Results of the phase IIa study to evaluate the efficacy and safety of rezivertinib (BPI-7711) for the first-line treatment of locally advanced or metastatic/recurrent NSCLC patients with EGFR mutation from a phase I/IIa study

Shi, Yuankai; Zhou, Jianying; Zhao, Yanqiu; Zhu, Bo; Zhang, Liangming; Li, Xingya; Fang, Jian; Shi, Jianhua; Zhuang, Zhixiang; Yang, Sheng; Wang, Donglin; Yu, Huiqing; Zhang, Longzhen; Ruan, Zheng; Greco, Michael N.; Wang, Tingting

doi:10.1186/s12916-022-02692-8

Cited by 3 publications

(2 citation statements)

References 31 publications

(46 reference statements)

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“…Rezivertinib selectively inhibits the proliferation of EGFR mutated cells in cell lines. 142,[169][170][171] Covalent EGFR inhibitors in clinical trials. Currently, several covalent EGFR inhibitors are undergoing clinical trials, all of which are third-generation or more advanced EGFR TKIs.…”

Section: Covalent Egfr Inhibitorsmentioning

confidence: 99%

“…427 In 2019, Macdonald et al discovered a class of Myc-WDR5 inhibitors with a sulfonamide structure via high-throughput screening (HTS). 428 Although compound (170) was the most active (IC 50 = 29 nM), it was unsuitable for in vivo studies. To address this, Chacon Simon et al identified several other compound fragments via NMR fragment screening, resulting in compound (171) (IC 50 = 100 nM).…”

Section: Myc Ppi Inhibitorsmentioning

confidence: 99%

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Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

Xie,

Yu,

et al. 2023

Sig Transduct Target Ther

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Undruggable proteins are a class of proteins that are often characterized by large, complex structures or functions that are difficult to interfere with using conventional drug design strategies. Targeting such undruggable targets has been considered also a great opportunity for treatment of human diseases and has attracted substantial efforts in the field of medicine. Therefore, in this review, we focus on the recent development of drug discovery targeting “undruggable” proteins and their application in clinic. To make this review well organized, we discuss the design strategies targeting the undruggable proteins, including covalent regulation, allosteric inhibition, protein–protein/DNA interaction inhibition, targeted proteins regulation, nucleic acid-based approach, immunotherapy and others.

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Section: Covalent Egfr Inhibitorsmentioning

confidence: 99%

Section: Myc Ppi Inhibitorsmentioning

confidence: 99%

Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

Xie,

Yu,

et al. 2023

Sig Transduct Target Ther

View full text Add to dashboard Cite

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Central nervous system efficacy of rezivertinib (BPI-7711) in advanced NSCLC patients with EGFR T790M mutation: A pooled analysis of two clinical studies

Yang¹,

Wu²,

Zhao³

et al. 2023

Lung Cancer

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Therapeutic advances of targeting receptor tyrosine kinases in cancer

Tomuleasa,

Tigu,

Munteanu

et al. 2024

Sig Transduct Target Ther

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Receptor tyrosine kinases (RTKs), a category of transmembrane receptors, have gained significant clinical attention in oncology due to their central role in cancer pathogenesis. Genetic alterations, including mutations, amplifications, and overexpression of certain RTKs, are critical in creating environments conducive to tumor development. Following their discovery, extensive research has revealed how RTK dysregulation contributes to oncogenesis, with many cancer subtypes showing dependency on aberrant RTK signaling for their proliferation, survival and progression. These findings paved the way for targeted therapies that aim to inhibit crucial biological pathways in cancer. As a result, RTKs have emerged as primary targets in anticancer therapeutic development. Over the past two decades, this has led to the synthesis and clinical validation of numerous small molecule tyrosine kinase inhibitors (TKIs), now effectively utilized in treating various cancer types. In this manuscript we aim to provide a comprehensive understanding of the RTKs in the context of cancer. We explored the various alterations and overexpression of specific receptors across different malignancies, with special attention dedicated to the examination of current RTK inhibitors, highlighting their role as potential targeted therapies. By integrating the latest research findings and clinical evidence, we seek to elucidate the pivotal role of RTKs in cancer biology and the therapeutic efficacy of RTK inhibition with promising treatment outcomes.

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Results of the phase IIa study to evaluate the efficacy and safety of rezivertinib (BPI-7711) for the first-line treatment of locally advanced or metastatic/recurrent NSCLC patients with EGFR mutation from a phase I/IIa study

Cited by 3 publications

References 31 publications

Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

Central nervous system efficacy of rezivertinib (BPI-7711) in advanced NSCLC patients with EGFR T790M mutation: A pooled analysis of two clinical studies

Therapeutic advances of targeting receptor tyrosine kinases in cancer

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