Efficacy and safety of domestic and imported gefitinib in patients with advanced non-small cell lung cancer

Cheng, Huawei; Liu, Hongyue; Du, Qin; Zhang, Hui; Zhang, Xiaodan; Wang, Yangkui; Shao, Jingjing; Yang, Feng; Zhang, Bo; Liu, Yuguo; Wu, Nan; Xu, Silu; Wei, Qing; Sun, Yongkang; Zhai, Qian; Yu, Bo

doi:10.21037/apm-20-2140

Cited by 6 publications

(5 citation statements)

References 8 publications

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“…23) In 2003, the FDA approved gefitinib for the treatment of locally advanced or metastatic NSCLC patients who had received chemotherapy or had contraindications to chemotherapy. 9) Gefitinib was not considered to have significant cardiotoxicity. 11) However, in recent years, there have been many reports of gefitinib-induced cardiotoxicity.…”

Section: Discussionmentioning

confidence: 99%

“…7,8) Gefitinib is a first-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI). 9,10) Different from other TKIs, gefitinib is not considered to have significant cardiotoxicity. 11,12) However, in recent years, more and more literatures have reported that gefitinib induces cardiotoxicity, mainly including acute coronary syndrome, 8) recurrent myocardial infarction, 11) myocarditis, 13) and QT interval prolongation.…”

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confidence: 99%

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Gefitinib Increases the Incidence of QT Prolongation in Patients with Non-Small Cell Lung Cancer

et al. 2023

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Gefitinib (GEF) may increase the risk of corrected QT prolongation (QTc). We aimed to evaluate whether gefitinib increases the risk of corrected QT interval (QTc) prolongation and analyze the associated risk factors.A total of 122 cases of advanced EGFR-mutated non-small cell lung cancer (NSCLC) who received gefitinib therapy from January 2015 to December 2020 were evaluated. The results of at least two resting 12-lead electrocardiogram before and after gefitinib treatment were obtained. The Bazett and Fridericia formulas were used to calculate the QTc interval, and the changes of QTc interval values before and after treatment were evaluated. The correlation between gefitinib and QTc interval prolongation and related risk factors were analyzed.After gefitinib-targeted therapy, 23 patients (18.9%) had a prolonged QTc interval, which increased from a mean of 446 ± 25 ms at baseline to 478 ± 18 ms (P < 0.001). Three of the patients met criteria for Grade 3 QTc prolongation in the common term V5.0 for clinical adverse events. Univariate analysis showed that age (ORR, 1.054; 95% confidence interval [CI], 1.003-1.107; P = 0.038), history of hypertension (ORR, 3.409; 95% CI,; P = 0.01), CCB medication history (ORR, 0.259; 95% CI, 0.094-0.712; P = 0.009), history of lung cancer surgery (ORR, 0.231; 95% CI, 0.064-0.829; P = 0.025), and baseline QT interval (ORR, 0.978; 95% CI, 0.964-0.993; P = 0.004) were important predictors of QTc interval prolongation in patients treated with gefitinib. The results of multivariate analysis showed that the history of lung cancer surgery and the baseline QT interval were important factors affecting QTc interval prolongation in patients treated with gefitinib.Gefitinib increases the risk of QTc prolongation in NSCLC patients, which may be more pronounced in patients with advanced age, hypertension, CCB therapy, lung cancer surgery, and a long QT interval at baseline.

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Section: Discussionmentioning

confidence: 99%

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confidence: 99%

Gefitinib Increases the Incidence of QT Prolongation in Patients with Non-Small Cell Lung Cancer

et al. 2023

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“…They bind to the EGFR kinase region in a competitive ATP-binding manner, reversibly inhibiting EGFR kinase activity and thus blocking downstream signaling. (1) Gefitinib was approved by the FDA in 2003 for the treatment of patients with advanced NSCLC who have failed chemotherapy [107]. (2) Erlotinib was approved by the FDA in 2004 for the treatment of locally advanced or metastatic NSCLC and was subsequently approved in combination with gemcitabine for the treatment of locally advanced or metastatic pancreatic cancer [108].…”

Section: Egfr Inhibitorsmentioning

confidence: 99%

Review of Personalized Medicine and Pharmacogenomics of Anti-Cancer Compounds and Natural Products

Zhou,

Peng,

Wang

et al. 2024

Genes

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In recent years, the FDA has approved numerous anti-cancer drugs that are mutation-based for clinical use. These drugs have improved the precision of treatment and reduced adverse effects and side effects. Personalized therapy is a prominent and hot topic of current medicine and also represents the future direction of development. With the continuous advancements in gene sequencing and high-throughput screening, research and development strategies for personalized clinical drugs have developed rapidly. This review elaborates the recent personalized treatment strategies, which include artificial intelligence, multi-omics analysis, chemical proteomics, and computation-aided drug design. These technologies rely on the molecular classification of diseases, the global signaling network within organisms, and new models for all targets, which significantly support the development of personalized medicine. Meanwhile, we summarize chemical drugs, such as lorlatinib, osimertinib, and other natural products, that deliver personalized therapeutic effects based on genetic mutations. This review also highlights potential challenges in interpreting genetic mutations and combining drugs, while providing new ideas for the development of personalized medicine and pharmacogenomics in cancer study.

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“…They bind to the EGFR kinase region in a competitive ATP-binding manner, reversibly inhibiting EGFR kinase activity and thus blocking downstream signaling. 1) Gefitinib Gefitinib was approved by the FDA in 2003 for the treatment of patients with advanced NSCLC who have failed chemotherapy [105]. Erlotinib was approved by the FDA in 2004 for the treatment of locally advanced or metastatic NSCLC and was subsequently approved in combination with gemcitabine for the treatment of locally advanced or metastatic pancreatic cancer [106].…”

Section: Egfr Inhibitorsmentioning

confidence: 99%

Review of Personalized Medicine and Pharmacogenomics of Anti-Cancer Compounds and Natural Products

Zhou¹,

Peng²,

Wang³

et al. 2023

Preprint

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In recent years, the FDA has approved numerous antitumor drugs that are mutation-based for clinical use. These drugs have improved the precision of treatment and reduced adverse effects and side effects. Personalized therapy is a prominent and hot topic of current medicine and also represents the future direction of development. With the continuous advancements in gene sequencing and high-throughput screening, research and development strategies for personalized clinical drugs have developed rapidly. This review elaborated the recent personalized treatment strategies, which include artificial intelligence, multi-omics analysis, chemical proteomics, and computation aided drug design. These technologies rely on the molecular classification of diseases, the global signaling network within organisms, and new models for all targets, which significantly support the development of personalized medicine. Meanwhile, we summarized chemical drugs such as lorlatinib, osimertinib, and other natural products that deliver personalized therapeutic effects based on genetic mutations. This review also highlights potential challenges in interpreting genetic mutations and combining drugs, while providing new ideas for the development of personalized medicine and pharmacogenomics in cancer study.

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Efficacy and safety of domestic and imported gefitinib in patients with advanced non-small cell lung cancer

Cited by 6 publications

References 8 publications

Gefitinib Increases the Incidence of QT Prolongation in Patients with Non-Small Cell Lung Cancer

Gefitinib Increases the Incidence of QT Prolongation in Patients with Non-Small Cell Lung Cancer

Review of Personalized Medicine and Pharmacogenomics of Anti-Cancer Compounds and Natural Products

Review of Personalized Medicine and Pharmacogenomics of Anti-Cancer Compounds and Natural Products

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