Molecular pharmacokinetic determinants of anticancer kinase inhibitors in humans

Scholler, Julie; Levêque, Dominique

doi:10.1007/s12156-011-0072-5

Cited by 6 publications

(3 citation statements)

References 103 publications

(178 reference statements)

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“…The initial oral cancer therapy agents, methotrexate and mercaptopurine, were approved in 1953 and have been obtainable in the United States for over half a century . To date, the number of oral cancer therapy drugs approved by the Food and Drug Administration has continued to increase, with more than 60 currently approved for use . Given the increasing incidence of cancer, it is expected that more patients will receive oral cancer treatment in the coming decades .…”

Section: Discussionmentioning

confidence: 99%

“…34 To date, the number of oral cancer therapy drugs approved by the Food and Drug Administration has continued to increase, with more than 60 currently approved for use. 35 Given the increasing incidence of cancer, it is expected that more patients will receive oral cancer treatment in the coming decades. 36 In addition, cancer survivors often require ongoing care and support.…”

Section: Discussionmentioning

confidence: 99%

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Geraniin inhibits oral cancer cell migration by suppressing matrix metalloproteinase‐2 activation through the FAK/Src and ERK pathways

Yeh

Hsieh

Yang

et al. 2019

Environmental Toxicology

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Geraniin has been reported to have numerous biological activities, including antiviral, antihypertensive, antihyperglycaemic, liver protective, antidiabetic, and apoptotic activities. However, the anti‐migration effects of geraniin on oral cancer remain elusive. In this study, we revealed the potential antitumor mechanisms of geraniin through the inhibition of the migration and invasion of human oral cancer cell lines SCC‐9 and SCC‐14. The results of gelatin zymography and Western blot assays revealed that geraniin significantly reduced the activity and expression of matrix metalloproteinase‐2 (MMP‐2) of oral cancer cells in a concentration‐dependent manner. Furthermore, geraniin potently suppressed the phosphorylation of focal adhesion kinase (FAK), Src, and extracellular signal‐regulated kinase (ERK)1/2 but did not affect the phosphorylation of p38 mitogen‐activated protein kinase (MAPK) and c‐Jun N‐terminal kinase 1/2. Moreover, blocking the MAPK/ERK1/2 pathway significantly enhanced the anti‐migration ability of geraniin in oral cancer cells. In conclusion, we demonstrated that geraniin inhibits the motility of SCC‐9 and SCC‐14 cells in vitro through a molecular mechanism that involves the attenuation of MMP‐2 expression and activity mediated by decreased FAK/Src and ERK1/2 pathways.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Geraniin inhibits oral cancer cell migration by suppressing matrix metalloproteinase‐2 activation through the FAK/Src and ERK pathways

Yeh

Hsieh

Yang

et al. 2019

Environmental Toxicology

View full text Add to dashboard Cite

show abstract

“…1 Since then, the number of Food and Drug Administration-approved oral cancer therapy drugs has continued to rise and is currently more than 60. 2 Given the aging of the US population, more patients are expected to receive oral cancer therapy in the coming decades. In fact, 52% of newly diagnosed cancer cases affect patients greater than 65 years of age.…”

Section: Introductionmentioning

confidence: 99%

Medication adherence to oral cancer therapy: The promising role of the pharmacist

Felton

Londen

Marcum

2014

J Oncol Pharm Pract

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Medication adherence to oral cancer therapy is a critical component to achieving optimal patient outcomes. As the US population ages, growing numbers of patients will be prescribed oral cancer therapy regimens, highlighting the need for innovative and scalable solutions. Clinical pharmacists offer tremendous promise to help patients improve their adherence to oral cancer therapy. Moreover, addition of oral chemotherapy to Centers for Medicare & Medicaid Services (CMS) medication adherence quality measures has the potential to improve care and result in better therapeutic outcomes with fewer costs for patients and payers. Future research is needed to test the use of pharmacist-managed interventions to improve adherence to oral cancer therapy.

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Inhibition of human UDP‐glucuronosyltransferase enzymes by midostaurin and ruxolitinib: implications for drug–drug interactions

Wang

Jia

et al. 2020

Biopharm & Drug Disp

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Cancer therapy with tyrosine kinase inhibitors (TKIs) is a rapidly developing field, and several TKIs have been reported to have an impact on the activities of UDP‐glucosyltransferases (UGTs), implying a potential risk for drug–drug interaction (DDI). Herein, we investigated the inhibitory effects of two commonly used TKIs, midostaurin and ruxolitinib, on human UGTs and quantitatively evaluated their DDI potential via UGT inhibition. It was found that midostaurin was a potent inhibitor of the majority of human UGTs, including UGT1A3, 1A4, 1A7, 1A8, 1A9, 1A10, 2B7, 2B15, and 2B17, with IC50 values lower than 4 μM (IC50 0.0128–3.85 μM), while ruxolitinib exhibited weak inhibition towards the activity of almost all the tested UGT isoforms. Furthermore, based on reversible inhibition, the co‐administration of midostaurin at the clinical available dose was predicted to increase the plasma exposure to sensitive UGT1A3, 1A7, and 1A8 substrates by at least 61.4%, 25.6%, and 651%, respectively. In summary, our data identify that midostaurin is a potent inhibitor of the majority of human UGTs and may bring a potential risk of DDI via inhibition against UGT1A3, 1A7, and 1A8, while ruxolitinib cannot trigger UGT‐mediated DDI due to its weak inhibition towards UGTs.

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Molecular pharmacokinetic determinants of anticancer kinase inhibitors in humans

Cited by 6 publications

References 103 publications

Geraniin inhibits oral cancer cell migration by suppressing matrix metalloproteinase‐2 activation through the FAK/Src and ERK pathways

Geraniin inhibits oral cancer cell migration by suppressing matrix metalloproteinase‐2 activation through the FAK/Src and ERK pathways

Medication adherence to oral cancer therapy: The promising role of the pharmacist

Inhibition of human UDP‐glucuronosyltransferase enzymes by midostaurin and ruxolitinib: implications for drug–drug interactions

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