A Subset of VEGFR-TKIs Activates AMPK in LKB1-mutant Lung Cancer - PubMed
Source : https://pubmed.ncbi.nlm.nih.gov/36459496/
The mutation of tumor suppressor gene liver kinase B1 (LKB1) has a prevalence of about 20% in non-small cell lung cancer (NSCLC). LKB1-mutant lung cancer is characterized by enhanced aggressiveness...
Conclusions: This study discovered AMPK as an important off-target of apatinib, and elucidated different effects of this cluster of VEGFR-TKIs on AMPK. This finding can be the basis for the accurate and combined application of these drugs in clinic, and highlights the subset of VEGFR-TKIs including apatinib and anlotinib are potentially valuable...
Phase I Study Evaluating Glesatinib (MGCD265), An Inhibitor of MET and AXL, in Patients with Non-small Cell Lung Cancer and Other Advanced Solid Tumors - Targeted Oncology
Source : https://link.springer.com/article/10.1007/s11523-022-00931-9
Background Heightened signaling by mesenchymal epithelial transition factor (MET) is implicated in tumorigenesis. Glesatinib is an investigational, oral inhibitor of MET and AXL. Objective This phase I study determined the...
Conclusions: The safety profile of single-agent glesatinib was acceptable. SDD 750 mg twice daily was selected as the preferred glesatinib formulation and dose based on clinical activity, safety, and PK data. Observations from this study led to initiation of a phase II study of glesatinib in patients with NSCLC stratified by type of MET...
Efficacy of immune checkpoint inhibitors in non-small cell lung cancer with uncommon histology: a propensity-score-matched analysis - PubMed
Source : https://pubmed.ncbi.nlm.nih.gov/34600514/
doi: 10.1186/s12890-021-01681-6. 1 Second Division, Department of Internal Medicine, Hamamatsu University School of Medicine, 1-20-1 Handayama, Hamamatsu, 431-3192, Japan. 2 Second Division, Department of Internal Medicine, Hamamatsu University School of...
Conclusions: ICIs had similar clinical efficacy for treatment of uNSCLC and cNSCLC. Good ECOG-PS and PD-L1 expression were predictive for efficacy of ICIs in uNSCLC.
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Albert Dekker3yrIt was suspected to be the case but nice to know
RNA Structural Dynamics Modulate EGFR-TKI Resistance Through Controlling YRDC Translation in NSCLC Cells
Source : https://www.sciencedirect.com/science/article/pii/S1672022922001425?via=ihub
Epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs) positively affect the initial control ratio of non-small cell lung cancer (NSC...
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Conclusions: Conclusions/Relevance: Our study reveals an unprecedented mechanism through which the RNA structure switch modulates EGFR-TKI resistance by controlling YRDC mRNA translation in an ELAVL1-dependent manner.
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Albert Dekker3yrI am lost a bit; so RNA is able to b self regulated on mRNA level?
Ongoing progress in BRAF-mutated non-small cell lung cancer - PubMed
Source : https://pubmed.ncbi.nlm.nih.gov/36331404/
Activating BRAF mutations are detected in 1.5% to 4.5% of patients with non-small cell lung cancer (NSCLC). These mutations involve the mitogen-activated protein kinase/extracellular signal-regulated kinase pathway, and affect proliferation,...
Relevance: First-generation BRAF inhibitors are not active in the class II and III BRAF mutations that form the other half of BRAF mutations in NSCLC. New RAF inhibitors are being investigated in early trials. Novel treatment combinations, particularly with immune checkpoint inhibitors, are also underway. Patient referral to expert centers and...
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Albert Dekker3yrobviously with Braf inhibitors it would be better