Pharmacokinetic Properties of Two Erlotinib 150 mg Formulations with a Genetic Effect Evaluation in Healthy Korean Subjects

Choi, Hee Joung; Jeon, Ji‐Young; Im, Yeon-Ho; Kim, Yun-Jeong; Song, Eun-Kee; Seo, Young Hwan; Cho, Seok-Je; Kim, Min‐Gul

doi:10.1007/s40261-014-0248-4

Cited by 11 publications

(5 citation statements)

References 38 publications

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“…Phenotyping studies assessing the effect of CYP3A4 variants on erlotinib metabolism were inconclusive and pre-emptive testing is not currently recommended. A PK study in a Korean population showed no difference in AUC exposure and C max of erlotinib in patients with CYP3A4 polymorphisms [206]. In a similar study, a polymorphism in CYP1A2*1 M resulted in a higher C max .…”

Section: Polymorphisms In Cyp3a4mentioning

confidence: 91%

“…Another contributing factor could be auto-induction of CYP3A4 by erlotinib. CYP450 induction often occurs on a transcriptional level and takes up to 2 weeks for increased expression, which may be missed in studies that do not assess steady state erlotinib levels [206,207]. There are limited studies evaluating the impact of CYP3A4 SNPs and gefitinib, osimertinib, and mobocertinib metabolism.…”

Section: Polymorphisms In Cyp3a4mentioning

confidence: 99%

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Integration of liquid biopsy and pharmacogenomics for precision therapy of EGFR mutant and resistant lung cancers

et al. 2022

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The advent of molecular profiling has revolutionized the treatment of lung cancer by comprehensively delineating the genomic landscape of the epidermal growth factor receptor (EGFR) gene. Drug resistance caused by EGFR mutations and genetic polymorphisms of drug metabolizing enzymes and transporters impedes effective treatment of EGFR mutant and resistant lung cancer. This review appraises current literature, opportunities, and challenges associated with liquid biopsy and pharmacogenomic (PGx) testing as precision therapy tools in the management of EGFR mutant and resistant lung cancers. Liquid biopsy could play a potential role in selection of precise tyrosine kinase inhibitor (TKI) therapies during different phases of lung cancer treatment. This selection will be based on the driver EGFR mutational status, as well as monitoring the development of potential EGFR mutations arising during or after TKIs treatment, since some of these new mutations may be druggable targets for alternative TKIs. Several studies have identified the utility of liquid biopsy in the identification of EGFR driver and acquired resistance with good sensitivities for various blood-based biomarkers. With a plethora of sequencing technologies and platforms available currently, further evaluations using randomized controlled trials (RCTs) in multicentric, multiethnic and larger patient cohorts could enable optimization of liquid-based assays for the detection of EGFR mutations, and support testing of CYP450 enzymes and drug transporter polymorphisms to guide precise dosing of EGFR TKIs.

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Section: Polymorphisms In Cyp3a4mentioning

confidence: 91%

Section: Polymorphisms In Cyp3a4mentioning

confidence: 99%

Integration of liquid biopsy and pharmacogenomics for precision therapy of EGFR mutant and resistant lung cancers

et al. 2022

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“…In lung cancer patients, the CYP1A2*1M variant has been associated with higher maximum plasma concentration values after the intake of 150 mg of erlotinib, suggesting reduced enzyme activity. The impact on drug efficacy and toxicity is so far unknown [11]. …”

Section: Cytochrome P450 (Cyp)-mediated Phase I-metabolizing Enzymesmentioning

confidence: 99%

Genotypes Affecting the Pharmacokinetics of Anticancer Drugs

2016

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Cancer treatment is becoming more and more individually based as a result of the large inter-individual differences that exist in treatment outcome and toxicity when patients are treated using population-based drug doses. Polymorphisms in genes encoding drug-metabolizing enzymes and transporters can significantly influence uptake, metabolism, and elimination of anticancer drugs. As a result, the altered pharmacokinetics can greatly influence drug efficacy and toxicity. Pharmacogenetic screening and/or drug-specific phenotyping of cancer patients eligible for treatment with chemotherapeutic drugs, prior to the start of anticancer treatment, can identify patients with tumors that are likely to be responsive or resistant to the proposed drugs. Similarly, the identification of patients with an increased risk of developing toxicity would allow either dose adaptation or the application of other targeted therapies. This review focuses on the role of genetic polymorphisms significantly altering the pharmacokinetics of anticancer drugs. Polymorphisms in DPYD, TPMT, and UGT1A1 have been described that have a major impact on the pharmacokinetics of 5-fluorouracil, mercaptopurine, and irinotecan, respectively. For other drugs, however, the association of polymorphisms with pharmacokinetics is less clear. To date, the influence of genetic variations on the pharmacokinetics of the increasingly used monoclonal antibodies has hardly been investigated. Some studies indicate that genes encoding the Fcγ-receptor family are of interest, but more research is needed to establish if screening before the start of therapy is beneficial. Considering the profound impact of polymorphisms in drug transporters and drug-metabolizing enzymes on the pharmacokinetics of chemotherapeutic drugs and hence, their toxicity and efficacy, pharmacogenetic and pharmacokinetic profiling should become the standard of care.

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“…Blood samples were collected before dosing and 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours after oral administration. [7] These blood sample collecting times, including the dosing time, are set in the schedule table located on the left side. All scheduled times, calculated from the schedule table, are shown in the columns of scheduled time table on the right side.…”

Section: Application To Clinical Trialsmentioning

confidence: 99%

Rooibos™: Automated schedule broadcast software for clinical pharmacology studies

Lee

Chong²,

Park³

et al. 2016

Transl Clin Pharmacol

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Pharmacokinetic Properties of Two Erlotinib 150 mg Formulations with a Genetic Effect Evaluation in Healthy Korean Subjects

Cited by 11 publications

References 38 publications

Integration of liquid biopsy and pharmacogenomics for precision therapy of EGFR mutant and resistant lung cancers

Integration of liquid biopsy and pharmacogenomics for precision therapy of EGFR mutant and resistant lung cancers

Genotypes Affecting the Pharmacokinetics of Anticancer Drugs

Rooibos™: Automated schedule broadcast software for clinical pharmacology studies

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