Article
Biology
Xiaolong Tang, Lizhi Cheng, Guo Li, Yong-Ming Yan, Fengting Su, Dan-Ling Huang, Shuping Zhang, Zuojun Liu, Minxian Qian, Ji Li, Yong-Xian Cheng, Baohua Liu
Summary: The small molecule compound D6 demonstrates promising efficacy in treating EGFR-TKI resistant NSCLC by targeting the protein-protein interaction between HSP90 and T790M-EGFR, offering a potential alternative strategy to overcome drug resistance.
COMMUNICATIONS BIOLOGY
(2021)
Review
Oncology
Yue Pan, Chao Deng, Zhenhua Qiu, Chenghui Cao, Fang Wu
Summary: This review discusses the resistance mechanisms of ALK TKIs in advanced NSCLC, providing a theoretical basis and research ideas for solving the problem of ALK drug resistance.
FRONTIERS IN ONCOLOGY
(2021)
Article
Chemistry, Medicinal
Meredith S. Eno, Jason D. Brubaker, John E. Campbell, Chris De Savi, Timothy J. Guzi, Brett D. Williams, Douglas Wilson, Kevin Wilson, Natasja Brooijmans, Joseph Kim, Aysegul Ozen, Emanuele Perola, John Hsieh, Victoria Brown, Kristina Fetalvero, Andrew Garner, Zhuo Zhang, Faith Stevison, Rich Woessner, Jatinder Singh, Yoav Timsit, Caitlin Kinkema, Clare Medendorp, Christopher Lee, Faris Albayya, Alena Zalutskaya, Stefanie Schalm, Thomas A. Dineen
Summary: While EGFR tyrosine kinase inhibitors have revolutionized the treatment of NSCLC, the development of resistance mutations remains a challenge. This study introduces a novel reversible inhibitor, BLU-945, that shows promising activity against different resistance mutations. Clinical trials are currently underway to evaluate its efficacy and safety.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Nidhi Saini, Ajmer Singh Grewal, Viney Lather, Suresh Kumar Gahlawat
Summary: Phytochemicals contribute to protection and interaction processes by acting as antioxidants, anti-mutagens, anticarcinogens, and antimicrobial agents. In this study, sanguinarine was found to be the most potent inhibitor of epidermal growth factor receptor (EGFR) compared to erlotinib. Other alkaloids also showed potent inhibition against EGFR, but their stability with EGFR varied. Out of the 31 alkaloids subjected to ADMET prediction, 29 alkaloids followed Lipinski's rule of five and were predicted to have high bioavailability, low toxicity, and ease of synthesis.
CHEMICO-BIOLOGICAL INTERACTIONS
(2022)
Article
Oncology
Yoichi Ohtaki, Kimihiro Shimizu, Hiroyuki Suzuki, Kenji Suzuki, Masahiro Tsuboi, Tetsuya Mitsudomi, Motoshi Takao, Tomohiro Murakawa, Hiroyuki Ito, Kenichi Yoshimura, Morihito Okada, Masayuki Chida
Summary: Salvage surgery after TKI treatment for non-small cell lung cancer patients is safe and feasible, potentially prolonging overall survival time by reducing the local tumor burden.
Article
Oncology
Qizhi Ma, Pei Shu, Kexun Zhou, Yongsheng Wang
Summary: We present a case of disease progression in a woman with non-small-cell lung cancer (NSCLC) during treatment with EGFR-tyrosine kinase inhibitor osimertinib due to an unplanned pregnancy. Termination of the pregnancy resulted in temporary improvement but subsequent deterioration. This case highlights the importance of vigilance and preventive measures in pregnant patients with EGFR-mutation lung cancer to manage tumor progression and emergencies.
FRONTIERS IN ONCOLOGY
(2023)
Review
Oncology
Tania Crombet Ramos, Orestes Santos Morales, Grace K. Dy, Kalet Leon Monzon, Agustin Lage Davila
Summary: CIMAvax-EGF is a novel approach for treating NSCLC by neutralizing EGF and inhibiting tumor growth, showing potential efficacy. Clinical trials have demonstrated that CIMAvax-EGF can prolong overall survival in advanced NSCLC patients, especially those with higher EGF concentrations.
FRONTIERS IN ONCOLOGY
(2021)
Review
Oncology
Robert Hsu, David J. J. Benjamin, Misako Nagasaka
Summary: This narrative review discusses the development of capmatinib, a reversible MET tyrosine kinase inhibitor approved for advanced NSCLC with MET exon 14 skipping mutation. Early-phase trials determined the recommended dose of 400 mg twice daily. The GEOMETRY mono-1 trial demonstrated efficacy in MET exon 14 skipping mutation, resulting in FDA approval of capmatinib. Ongoing clinical trials are assessing combination therapy with capmatinib and exploring new drug agents, such as antibody-drug conjugates, to broaden the indications and improve efficacy of capmatinib in the treatment of MET dysregulated NSCLC.
Article
Oncology
Ying-Ting Liao, Lei-Chi Wang, Ruei-Lin Sun, Yi-Chen Yeh, Hsu-Ching Huang, Chia- Shen, Yen-Han Tseng, Tsu-Hui Hsiao, Heng-Sheng Chao, Yung-Hung Luo, Yuh-Min Chen, Chi-Lu Chiang
Summary: This study aimed to elucidate the characteristics and treatment patterns of non-small cell lung cancer (NSCLC) patients with epidermal growth factor receptor (EGFR) exon 20 insertions (ex20ins) in Taiwan. The results showed that platinum-based chemotherapy (PtC) was associated with higher response rates, disease control rates, and longer progression-free survival compared to EGFR tyrosine kinase inhibitor (TKI) in both first-line and second-line treatments. Heterogeneous clinical characteristics and treatment patterns were observed in EGFR ex20ins NSCLC patients.
JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY
(2023)
Review
Oncology
Leah Wells, Angel Qin
Summary: EGFR tyrosine kinase inhibitors (TKI) are the first-line treatment for NSCLC with atypical EGFR mutations. The choice of TKI depends on the specific mutation, with afatinib being the FDA-approved option for atypical EGFR mutations. Dacomitinib can also be considered, while osimertinib is recommended for classical-like mutations such as L861Q. Comprehensive sequencing is crucial for identifying these mutations.
CURRENT TREATMENT OPTIONS IN ONCOLOGY
(2023)
Review
Oncology
Leylah M. Drusbosky, Richa Dawar, Estelamari Rodriguez, Chukwuemeka Ikpeazu
Summary: The MET exon 14 skipping mutation is present in a small percentage of lung cancer patients, but targeted inhibitors like capmatinib and tepotinib show promising clinical activity with tolerable toxicity profiles. Ongoing research aims to overcome acquired resistance and enhance the effectiveness of these agents.
JOURNAL OF HEMATOLOGY & ONCOLOGY
(2021)
Article
Biotechnology & Applied Microbiology
Jun Ni, Li Zhang
Summary: HER2, a member of the ErbB receptor tyrosine kinase family, can form various dimers with other receptors to affect signal pathways and promote proliferation, differentiation, and tumorigenesis in NSCLC. Different HER2 aberrations in NSCLC, including mutation, amplification, and overexpression, have varying clinical relevance and responses to treatment. While HER2 mutations are generally considered more clinically relevant, there is still no consensus on detection and targeted treatments for HER2 abnormalities in NSCLC.
ONCOTARGETS AND THERAPY
(2021)
Review
Oncology
Taisuke Araki, Shintaro Kanda, Hidehito Horinouchi, Yuichiro Ohe
Summary: Osimertinib is the standard therapy for EGFR-mutated non-small cell lung cancer, but resistance is a challenge, leading to the need for new therapeutic strategies.
JAPANESE JOURNAL OF CLINICAL ONCOLOGY
(2023)
Article
Pharmacology & Pharmacy
Wang Shujun, Lou Lili, Yang Lei, Wang Feng, Zhan Hefeng
Summary: Osimertinib is a standard treatment for NSCLC with fewer side effects, but colitis may occur after months of treatment. Aumolertinib, a novel third-generation EGFR-TKI, could be an effective alternative for patients experiencing colitis from osimertinib.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Medicine, Research & Experimental
Dan Yan, Justus M. Huelse, Dmitri Kireev, Zikang Tan, Luxiao Chen, Subir Goyal, Xiaodong Wang, Stephen Frye, Madhusmita Behera, Frank Schneider, Suresh S. Ramalingam, Taofeek Owonikoko, H. Shelton Earp, Deborah DeRyckere, Douglas K. Graham
Summary: Acquired resistance is inevitable in non-small cell lung cancers (NSCLCs) treated with osimertinib (OSI). Activation of MERTK is associated with OSI resistance and inhibition of MERTK kinase can resensitize resistant cells to OSI.
JOURNAL OF CLINICAL INVESTIGATION
(2022)
