Oral epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of non-small cell lung cancer: Comparative pharmacokinetics and drug–drug interactions

Peters, Solange; Zimmermann, Stefan; Adjei, Alex A.

doi:10.1016/j.ctrv.2014.06.010

Cited by 163Lung Cancer Treatments and MutationsHER2/EGFR in Cancer ResearchPharmacogenetics and Drug Metabolism

Oral epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of non-small cell lung cancer: Comparative pharmacokinetics and drug–drug interactions

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Peters, Solange, Zimmermann, Stefan, Adjei, Alex A.·2014·Cancer Treatment Reviews

DOI 10.1016/j.ctrv.2014.06.010

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Abstract

The development of orally active small molecule inhibitors of the epidermal growth factor receptor (EGFR) has led to new treatment options for non-small cell lung cancer (NSCLC). Patients with activating mutations of the EGFR gene show sensitivity to, and clinical benefit from, treatment with EGFR tyrosine kinase inhibitors (EGFR-TKls). First generation reversible ATP-competitive EGFR-TKls, gefitinib and erlotinib, are effective as first, second-line or maintenance therapy. Despite initial benefit, most patients develop resistance within a year, 50-60% of cases being related to the appearance of a T790M gatekeeper mutation. Newer, irreversible EGFR-TKls - afatinib and dacomitinib - covalently bind to and inhibit multiple receptors in the ErbB family (EGFR, HER2 and HER4). These agents have been mainly evaluated for first-line treatment but also in the setting of acquired resistance to first-generation EGFR-TKls. Afatinib is the first ErbB family blocker approved for patients with NSCLC with activating EGFR mutations; dacomitinib is in late stage clinical development. Mutant-selective EGFR inhibitors (AZD9291, CO-1686, HM61713) that specifically target the T790M resistance mutation are in early development. The EGFR-TKIs differ in their spectrum of target kinases, reversibility of binding to EGFR receptor, pharmacokinetics and potential for drug-drug interactions, as discussed in this review. For the clinician, these differences are relevant in the setting of polymedicated patients with NSCLC, as well as from the perspective of innovative anticancer drug combination strategies.

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Afatinib is highly soluble across the physiological pH range of 1-7.5 and is not expected to interact with acid-reducing agents.
“Afatinib is highly soluble across the physiological pH range of 1–7.5 and is not expected to interact with acid-reducing agents.”
From Afatinib for the treatment of EGFR mutation-positive NSCLC: A review of clinical findings (2020) · cites this paper as [61]
CYP enzymes play a negligible role in the metabolism of afatinib.
“CYP enzymes play a negligible role in the metabolism of afatinib.”
From Afatinib for the treatment of EGFR mutation-positive NSCLC: A review of clinical findings (2020) · cites this paper as [61]

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Stopfer, P., Marzin, K., Narjes, H., Gansser, D., Shahidi, M., Uttereuther-Fischer, M., & Ebner, T. (2012) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-011-1803-9 · Cited by 137 · see citing works
Metabolic disposition of gefitinib, an epidermal growth factor receptor tyrosine kinase inhibitor, in rat, dog and man.
McKillop, D., Hutchison, M., Partridge, E. A., Bushby, N., Cooper, C. M. F., Clarkson-Jones, J. A., Herron, W., & Swaisland, H. C. (2004) · Xenobiotica · doi:10.1080/00498250400009171 · Cited by 130 · see citing works
The effects of CYP3A4 inhibition on erlotinib pharmacokinetics: computer-based simulation (SimCYP™) predicts in vivo metabolic inhibition
Rakhit, A. K., Pantze, M. P., Fettner, S. H., Jones, H. M., Charoin, J., Riek, M., Lum, B. L., & Hamilton, M. (2007) · European Journal of Clinical Pharmacology · doi:10.1007/s00228-007-0396-z · Cited by 122 · see citing works
Pharmacokinetics and Tolerability of the Orally Active Selective Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor ZD1839 in Healthy Volunteers
Swaisland, H., Laight, A., Stafford, L. E., Jones, H., Morris, C. Q., Dane, A. L., & Yates, R. (2001) · Clinical Pharmacokinetics · doi:10.2165/00003088-200140040-00005 · Cited by 116 · see citing works
The biological and clinical role of drug transporters at the intestinal barrier
Oostendorp, R. L., Beijnen, J. H., & Schellens, J. H. M. (2008) · Cancer Treatment Reviews · doi:10.1016/j.ctrv.2008.09.004 · Cited by 113 · see citing works
Evaluation of the Absolute Oral Bioavailability and Bioequivalence of Erlotinib, an Inhibitor of the Epidermal Growth Factor Receptor Tyrosine Kinase, in a Randomized, Crossover Study in Healthy Subjects
Frohna, P., Lu, J., Eppler, S., Hamilton, M., Wolf, J. L., Rakhit, A. K., Ling, J., Kenkare-Mitra, S., & Lum, B. L. (2006) · The Journal of Clinical Pharmacology · doi:10.1177/0091270005284193 · Cited by 111 · see citing works
CYP3A Phenotyping Approach to Predict Systemic Exposure to EGFR Tyrosine Kinase Inhibitors
Li, J., Karlsson, M. O., Brahmer, J. R., Spitz, A. N., Zhao, M., Hidalgo, M. M., & Baker, S. D. (2006) · JNCI Journal of the National Cancer Institute · doi:10.1093/jnci/djj466 · Cited by 106 · see citing works
Pharmacokinetics of Afatinib, a Selective Irreversible ErbB Family Blocker, in Patients with Advanced Solid Tumours
Wind, S., Schmid, M., Erhardt, J., Goeldner, R.-G., & Stopfer, P. (2013) · Clinical Pharmacokinetics · doi:10.1007/s40262-013-0091-4 · Cited by 94 · see citing works
Effect of food on the pharmacokinetics of erlotinib, an orally active epidermal growth factor receptor tyrosine-kinase inhibitor, in healthy individuals
Ling, J., Fettner, S. H., Lum, B. L., Riek, M., & Rakhit, A. K. (2008) · Anti-Cancer Drugs · doi:10.1097/cad.0b013e3282f2d8e4 · Cited by 89 · see citing works
Binding of gefitinib, an inhibitor of epidermal growth factor receptor-tyrosine kinase, to plasma proteins and blood cells: in vitro and in cancer patients
Li, J., Brahmer, J. R., Messersmith, W. A., Hidalgo, M. M., & Baker, S. D. (2006) · Investigational New Drugs · doi:10.1007/s10637-006-5269-2 · Cited by 89 · see citing works
Effects of Tobacco Smoking and Nicotine on Cancer Treatment
Petros, W. P., Younis, I. R., Ford, J. N., & Weed, S. A. (2012) · Pharmacotherapy The Journal of Human Pharmacology and Drug Therapy · doi:10.1002/j.1875-9114.2012.01117 · Cited by 86 · see citing works
Population pharmacokinetics of erlotinib and its pharmacokinetic/pharmacodynamic relationships in head and neck squamous cell carcinoma
Thomas, F., Rochaix, P., White‐Koning, M., Hennebelle, I., Sarini, J., Benlyazid, A., Malard, L., Lefebvre, J., Chatelut, É., & Delord, J. P. (2009) · European Journal of Cancer · doi:10.1016/j.ejca.2009.05.007 · Cited by 81 · see citing works
Overall survival (OS) in patients (pts) with advanced non-small cell lung cancer (NSCLC) harboring common (Del19/L858R) epidermal growth factor receptor mutations (EGFR mut): Pooled analysis of two large open-label phase III studies (LUX-Lung 3 [LL3] and LUX-Lung 6 [LL6]) comparing afatinib with chemotherapy (CT).
Yang, J. C., Sequist, L. V. D., Schüler, M., Mok, T. S. K., Yamamoto, N., O'Byrne, K. J., Hirsh, V., Geater, S. L., Zhou, C., Dan Massey, G., et al. (2014) · Journal of Clinical Oncology · doi:10.1200/jco.2014.32.15_suppl.8004 · Cited by 72 · see citing works
Clinical activity and safety of HM61713, an EGFR-mutant selective inhibitor, in advanced non-small cell lung cancer (NSCLC) patients (pts) with EGFR mutations who had received EGFR tyrosine kinase inhibitors (TKIs).
Kim, D., Lee, K. H., Kang, J. H., Park, K., Han, J., Lee, J.-S., Jang, I., Kim, H.-Y., Son, J., & Kim, J.-H. (2014) · Journal of Clinical Oncology · doi:10.1200/jco.2014.32.15_suppl.8011 · Cited by 70 · see citing works
In Vitro and In Vivo Characterization of Irreversible Mutant-Selective EGFR Inhibitors That Are Wild-Type Sparing
Sjin, R. T. T., Lee, K., Walter, A. O., Dubrovskiy, A., Sheets, M. P., Martin, T. S., Labenski, M., Zhu, Z., Tester, R. W., Karp, R., et al. (2014) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-13-0966 · Cited by 68 · see citing works
Phase I and pharmacokinetic study of dacomitinib (PF-00299804), an oral irreversible, small molecule inhibitor of human epidermal growth factor receptor-1, -2, and -4 tyrosine kinases, in Japanese patients with advanced solid tumors
Takahashi, T., Boku, N., Murakami, H., Naito, T., Tsuya, A., Nakamura, Y., Ono, A., Machida, N., Yamazaki, K., Watanabe, J., et al. (2012) · Investigational New Drugs · doi:10.1007/s10637-011-9789-z · Cited by 64 · see citing works
Exploring the Relationship Between Expression of Cytochrome P450??Enzymes and Gefitinib Pharmacokinetics
Swaisland, H., Cantarini, M., Fuhr, R., & Holt, A. (2006) · Clinical Pharmacokinetics · doi:10.2165/00003088-200645060-00006 · Cited by 64 · see citing works
Pharmacokinetic Drug Interactions of Afatinib with Rifampicin and Ritonavir
Wind, S., Giessmann, T., Jungnik, A., Brand, T., Marzin, K., Bertulis, J., Hocke, J., Gansser, D., & Stopfer, P. (2014) · Clinical Drug Investigation · doi:10.1007/s40261-013-0161-2 · Cited by 63 · see citing works
An evaluation of the possible interaction of gastric acid suppressing medication and the EGFR tyrosine kinase inhibitor erlotinib
Hilton, J. F., Tu, D., Seymour, L., Shepherd, F. A., & Bradbury, P. A. (2013) · Lung Cancer · doi:10.1016/j.lungcan.2013.06.008 · Cited by 60 · see citing works
Epidermal growth factor receptor tyrosine kinase inhibitors: similar but different?
Rukazenkov, Y., Speake, G., Marshall, G. B., Anderton, J., Davies, B. R., Wilkinson, R. W., Hickinson, D. M., & Swaisland, A. J. (2009) · Anti-Cancer Drugs · doi:10.1097/cad.0b013e32833034e1 · Cited by 59 · see citing works
Population pharmacokinetics of afatinib, an irreversible ErbB family blocker, in patients with various solid tumors
Freiwald, M., Schmid, U., Fleury, A., Wind, S., Stopfer, P., & Staab, A. (2014) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-014-2403-2 · Cited by 54 · see citing works
Rhabdomyolysis Resulting from Pharmacologic Interaction Between Erlotinib and Simvastatin
Veeraputhiran, M. K., & Sundermeyer, M. L. (2008) · Clinical Lung Cancer · doi:10.3816/clc.2008.n.036 · Cited by 52 · see citing works
Cytokeratin 19 Fragment Predicts the Efficacy of Epidermal Growth Factor Receptor–Tyrosine Kinase Inhibitor in Non–Small-Cell Lung Cancer Harboring EGFR Mutation
Tanaka, K., Hata, A., Kaji, R., Fujita, S., Otoshi, T., Fujimoto, D., Kawamura, T., Tamai, K., Takeshita, J., Matsumoto, T., et al. (2013) · Journal of Thoracic Oncology · doi:10.1097/jto.0b013e31828c3929 · Cited by 46 · see citing works
The effect of rifampicin, a prototypical CYP3A4 inducer, on erlotinib pharmacokinetics in healthy subjects
Hamilton, M., Wolf, J. L., Drolet, D. W., Fettner, S. H., Rakhit, A. K., Witt, K., & Lum, B. L. (2014) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-014-2390-3 · Cited by 46 · see citing works
A phase I, open-label, mass balance study of [14C] dacomitinib (PF-00299804) in healthy male volunteers
Bello, C. L., Smith, E., Ruiz-Garcı́a, A., Ni, G., Alvey, C. W., & Loi, C. (2013) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-013-2207-9 · Cited by 45 · see citing works
Correlation between erlotinib pharmacokinetics, cutaneous toxicity and clinical outcomes in patients with advanced non-small cell lung cancer (NSCLC)
Tiseo, M., Andreoli, R., Gelsomino, F., Mozzoni, P., Azzoni, C., Bartolotti, M., Bortesi, B., Goldoni, M., Silini, E. M., Palma, G. D., et al. (2013) · Lung Cancer · doi:10.1016/j.lungcan.2013.12.001 · Cited by 44 · see citing works
Pharmacokinetics of afatinib in subjects with mild or moderate hepatic impairment
Schnell, D., Buschke, S., Fuchs, H., Gansser, D., Goeldner, R.-G., Uttenreuther-Fischer, M., Stopfer, P., Wind, S., Petersen-Sylla, M., Halabi, A., et al. (2014) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-014-2484-y · Cited by 44 · see citing works
First-in-human evaluation of CO-1686, an irreversible, selective, and potent tyrosine kinase inhibitor of EGFR T790M.
Sequist, L. V. D., Soria, J., Gadgeel, S. M., Wakelee, H. A., Camidge, D. R., Varga, A., Fidias, P., Wozniak, A. J., Neal, J. W., Doebele, R. C., et al. (2013) · Journal of Clinical Oncology · doi:10.1200/jco.2013.31.15_suppl.2524 · Cited by 42 · see citing works
First-line dacomitinib (PF-00299804), an irreversible pan-HER tyrosine kinase inhibitor, for patients with EGFR-mutant lung cancers.
Kris, M. G., Mok, T. S. K., Ou, S. I., Martins, R. G., Kim, D., Goldberg, Z., Zhang, H., Taylor, I. W., Letrent, S. P., & Janne, P. A. (2012) · Journal of Clinical Oncology · doi:10.1200/jco.2012.30.15_suppl.7530 · Cited by 41 · see citing works
Gefitinib–phenytoin interaction is not correlated with the14C‐erythromycin breath test in healthy male volunteers
Chhun, S., Verstuyft, C., Rizzo‐Padoin, N., Simoneau, G., Becquemont, L., Idy-Peretti, I., Swaisland, A. J., Wortelboer, R., Bergmann, J., & Mouly, S. J. (2009) · British Journal of Clinical Pharmacology · doi:10.1111/j.1365-2125.2009.03438.x · Cited by 39 · see citing works
Significant drug interaction: Phenytoin toxicity due to erlotinib
Grenader, T., Gips, M., Shavit, L., & Gabizón, A. (2007) · Lung Cancer · doi:10.1016/j.lungcan.2007.02.011 · Cited by 38 · see citing works
Targeting the epidermal growth factor receptor in solid tumors: focus on safety
Lucchini, E., Pilotto, S., Spada, E. L., Melisi, D., Bria, E., & Tortora, G. (2014) · Expert Opinion on Drug Safety · doi:10.1517/14740338.2014.904283 · Cited by 37 · see citing works
The effect of different etiologies of hepatic impairment on the pharmacokinetics of gefitinib
Horák, J., White, J., Harris, A. L., Verrill, M. W., Carmichael, J., Holt, A., Cantarini, M., Macpherson, M. P., Swaisland, A. J., Swaisland, H., et al. (2011) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-011-1611-2 · Cited by 35 · see citing works
A phase I dose-escalation and bioavailability study of oral and intravenous formulations of erlotinib (Tarceva®, OSI-774) in patients with advanced solid tumors of epithelial origin
Ranson, M., Shaw, H. M., Wolf, J., Hamilton, M., McCarthy, S. P., Dean, E. J., Reid, A. H. M., & Judson, I. R. (2009) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-009-1133-3 · Cited by 35 · see citing works
Continuation of afatinib beyond progression: Results of a randomized, open-label, phase III trial of afatanib plus paclitaxel (P) versus investigator’s choice chemotherapy (CT) in patients (pts) with metastatic non-small cell lung cancer (NSCLC) progressed on erlotinib/gefitinib (E/G) and afatanib—LUX-Lung 5 (LL5).
Schüler, M., Yang, C.-H., Park, K., Bennouna, J., Chen, Y., CHOUAID, C., de Marinis, F., Feng, J., Grossi, F., Kim, D., et al. (2014) · Journal of Clinical Oncology · doi:10.1200/jco.2014.32.15_suppl.8019 · Cited by 34 · see citing works
The effect of dacomitinib (PF-00299804) on CYP2D6 activity in healthy volunteers who are extensive or intermediate metabolizers
Bello, C. L., LaBadie, R. R., Ni, G., Boutros, T., McCormick, C., & Ndongo, M.-N. (2011) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-011-1793-7 · Cited by 32 · see citing works
Clinical and comparative utility of afatinib in non-small cell lung cancer
Hirsch, F. R., & D’Arcangelo, M. (2014) · Biologics · doi:10.2147/btt.s40567 · Cited by 31 · see citing works
Elevated International Normalized Ratio associated with concomitant warfarin and erlotinib
Thomas, K., Billingsley, A., Amarshi, N., & Nair, B. A. (2010) · American Journal of Health-System Pharmacy · doi:10.2146/ajhp090202 · Cited by 30 · see citing works
Erlotinib and pantoprazole: a relevant interaction or not?
ter Heine, R., Fanggiday, J. C., Lankheet, N. A. G., Beijnen, J. H., van der Westerlaken, M. M. L., Staaks, G., & Malingré, M. M. (2010) · British Journal of Clinical Pharmacology · doi:10.1111/j.1365-2125.2010.03748.x · Cited by 29 · see citing works
An open-label study to describe pharmacokinetic parameters of erlotinib in patients with advanced solid tumors with adequate and moderately impaired hepatic function
O’Bryant, C. L., Haluska, P., Rosen, L. S., Ramanathan, R. K., Venugopal, B., Leong, S., Boinpally, R., Franke, A., Witt, K., Evans, J., et al. (2011) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-011-1733-6 · Cited by 25 · see citing works
Interactions between oral antineoplastic agents and concomitant medication: a systematic review
Carcelero, E., Anglada-Martínez, H., Tuset, M., & Creus, N. (2013) · Expert Opinion on Drug Safety · doi:10.1517/14740338.2013.784268 · Cited by 25 · see citing works
A phase I open-label study to investigate the potential drug-drug interaction between single-dose dacomitinib and steady-state paroxetine in healthy volunteers
Ruiz-Garcı́a, A., Giri, N., LaBadie, R. R., Ni, G., Boutros, T., Richie, N. A., Kocinsky, H. S., Checchio, T., & Bello, C. L. (2013) · The Journal of Clinical Pharmacology · doi:10.1002/jcph.243 · Cited by 24 · see citing works
PF-00299804 (PF299) in Asian patients (pts) with non-small cell lung cancer (NSCLC) refractory to chemotherapy (CT) and erlotinib (E) or gefitinib (G): A phase (P) I/II study.
Park, K., Heo, D. S., Cho, B., Kim, D., Ahn, M.-J., Lee, S., Millham, R., Campbell, A., Zhang, H., & Kim, J. (2010) · Journal of Clinical Oncology · doi:10.1200/jco.2010.28.15_suppl.7599 · Cited by 23 · see citing works
Pharmacokinetic study of the phase III, randomized, double-blind, multicenter trial (TRIBUTE) of paclitaxel and carboplatin combined with erlotinib or placebo in patients with advanced Non-small Cell Lung Cancer (NSCLC)
Tran, H. T., Zinner, R., Blumenschein, G. R., Oh, Y. W., Papadimitrakopoulou, V. A., Kim, E. S., Lu, C. S., Malik, M., Lum, B. L., & Herbst, R. S. (2010) · Investigational New Drugs · doi:10.1007/s10637-009-9380-z · Cited by 19 · see citing works
Randomized, double-blinded study of dacomitinib, an irreversible pan-human epidermal growth factor receptor (HER) inhibitor, versus erlotinib for second-line/third-line therapy of locally advanced/metastatic non-small cell lung cancer (ARCHER 1009).
Ramalingam, S. S., Janne, P. A., Mok, T. S. K., O'Byrne, K. J., Boyer, M. J., Zhang, H., Liang, J. Q., Doherty, J. P., Taylor, I. W., Mather, C. A., et al. (2014) · Journal of Clinical Oncology · doi:10.1200/jco.2014.32.15_suppl.8018 · Cited by 16 · see citing works
NCIC CTG BR.26: A phase III randomized, double blind, placebo controlled trial of dacomitinib versus placebo in patients with advanced/metastatic non-small cell lung cancer (NSCLC) who received prior chemotherapy and an EGFR TKI.
Ellis, P. M., Liu, G., Millward, M. J., Perrone, F., Shepherd, F. A., Sun, S. B., Cho, B. C., Morabito, A., Stockler, M. R., Wierzbicki, R. F., et al. (2014) · Journal of Clinical Oncology · doi:10.1200/jco.2014.32.15_suppl.8036 · Cited by 14 · see citing works
Drug interactions among the epidermal growth factor receptor inhibitors, other biologics and cytotoxic agents
Visentin, M., Biason, P., & Toffoli, G. (2010) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2010.05.005 · Cited by 13 · see citing works
The influence of gastric secretion inhibitors on gefitinib therapy in patients with non-small cell lung cancer harboring epidermal growth factor receptor activating mutations.
Saeki, S., Sasaki, J., Morioka, J., Sato, R., Sakata, S., Ichiyasu, H., Fujii, K., Saita, N., & Kohrogi, H. (2012) · Journal of Clinical Oncology · doi:10.1200/jco.2012.30.15_suppl.e18059 · Cited by 6 · see citing works
Efficacy and safety results from CurrentS, a double-blind, randomized, phase III study of second-line erlotinib (150 mg versus 300 mg) in current smokers with advanced non-small cell lung cancer (NSCLC).
Smit, E. F., Gervais, R., Zhou, C., Felip, E., Feng, J., Güçlü, S. Z., Hoiczyk, M., Dorokhova, E., Freudensprung, U., Pérez-Moreno, P. D., et al. (2014) · Journal of Clinical Oncology · doi:10.1200/jco.2014.32.15_suppl.8046 · Cited by 5 · see citing works
Randomized phase II study of neratinib with or without temsirolimus in patients (pts) with non-small cell lung cancer (NSCLC) carrying HER2-activating mutations.
Gandhi, L., Soria, J., Bryce, R. P., & Besse, B. (2013) · Journal of Clinical Oncology · doi:10.1200/jco.2013.31.15_suppl.tps8124 · Cited by 3 · see citing works
Abstract CT208: Absolute bioavailability of dacomitinib (PF-00299804): Comparison of oral and intravenous administration in healthy volunteers
Giri, N., LaBadie, R. R., Liang, Y., Boutros, T., Goldberg, Z., & Bello, C. L. (2014) · Cancer Research · doi:10.1158/1538-7445.am2014-ct208 · Cited by 2 · see citing works
Influence of mild and moderate hepatic impairment on the pharmacokinetics (PK) of the pan-HER inhibitor dacomitinib.
Giri, N., Plotka, A., Liang, Y., Boutros, T., Ni, G., Masters, J. C., DeMicco, M. P., Pardo, P., Bello, C. L., & O'Connell, J. P. (2013) · Journal of Clinical Oncology · doi:10.1200/jco.2013.31.15_suppl.2568 · Cited by 2 · see citing works

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Osimertinib: First Global Approval
Greig, S. L. (2016) · Drugs · doi:10.1007/s40265-015-0533-4 · Cited by 334 · see citing works
Signaling Pathways in Cancer: Therapeutic Targets, Combinatorial Treatments, and New Developments
Yip, H. Y. K., & Papa, A. (2021) · Cells · doi:10.3390/cells10030659 · Cited by 332 · see citing works
Small Molecule Kinase Inhibitor Drugs (1995–2021): Medical Indication, Pharmacology, and Synthesis
Ayala-Aguilera, C. C., Valero, T., Lorente‐Macías, Á., Baillache, D. J., Croke, S., & Unciti‐Broceta, A. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c00963 · Cited by 287 · see citing works
The association between PD-L1 and EGFR status and the prognostic value of PD-L1 in advanced non-small cell lung cancer patients treated with EGFR-TKIs
Tang, Y., Fang, W., Zhang, Y., Hong, S., Kang, S., Yan, Y., Chen, N., Zhan, J., He, X., Qin, T., et al. (2015) · Oncotarget · doi:10.18632/oncotarget.3694 · Cited by 243 · see citing works
Renal Drug Transporters and Drug Interactions
Ivanyuk, A., Livio, F., Biollaz, J., & Buclin, T. (2017) · Clinical Pharmacokinetics · doi:10.1007/s40262-017-0506-8 · Cited by 221 · see citing works
Combined inhibition of DDR1 and Notch signaling is a therapeutic strategy for KRAS-driven lung adenocarcinoma
Ambrogio, C., Goméz-López, G., Falcone, M., Vidal, A., Nadal, E., Crosetto, N., Blasco, R. B., Fernández-Marcos, P. J., Sánchez‐Céspedes, M., Ren, X., et al. (2016) · Nature Medicine · doi:10.1038/nm.4041 · Cited by 175 · see citing works
Olmutinib: First Global Approval
Kim, E. S. (2016) · Drugs · doi:10.1007/s40265-016-0606-z · Cited by 170 · see citing works
Recent updates on third generation EGFR inhibitors and emergence of fourth generation EGFR inhibitors to combat C797S resistance
Patel, H., Pawara, R., Ansari, A., & Surana, S. (2017) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2017.05.027 · Cited by 170 · see citing works
Long non-coding RNA UCA1 induces non-T790M acquired resistance to EGFR-TKIs by activating the AKT/mTOR pathway in EGFR-mutant non-small cell lung cancer
Cheng, N., Cai, W., Ren, S., Li, X., Wang, Q., Pan, H., Zhao, M., Li, J., Zhang, Y., Zhao, C., et al. (2015) · Oncotarget · doi:10.18632/oncotarget.4361 · Cited by 148 · see citing works
Repurposing of Kinase Inhibitors for Treatment of COVID-19
Weisberg, E., Parent, A., Yang, P. L., Sattler, M., Liu, Q., Liu, Q., Wang, J., Meng, C., Buhrlage, S. J., Gray, N. S., et al. (2020) · Pharmaceutical Research · doi:10.1007/s11095-020-02851-7 · Cited by 137 · see citing works
Small Molecule Kinase Inhibitors for the Treatment of Brain Cancer
Heffron, T. P. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b00618 · Cited by 141 · see citing works
Afatinib for the treatment of EGFR mutation-positive NSCLC: A review of clinical findings
Harvey, R. D., Adams, V. R., Beardslee, T., & Medina, P. (2020) · Journal of Oncology Pharmacy Practice · doi:10.1177/1078155220931926 · Cited by 115 · see citing works
Optimizing outcomes in EGFR Mutation-Positive Nsclc: Which Tyrosine Kinase Inhibitor and When?
Girard, N. (2018) · Future Oncology · doi:10.2217/fon-2017-0636 · Cited by 103 · see citing works
Safety and Tolerability of Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitors in Oncology
Shah, R. R., & Shah, D. R. (2019) · Drug Safety · doi:10.1007/s40264-018-0772-x · Cited by 99 · see citing works
Ultrasmall Core-Shell Silica Nanoparticles for Precision Drug Delivery in a High-Grade Malignant Brain Tumor Model
Juthani, R. G., Madajewski, B., Yoo, B., Zhang, L., Chen, P.-M., Chen, F., Turker, M. Z., Ma, K., Overholtzer, M., Longo, V. A., et al. (2019) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-19-1834 · Cited by 96 · see citing works
Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer
Meng, Y., Yu, B., Huang, H., Peng, Y., Li, E., Yao, Y., Song, C., Yu, W., Zhu, K., Wang, K., et al. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c02005 · Cited by 76 · see citing works
Challenges in the Use of Targeted Therapies in Non–Small Cell Lung Cancer
Rivera‐Concepción, J., Uprety, D., & Adjei, A. A. (2022) · Cancer Research and Treatment · doi:10.4143/crt.2022.078 · Cited by 80 · see citing works
Self-citation
The characterization, management, and future considerations for ErbB-family TKI-associated diarrhea
Rugo, H. S., Palma, J. A. D., Tripathy, D., Bryce, R. P., Moran, S. E., Olek, E. A., & Bosserman, L. D. (2019) · Breast Cancer Research and Treatment · doi:10.1007/s10549-018-05102-x · Cited by 76 · see citing works
Synthetic Approaches to New Drugs Approved During 2016
Flick, A. C., Ding, H. X., Leverett, C. A., Fink, S. J., & O’Donnell, C. J. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b00260 · Cited by 70 · see citing works
Next-Generation Covalent Irreversible Kinase Inhibitors in NSCLC: Focus on Afatinib
Hirsh, V. (2015) · BioDrugs · doi:10.1007/s40259-015-0130-9 · Cited by 68 · see citing works
Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors
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Authors: Peters, S., Zimmermann, S., & Adjei, A. A.
Affiliations: Centre Hospitalier Universitaire Vaudois (CH)
Roswell Park Comprehensive Cancer Center (US)
Corresponding author: Peters, Solange
ORCID: Peters, Solange
Zimmermann, Stefan
Adjei, Alex A.
Venue: Cancer Treatment Reviews
Publisher: Elsevier BV
Published: 2014-09
Volume: 40
Issue: 8
Pages: 917-926
ISSN: 0305-7372 (ISSN-L)
DOI: 10.1016/j.ctrv.2014.06.010
OpenAlex: W2097781997
Cited by: 155
References: 115
Citations by year: 2026: 5 · 2025: 10 · 2024: 10 · 2023: 9 · 2022: 14 · 2021: 12 · 2020: 10 · 2019: 24 · 2018: 10 · 2017: 18 · 2016: 16 · 2015: 16 · 2014: 1
FWCI: 13.64
Type: journal article
Language: en
Open access: hybrid
doi.org
Licence: cc-by-nc-nd
www.elsevier.com/tdm/userlicense/1.0/ (tdm)
creativecommons.org/licenses/by-nc-nd/3.0/ (vor)
Locations: Cancer Treatment Reviews (publishedVersion, cc-by-nc-nd)
PubMed (publishedVersion)
IRIS (submittedVersion)
SERVAL (Université de Lausanne) (submittedVersion)
Topics: Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Lung Cancer Treatments and Mutations
Health Sciences › Medicine › Oncology › HER2/EGFR in Cancer Research
Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
Keywords: EGFR tyrosine kinase inhibitors, non-small cell lung cancer, gefitinib, erlotinib, afatinib, dacomitinib, T790M mutation, acquired drug resistance, pharmacokinetics, drug-drug interactions, ErbB family, mutant-selective inhibitors, oral anticancer drugs, combination therapy
MeSH terms: Administration, Oral, Carcinoma, Non-Small-Cell Lung, Drug Interactions, Humans, Lung Neoplasms, Protein Kinase Inhibitors, ErbB Receptors

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Oral epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of non-small cell lung cancer: Comparative pharmacokinetics and drug–drug interactions

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