lapatinib / Generic mfg. 
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 236 Diseases   41 Trials   41 Trials   3914 News 


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  • ||||||||||  Gilotrif (afatinib) / Boehringer Ingelheim
    Journal:  Quantitative Structure-Mutation-Activity Relationship Tests (QSMART) model for protein kinase inhibitor response prediction. (Pubmed Central) -  Dec 1, 2020   
    By integrating multi-omics data in the QSMART model, we not only predict drug responses in cancer cell lines with high accuracy but also identify features and explainable interaction terms contributing to the accuracy. Although we have tested our multi-component explainable framework on protein kinase inhibitors, it can be extended across the proteome to investigate the complex relationships connecting genotypes and drug sensitivity profiles.
  • ||||||||||  lapatinib / Generic mfg.
    Journal:  Precise safety pharmacology studies of lapatinib for onco-cardiology assessed using in vivo canine models. (Pubmed Central) -  Nov 27, 2020   
    The therapeutic concentration of lapatinib significantly increased total peripheral vascular resistance, QT, QTc, monophasic action potential (MAP) MAP, effective refractory period, and plasma concentration of cardiac troponin I (cTnI), suggesting that lapatinib prolonged the ventricular repolarization without inducing lethal ventricular arrhythmia. Careful monitoring of plasma cTnI concentration and an electrocardiogram could be supportive biomarkers, predicting the onset of lapatinib-induced cardiovascular adverse events.
  • ||||||||||  Herceptin (trastuzumab) / Roche, AUM302 / AUM Biosci
    Preclinical, Journal:  Preclinical evaluation of a novel triple-acting PIM/PI3K/mTOR inhibitor, IBL-302, in breast cancer. (Pubmed Central) -  Nov 22, 2020   
    The combination of trastuzumab and IBL-302 significantly increased the anti-proliferative effect in HER2+ breast cancer cell line, and matched trastuzumab-resistant line, relative to testing either drug alone. We thus believe that the novel PIM and PI3K/mTOR inhibitor, IBL-302, represents an exciting new potential treatment option for breast cancer, and that it should be considered for clinical investigation.
  • ||||||||||  Perjeta (pertuzumab) / Roche
    Clinical, Journal, HEOR:  A cost-effectiveness analysis of trastuzumab-containing treatment sequences for HER-2 positive metastatic breast cancer patients in Taiwan. (Pubmed Central) -  Nov 21, 2020   
    We thus believe that the novel PIM and PI3K/mTOR inhibitor, IBL-302, represents an exciting new potential treatment option for breast cancer, and that it should be considered for clinical investigation. From the perspective of the TNHIA, trastuzumab plus docetaxel as 1st line followed by T-DM1 and trastuzumab plus lapatinib as 2nd and 3rd line represents the most cost-effective strategy among the four sequences considered for treating HER-2-positive mBC patients.
  • ||||||||||  paclitaxel / Generic mfg.
    Journal:  Escalating and De-escalating Therapy for Early-Stage HER2-Positive Breast Cancer. (Pubmed Central) -  Nov 21, 2020   
    Higher clinical stage HER2+ disease is still treated aggressively, although intrinsic subtype or activated immune tumor microenvironment may identify those with augmented treatment response or better outcome. It is likely that future strategies to escalate and de-escalate treatment with less chemotherapy, fewer anti-HER2 drugs, or shorter duration will depend upon integrated clinical and genomic modeling.
  • ||||||||||  elsiglutide (ZP1846) / Zealand Pharma
    Preclinical, Journal:  The GLP-2 analogue elsiglutide reduces diarrhoea caused by the tyrosine kinase inhibitor lapatinib in rats. (Pubmed Central) -  Nov 19, 2020   
    This does not appear to be via reduction in inflammation or barrier permeability, and may be due to thickening of mucosa, leading to increased surface area for fluid absorption in the distal small intestine. Microbial changes seen in this study require further research to fully elucidate their role in the development of diarrhoea.
  • ||||||||||  paclitaxel / Generic mfg.
    Preclinical, Journal:  Assessment of modelling strategies for drug response prediction in cell lines and xenografts. (Pubmed Central) -  Nov 19, 2020   
    Furthermore, we assessed our ability to predict drug response in four xenograft cohorts (treated either with erlotinib, gemcitabine or paclitaxel) using models trained on cell line data. We could predict response in an erlotinib-treated cohort with a moderate accuracy (correlation ≈ 0.5), but were unable to correctly predict responses in cohorts treated with gemcitabine or paclitaxel.
  • ||||||||||  Preclinical, Journal:  Comparative anti-proliferative effects of potential HER2 inhibitors on a panel of breast cancer cell lines. (Pubmed Central) -  Nov 14, 2020   
    Besides, a good correlation was found between the calculated binding energies for each ligand@protein complex and the relative affinities observed in competition experiments. Our pharmacophore model resulted in a high potent ligand that shows high potency against HER2 positive breast cancer and relatively low toxicity towards the normal human cells.
  • ||||||||||  Journal:  Treatment Landscape and Prognosis After Treatment with Trastuzumab Emtansine. (Pubmed Central) -  Nov 14, 2020   
    P=N/A
    Purpose Pertuzumab and T-DM1 are two efficient anti-HER2 treatments for patients with HER2-positive advanced breast cancer...Following T-DM1, lapatinib, trastuzumab and chemotherapy were the main therapy choices...Conclusions Therapy options after T-DM1 in a real-world setting seem to exhibit a relevant clinical efficacy, supporting the concept of continuous anti-HER2 treatments in the advanced therapy setting for breast cancer patients. Novel therapies are needed to improve the rather short median progression-free survival.
  • ||||||||||  foretinib (GSK1363089) / Exelixis
    Journal:  Combination effect of lapatinib with foretinib in HER2 and MET co-activated experimental esophageal adenocarcinoma. (Pubmed Central) -  Nov 12, 2020   
    In the OE19 EAC cell line with mainly HER2 phosphorylation, and the ESO51 EAC cell line with mainly MET phosphorylation, profound cell growth inhibition with induction of apoptosis was observed in response to single agent with lack of enhanced growth inhibition when the two agents were combined. These data suggest that combination therapy with foretinib and lapatinib should be tested as a treatment option for HER2 positive patients with MET-overexpressing EAC, and could be a novel treatment strategy for specific EAC patients.
  • ||||||||||  Herceptin (trastuzumab) / Roche
    Clinical, Journal, Real-World Evidence:  Efficacy of lapatinib combined with capecitabine in patients with HER2-positive metastatic breast cancer in a real-world study. (Pubmed Central) -  Nov 11, 2020   
    A limited number of adverse events were observed with the combination of lapatinib and capecitabine. Therefore, the findings of the present study suggested that lapatinib-based treatment is effective in patients with HER2 MBC (even in trastuzumab-pretreated patients), and the combination of lapatinib with capecitabine may be recommended due to its good efficacy, convenience and tolerability.
  • ||||||||||  Enrollment open, Tumor mutational burden, PD(L)-1 Biomarker:  The Rome Trial From Histology to Target: the Road to Personalize Target Therapy and Immunotherapy (clinicaltrials.gov) -  Nov 9, 2020   
    P2,  N=384, Recruiting, 
    Our results suggest that the use of OID alone or in combination with tyrosine kinase inhibitors could be considered as adjuvants in the treatment of cancer. Not yet recruiting --> Recruiting
  • ||||||||||  lapatinib / Generic mfg., erlotinib / Generic mfg.
    Journal:  Targeting of HER/ErbB family proteins using broad spectrum Sec61 inhibitors coibamide A and apratoxin A. (Pubmed Central) -  Nov 6, 2020   
    Coibamide A potentiated the cytotoxic efficacy of small molecule kinase inhibitors lapatinib and erlotinib in breast and lung cancer cell types, respectively. These data indicate that natural product modulators of Sec61 function have value as chemical probes to interrogate HER/ErbB signaling in treatment-resistant human cancers.
  • ||||||||||  lapatinib / Generic mfg., erlotinib / Generic mfg.
    Journal:  Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors. (Pubmed Central) -  Oct 20, 2020   
    Through SAR analysis, we developed compound 5 (JCN037) from an anilinoquinazoline scaffold by ring fusion of the 6,7-dialkoxy groups to reduce the number of rotatable bonds and polar surface area and by introduction of an ortho-fluorine and meta-bromine on the aniline ring for improved potency and BBB penetration. Relative to the conventional EGFR TKIs erlotinib and lapatinib, JCN037 displayed potent activity against EGFR amplified/mutant patient-derived cell cultures, significant BBB penetration (2:1 brain-to-plasma ratio), and superior efficacy in an EGFR-driven orthotopic glioblastoma xenograft model.
  • ||||||||||  lapatinib / Generic mfg., cisplatin / Generic mfg.
    [VIRTUAL] Establishment and application of a series of genetically engineered mouse derived breast cancer homograft models () -  Oct 14, 2020 - Abstract #SITC2020SITC_1761;    
    Varying response to the cytotoxic treatments was observed among different models, with cisplatin producing robust response of TGI over 80% in all five of the tested models. Conclusions We have generated and characterized a series of mouse breast cancer homograft models from GEMMs to facilitate both mechanistic investigation and preclinical testing of novel therapeutics.
  • ||||||||||  lapatinib / Generic mfg., cisplatin / Generic mfg.
    [VIRTUAL] Establishment and application of a series of genetically engineered mouse derived breast cancer homograft models () -  Oct 14, 2020 - Abstract #SITC2020SITC_1026;    
    Varying response to the cytotoxic treatments was observed among different models, with cisplatin producing robust response of TGI over 80% in all five of the tested models. Conclusions We have generated and characterized a series of mouse breast cancer homograft models from GEMMs to facilitate both mechanistic investigation and preclinical testing of novel therapeutics.
  • ||||||||||  Herceptin (trastuzumab) / Roche
    Journal:  Pathway-Based Drug Response Prediction Using Similarity Identification in Gene Expression. (Pubmed Central) -  Oct 10, 2020   
    Moreover, machine learning models, built using multiple algorithms including logistic regression, naive Bayes, random forest, k-nearest neighbor, and support vector machine, for predicting drug response in the NeoALTTO clinical trial, resulted in lower performance compared to our pathway-based approach. Our results indicate that transcriptional similarity of biological pathways can be used to predict lapatinib and trastuzumab response in HER2+ breast cancer.
  • ||||||||||  Biomarker, Clinical Trial,Phase II, Journal:  Predictive Role of TP53, PIK3CA and MLL2 in ER+ HER2+ Breast Bancer: Biomarker Analysis of Neo-ALL-IN [NCT 01275859]. (Pubmed Central) -  Oct 8, 2020   
    Our results indicate that transcriptional similarity of biological pathways can be used to predict lapatinib and trastuzumab response in HER2+ breast cancer. Mutations in TP53 and PIK3CA hotspot at exon 9 may be potential negative predictors of ER+HER2+ BC treated with neoadjuvant letrozole and lapatinib, while MLL2 inactivating mutation might confer therapeutic benefit in these patients.
  • ||||||||||  pyrotinib (SHR-1258) / Jiangsu Hengrui Medicine, Herceptin (trastuzumab) / Roche
    [VIRTUAL] Efficacy and safety analysis of pyrotinib in lapatinib resistant HER2-positive metastatic breast cancer: A retrospective study (On-Demand e-Poster Display) -  Oct 8, 2020 - Abstract #ESMOAsia2020ESMO_Asia_1117;    
    Legal entity responsible for the study: The authors. Funding: National Key Research and Development Program of China (ZDZX2017ZL-01), High-level Innovation Team of Nanjing Medical University (JX102GSP201727), Wu Jieping Foundation (320.6750.17006), Key Medical Talents (ZDRCA2016023), 333 Project of Jiangsu Province (BRA2017534 and BRA2015470), The collaborative innovation center for tumor individualization focuses on open topics (JX21817902/008) and Project of China key research and development program precision medicine research (2016YFC0905901).
  • ||||||||||  pyrotinib (SHR-1258) / Jiangsu Hengrui Medicine, Herceptin (trastuzumab) / Roche
    [VIRTUAL] Efficacy and safety analysis of pyrotinib in lapatinib resistant HER2positive metastatic breast cancer: A retrospective study (On-Demand e-Poster Display) -  Oct 8, 2020 - Abstract #ESMOAsia2020ESMO_Asia_752;    
    For patients who benefited from lapatinib ≥ 6.0 months in 3 or later line therapy, pyrotinib could provide a clinically meaningful longer PFS. National Key Research and Development Program of China (ZDZX2017ZL-01), High-level Innovation Team of Nanjing Medical University (JX102GSP201727), Wu Jieping Foundation (320.6750.17006), Key Medical Talents (ZDRCA2016023), 333 Project of Jiangsu Province (BRA2017534 and BRA2015470), The collaborative innovation center for tumor individualization focuses on open topics (JX21817902/008) and Project of China key research and development program precision medicine research (2016YFC0905901).
  • ||||||||||  pyrotinib (SHR-1258) / Jiangsu Hengrui Medicine, Herceptin (trastuzumab) / Roche
    [VIRTUAL] Efficacy and safety analysis of pyrotinib in lapatinib resistant HER2positive metastatic breast cancer: A retrospective study (On-Demand e-Poster Display) -  Oct 8, 2020 - Abstract #ESMOAsia2020ESMO_Asia_377;    
    For patients who benefited from lapatinib ≥ 6.0 months in 3 or later line therapy, pyrotinib could provide a clinically meaningful longer PFS. National Key Research and Development Program of China (ZDZX2017ZL-01), High-level Innovation Team of Nanjing Medical University (JX102GSP201727), Wu Jieping Foundation (320.6750.17006), Key Medical Talents (ZDRCA2016023), 333 Project of Jiangsu Province (BRA2017534 and BRA2015470), The collaborative innovation center for tumor individualization focuses on open topics (JX21817902/008) and Project of China key research and development program precision medicine research (2016YFC0905901).
  • ||||||||||  Nerlynx (neratinib) / Puma, Knight Therap, Pierre Fabre
    Journal:  Neratinib: the emergence of a new player in the management of HER2+ breast cancer brain metastasis. (Pubmed Central) -  Oct 7, 2020   
    The randomized, Phase III, NALA trial compares neratinib plus capecitabine to a currently prevailing regimen of lapatinib plus capecitabine and is provided herein. Analysis of NALA portends meaningful changes on the horizon for the management of HER2+ metastatic breast cancer.
  • ||||||||||  lapatinib / Generic mfg.
    Biomarker, Journal:  Screening and Identification of Key Biomarkers in Acquired Lapatinib-Resistant Breast Cancer. (Pubmed Central) -  Oct 7, 2020   
    Meanwhile, the prediction model of lapatinib sensitivity was constructed, and emerging role of the model was further analyzed using several webtools. In conclusion, hub genes are involved in the complex mechanisms underlying ALR in breast cancer and provide favorable support for treatment of ALR in future.