lapatinib / Generic mfg. 
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  • ||||||||||  lapatinib / Generic mfg.
    Journal:  Lapatinib ameliorates skin fibrosis by inhibiting TGF-?1/Smad and non-Smad signaling pathway. (Pubmed Central) -  Mar 12, 2025   
    Our findings suggest that lapatinib may be a promising therapeutic agent for skin fibrosis by targeting ErbB1/ErbB2 and modulating the TGF-?1/Smad2/3/Erk/Akt signalling pathways. These results warrant further clinical investigation into lapatinib for treating skin fibrosis and related conditions.
  • ||||||||||  lapatinib / Generic mfg., paclitaxel / Generic mfg.
    Trial completion, Trial completion date, Trial primary completion date:  Dose Escalation of Lapatinib With Paclitaxel in Ovarian Cancer (clinicaltrials.gov) -  Mar 11, 2025   
    P1,  N=15, Completed, 
    These results warrant further clinical investigation into lapatinib for treating skin fibrosis and related conditions. Active, not recruiting --> Completed | Trial completion date: Jun 2025 --> May 2024 | Trial primary completion date: Jun 2025 --> May 2024
  • ||||||||||  lapatinib / Generic mfg.
    Journal:  Discovery of isoquinoline-tethered quinazoline derivatives with enhanced HER2 inhibition over EGFR. (Pubmed Central) -  Mar 10, 2025   
    These derivatives demonstrated significantly improved selectivity for HER2 over EGFR, with a 7- to 12-fold enhancement compared to lapatinib in kinase assays...Additionally, compound 14f exhibited high HER2 selectivity, significantly inhibited colony formation in SKBR3 cells, and displayed good metabolic stability. These findings suggest the potential of these compounds as novel therapeutic candidates for HER2-positive cancers.
  • ||||||||||  Clinical, Retrospective data, Journal, Real-world evidence:  A Retrospective Real-World Study of Pyrotinib in HER-2 Positive Advanced Breast Cancer. (Pubmed Central) -  Mar 10, 2025   
    The most common adverse reaction associated with pyrotinib is diarrhea, which can be well controlled through antidiarrheal treatment. Pyrotinib combined with vinorelbine has similar efficacy to pyrotinib combined with capecitabine and has fewer side effects, and can be used as an alternative to capecitabine.
  • ||||||||||  lapatinib / Generic mfg., Ibrance (palbociclib) / Pfizer, Synribo (omacetaxine mepesuccinate) / Teva
    Journal, IO biomarker:  A prognostic model of lung adenocarcinoma constructed based on circadian rhythm genes and its potential clinical significance. (Pubmed Central) -  Mar 5, 2025   
    Ultimately, the experimental results confirmed that the expression trends of CDK1 and HLA-DMA in our collected clinical samples were in line with the expression trends in the TCGA-LUAD dataset. In conclusion, a CR-relevant risk model based on CDK1 and HLA-DMA was constructed by using bioinformatics analysis, which might supply a new insight into the improved prognosis of LUAD.
  • ||||||||||  lapatinib / Generic mfg., tamoxifen / Generic mfg., Caprelsa (vandetanib) / Sanofi
    Journal:  Kinase Plasticity in Response to Vandetanib Enhances Sensitivity to Tamoxifen and Identifies Co-Treatment Strategies in Estrogen Receptor Positive Breast Cancer. (Pubmed Central) -  Feb 20, 2025   
    Finally, we use our operating room-to-laboratory assay that measures drug response in individual primary tumor cells in short term cultures to demonstrate conserved gene expression changes, including increased HER2 activity signatures, in vandetanib treated cells, and identify features associated with vandetanib response. These results support future investigation of RET targeting strategies considering reprogrammed networks, such as activated HER2, in patients with ET resistant ER+ breast cancer.
  • ||||||||||  Pozenveo (poziotinib) / Assertio
    Journal:  The Brain-Penetrant Pan ErbB Inhibitor Poziotinib Effectively Targets HER2+ Breast Cancer Brain Metastases. (Pubmed Central) -  Feb 11, 2025   
    Despite effective HER2-targeted treatments of peripheral HER2+ breast cancer with trastuzumab and HER2 inhibitors, limited brain permeability renders these treatments inefficient for HER2+ breast cancer brain metastasis (BCBM)...The clinical receptor tyrosine kinase inhibitor (RTKi) lapatinib blocked phosphorylation of all ErbB receptors (ErbB1-4) and induced the intrinsic apoptosis pathway in BCBM94...Two weeks of poziotinib treatment successfully ablated BCBM94 and BT474 HER2+ brain tumors in vivo. In conclusion, this study established a patient-derived HER2+ BCBM model and identified poziotinib as highly efficacious RTKi with excellent brain penetrability that eliminated HER2+ BCBM.
  • ||||||||||  lapatinib / Generic mfg.
    Journal:  Repurposing lapatinib as a triple antagonist of chemokine receptors 3, 4, and 5. (Pubmed Central) -  Feb 7, 2025   
    Using these models, we identified lapatinib as a potent inhibitor of CCR3, CCR4, and CCR5. Our study illustrates the potential of machine learning in identifying molecules for repurposing as antagonists for G protein-coupled receptors, including CCR3, CCR4, and CCR5, which have various therapeutic applications.
  • ||||||||||  lapatinib / Generic mfg.
    Journal:  Tanshinlactone triggers methuosis in breast cancer cells via NRF2 activation. (Pubmed Central) -  Feb 5, 2025   
    Tanshinlactone as a novel therapeutic agent, is capable of selectively inhibiting ER+ and HER2+/EGFR + breast tumors through a unique mechanism of inducing catastrophic macropinocytosis. This regimen holds promise for targeted therapy with minimized side effects and offers a new therapeutic avenue for breast patients with drug-resistant diseases.
  • ||||||||||  lapatinib / Generic mfg., methotrexate / Generic mfg., gefitinib / Generic mfg.
    Journal, Gene Signature, IO biomarker:  Regulatory T cell-associated gene signature correlates with prognostic risk and immune infiltration in patients with breast cancer. (Pubmed Central) -  Jan 16, 2025   
    Moreover, sensitivity to 83 chemotherapeutic drugs such as lapatinib, methotrexate, and gefitinib were significantly differed between the two risk groups (all P<0.001). This is the first to develop a Treg-associated gene signature for breast cancer, which could predict prognosis of patients and help to identify patients who might be benefit from immunotherapy and/or chemotherapy.
  • ||||||||||  Kadcyla (ado-trastuzumab emtansine) / Roche
    Journal:  HER-2 SMASH. (Pubmed Central) -  Dec 23, 2024   
    The smash method can switch HER-2 negative or HER-2 low tumors into HER-2 overexpressed, iatrogenically. Thus, we can use her2-targeted therapies in all cancer patients instead of a small portion.
  • ||||||||||  Herceptin (trastuzumab) / Roche
    Trial completion, Trial completion date:  Lapatinib in Combination With Trastuzumab in Patients With HER2-Positive, Metastatic Breast Cancer (clinicaltrials.gov) -  Dec 19, 2024   
    P2,  N=87, Completed, 
    Further in vitro studies involving gene silencing could provide more detailed insights into the mechanism by which ACA combats lapatinib resistance. Active, not recruiting --> Completed | Trial completion date: Dec 2024 --> Aug 2024
  • ||||||||||  Tukysa (tucatinib) / Pfizer, Nerlynx (neratinib) / Puma
    Journal:  Quantum DFT analysis and molecular docking investigation of various potential breast cancer drugs. (Pubmed Central) -  Dec 18, 2024   
    In contrast, anastrozole and letrozole show lower binding affinities for HER2 and EGFR due to their simpler structures but are potent aromatase inhibitors, making them effective in treating estrogen receptor-positive (ER-positive) breast cancers. In conclusion, DFT and molecular docking studies affirm the suitability of lapatinib, tucatinib, and neratinib for HER2-positive cancers, while anastrozole and letrozole are effective in ER-positive cancers, emphasizing the role of molecular structure and binding affinity in optimizing cancer treatment strategies.
  • ||||||||||  lapatinib / Generic mfg.
    Biomarker, Journal, PD(L)-1 Biomarker, IO biomarker:  TRPC6 is a Biomarker for Prognosis and Immunotherapy of Stomach Adenocarcinoma Based on Bioinformatic Analysis and Experimental Validation. (Pubmed Central) -  Dec 18, 2024   
    TRPC6 expression correlated strongly with immune cell infiltration, immune checkpoint genes, and sensitivity to therapies such as Lapatinib, anti-CTLA4, and anti-PD1 treatments...This study highlights the prognostic significance of TRPC6 in STAD and its potential as a therapeutic target. TRPC6's involvement in immune regulation and cancer cell progression underscores its dual role in STAD pathogenesis and treatment, offering new avenues for targeted therapy development.
  • ||||||||||  Erbitux (cetuximab) / Eli Lilly, Herceptin (trastuzumab) / Roche
    Journal:  Potential Drug Synergy Through the ERBB2 Pathway in HER2+ Breast Tumors. (Pubmed Central) -  Dec 17, 2024   
    We visualized these interactions using Cytoscape to generate individual and combined drug-gene networks, focusing on frequently used drugs such as Erlotinib, Gefitinib, Lapatinib, and Cetuximab...Combined drug networks, such as those for Cetuximab with Lapatinib, Cetuximab with Erlotinib, and Erlotinib with Lapatinib, revealed potential synergies that could enhance therapeutic efficacy by simultaneously influencing multiple genes and pathways. Our findings suggest that a network-based approach to analyzing drug combinations provides valuable insights into the molecular mechanisms of HER2+ breast cancer and offers promising strategies for overcoming drug resistance and improving treatment outcomes.
  • ||||||||||  lapatinib / Generic mfg., mitomycin / Generic mfg.
    Biomarker, Journal:  Study of TRAF3IP3 for prognosis and immune infiltration in hepatocellular carcinoma. (Pubmed Central) -  Dec 16, 2024   
    Notably, the half-maximal inhibitory concentration (IC50) of commonly used chemotherapeutic drugs, such as lapatinib and mitomycin, was inversely associated with TRAF3IP3 expression in HCC patients. TRAF3IP3 may be as a novel and promising biomarker for prognosis prediction and immunological evaluation of HCC.
  • ||||||||||  Journal:  Reactivation of MAPK-SOX2 pathway confers ferroptosis sensitivity in KRASG12C inhibitor resistant tumors. (Pubmed Central) -  Dec 9, 2024   
    The clinical success of KRASG12C inhibitors (G12Ci) including AMG510 and MRTX849 is limited by the eventual development of acquired resistance...We found the ferroptosis inducers including sorafenib and lapatinib stood out with an obvious growth inhibition in the G12Ci resistant cells...Ferroptosis induced by sulfasalazine (SAS) achieved obvious inhibition on the tumor growth of xenografts derived from AMG510-resistant KRASG12C-mutant cells. Collectively, our results suggest a novel therapeutic strategy to treat patients bearing G12Ci resistant cancers with ferroptosis inducers.
  • ||||||||||  Herceptin (trastuzumab) / Roche
    Journal, Metabolomic study:  LC-HRMS-based global metabolomics profiling unravels the distinct metabolic signature of lapatinib-resistant and trastuzumab-resistant HER2+ breast cancer cells. (Pubmed Central) -  Dec 3, 2024   
    Joint pathway enrichment analysis of LAP-resistant DEMs and differentially expressed genes (DEGs) showed enrichment in glutathione metabolism, while that of TRZ-resistance and DEGs showed enrichment in carbohydrate metabolism, namely pentose and glucuronate interconversions, starch and sucrose metabolism, and galactose metabolism. The findings from this study indicate considerable metabolic changes in LAP- and TRZ-resistant HCC1954 cells, which are crucial for understanding the resistance mechanisms and developing strategies to overcome these problems.
  • ||||||||||  lapatinib / Generic mfg.
    Journal:  Structure-based pharmacophore modelling for ErbB4-kinase inhibition: a systematic computational approach for small molecule drug discovery for breast cancer. (Pubmed Central) -  Dec 2, 2024   
    Furthermore, the ADMET profiles of 11 shortlisted candidates were assessed to verify their pharmacokinetic and toxicity properties, identifying Chembl310724, Chembl521284, and Chembl4168686 as promising inhibitors of ErbB4 kinase activity with the binding free energy (?Gbind) values of -99.84, -89.42 and -86.06?kcal/mol, respectively. This integrated methodology not only enhances our understanding of ErbB4 inhibition but also sets a foundation for the rational design of targeted therapies addressing breast cancer with ErbB4 dependency.
  • ||||||||||  Iclusig (ponatinib) / Takeda, Otsuka
    Journal:  Potential protein kinase inhibitors that target G-quadruplex DNA structures in the human telomeric regions. (Pubmed Central) -  Dec 2, 2024   
    Thus, it is hypothesized that Ponatinib and Lapatinib may stabilize human telomeric G4 DNA in addition to their ability to inhibit BCR-ABL and the other members of the EGFR family. As a result, we also hypothesize that the stabilization of G4 DNA might represent an additional underlying mechanism contributing to their efficacy in exerting anti-cancer effects.
  • ||||||||||  Enhertu (fam-trastuzumab deruxtecan-nxki) / Daiichi Sankyo, AstraZeneca
    Journal:  Case report: Efficacy of later-line fam-trastuzumab deruxtecan in a patient with triple-positive breast cancer with brain metastases. (Pubmed Central) -  Nov 19, 2024   
    The patient then received capecitabine, neratinib, GnRH agonist, and letrozole; however, her brain metastases still progressed after 7 months...Now aged 30, the patient is continuing to receive T-DXd treatment to prevent recurrence. We conclude that T-DXd was effective for the treatment of brain metastases in this young patient with triple-positive metastatic breast cancer who had multiple risk factors and had received several anti-HER2 therapies prior to T-DXd.
  • ||||||||||  lapatinib / Generic mfg.
    Journal:  Structure-based virtual screening and fragment replacement to design novel inhibitors of Coxsackievirus A16 (CVA16). (Pubmed Central) -  Nov 14, 2024   
    The results indicated that all three molecules retain inside the pocket of CAV16 receptor throughout the simulation process, and he binding energy calculated from the MD simulation trajectories also support the strong affinity of the top three molecules towards the CVA16. These results will provide new ideas and technical guidance for designing and applying CVA16 therapeutics.Communicated by Ramaswamy H. Sarma.
  • ||||||||||  lapatinib / Generic mfg., Tukysa (tucatinib) / Pfizer, Nerlynx (neratinib) / Puma
    Review, Journal:  A review on tyrosine kinase inhibitors for targeted breast cancer therapy. (Pubmed Central) -  Nov 13, 2024   
    TKIs have emerged as a promising therapeutic option for patients with breast cancer and hold potential for treating other breast cancer subtypes. The development of new TKIs and their integration into personalized treatment strategies will continue to shape the future of breast cancer therapy.