chenodeoxycholic acid 24-acyl-β-glucuronidation, and UGT1A4-catalyzed trifluoperazine N-β-d-glucuronida

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Kim, Sunjoo, Dong Kyun Kim, Yongho Shin, Ji-Hyeon Jeon, Im-Sook Song, and Hye Suk Lee. "In Vitro Interaction of AB-FUBINACA with Human Cytochrome P450, UDP-Glucuronosyltransferase Enzymes and Drug Transporters." Molecules 25, no. 19 (2020): 4589. http://dx.doi.org/10.3390/molecules25194589.

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AB-FUBINACA, a synthetic indazole carboxamide cannabinoid, has been used worldwide as a new psychoactive substance. Because drug abusers take various drugs concomitantly, it is necessary to explore potential AB-FUBINACA-induced drug–drug interactions caused by modulation of drug-metabolizing enzymes and transporters. In this study, the inhibitory effects of AB-FUBINACA on eight major human cytochrome P450s (CYPs) and six uridine 5′-diphospho-glucuronosyltransferases (UGTs) of human liver microsomes, and on eight clinically important transport activities including organic cation transporters (O

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13

Roll, Sibylle Christine, and Martina Hahn. "Rates of Divergent Pharmacogenes in a Psychiatric Cohort of Inpatients with Depression—Arguments for Preemptive Testing." Journal of Xenobiotics 12, no. 4 (2022): 317–28. http://dx.doi.org/10.3390/jox12040022.

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Background: The international drug agencies annotate pharmacogenes for many years. Pharmacogenetic testing is thus far only established in few settings, assuming that only few patients are actually affected by drug-gene interactions. Methods: 108 hospitalized patients with major depressive disorder were genotyped for CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP3A4, CYP3A5, NAT2, DPYD; VKORC1 and TMTP. Results: We found 583 (mean 5.4, median 5) divergent phenotypes (i.e., divergent from the common phenotypes considered normal, e.g., extensive metabolizer) in the 12 analyzed pharmacokine

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14

Milovanovic, DD, JR Milovanovic, M. Radovanovic, et al. "The influence of CYP2C8*3 on carbamazepine serum concentration in epileptic pediatric patients." Balkan Journal of Medical Genetics 19, no. 1 (2016): 21–28. http://dx.doi.org/10.1515/bjmg-2016-0003.

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AbstractThe aim of the present study was to investigate the distribution of CYP2C8 variants *3 and *5, as well as their effect on carbamazepine pharmacokinetic properties, in 40 epileptic pediatric patients on carbamazepine treatment. Genotyping was conducted using polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP), and allele-specific (AS)-PCR methods, and steady-state carbamazepine plasma concentrations were determined by high performance liquid chromatography (HPLC). The CYP2C8 *3 and *5 polymorphisms were found at frequencies of 17.5 and 0.0%, respectively. After

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Patil, Madhavi N., Kailas D. Datkhile, Anand K. Gudur, Rashmi A. Gudur, and Satish R. Patil. "Single-nucleotide polymorphism in CYP1A1, CYP1B1, CYP2B6, CYP2C8, and CYP2C9 genes and their association with gastrointestinal cancer: A hospital-based case-control study." Journal of Cancer Research and Therapeutics 20, no. 1 (2023): 216–23. http://dx.doi.org/10.4103/jcrt.jcrt_294_22.

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Background: Cytochrome P450 (CYP) comprises a group of phase-I metabolizing enzymes that are important in xenobiotics metabolism. Genetic polymorphism of CYPs has been comprehensively studied for their association with a range of diseases. In this study, we assessed single-nucleotide polymorphism (SNP) of CYP1A, CYP1B, CYP2B, and CYP2C and their role in gastrointestinal (GI) cancer susceptibility in the rural population of Maharashtra. Materials and Methods: In this hospital-based case-control study, the association of polymorphism of CYP genes was studied by the polymerase chain reaction-rest

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Zhang, Jiang-Wei, Yong Liu, Jie Cheng, et al. "Inhibition of Human Liver Cytochrome P450 by Star Fruit Juice." Journal of Pharmacy & Pharmaceutical Sciences 10, no. 4 (2007): 496. http://dx.doi.org/10.18433/j30593.

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Purpose. To examine the inhibitory effects of star fruit (Averrhoa carambola) juice towards seven major cytochrome P450 (CYP) isoforms and NADPH-cytochrome P450 reductase (CPR). Methods. The inhibitory effects of star fruit juice (0.5 to 5%, v/v) against the activities of seven CYP isoforms including CYP1A2, CYP2A6, CYP2C8, CYP2C9, CYP2D6, CYP2E1, CYP3A4 and CPR were examined in human liver microsomes. To identify time-dependent inhibition, star fruit juice (2.5%, v/v) was preincubated with microsomes and a NADPH-generating system for 0-15 min, and then the extent of inhibition towards seven C

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Ferrante, Karen J., Douglas B. Jacoby, and Daryl Sonnichsen. "A drug-drug interaction (DDI) study to assess the effect of oral galeterone on the pharmacokinetics (PK) of oral midazolam." Journal of Clinical Oncology 34, no. 2_suppl (2016): 316. http://dx.doi.org/10.1200/jco.2016.34.2_suppl.316.

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316 Background: Galeterone (gal) is a semisynthetic steroid that targets androgen receptor (AR) signaling via increased AR protein degradation, inhibition of CYP17 activity, and inhibition of androgen binding to AR. Gal is a novel potential treatment for prostate cancer. In vitro, gal competitively inhibits CYP3A4 (IC50 = 5.5 μM; midazolam as substrate). This clinical study evaluated whether multiple daily doses of gal alter the single-dose PK of midazolam, a sensitive probe substrate for functional CYP3A4 intestinal and hepatic activity. Methods: In an open-label, fixed sequence, DDI study, 1

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Antunes, Natalícia de Jesus, Fernanda de Lima Moreira, Karin Kipper, et al. "Prospective Prediction of Dapaconazole Clinical Drug–Drug Interactions Using an In Vitro to In Vivo Extrapolation Equation and PBPK Modeling." Pharmaceuticals 16, no. 1 (2022): 28. http://dx.doi.org/10.3390/ph16010028.

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This study predicted dapaconazole clinical drug–drug interactions (DDIs) over the main Cytochrome P450 (CYP) isoenzymes using static (in vitro to in vivo extrapolation equation, IVIVE) and dynamic (PBPK model) approaches. The in vitro inhibition of main CYP450 isoenzymes by dapaconazole in a human liver microsome incubation medium was evaluated. A dapaconazole PBPK model (Simcyp version 20) in dogs was developed and qualified using observed data and was scaled up for humans. Static and dynamic models to predict DDIs following current FDA guidelines were applied. The in vitro dapaconazole inhib

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Morozova, T. E., D. A. Shatsky, N. V. Shikh, et al. "Pharmacogenetic Aspects of Postoperative Anesthesia with Ketoprofen in Cardiac Surgery Patients." Rational Pharmacotherapy in Cardiology 17, no. 5 (2021): 719–23. http://dx.doi.org/10.20996/1819-6446-2021-10-11.

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Aim. Evaluation of the effect of polymorphisms of the CYP2D6, CYP2C8 genes on the efficacy and safety of postoperative analgesia with ketoprofen in patients with coronary artery disease after cardiac surgery.Material and methods. The study included 90 patients with an established diagnosis of coronary artery disease and postoperative period after cardiac surgery. Patients received ketoprofen 100 mg intramuscularly 2 times a day for 5 days. The intensity of pain was rated by Numeric Rating Scale. The severity of dyspepsia was assessed by the Gastrointestinal Symptom Rating Scale (GSRS) question

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Alvarado, Angel T., Mario Bolarte-Arteaga, Mario Pineda-Pérez, et al. "CYP3A4*20, CYP3A4*22, CYP2C8*3 and SLCO1B1 as genetic biomarkers to predict peripheral neuropathy induced by paclitaxel and docetaxel: A systematic review." Journal of Pharmacy & Pharmacognosy Research 13, no. 3 (2025): 955–67. https://doi.org/10.56499/jppres24.2125_13.3.955.

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Context: Cancer is a global health problem with a growing incidence year after year, and it is projected that by 2040, there will be more than 2.4 million cases in Latin America and the Caribbean, being the second cause of death in these countries. The variability of serum levels, efficacy and safety of paclitaxel and docetaxel have been associated with allelic variants of transporter and metabolizing proteins. Aims: To review the most updated and available scientific evidence on allelic variants of CYP3A4*20, CYP3A4*22, CYP2C8*3, and SLCO1B1 as genetic biomarkers to predict peripheral neuropa

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Lee, Rowoon, Vitchan Kim, Youngjin Chun, and Donghak Kim. "Structure-Functional Analysis of Human Cytochrome P450 2C8 Using Directed Evolution." Pharmaceutics 13, no. 9 (2021): 1429. http://dx.doi.org/10.3390/pharmaceutics13091429.

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The human genome includes four cytochrome P450 2C subfamily enzymes, and CYP2C8 has generated research interest because it is subject to drug–drug interactions and various polymorphic outcomes. To address the structure-functional complexity of CYP2C8, its catalytic activity was studied using a directed evolution analysis. Consecutive rounds of random mutagenesis and screening using 6-methoxy-luciferin produced two mutants, which displayed highly increased luciferase activity. Wild-type and selected mutants were expressed on a large scale and purified. The expression levels of the D349Y and D34

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Dorado, P., I. Cavaco, M. C. Cáceres, R. Piedade, V. Ribeiro, and A. LLerena. "Relationship between CYP2C8 genotypes and diclofenac 5-hydroxylation in healthy Spanish volunteers." European Journal of Clinical Pharmacology 64, no. 10 (2008): 967–70. http://dx.doi.org/10.1007/s00228-008-0508-4.

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Pavlov, Tengis S., Daria V. Ilatovskaya, Vladislav Levchenko, David L. Mattson, Richard J. Roman, and Alexander Staruschenko. "Effects of cytochrome P-450 metabolites of arachidonic acid on the epithelial sodium channel (ENaC)." American Journal of Physiology-Renal Physiology 301, no. 3 (2011): F672—F681. http://dx.doi.org/10.1152/ajprenal.00597.2010.

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Sodium reabsorption via the epithelial Na+ channel (ENaC) in the aldosterone-sensitive distal nephron plays a central role in the regulation of body fluid volume. Previous studies have indicated that arachidonic acid (AA) and its metabolite 11,12-EET but not other regioisomers of EETs inhibit ENaC activity in the collecting duct. The goal of this study was to investigate the endogenous metabolism of AA in cultured mpkCCDc14 principal cells and the effects of these metabolites on ENaC activity. Liquid chromatography/mass spectrometry analysis of the mpkCCDc14 cells indicated that these cells pr

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Ikeda, R., K. Yoshida, A. Takagane, et al. "Pharmacogenomic (PG) analysis for prediction of individual response to paclitaxel in 5-FU-refractory metastatic gastric cancer: Prediction formula of tumor response using novel marker genes and genotypes associated with the toxicity." Journal of Clinical Oncology 25, no. 18_suppl (2007): 2538. http://dx.doi.org/10.1200/jco.2007.25.18_suppl.2538.

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2538 Background: Taxanes offer hope for improving outcomes of metastatic gastric cancer patients including 5-FU failure cases, but the response remarkably varies among patients. We conducted this prospective PG study for paclitaxel monotherapy to develop a prediction formula of efficacy and to identify potent genetic markers of toxicity. Methods: Paclitaxel was intravenously given on Days 1, 8, and 15, every 4 weeks in 5-FU failure metastatic gastric cancer patients with typical eligibility criteria. Tumor and blood samples were collected before the initial paclitaxel administration for PG. PK

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Klyushova, L. S., Yu A. Golubeva, V. A. Vavilin, and A. Yu Grishanova. "Modulating effect of Cu(II) complexes with enamine and tetrazole derivatives on CYP2C and CYP3A and their cytotoxic and antiproliferative properties in HepG2 spheroids." Acta Biomedica Scientifica 7, no. 5-2 (2022): 31–41. http://dx.doi.org/10.29413/abs.2022-7.5-2.4.

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CYP2C and CYP3A cytochromes are induced by a variety of compounds and affect the pharmacokinetics and pharmacodynamics of a large number of drugs. Currently, the possibility of using copper coordination compounds in antitumor therapy is being actively studied. Evaluation of potential interactions between new molecules and P450 cytochromes is necessary at an early stage of drug design.The aim. To study the modulating effect of Cu(II) complexes with enamine and tetrazole derivatives on CYP2C9, CYP2C19 and CYP3A4 and their cytotoxic and antiproliferative properties on normal human lung fibroblast

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Webler, Anke C., U. Ruth Michaelis, Rüdiger Popp, et al. "Epoxyeicosatrienoic acids are part of the VEGF-activated signaling cascade leading to angiogenesis." American Journal of Physiology-Cell Physiology 295, no. 5 (2008): C1292—C1301. http://dx.doi.org/10.1152/ajpcell.00230.2008.

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Cytochrome P-450 (CYP) epoxygenases metabolize arachidonic acid to epoxyeicosatrienoic acid (EET) regioisomers, which activate several signaling pathways to promote endothelial cell proliferation, migration, and angiogenesis. Since vascular endothelial growth factor (VEGF) plays a key role in angiogenesis, we assessed a possible role of EETs in the VEGF-activated signal transduction cascade. Stimulation with VEGF increased CYP2C promoter activity in endothelial cells and enhanced CYP2C8 mRNA and protein expression resulting in increased intracellular EET levels. VEGF-induced endothelial cell t

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Zhiryakova, A. S., N. P. Denisenko, S. N. Tuchkova, et al. "Pharmacogenetic aspects of the efficacy of nonsteroidal anti-inflammatory drugs and opioid analgesics for postoperative pain relief after total joint arthroplasty." Modern Rheumatology Journal 19, no. 3 (2025): 40–47. https://doi.org/10.14412/1996-7012-2025-3-40-47.

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Objective: to investigate possible associations between genetic, clinical, laboratory, and demographic parameters and the level of pain in the early postoperative (p/o) period, the need for opioid analgesics, and gastrointestinal symptoms in patients who underwent primary total knee (TKR) or hip replacement (THR).Material and methods. Sixty-one patients hospitalized for THR or TKR were included in the study. P/o pain relief was achieved using nonsteroidal anti-inflammatory drugs (NSAIDs) – ketoprofen or ketorolac – with tramadol prescribed "on demand." Pain was assessed in all patients using t

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Lozano, María L., Elkin A. Niño, Ana Isabel Anton, et al. "Influence of Genetic Polymorphisms in CYP2C8 and ABCB1 on the Mobilization Ability and Toxicity of Paclitaxel,." Blood 118, no. 21 (2011): 4050. http://dx.doi.org/10.1182/blood.v118.21.4050.4050.

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Abstract Abstract 4050 Introduction. We and others have described the efficacy of paclitaxel-based chemotherapy in mobilizing large amounts of hematopoietic progenitors (HP) both in patients with solid tumors,(Bone Marrow Transplant 2000;25:231–5), and with hematological malignancies (Haematologica 2008; 93:161–3). Like most drugs, the taxanes are not controlled by the actions of one gene, but believed to be dependent on several polymorphic proteins. Single nucleotide polymorphisms (SNPs) in the ABCB1 gene, which encodes the transport protein P-glycoprotein, or in in metabolic enzymes, such as

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Brown, Charles, Christopher Larbie, and Dominic Amuzu. "Prevalence of the Genetic Mutation CYP2C8*5 in Selected Ethnic Groups in Southern Ghana." International Journal of Biochemistry Research & Review 12, no. 3 (2016): 1–9. http://dx.doi.org/10.9734/ijbcrr/2016/25680.

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Špičáková, Alena, Zuzana Horáčková, Pavel Kopel, and Pavel Anzenbacher. "In Vitro Interaction of Binuclear Copper Complexes with Liver Drug-Metabolizing Cytochromes P450." Pharmaceuticals 17, no. 9 (2024): 1194. http://dx.doi.org/10.3390/ph17091194.

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Two copper(II) mixed ligand complexes with dicarboxylate bridges were prepared and studied, namely [Cu2(μ-fu)(pmdien)2(H2O)2](ClO4)2 (complex No. 5) and [Cu2(μ-dtdp)(pmdien)2(H2O)2](ClO4)2 (complex No. 6), where H2fu = fumaric acid, pmdien = N,N,N′,N″,N″ pentamethyldiethylenetriamine, and H2dtdp = 3,3′-dithiodipropionic acid. The copper atoms are coordinated in the same mode by the tridentate pmdien ligand and oxygen of water molecules, and they only differ in the dicarboxylate bridge. This work is focused on the study of the inhibitory effect of these potential antimicrobial drugs on the acti

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Grau, J. J., M. Monzo, M. Vargas, et al. "Single nucleotide polymorphisms (SNPs) analysis of CYP2C8, GSTT1, GSTP1, MDR1(A), MDR1(B) and ERCC1 as predictor of survival after weekly paclitaxel for relapsed advanced head & neck cancer patients (AHNCP)." Journal of Clinical Oncology 25, no. 18_suppl (2007): 2540. http://dx.doi.org/10.1200/jco.2007.25.18_suppl.2540.

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2540 Background: Gene SNPs correlate with survival in cancer patients (pts) treated with chemotherapy (CHM). CYP2C8 and GSTT1, GTSP1 genes are involved in phase 1 and 2 drug cellular metabolisms respectively; MDR1(A) and MDR1(B) are involved in drug membrane transport and ERCC1 in DNA repair Methods: We evaluated the presence of SNPs of these 6 genes and the survival of AHNCP treated with weekly paclitaxel, 80 mg/m2 iv for 6 weeks. Responding pts continue CHM till progression. All pts were cisplatin resistant and no other local therapies were available. We analysed paraffin-embedded biopsies f

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Trescot, Andrea M. "A Review of the Role of Genetic Testing in Pain Medicine." Pain Physician 5;17, no. 5;9 (2014): 425–45. http://dx.doi.org/10.36076/ppj.2014/17/425.

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Background: Pain clinicians have always been challenged by the variability of response to pain treatment. Differences in the degree of pain stimulation and pain sensitivity, weight and age differences, prior opioid use and tolerance, as well as the differences in bioavailability of various opioid formulations have been cited as causes for the wide variability in analgesia seen with opioids. Genetics may explain the variability of responses and help to predict more effective (or less dangerous) medication choices and doses. Genetics may also help to predict the response to specific opioids and

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Pereira de Sena, Luann Wendel, Hellen Thais Fuzii, Fabiola Elizabeth Villanova, et al. "Influence of CYP2C8 Polymorphism on the Exposure to Chloroquine in Patients with Malaria by Plasmodium vivax—A Preliminary Study." International Journal of Environmental Research and Public Health 22, no. 3 (2025): 336. https://doi.org/10.3390/ijerph22030336.

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Aim: To assess the impact of the CYP2C82 polymorphism on chloroquine and desethylchloroquine concentrations in patients with malaria caused by P. vivax. Methods: A prospective study was conducted on patients with malaria in an endemic area of the Amazon basin. Liquid chromatography was employed to measure the levels of chloroquine and desethylchloroquine, while molecular methods estimated the frequency of the CYP2C82 variant. Results: This study revealed that plasma levels of chloroquine were higher in patients with the CYP2C82 polymorphism compared to those without this variant. The differenc

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Jamani, Rehana, Esther K. Lee, Scott R. Berry, Carlo DeAngelis, Angie Giotis, and Urban Emmenegger. "Drug-drug interactions in patients with castration-resistant prostate cancer undergoing abiraterone therapy: Characterizing the scale of the problem." Journal of Clinical Oncology 33, no. 7_suppl (2015): 269. http://dx.doi.org/10.1200/jco.2015.33.7_suppl.269.

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269 Background: Abiraterone acetate (AA), used to treat CRPC, inhibits androgen biosynthesis by blocking cytochrome P450 (CYP) 17. It also inhibits other cytochromes involved in the metabolism of various widely-used medications (strong inhibition of CYP1A2, CYP2D6, and CYP2C8; moderate inhibition of CYP2C9, CYP2C19 and CYP3A4/5). Hence, there is presumably a high potential for drug-drug interactions (DDI) that can either diminish the efficacy of AA or concurrent medications, or increase the risk of DDI-related adverse events (AE); however, the scale of AA-associated DDI is currently unknown. M

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Cabanillas, Maria E., Marcia S. Brose, David A. Ramies, Yihua Lee, Dale Miles, and Steven I. Sherman. "Antitumor activity of cabozantinib (XL184) in a cohort of patients (pts) with differentiated thyroid cancer (DTC)." Journal of Clinical Oncology 30, no. 15_suppl (2012): 5547. http://dx.doi.org/10.1200/jco.2012.30.15_suppl.5547.

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5547 Background: Cabozantinib (cabo) is an oral, potent inhibitor of MET, VEGFR2, and RET that is currently undergoing evaluation in several oncology indications. Differentiated thyroid cancer (DTC) pts were included in this study based on involvement of the MET, VEGFR, and RET signaling pathways in this disease. The primary objective of this study is to determine the effect of cabo on single dose PK of the CYP2C8 substrate rosiglitazone (rosi). Anti-tumor activity and safety were also evaluated. Methods: Metastatic DTC pts who were enrolled to this study were required to be RAI-refractory, ha

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Melea, Pelagia, Tina Bagratuni, Evangelos Terpos, et al. "Genetic Factors Related with Early Onset of Osteonecrosis of the Jaw in Patients with Multiple Myeloma Under Zoledronic Acid Therapy." Blood 124, no. 21 (2014): 2115. http://dx.doi.org/10.1182/blood.v124.21.2115.2115.

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Abstract Bisphosphonates are extensively used in the treatment of myeloma-related bone disease as they reduce pain and skeletal related events (SREs), such as pathologic fractures, need for radiation and surgery to the bone. One of the complications of prolonged therapy with bisphosphonates, especially of amino-bisphosphonates, such as zoledronic acid (ZA) is osteonecrosis of the jaw (ONJ). Recent studies have attempted to correlate specific genetic polymorphisms (SNPs) and ONJ. Such SNPs include cytochrome P4502C8 (CYP2C8; Sarasquete et al, Blood 2008) and peroxisome proliferator-activated re

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Frudakis, Tony, Matthew Thomas, Zach Gaskin, et al. "Sequences Associated With Human Iris Pigmentation." Genetics 165, no. 4 (2003): 2071–83. http://dx.doi.org/10.1093/genetics/165.4.2071.

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Abstract To determine whether and how common polymorphisms are associated with natural distributions of iris colors, we surveyed 851 individuals of mainly European descent at 335 SNP loci in 13 pigmentation genes and 419 other SNPs distributed throughout the genome and known or thought to be informative for certain elements of population structure. We identified numerous SNPs, haplotypes, and diplotypes (diploid pairs of haplotypes) within the OCA2, MYO5A, TYRP1, AIM, DCT, and TYR genes and the CYP1A2-15q22-ter, CYP1B1-2p21, CYP2C8-10q23, CYP2C9-10q24, and MAOA-Xp11.4 regions as significantly

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Cheng, Keling, Xuan Zeng, Hao Wu, et al. "Effects of Naringin on the Activity and mRNA Expression of CYP Isozymes in Rats." Natural Product Communications 14, no. 12 (2019): 1934578X1989418. http://dx.doi.org/10.1177/1934578x19894180.

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Naringin (NRG) is a common dietary flavonoid in citrus fruits and has been documented to possess multiple pharmacological activities, including anti-oxidant, anti-inflammatory, and neuroprotective effects. Naringin is frequently consumed in combination with common clinical drugs. To date, the effects of NRG on cytochrome P450 enzymes have not been fully investigated yet. In this study, the activities of hepatic CYP1A2, CYP2D2, CYP2C9, CYP2C19, and CYP2E1 in rats after the continuous oral administration of NRG (50 and 500 mg/kg) were evaluated using cocktail probe-drug method. The concentration

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Rezaeian, Iman, Eliseos J. Mucaki, Katherina Baranova, et al. "Predicting Outcomes of Hormone and Chemotherapy in the Molecular Taxonomy of Breast Cancer International Consortium (METABRIC) Study by Biochemically-inspired Machine Learning." F1000Research 5 (August 31, 2016): 2124. http://dx.doi.org/10.12688/f1000research.9417.1.

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Genomic aberrations and gene expression-defined subtypes in the large METABRIC patient cohort have been used to stratify and predict survival. The present study used normalized gene expression signatures of paclitaxel drug response to predict outcome for different survival times in METABRIC patients receiving hormone (HT) and, in some cases, chemotherapy (CT) agents. This machine learning method, which distinguishes sensitivity vs. resistance in breast cancer cell lines and validates predictions in patients, was also used to derive gene signatures of other HT (tamoxifen) and CT agents (methotr

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Rezaeian, Iman, Eliseos J. Mucaki, Katherina Baranova, et al. "Predicting Outcomes of Hormone and Chemotherapy in the Molecular Taxonomy of Breast Cancer International Consortium (METABRIC) Study by Biochemically-inspired Machine Learning." F1000Research 5 (January 27, 2017): 2124. http://dx.doi.org/10.12688/f1000research.9417.2.

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Genomic aberrations and gene expression-defined subtypes in the large METABRIC patient cohort have been used to stratify and predict survival. The present study used normalized gene expression signatures of paclitaxel drug response to predict outcome for different survival times in METABRIC patients receiving hormone (HT) and, in some cases, chemotherapy (CT) agents. This machine learning method, which distinguishes sensitivity vs. resistance in breast cancer cell lines and validates predictions in patients; was also used to derive gene signatures of other HT (tamoxifen) and CT agents (methotr

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Mucaki, Eliseos J., Katherina Baranova, Huy Q. Pham, et al. "Predicting Outcomes of Hormone and Chemotherapy in the Molecular Taxonomy of Breast Cancer International Consortium (METABRIC) Study by Biochemically-inspired Machine Learning." F1000Research 5 (May 12, 2017): 2124. http://dx.doi.org/10.12688/f1000research.9417.3.

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Genomic aberrations and gene expression-defined subtypes in the large METABRIC patient cohort have been used to stratify and predict survival. The present study used normalized gene expression signatures of paclitaxel drug response to predict outcome for different survival times in METABRIC patients receiving hormone (HT) and, in some cases, chemotherapy (CT) agents. This machine learning method, which distinguishes sensitivity vs. resistance in breast cancer cell lines and validates predictions in patients; was also used to derive gene signatures of other HT (tamoxifen) and CT agents (methotr

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Chan, Nancy, Daniella E. Portal, Rebecca Anne Moss, et al. "A phase I study of pazopanib with weekly paclitaxel and carboplatin in advanced solid tumors." Journal of Clinical Oncology 37, no. 15_suppl (2019): 3021. http://dx.doi.org/10.1200/jco.2019.37.15_suppl.3021.

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3021 Background: Pazopanib (pazo) is an oral tyrosine kinase inhibitor of VEGFR, PDGFR and c-Kit. It is a weak inhibitor of CYP3A4 and CYP2C8 and may decrease paclitaxel (P) clearance. Daily pazo with P and carboplatin (C) every 21 days was not feasible on a previous study. We hypothesized that pazo dosed intermittently and on a different day from P and C may be tolerable. We sought to determine the maximum tolerated dose (MTD), dose-limiting toxicity (DLT), and pharmacokinetics (PK) of pazo with weekly P and C. Methods: Using a 3+3 standard design, a schedule of P 60-80 mg/m2 and C AUC2 on da

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Ivashchenko, D. V., K. A. Ryzhikova, Zh A. Sozaeva, et al. "IMPACT OF CYP3A5, CYP2C9, CYP2C19, AND CYP2D6 POLYMORPHISMS ON PHENAZEPAM SAFETY IN PATIENTS WITH ALCOHOL WITHDRAWAL SYNDROME." Annals of the Russian academy of medical sciences 73, no. 3 (2018): 206–14. http://dx.doi.org/10.15690/vramn989.

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Introduction: Phenazepam is the Russian original benzodiazepine tranquilizer. We conducted first pharmacogenetic study on Phenazepam’s safety in patients with alcohol withdrawal syndrome. Isoenzymes CYP3A4, CYP3A5, CYP2C9, and CYP2C19 are involved into benzodiazepine tranquilizers’ metabolism.Aim: To determine predictive value of CYP3A5, CYP2C9, CYP2C19, and CYP2D6 genetic polymorphisms and their haplotypes for adverse reaction risk associated with the treatment with phenazepam.Materials and methods: The study enrolled 102 male patients with non-comlicated alcohol withdrawal syndrome (F10.3 by

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Nthontho, Keneuoe Cecilia, Maria Paganotti, and Andrew Khulekani Ndlovu. "Breast Cancer Pharmacogenetics in Botswana." JCO Global Oncology 10, Supplement_1 (2024): 32. http://dx.doi.org/10.1200/go-24-29000.

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PURPOSE Breast cancer is one of the utmost neoplastic diseases, with a high mortality globally and especially in sub-Saharan Africa, where, despite a relatively low incidence, mortality is high. In Botswana, breast cancer represents almost 20% of all cancers and accounts for more than 10% of cancer-associated deaths among women. Moreover, the median age of women presenting with breast cancer is younger than those of high-income countries and patients are more likely to present with advanced stage disease. In addition, there is limited availability/access to treatments. Breast cancer in Botswan

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Tantsura, L. M., O. Yu Pylypets, Ye O. Tantsura та D. V. Tretiakov. "Дослідження поліморфізмів гена сур2с19 у дітей з фармакорезистентними епілепсіями". Експериментальна і клінічна медицина 82, № 1 (2020): 28–36. http://dx.doi.org/10.35339/ekm.2019.01.05.

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Проведено фармакогенетичне дослідження 83 дітей з фармакорезистентними епілепсіями віком від 11 місяців до 18 років. За допомогою алель-специфічної полімеразної ланцюгової реакції (ПЛР), визначали поліморфізми гена CYP2C19 (CYP2C19*1, CYP2C19*2). Алель CYP2C19*2 нами зафіксований у 33 (39,76 %) пацієнтів. У 5-х (15,15 %) з них носійство генотипу CYP2C19*2 виявлено в комбінації з іншими поліморфізмами генів (СYP2C9*2, CYP2C9*3, CYP3A4*1B). Поліморфізм CYP2C19*2 в обстежуваних нами пацієнтів зустрічався достовірно частіше ніж в українських та інших європейських популяціях. 

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Tantsura, Liudmyla M., Olena Yu Pylypets, Dmytro V. Tretiakov, and Yevhen O. Tantsura. "VARIANTS OF THE FORMATION AND COURSE OF DRUG-RESISTANT EPILEPSY IN CHILDREN WITH GENETIC POLYMORPHISMS OF CYP2C9, CYP2C19, CYP3A4." Wiadomości Lekarskie 76, no. 5 (2023): 1007–13. http://dx.doi.org/10.36740/wlek202305118.

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The aim: To clarify the frequency with which various variants of the formation and course of drug-resistant epilepsy occur in children with genetic polymor¬phisms of cytochromes CYP2C9, CYP2C19, CYP3A4. Materials and methods: The genotyping of CYP2C9*2, CYP2C9*3, CYP2C19*2, CYP3A4*1B by the allele-specific polymerase chain reaction was performed in 116 children with drug-resistant epilepsy aged from 2 to 17 years. Thirty cases (boys-15; girls-15) with a follow-up period of more than 5 years were analyzed in detail. Results: Of 30 cases analyzed, polymorphisms were not detected in 8 (26.67%) ch

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Loer, Helena Leonie Hanae, Denise Türk, José David Gómez-Mantilla, Dominik Selzer, and Thorsten Lehr. "Physiologically Based Pharmacokinetic (PBPK) Modeling of Clopidogrel and Its Four Relevant Metabolites for CYP2B6, CYP2C8, CYP2C19, and CYP3A4 Drug–Drug–Gene Interaction Predictions." Pharmaceutics 14, no. 5 (2022): 915. http://dx.doi.org/10.3390/pharmaceutics14050915.

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The antiplatelet agent clopidogrel is listed by the FDA as a strong clinical index inhibitor of cytochrome P450 (CYP) 2C8 and weak clinical inhibitor of CYP2B6. Moreover, clopidogrel is a substrate of—among others—CYP2C19 and CYP3A4. This work presents the development of a whole-body physiologically based pharmacokinetic (PBPK) model of clopidogrel including the relevant metabolites, clopidogrel carboxylic acid, clopidogrel acyl glucuronide, 2-oxo-clopidogrel, and the active thiol metabolite, with subsequent application for drug–gene interaction (DGI) and drug–drug interaction (DDI) prediction

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Suttle, B., S. Jones, A. Dowlati, et al. "Phase I study of the safety and pharmacokinetics (PK) of paclitaxel or paclitaxel with carboplatin administered in combination with pazopanib (GW786034)." Journal of Clinical Oncology 25, no. 18_suppl (2007): 14118. http://dx.doi.org/10.1200/jco.2007.25.18_suppl.14118.

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14118 Background: Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit. Pazopanib also is a moderate inhibitor of CYP2C8 and CYP3A4 in vitro. Paclitaxel (T), a substrate for CYP2C8 and CYP3A4, administered alone and in combination with carboplatin (Cb) is highly active in breast, NSCLC, and ovarian cancers. The additive benefit of the anti-VEGF agent bevacizumab with T or T-Cb in breast and NSCLC provides strong rationale for use of a multi-targeted TKI with T or T-Cb. Methods: Pts with advanced cancer (ECOG PS

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Guevara, Mariela, Fernanda Rodrigues-Soares, Carla González de la Cruz, et al. "Afro-Latin American Pharmacogenetics of CYP2D6, CYP2C9, and CYP2C19 in Dominicans: A Study from the RIBEF-CEIBA Consortium." Pharmaceutics 16, no. 11 (2024): 1399. http://dx.doi.org/10.3390/pharmaceutics16111399.

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Background/Objectives: Research on pharmacogenetic variability in response to prescribed drugs and across ethnic groups is essential for personalized medicine, particularly in admixed and unstudied populations. For the first time, this study examines CYP2D6, CYP2C9, and CYP2C19 alleles and genotypes in 197 healthy volunteers from the Dominican Republic, as part of the RIBEF-CEIBA collaborative network. Methods: The analysis focuses on the participants’ tri-hybrid genomic ancestry, with CYP alleles determined by real-time PCR and molecular ancestry inferred using 90 AIMs. Linear regression was

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Rodriguez-Vera, Leyanis, Xuefen Yin, Mohammed Almoslem, et al. "Comprehensive Physiologically Based Pharmacokinetic Model to Assess Drug–Drug Interactions of Phenytoin." Pharmaceutics 15, no. 10 (2023): 2486. http://dx.doi.org/10.3390/pharmaceutics15102486.

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Regulatory agencies worldwide expect that clinical pharmacokinetic drug–drug interactions (DDIs) between an investigational new drug and other drugs should be conducted during drug development as part of an adequate assessment of the drug’s safety and efficacy. However, it is neither time nor cost efficient to test all possible DDI scenarios clinically. Phenytoin is classified by the Food and Drug Administration as a strong clinical index inducer of CYP3A4, and a moderate sensitive substrate of CYP2C9. A physiologically based pharmacokinetic (PBPK) platform model was developed using GastroPlus

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