lapatinib / Generic mfg. 
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  • ||||||||||  Journal, PD(L)-1 Biomarker, IO biomarker:  Integrated analysis of (Pubmed Central) -  Oct 22, 2023   
    Taken together, the current study offers insights into the potential repositioning of LAP as a disease-modifying drug in PD. A new signature of hepatocyte NK cell marker genes possesses a powerful ability to predict prognosis and immunotherapeutic response in patients with hepatocellular carcinoma.
  • ||||||||||  lapatinib / Generic mfg.
    Journal:  The involvement of hepatic cytochrome P450s in the cytotoxicity of lapatinib. (Pubmed Central) -  Oct 3, 2023   
    We compared the cytotoxicity of lapatinib and its three metabolites in primary human hepatocytes, HepaRG cells, and HepG2 cells and demonstrate that N-dealkylated lapatinib is more toxic than the parent drug and the other metabolites. Taken together, our results indicate that lapatinib-induced cytotoxicity involves multiple mechanisms, such as apoptosis and DNA damage; that N-dealkylated lapatinib is a toxic metabolite contributing to the toxic effect of lapatinib; and that CYP3A5- and 3A7-mediated metabolism plays a role in attenuating the cytotoxicity of lapatinib.
  • ||||||||||  Trial completion date, Trial primary completion date, Tumor mutational burden:  The Rome Trial From Histology to Target: the Road to Personalize Target Therapy and Immunotherapy (clinicaltrials.gov) -  Oct 3, 2023   
    P2,  N=400, Active, not recruiting, 
    Taken together, our results indicate that lapatinib-induced cytotoxicity involves multiple mechanisms, such as apoptosis and DNA damage; that N-dealkylated lapatinib is a toxic metabolite contributing to the toxic effect of lapatinib; and that CYP3A5- and 3A7-mediated metabolism plays a role in attenuating the cytotoxicity of lapatinib. Trial completion date: Aug 2024 --> Jun 2025 | Trial primary completion date: Apr 2024 --> Dec 2024
  • ||||||||||  lapatinib / Generic mfg.
    Preclinical, Journal, Metastases:  A novel near-infrared EGFR targeting probe for metastatic lymph node imaging in preclinical mouse models. (Pubmed Central) -  Sep 26, 2023   
    Here, we report the synthesis, good biocompatibility, and in vivo evaluation of a new small molecule near-infrared (NIR) fluorescence probe by the conjugation of Lapatinib to S0456 (LP-S)...Scheme. Chemical synthesis and application of EGFR targeting probe LP-S for imaging of metastatic lymph nodes (mLNs) in OSCC.
  • ||||||||||  lapatinib / Generic mfg.
    Journal:  Lapatinib-induced PRIDE complex: a new kid on the block. (Pubmed Central) -  Sep 25, 2023   
    Chemical synthesis and application of EGFR targeting probe LP-S for imaging of metastatic lymph nodes (mLNs) in OSCC. No abstract available
  • ||||||||||  lapatinib / Generic mfg.
    Preclinical, Journal:  Rhizochalinin Exhibits Anticancer Activity and Synergizes with EGFR Inhibitors in Glioblastoma In Vitro Models. (Pubmed Central) -  Sep 21, 2023   
    Preliminary in vitro data generated using a parallel artificial membrane permeability (PAMPA) assay suggested that Rhiz cannot cross the blood brain barrier and therefore alternative drug delivery methods should be used in the further in vivo studies. In conclusion, Rhiz is a promising new candidate for the treatment of human glioblastoma, which should be further developed in combination with EGFR inhibitors.
  • ||||||||||  Kadcyla (ado-trastuzumab emtansine) / Roche
    Biomarker, Journal:  Potential Biomarkers Associated with Prognosis and Trastuzumab Response in HER2+ Breast Cancer. (Pubmed Central) -  Sep 9, 2023   
    We propose that vinculin and cortactin might contribute to Tz-sensibility/resistance in BC cells. Finally, we identify potential prognostic and predictive biomarkers that are promising for personalized BC management that would allow efficient patient selection in order to mitigate resistance and maximize the safety and efficacy of anti-HER2 therapies.
  • ||||||||||  Xalkori (crizotinib) / Pfizer, Zykadia (ceritinib) / Novartis, Fotivda (tivozanib) / Kyowa Kirin, Jazz, LG Chem
    Journal:  Comparative docking analysis of tyrosine kinase inhibitors with HER2 and HER4 receptors. (Pubmed Central) -  Sep 1, 2023   
    Lapatinib is identified as a potential inhibitor for both the RTKs. Our study thus suggests the probable direction that could be further explored in inhibiting EGFR protein harboring breast cancer.
  • ||||||||||  lapatinib / Generic mfg., everolimus / Generic mfg.
    Preclinical, Journal:  Proteomic Dynamics of Breast Cancer Cell Lines Identifies Potential Therapeutic Protein Targets. (Pubmed Central) -  Aug 28, 2023   
    In TNBC, metabolism pathways were dysregulated after EGFR/mTOR inhibitor treatment, while RNA modification and cell cycle pathways were affected by AKT inhibitor. This systematic multi-omics and in-depth analysis of the proteome of BC cells can help prioritize potential therapeutic targets and provides insights into adaptive resistance in TNBC.
  • ||||||||||  Safety and Efficacy of Stereotactic Radiosurgery with Concurrent Targeted Systemic Therapy for Brain Metastases (Hall B2; In Person Only; Screen: 11) -  Aug 22, 2023 - Abstract #ASTRO2023ASTRO_663;    
    Although heterogeneous, patients treated with SRS/SRT and ongoing CNS-active targeted systemic therapies have on average >6 month intracranial PFS and little evidence of significant toxicity. We observed <6% G2+ radiation necrosis for this cohort, and no particular class of agent was associated with a significantly higher rate of G2+ radiation necrosis.
  • ||||||||||  Votrient (pazopanib) / Novartis, BeiGene, vatalanib (PTK787) / Novartis, Bayer
    Journal, Machine learning:  Machine learning model for anti-cancer drug combinations: Analysis, prediction, and validation. (Pubmed Central) -  Aug 21, 2023   
    Furthermore, we incorporated molecular features to identify potential biomarkers for synergistic drug pairs, and almost all potential biomarkers found connections between drug targets and corresponding molecular features using protein-protein interaction network. Overall, this study provides valuable insights to complement and guide rational efforts to develop drug combination treatments.
  • ||||||||||  mirdametinib (PD-0325901) / SpringWorks Therap, BeiGene, Mekinist (trametinib) / Novartis, BeiGene
    Journal, Tumor mutational burden, IO biomarker, Pan tumor:  Pan-cancer and single-cell analysis reveal the prognostic value and immune response of NQO1. (Pubmed Central) -  Aug 16, 2023   
    NQO1 expression was significantly associated with prognosis, immune infiltrates, and drug resistance in multiple cancer types. The inhibition of the NQO1-dependent signaling pathways may provide a promising strategy for developing new cancer-targeted therapies.
  • ||||||||||  lapatinib / Generic mfg.
    Enrollment change, Trial completion date, Trial withdrawal, Trial primary completion date:  INST 0514C- Biologic Correlative Study: Trial of GW572016 in HER2 Overexpressing Breast Cancer Patients (clinicaltrials.gov) -  Aug 14, 2023   
    P2,  N=0, Withdrawn, 
    These findings reveal regulation of viral replication, inflammation, and tissue injury via ErbBs and establish a proof-of-principle for a repurposed, ErbB-targeted approach to combat emerging viruses. N=55 --> 0 | Trial completion date: Oct 2009 --> Jul 2023 | Completed --> Withdrawn | Trial primary completion date: Oct 2009 --> Jul 2023
  • ||||||||||  lapatinib / Generic mfg., tamoxifen / Generic mfg., fulvestrant / Generic mfg.
    Journal:  Resistance to hormone therapy in breast cancer cells promotes autophagy and EGFR signaling pathway. (Pubmed Central) -  Aug 14, 2023   
    In the current study, we have developed MCF-7 cell lines resistant to Fulvestrant (MCF-7Fulv) and Tamoxifen (MCF-7Tam) aiming at investigating mechanisms underlying resistance...Tyrosine kinase inhibitors tested against resistant MCF-7Fulv and MCF-7Tam cells, showed moderate efficacy to inhibit cell proliferation except for lapatinib, which concomitantly inhibits both EGFR and HER2 receptors, and strongly reduced cell proliferation...The increased autophagy in resistant cells is not associated with increased apoptosis suggesting a cytoprotective role for autophagy that may favor cells' survival and aggressiveness. Thus, by exploiting those underlying mechanisms, new targets could be established to overcome endocrine resistance.
  • ||||||||||  Tarlox (tarloxotinib bromide) / Molecular Templates, Proacta, Rain Oncology, Signpath Pharma
    Application and mechanism of tarloxotinib in HER2-positive breast cancer () -  Jul 27, 2023 - Abstract #ESMO2023ESMO_1685;    
    Conclusions Tarloxotinib released Tarloxotinib-E under hypoxic microenvironment of breast tumors, and inhibited the phosphorylation of HER2 dimers and downstream pathways to induce apoptosis in HER2-positive cells through a ROS-dependent manner. This lays a foundation for the further development of Tarloxotinib in HER2-positive breast cancer.
  • ||||||||||  Tagrisso (osimertinib) / AstraZeneca
    Journal:  Synthesis, and biological evaluation of EGFR/HER2-NAMPT conjugates for tumor treatment. (Pubmed Central) -  Jul 23, 2023   
    In Osimertinib-resistant cells (NCI-1975 cells with the L858R/T790M/C797S triple mutation and Ba/F3 cells with the Del19/T790M/C797S triple mutation), the anti-proliferative activity of compound 20c was increased by more than twofold compared with Osimertinib, so as to obtain better curative effect. This strategy is a promising method of embedding multiple pharmacophores into a single molecule, which lays a good foundation for the design and synthesis of small molecule drug conjugates with strong targeting ability and high cytotoxicity.
  • ||||||||||  lapatinib / Generic mfg., temozolomide / Generic mfg.
    Trial completion date, Trial primary completion date, Combination therapy:  Lapatinib With Temozolomide and Regional Radiation Therapy for Patients With Newly-Diagnosed Glioblastoma Multiforme (clinicaltrials.gov) -  Jul 12, 2023   
    P2,  N=50, Active, not recruiting, 
    Moreover, an exceptionally strong synergistic interaction was discovered between kinase targeting and apoptosis induction which is suitable for further clinical evaluation as multi-targeted combination therapy. Trial completion date: Jun 2024 --> Jun 2025 | Trial primary completion date: Jun 2023 --> Jun 2024
  • ||||||||||  lapatinib / Generic mfg.
    Journal:  ErbBs in Lens Cell Fibrosis and Secondary Cataract. (Pubmed Central) -  Jul 11, 2023   
    Short-term exposure to lower doses of lapatinib is also capable of eliciting a durable response when combined with suboptimal levels of a mechanistically distinct multikinase inhibitor. Our findings support ErbB1 as a therapeutic target for fibrotic PCO, which could be leveraged to pharmaceutically preserve the vision of millions of patients with cataracts.