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DRUG:

gefitinib

i
Other names: ZD1839
Company:
Generic mfg.
Drug class:
EGFR inhibitor
Related drugs:
9d
Knockdown of Inhibin Beta A Reversed the Epithelial Growth Factor Receptor Tyrosine Kinase Inhibitor Resistance and Enhanced the Therapeutic Effect of Radiotherapy in Non-Small Cell Lung Cancer. (PubMed, Biochem Genet)
Gefitinib treatment affected NSCLC resistant cells...Both INHBA silencing and X-ray treatment inhibited EMT development. This study demonstrated that INHBA silencing ameliorates EGFR-TKI resistance and enhances the therapeutic effect of radiotherapy in NSCLC.
Journal
|
INHBA (Inhibin, beta A)
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gefitinib
10d
New trial
|
Tagrisso (osimertinib) • erlotinib • gefitinib
15d
The Effects of Nebivolol-Gefitinib-Loratadine Against Lung Cancer Cell Lines. (PubMed, In Vivo)
The nebivolol-gefitinib-loratadine combination may be a promising alternative for lung cancer treatment.
Preclinical • Journal
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR H1975
|
gefitinib
15d
Epidermal growth factor receptor signaling governs the host inflammatory response to invasive aspergillosis. (PubMed, mBio)
In a corticosteroid immunosuppressed mouse model of invasive pulmonary aspergillosis, inhibition of EGFR with gefitinib decreased whole-lung cytokine and chemokine levels and reduced accumulation of phagocytes in the lung, leading to a decrease in fungal killing, an increase in pulmonary fungal burden, and accelerated mortality...This leads to decreased accumulation of neutrophils and dendritic cells in the lungs, reduced A. fumigatus killing, and increased mortality. These results provide a potential explanation as to why some cancer patients who are treated with EGFR inhibitors develop invasive aspergillosis.
Journal
|
EGFR (Epidermal growth factor receptor)
|
gefitinib
15d
First-line treatment with gefitinib in combination with bevacizumab and chemotherapy in advanced non-squamous NSCLC with EGFR-mutation. (PubMed, BMC Cancer)
The results of this study demonstrate that the four-drug combination regimen, led by gefitinib, is manageable and tolerated and effective for patients with EGFR-mutated advanced non-squamous NSCLC.
Journal • Combination therapy • Metastases
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation
|
Avastin (bevacizumab) • carboplatin • gefitinib • pemetrexed
16d
Gefitinib Reverses PD-L1-Mediated Immunosuppression Induced by long-term Glutamine blockade in Bladder Cancer. (PubMed, Cancer Immunol Res)
Combination treatment of JHU083 and gefitinib reversed the up-regulation of PD-L1 in bladder cancer cells induced by prolonged glutamine blockade, resulting in the alleviation of T-cell immunosuppression and a significant improvement in therapeutic outcome. These preclinical findings show promise for glutamine metabolism targeting as a viable therapeutic strategy for bladder cancer, with the potential for further enhancement through combined treatment with gefitinib.
Journal • PD(L)-1 Biomarker • IO biomarker
|
PD-L1 (Programmed death ligand 1) • JUN (Jun proto-oncogene)
|
PD-L1 expression
|
gefitinib • JHU083
19d
A Multi-Omics Prognostic Model Capturing Tumor Stemness and the Immune Microenvironment in Clear Cell Renal Cell Carcinoma. (PubMed, Biomedicines)
The CRCS2 subtype was in a hypoxic state and was characterized by suppression and exclusion of immune function, which was sensitive to gefitinib, erlotinib, and saracatinib. Our findings highlight the key role of CSCs in shaping the ccRCC tumor microenvironment, crucial for therapy research and clinical guidance. Recognizing tumor stemness helps to predict treatment efficacy, recurrence, and drug resistance, informing treatment strategies and enhancing ccRCC patient outcomes.
Journal
|
SAA2 (Serum Amyloid A2)
|
erlotinib • gefitinib • saracatinib (AZD0530)
19d
ARAF Amplification in Small-Cell Lung Cancer-Transformed Tumors Following Resistance to Epidermal Growth Factor Receptor-Tyrosine Kinase Inhibitors. (PubMed, Cancers (Basel))
ARAF amplification was identified in 5-8% of EGFR-TKI-resistant tumors. The possible roles of ARAF in SCLC transformation warrant further investigation.
Journal
|
EGFR (Epidermal growth factor receptor) • ARAF (A-Raf Proto-Oncogene)
|
EGFR mutation • EGFR exon 19 deletion
|
Tagrisso (osimertinib) • erlotinib • gefitinib
19d
Amphiregulin promotes activated regulatory T cell-suppressive function via the AREG/EGFR pathway in laryngeal squamous cell carcinoma. (PubMed, Head Face Med)
Collectively, this study revealed the role and mechanism of AREG in negative immune regulation, and targeting AREG might be a novel immunotherapy for LSCC.
Journal • IO biomarker
|
AREG (Amphiregulin) • CD4 (CD4 Molecule) • FOXP3 (Forkhead Box P3)
|
AREG expression • FOXP3 expression
|
gefitinib
19d
Cytochalasin H enhances sensitivity to gefitinib in non-small-cell lung cancer cells through inhibiting EGFR activation and PD-L1 expression. (PubMed, Sci Rep)
Furthermore, CyH inhibited the activation of JAK3/STAT signaling pathway. Taken together, our findings suggest that CyH promotes the sensitivity to gefitinib in NSCLC cells through the inhibition of EGFR activation and PD-L1 expression.
Journal • PD(L)-1 Biomarker • IO biomarker
|
EGFR (Epidermal growth factor receptor) • PD-1 (Programmed cell death 1) • JAK3 (Janus Kinase 3)
|
PD-L1 expression • EGFR mutation • EGFR expression • EGFR wild-type • EGFR H1975
|
gefitinib
20d
Piperlongumine in combination with EGFR tyrosine kinase inhibitors for the treatment of lung cancer cells. (PubMed, Oncol Res)
Anticancer efficacy of PPL, erlotinib (ERL), gefitinib (GEF), and cisplatin (CIS) were investigated in H1299 and H1975 cell lines. Treatment with PPL alone and in combination induced anti-mitogenic and apoptotic responses at the molecular level. PPL sensitized lung cancer cells to EGFR-TKI and induced potent cytotoxic effects at low concentrations.
Journal • Combination therapy
|
EGFR (Epidermal growth factor receptor)
|
EGFR H1975
|
cisplatin • erlotinib • gefitinib
22d
Bee venom prompts the inhibition of gefitinib on proliferation, migration, and invasion of non-small cell lung cancer cells via EGFR-mediated autophagy. (PubMed, Toxicon)
Ultimately, Western blot assays showed BV alone or combined with gefitinib significantly decreased the protein expression of phosphorylated EGFR (p-EGFR) and the protein expression ratio of p-EGFR to EGFR, and increased the protein expression ratio of LC3-II to LC3-I in PC-9 cells or epidermal growth factor-activated PC-9 cells. The results demonstrated that BV could prompt the inhibition of gefitinib on proliferation, migration, and invasion of NSCLC cells via EGFR-mediated autophagy, showing the synergistic anti-NSCLC potential when combined with gefitinib.
Journal
|
EGFR (Epidermal growth factor receptor)
|
gefitinib
26d
YAP1 modulation of primary cilia-mediated ciliogenesis in 2D and 3D prostate cancer models. (PubMed, FEBS Lett)
We explored the role of ciliated cells in prostate cancer by using Gefitinib and Jasplakinolide compounds to induce ciliated cells in both normal and tumor-like prostate cell lines...Finally, we examined these compounds in 3D cell models, aiming to simulate in vivo conditions. Our study highlights YAP1 as a potential target for novel genetic models to understand the primary cilium's role in mediating resistance to anticancer treatments.
Preclinical • Journal
|
YAP1 (Yes associated protein 1) • GLI1 (GLI Family Zinc Finger 1)
|
gefitinib
28d
Real-World Data Presenting the Descriptive Analysis of the Use of Tyrosine Kinase Inhibitors (TKIs) Among Metastatic Non-Small-Cell Lung Cancer (mNSCLC) Patients in Qatar: A Nationwide Retrospective Cohort Study. (PubMed, Clin Med Insights Oncol)
The TKIs used during this period include EGFR inhibitors such as afatinib, erlotinib, gefitinib, and osimertinib and ALK inhibitors such as alectinib and crizotinib. The EGFR-targeted and ALK-targeted therapies appear to have acceptable clinical response rate and safety profile in our population. Close and frequent monitoring of adverse events is advised to ensure a good quality of life and prevent serious complications.
Retrospective data • Journal • Real-world evidence • Real-world • Metastases
|
ALK (Anaplastic lymphoma kinase)
|
ALK rearrangement
|
Xalkori (crizotinib) • Tagrisso (osimertinib) • erlotinib • Gilotrif (afatinib) • gefitinib • Alecensa (alectinib)
30d
Targeted nanoliposomes of oncogenic protein degraders: Significant inhibition of tumor in lung-cancer bearing mice. (PubMed, J Control Release)
T-BEPRO revealed a particle size of 109.22 ± 0.266 nm with enhanced cellular uptake and activity. Remarkably, parenterally delivered T-BEPRO in tumor-bearing mice showed a substantially higher % tumor growth inhibition (TGI) of 77.6 % with long-lasting tumor inhibitory potential as opposed to individual drugs.
Preclinical • Journal
|
KRAS (KRAS proto-oncogene GTPase) • MYC (V-myc avian myelocytomatosis viral oncogene homolog) • BRD4 (Bromodomain Containing 4)
|
gefitinib • ARV-825
1m
Griffithazanone A, a sensitizer of EGFR-targeted drug in Goniothalamus yunnanensis for non-small cell lung cancer. (PubMed, Heliyon)
Moreover, griffithazanone A treatment enhanced the efficacy of gefitinib and osimertinib and reversed osimertinib resistance. Overall, our study highlights the potential of griffithazanone A in inhibiting the progression of NSCLC by targeting PIM1 and reversing resistance to EGFR targeted drugs.
Journal • IO biomarker
|
BCL2 (B-cell CLL/lymphoma 2) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • PIM1 (Pim-1 Proto-Oncogene)
|
BAX expression
|
Tagrisso (osimertinib) • gefitinib
1m
Role of disulfidptosis in colorectal adenocarcinoma: implications for prognosis and immunity. (PubMed, Front Immunol)
We also predicted that drugs such as 5-Fluorouracil, Oxaliplatin, Gefitinib, and Sorafenib would be more effective in low-risk patients, while drugs like Luminesib and Staurosporine would be more effective in high-risk patients. Finally, the expression of these key genes was verified in clinical samples, with consistent results. Our research findings provide evidence for the role of disulfidptosis in COAD and offer new insights for personalized and precise treatment of COAD.
Journal • MSi-H Biomarker
|
TMB (Tumor Mutational Burden) • MSI (Microsatellite instability) • CXCL10 (Chemokine (C-X-C motif) ligand 10) • CCL11 (C-C Motif Chemokine Ligand 11) • SLC7A11 (Solute Carrier Family 7 Member 11) • HOXC6 (Homeobox C6)
|
TMB-H • MSI-H/dMMR • SLC7A11 expression
|
gefitinib • sorafenib • 5-fluorouracil • oxaliplatin
1m
Ubiquitin-specific protease 10 determines colorectal cancer outcome by modulating epidermal growth factor signaling via inositol polyphosphate-4-phosphatase type IIB. (PubMed, Oncogenesis)
Specifically, our study demonstrates that the loss of USP10 results in reduced sensitivity to the EGFR tyrosine kinase inhibitors gefitinib and osimertinib. The findings enhance our understanding of CRC pathobiology and reveal a new regulatory axis involving USP10 and INPP4B in CRC progression. This unique insight identifies USP10 and INPP4B as potential therapeutic targets in CRC.
Journal
|
INPP4B (Inositol polyphosphate-4-phosphatase type II B) • EGF (Epidermal growth factor)
|
Tagrisso (osimertinib) • gefitinib
1m
FTO/m6A mediates miR-138-5p maturation and regulates gefitinib resistance of lung adenocarcinoma cells by miR-138-5p/LCN2 axis. (PubMed, BMC Cancer)
FTO suppressed the processing of miR-138-5p and then modulated the proliferation, death, and ferroptosis of gefitinib-resistant cells through the miR-138-5p/LCN2 pathway, which may put forward novel insights for clinically ameliorating the therapeutic effect of gefitinib in LUAD.
Journal
|
LCN2 (Lipocalin-2) • FTO (Alpha-Ketoglutarate-Dependent Dioxygenase FTO) • MIR138 (MicroRNA 138)
|
gefitinib
1m
First-line zorifertinib for EGFR-mutant non-small cell lung cancer with central nervous system metastases: The phase 3 EVEREST trial. (PubMed, Med)
Zorifertinib significantly improved systemic and intracranial PFS versus first-generation EGFR-TKIs; adverse events were manageable. Sequential use of zorifertinib and third-generation EGFR-TKIs showed the potential to prolong patients' survival. The results favor zorifertinib as a novel, well-validated first-line option for CNS-metastatic patients with EGFR-mutant NSCLC.
P3 data • Journal
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR L858R
|
erlotinib • gefitinib • zorifertinib (AZD3759)
1m
New P2 trial • Metastases
|
Lynparza (olaparib) • Tagrisso (osimertinib) • carboplatin • gefitinib • gemcitabine • paclitaxel • temozolomide • tamoxifen • Verzenio (abemaciclib) • pemetrexed • fulvestrant • letrozole • pegylated liposomal doxorubicin • exemestane • Myocet (non-pegylated liposomal doxorubicin) • Duomeisu (pegylated liposomal doxorubicin)
1m
Journal
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation
|
Tagrisso (osimertinib) • gefitinib
1m
Paeoniae radix overcomes resistance to EGFR-TKIs via aurora B pathway suppression in lung adenocarcinoma. (PubMed, Life Sci)
This study explored the synergistic effects of combining Paeoniae Radix (PR) with first-generation EGFR-tyrosine kinase inhibitors (TKIs), erlotinib and gefitinib, to overcome this resistance. Additionally, gene expression changes confirmed these combined effects, with the suppression of the Aurora B pathway and upregulation of the apoptotic pathway, which was accompanied by increased expression of multiple pro-apoptotic genes. Our findings contribute to the development of natural product-based therapeutic strategies to mitigate drug resistance in LUAD.
Journal
|
AURKA (Aurora kinase A)
|
EGFR mutation
|
erlotinib • gefitinib
1m
High-throughput screening of the natural STK11 agonist dauricine: a biphenylisoquinoline alkaloid exerting anti-NSCLC effects and reversing gefitinib resistance. (PubMed, Eur J Pharmacol)
Dauricine, a natural agonist of STK11, effectively inhibited NSCLC, and its combination treatment with gefitinib reversed drug-resistant NSCLC.
Journal
|
STK11 (Serine/threonine kinase 11)
|
AURKB overexpression • STK11 deletion
|
gefitinib
1m
Combined inhibition of MET and VEGF enhances therapeutic efficacy of EGFR TKIs in EGFR-mutant non-small cell lung cancer with concomitant aberrant MET activation. (PubMed, Exp Hematol Oncol)
Our work reveals a positive feedback loop between MET and VEGF/VEGFR2, resulting in continuous downstream signal activation. Combined inhibition of MET and VEGF/VEGFR2 signaling pathway may be beneficial for reversing EGFR TKIs resistance.
Journal
|
ETS1 (ETS Proto-Oncogene 1)
|
EGFR mutation • KDR expression
|
Avastin (bevacizumab) • Xalkori (crizotinib) • gefitinib
2ms
HIF-1α-HPRT1 axis promotes tumorigenesis and gefitinib resistance by enhancing purine metabolism in EGFR-mutant lung adenocarcinoma. (PubMed, J Exp Clin Cancer Res)
Our study reveals that muEGFR-HIF-1α-HPRT1 axis plays a key role in EGFR-mutant LUAD and provides a new strategy-inhibiting purine metabolism for treating EGFR-mutant LUAD.
Journal
|
EGFR (Epidermal growth factor receptor) • HIF1A (Hypoxia inducible factor 1, alpha subunit) • HPRT1 (Hypoxanthine Phosphoribosyltransferase 1)
|
EGFR mutation • HIF1A expression
|
gefitinib
2ms
Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Cancer: Current Use and Future Prospects. (PubMed, Int J Mol Sci)
For example, patients on gefitinib, a first-generation TKI, experienced a progression-free survival (PFS) of 10 months compared to 5 months with conventional chemotherapy. Second-generation TKI afatinib outperformed erlotinib and extended PFS to 11.1 months compared to 6.9 months with cisplatin...Several trials have started showing promising in vitro and in vivo results, but more trials are needed before clinical approval. This review underscores notable advancements in the field of EGFR TKIs, offering a comprehensive analysis of their mechanisms of action and the progression of various TKI generations in response to resistance.
Review • Journal
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR T790M • EGFR C797S
|
cisplatin • erlotinib • Gilotrif (afatinib) • gefitinib
2ms
HER-2 Receptor and αvβ3 Integrin Dual-Ligand Surface-Functionalized Liposome for Metastatic Breast Cancer Therapy. (PubMed, Pharmaceutics)
Targeted therapies have revolutionized treatment efficacy, with Trastuzumab (Trast), a monoclonal antibody, targeting HER2-positive advanced breast cancer...Gefitinib (GFB) is a potential anticancer drug against HER2-positive breast cancer, while Lycorine hydrochloride (LCH) is a natural compound with anticancer and anti-inflammatory properties...Additionally, the blood compatibility study showed minimal hemolysis (less than 5% RBC lysis), indicating good biocompatibility and biosafety. Overall, these findings suggest that TPGS-COOH-coated, GFB and LCH co-loaded, dual-ligand (iRGD and Trast) functionalized, multifunctional liposomes could be a promising therapeutic strategy for treating HER2-positive metastatic breast cancer.
Journal • Metastases
|
HER-2 (Human epidermal growth factor receptor 2)
|
HER-2 positive • EGFR positive
|
Herceptin (trastuzumab) • gefitinib
2ms
Global trends and hotspots in research of paronychia: A bibliometric analysis. (PubMed, Medicine (Baltimore))
In this area, most of the recent hotspots are not focused on the basic research about paronychia due to the basic research about traditional paronychia already reached a relative mature stage. However, with the widespread clinical application of EGFRI anticancer drugs, the incidence of drug-induced paronychia is inevitably on the rise. Therefore, with the expanding diversity in the etiology of paronychia, this area deserves a multiple discipline cooperation with a much wider international communication.
Review • Journal
|
EGFR (Epidermal growth factor receptor)
|
erlotinib • Gilotrif (afatinib) • gefitinib
2ms
Efficacy and patient-reported outcomes in advanced non-small cell lung cancer patients receiving aumolertinib as first-line therapy: a real-world study. (PubMed, Front Pharmacol)
Aumolertinib demonstrated superior progression-free survival (PFS) and a well-tolerated toxicity profile compared to gefitinib in front-line treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) in the AENEAS trial. In this real-world study, aumolertinib showed comparable disease control and objective response rates as reported in the AENEAS trial for advanced NSCLC patients with EGFR-sensitizing mutations. Aumolertinib treatment improved PROs, further supporting it in first-line clinical practice.
Journal • Real-world evidence • Patient reported outcomes • Real-world • Metastases
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation
|
gefitinib • Ameile (aumolertinib)
2ms
USP22 promotes gefitinib resistance and inhibits ferroptosis in non-small cell lung cancer by deubiquitination of MDM2. (PubMed, Thorac Cancer)
USP22/MDM2 promoted gefitinib resistance and inhibited ferroptosis in NSCLC, which might offer a novel strategy for overcoming gefitinib resistance in NSCLC.
Journal
|
MDM2 (E3 ubiquitin protein ligase) • USP22 (Ubiquitin Specific Peptidase 22)
|
USP22 overexpression
|
gefitinib
2ms
Epidermal Growth Factor Receptor Signaling Governs the Host Inflammatory Response to Invasive Aspergillosis. (PubMed, bioRxiv)
In a corticosteroid immunosuppressed mouse model of invasive pulmonary aspergillosis, inhibition of EGFR with gefitinib decreased whole lung chemokine levels and reduced accumulation of phagocytes in the lung, leading to a decrease in fungal killing, an increase in pulmonary fungal burden, and accelerated mortality...This leads to decreased accumulation of neutrophils and dendritic cell in the lungs, reduced A. fumigatus killing, and increased mortality. These results provide a potential explanation as to why some cancer patients who are treated with EGFR inhibitors develop invasive aspergillosis.
Journal
|
EGFR (Epidermal growth factor receptor)
|
gefitinib
2ms
KEAP1-NRF2 pathway as a novel therapeutic target for EGFR-mutant non-small cell lung cancer. (PubMed, Tuberc Respir Dis (Seoul))
We identified that NRF2 inhibition enhanced cell death and inhibited tumor growth in TKI-resistant lung cancer with EGFR-mutation. Thus, NRF2 modulation may be a novel therapeutic strategy to overcome the resistance to EGFR-tyrosine kinase inhibitors.
Journal • IO biomarker
|
EGFR (Epidermal growth factor receptor) • KEAP1 (Kelch Like ECH Associated Protein 1) • NFE2L2 (Nuclear Factor, Erythroid 2 Like 2)
|
EGFR mutation • EGFR expression • KEAP1 mutation • NFE2L2 mutation
|
Tagrisso (osimertinib) • gefitinib
2ms
Impact of First-Line Osimertinib and Other EGFR-Tyrosine Kinase Inhibitors on Overall Survival in Untreated Advanced EGFR-Mutated Non-small Cell Lung Cancer in Japan: Updated Data from TREAD Project 01. (PubMed, Target Oncol)
Based on real-world data, osimertinib did not show a significant improvement in overall survival compared to other EGFR-TKIs as a first-line treatment for EGFR-mutated advanced non-small cell lung cancer in the Japanese (Asian) population.
Clinical • Journal • Metastases
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR L858R
|
Tagrisso (osimertinib) • erlotinib • Gilotrif (afatinib) • gefitinib
2ms
cost-effectiveness of aumolertinib as first-line treatment for EGFR-mutated advanced nonsmall-cell lung cancer. (PubMed, Future Oncol)
Sensitivity and scenario analyses were performed to explore the robustness of the model. Compared with gefitinib, aumolertinib yielded an additional 0.941 expected life-years and 0.692 quality-adjusted life-years (QALYs), with an incremental cost of $18,855.55 over a 20-year time horizon. The incremental cost-effectiveness ratios were $20,051.67/life-year and $27,272.29/QALY, that below the willing-to-pay threshold of $38,223.34/QALY. Aumolertinib was a cost-effective alternative first-line treatment for patients with epidermal growth factor receptor-positive advanced nonsmall-cell lung cancer in China.
Journal • HEOR • Cost-effectiveness • Cost effectiveness • Metastases
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR positive
|
gefitinib • Ameile (aumolertinib)
2ms
Study of EGF816 in Combination With Selected Targeted Agents in EGFR-mutant NSCLC (clinicaltrials.gov)
P1, N=105, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Dec 2024 --> Apr 2025 | Trial primary completion date: Dec 2024 --> Apr 2025
Trial completion date • Trial primary completion date • Combination therapy
|
EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR exon 20 insertion • EGFR exon 20 mutation
|
Mekinist (trametinib) • gefitinib • Kisqali (ribociclib) • Tabrecta (capmatinib) • naporafenib (ERAS-254) • nazartinib (EGF816)
2ms
New P2 trial
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR L858R • EGFR exon 19 deletion
|
gefitinib • Conmana (icotinib)
2ms
A Clinical Study of Sorafenib Combined With Gefitinib for the Treatment of pNET (clinicaltrials.gov)
P=N/A, N=20, Not yet recruiting, Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine
New trial
|
gefitinib • sorafenib
2ms
Association of mean platelet volume (MPV), MPV/PLATELET (PLT) ratio, and lymphocyte/monocyte ratio (LMR) as poor prognostic factor in EGFR-mutant lung adenocarcinoma treated with EGFR tyrosine kinase inhibitor. (PubMed, Tuberk Toraks)
The independent factors determining OS in multivariate Cox regression analysis were being male, platelet increase, MPV > 7.55, gefitinib treatment, and smoking. MPV, MPV/PLT, and LMR are potential biomarkers that can be used for the clinical follow-up of lung ADC patients receiving EGFR-TKI treatment.
Retrospective data • Journal
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR positive
|
gefitinib
2ms
Investigation through naphtho[2,3-a]pyrene on mutated EGFR mediated autophagy in NSCLC: Cellular model system unleashing therapeutic potential. (PubMed, IUBMB Life)
It showed synergistic activity against NSCLC when coupled with gefitinib, chloroquine, and radiation. Altogether, our study highlights naphtho[2,3-a]pyrene's therapeutic promise in NSCLC by focusing on EGFR-mediated autophagy and providing a new strategy to fight drug resistance and tumor survival.
Journal
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation
|
gefitinib • chloroquine phosphate
2ms
CIB2 mediates acquired gefitinib resistance by inducing ZEB1 expression and epithelial-mesenchymal transition. (PubMed, Aging (Albany NY))
Finally, CIB2 rendered tumors resistant to gefitinib treatment in vivo. Our results explored a new mechanism: upregulated CIB2 promoted EMT through ZEB1 to regulate gefitinib resistance, which could be a candidate therapeutic target for overcoming acquired resistance to EGFR-TKIs in NSCLC patients.
Journal
|
FOSL1 (FOS Like 1) • ZEB1 (Zinc Finger E-box Binding Homeobox 1)
|
EGFR mutation • ZEB1 expression
|
gefitinib
2ms
Increasing the tumour targeting of antitumour drugs through anlotinib-mediated modulation of the extracellular matrix and the RhoA/ROCK signalling pathway. (PubMed, J Pharm Anal)
Our bioinformatic analysis revealed a potential positive relationship between the ECM pathway and gefitinib resistance, poor treatment outcomes for programmed death 1 (PD-1) targeting, and unfavourable prognosis following chemotherapy in lung cancer patients. These findings suggest that, in addition to its antiangiogenic and vessel normalization effects, anlotinib can increase the distribution and retention of antitumour drugs in tumours by modulating ECM expression and physical properties through the RhoA/ROCK signalling pathway. These valuable insights contribute to the development of combination therapies aimed at improving tumour targeting in cancer treatment.
Journal • PD(L)-1 Biomarker • IO biomarker
|
RHOA (Ras homolog family member A)
|
gefitinib • Focus V (anlotinib)