lapatinib / Generic mfg. 
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  • ||||||||||  miransertib (MK-7075) / Merck (MSD), Gilotrif (afatinib) / Boehringer Ingelheim
    Journal:  The Combination of Afatinib With Dasatinib or Miransertib Results in Synergistic Growth Inhibition of Stomach Cancer Cells. (Pubmed Central) -  Mar 28, 2024   
    Of various human epidermal growth factor receptor (HER) inhibitors, only the anti-HER2 monoclonal antibody (mAb) Herceptin/trastuzumab and the antibody-drug conjugate trastuzumab deruxtecan (T-Dxd) has been approved for the treatment of patients with stomach cancer...Of various HER inhibitors, the irreversible pan-HER family inhibitors (e.g., afatinib) were more effective than the reversible dual epidermal growth factor receptor (EGFR)/HER2 tyrosine kinase inhibitor (TKI) lapatinib and the EGFR-specific TKI erlotinib in inhibiting the growth of HSCCLs. Of agents targeting different downstream cell signaling molecules, dasatinib targeting Ab1/Src/C-Kit, trametinib targeting MERK1/2 and miransertib targeting AKT1/2/3 inhibited growth of majority of HSCCLs, with the IC50 values ranging from 2 nM to 7
  • ||||||||||  Biomarker, Journal, Tumor microenvironment, IO biomarker:  DNA hypomethylation patterns and their impact on the tumor microenvironment in colorectal cancer. (Pubmed Central) -  Mar 23, 2024   
    This study unveils a novel epigenetic phenotype in CRC linked to resistance against immune checkpoint inhibitors, presenting a significant step toward personalized medicine by suggesting epigenetic classifications as a means to identify ideal candidates for immunotherapy in CRC. Our findings also highlight potential therapeutic agents for the DMP subtype, offering new avenues for tailored CRC treatment strategies.
  • ||||||||||  Sutent (sunitinib) / Pfizer
    Journal:  Pterostilbene Induces Apoptosis from Endoplasmic Reticulum Stress Synergistically with Anticancer Drugs That Deposit Iron in Mitochondria. (Pubmed Central) -  Mar 17, 2024   
    We have reported that pterostilbene (PTE), a plant stilbene, enhances the antitumor effect of low doses of sunitinib in gastric cancer cells accumulating mitochondrial iron (II) (mtFe) at low doses...For this study, we used 5-fluorouracil (5FU), cisplatin (CPPD), and lapatinib (LAP), which are frequently used in the treatment of GC, and doxorubicin (DOX), which is known to deposit mtFe...These findings would help in developing novel therapeutic strategies for GC. However, further clinical investigations are required.
  • ||||||||||  lapatinib / Generic mfg.
    Journal:  Synthesis, spectroscopic analysis, and computational-based investigations on 'azo-coumarin-Co(II)-galangin' hybrids exhibit multipotential activities. (Pubmed Central) -  Mar 15, 2024   
    Further, the MD-simulation (RMSD, RMSF, Rg, and H-bonds) of the most potential docking complex, 'HER2-6d', showed a minimum deviation similar to the standard drug (lapatinib) at 100?ns, indicating that 6d could be a potential noncovalent anticancer inhibitor...Among all six ligands, 6c and 6d were the two most multipotent therapeutic agents from the above analyses. In summary, this could be a feasible approach towards the utilization of phytochemicals in mainstream therapeutic applications, where bioinformatics tools help to select a lead drug candidate at an early stage and guide for higher experimental success by proceeding with potential candidates.Communicated by Ramaswamy H. Sarma.
  • ||||||||||  lapatinib / Generic mfg., tamoxifen / Generic mfg.
    Trial completion, Metastases:  LAPATAM: Lapatinib and Tamoxifen in Treating Patients With Advanced or Metastatic Breast Cancer (clinicaltrials.gov) -  Mar 12, 2024   
    P1,  N=20, Completed, 
    The safety profile of T-DXd continues to be manageable, with no long-term toxicity observed with longer F/U. Unknown status --> Completed
  • ||||||||||  lapatinib / Generic mfg.
    Journal:  Artemisia argyi extracts overcome lapatinib resistance via enhancing TMPRSS2 activation in HER2-positive breast cancer. (Pubmed Central) -  Mar 6, 2024   
    Our findings propose TMPRSS2 as a critical determinant in lapatinib sensitivity, and Artemisia argyi emerges as a potential agent to overcome lapatinib via activating TMPRSS2 in HER2-positive breast cancer. This study not only unravels the molecular mechanisms driving cell death in HER2-positive breast cancer cells induced by Artemisia argyi but also lays the groundwork for developing novel inhibitors to enhance therapy outcomes.
  • ||||||||||  Enrollment closed, Enrollment change, IO biomarker:  MULTISARC: Molecular Profiling of Advanced Soft-tissue Sarcomas (clinicaltrials.gov) -  Mar 5, 2024   
    P3,  N=603, Active, not recruiting, 
    This study not only unravels the molecular mechanisms driving cell death in HER2-positive breast cancer cells induced by Artemisia argyi but also lays the groundwork for developing novel inhibitors to enhance therapy outcomes. Recruiting --> Active, not recruiting | N=960 --> 603
  • ||||||||||  Applications of a novel fibrous extracellular matrix for advanced in vitro cancer models (Section 6) -  Mar 5, 2024 - Abstract #AACR2024AACR_9715;    
    The primary cells from human tumors formed cell clusters resembling the original tumor tissue's structure. In conclusion, the novel micro-fibrous scaffold, closely mimicking natural extracellular matrixes, promotes significant cell-to-cell and cell-to-matrix interactions, while also facilitating cell growth over extended periods providing a more physiologically relevant platform for evaluating drug responses for various cancer cell types, further showing the importance of 3D culture systems in cancer research.
  • ||||||||||  GMX1778 / Teva
    Orthogonal targeting of NAD metabolism and ErbB2/ErbB3 signaling in pancreatic adenocarcinoma (Section 26) -  Mar 5, 2024 - Abstract #AACR2024AACR_9279;    
    Furthermore, our data suggests combining chemical or biologic inhibitors of ErbB2/3 with an inhibitor of NAD synthesis may result in highly synergistic cytotoxic effects in PDAC cells and PDAC preclinical models. Such data could support the future development of a human PDAC clinical trial repurposing agents targeting NAD synthesis and ErbB2/3 that are already FDA-approved or currently in clinical testing.
  • ||||||||||  Clinical efficacy and safety of HER2 targeted therapy in patients with metastatic colorectal cancer: A systematic review and meta-analysis (Section 46) -  Mar 5, 2024 - Abstract #AACR2024AACR_5145;    
    Systematic review identified 9 study cohorts which were utilized in the meta-analysis, encompassing a total of 279 patients with mCRC who received Trastuzumab (T) in combination with either Pertuzumab (P), Tucatinib (Tu), Pyrotinib (Py), or Lapatinib (L). Overall, this comprehensive meta-analysis confirms that dual HER2 targeting therapies yield meaningful clinical efficacy, with favorable safety profiles, and improve outcomes in patients with RAS-WT HER2-positive mCRC.
  • ||||||||||  lapatinib / Generic mfg.
    Whole genome and targeted proteome analysis of single cancer cells (Section 42) -  Mar 5, 2024 - Abstract #AACR2024AACR_4931;    
    Our novel multiplex G&P technique is capable of generating multiparametric measurements linking DNA copy numbers and expression levels of selected genes of interest. The method is optimized for analysis of single cells from rare cell populations and is readily translatable to study circulating tumor cells (CTCs) and disseminated cancer cells (DCCs), enabling for the first time pathway analysis via phosphoprotein analyses of these cells.
  • ||||||||||  lapatinib / Generic mfg.
    Anticancer mechanisms of epigallocatechin gallate revealed via cellular and molecular profiling (Section 21) -  Mar 5, 2024 - Abstract #AACR2024AACR_2618;    
    This study provides a comprehensive examination of the differential impact of EGCG treatment on cancer cells. Subsequent research on the timing and duration of the changes, along with pathway enrichment analyses, will potentially guide the translational potential of EGCG and its chemical analogs in personalized cancer treatment approaches.
  • ||||||||||  Tasigna (nilotinib) / Novartis, Inhibikase
    Journal, IO biomarker:  Construction and Analysis of a Mitochondrial Metabolism-Related Prognostic Model for Breast Cancer to Evaluate Survival and Immunotherapy. (Pubmed Central) -  Mar 5, 2024   
    The drug sensitivity results unmasked that the LR group demonstrated higher sensitivity to Irinotecan, Nilotinib, and Oxaliplatin, while the HR group demonstrated higher sensitivity to Lapatinib. The development of MMRG characteristics provides a comprehensive understanding of mitochondrial metabolism in BC, aiding in the prediction of prognosis and tumor microenvironment, and offering promising therapeutic choices for BC patients with different MMRG risk scores.
  • ||||||||||  lapatinib / Generic mfg., paclitaxel / Generic mfg.
    Enrollment closed:  Dose Escalation of Lapatinib With Paclitaxel in Ovarian Cancer (clinicaltrials.gov) -  Mar 1, 2024   
    P1,  N=15, Active, not recruiting, 
    These results show the prospects of Raman microscopy in drug evaluation and presumably in drug discovery. Recruiting --> Active, not recruiting
  • ||||||||||  Votrient (pazopanib) / Novartis, BeiGene, Stivarga (regorafenib) / Bayer, Sutent (sunitinib) / Pfizer
    Journal, Adverse events:  Integrating network pharmacology and drug side-effect data to explore mechanism of liver injury-induced by tyrosine kinase inhibitors. (Pubmed Central) -  Feb 28, 2024   
    Based on the target prediction results of drugs and reactive metabolites, we also shed light on the association between toxic metabolites and severe hepatic adverse reactions, and thinking HSPA8, HSPA1A, CYP1A1, CYP1A2 and CYP3A4 were potential therapeutic or preventive targets against TKI-induced liver injury. In conclusion, our research provides comprehensive insights into the mechanism underlying severe liver injury caused by TKIs, offering a better understanding of how to enhance patient safety and treatment efficacy.
  • ||||||||||  Talzenna (talazoparib) / Pfizer, Gilotrif (afatinib) / Boehringer Ingelheim, Lynparza (olaparib) / Merck (MSD), AstraZeneca
    Multi-Gene Sequencing Reveals Actionable Mutations in Primary and Recurrent Phyllodes Tumours of the Breast (Exhibit Hall; Poster Board Number: 30) -  Feb 18, 2024 - Abstract #USCAP2024USCAP_1502;    
    Genomic profiling demonstrated presence of mutations which may be involved in PT recurrence and metastasis. Further studies are needed to ascertain if these could have potentially actionable roles as prognostic and predictive biomarkers.
  • ||||||||||  Enrollment change, Trial completion date, Trial primary completion date, Tumor mutational burden, Metastases:  MOST plus: Adapting Treatment to the Tumor Molecular Alterations for Patients With Advanced Solid Tumors: MyOwnSpecificTreatment (clinicaltrials.gov) -  Feb 15, 2024   
    P2,  N=900, Recruiting, 
    The L-JIMT breast cancer lung metastasis model developed may be useful in the evaluation of anti-cancer agents for multiresistant HER2-positive advanced breast cancer. N=560 --> 900 | Trial completion date: Oct 2026 --> Oct 2027 | Trial primary completion date: Jan 2025 --> Jan 2026
  • ||||||||||  zorifertinib (AZD3759) / Alpha Biopharma, AstraZeneca
    Journal, Gene Signature, IO biomarker:  A Six-gene Prognostic Model Based on Neutrophil Extracellular Traps (NETs)-related Gene Signature for Lung Adenocarcinoma. (Pubmed Central) -  Feb 15, 2024   
    N=560 --> 900 | Trial completion date: Oct 2026 --> Oct 2027 | Trial primary completion date: Jan 2025 --> Jan 2026 Altogether, this study has identified a novel NET-score signature based on six novel NET-related genes to predict the prognosis of LUAD and ABCC2 and has also explored a new method for personalized chemo-/immuno-therapy of LUAD.
  • ||||||||||  lapatinib / Generic mfg., letrozole / Generic mfg., fulvestrant / Generic mfg.
    Journal, Metastases:  Elderly Advanced Breast Cancer Effectively Treated with Locoregional Therapy-A Case Report (Pubmed Central) -  Feb 6, 2024   
    By changing the endocrine therapy to toremifene followed by fulvestrant, the therapy achieved a partial response...She was administered lapatinib as anti-HER2 therapy in addition to the endocrine therapy. Two years and 6 months after surgery, there has been no worsening of bone metastasis or appearance of visceral metastasis.
  • ||||||||||  Irene (pyrotinib) / Jiangsu Hengrui Pharma
    Journal:  Pyrotinib shows a potent antitumor effect on HER2-positive esophageal cancer cells by promoting HER2 proteasomal degradation. (Pubmed Central) -  Jan 31, 2024   
    In vitro and in vivo experiments further revealed that pyrotinib effectively suppresses cancer cell invasion and migration, as well as the growth of tumors in nude mice. Overall, our results suggest that pyrotinib is a superior TKI over lapatinib in inhibiting esophageal cancer cell proliferation and tumorigenic potential, and can be chosen as a neo-adjuvant for esophageal cancer treatment.
  • ||||||||||  Gilotrif (afatinib) / Boehringer Ingelheim
    Journal:  Facilitated Transport of EGFR Inhibitors Plays an Important Role in Their Cellular Uptake. (Pubmed Central) -  Jan 31, 2024   
    Leveraging this property, we apply hyperspectral stimulated Raman scattering imaging to directly visualize and quantify two Food and Drug Administration-approved EGFR inhibitor drugs (lapatinib and afatinib) inside living cells and the changes in their cellular uptake upon the addition of organic cation transporter inhibitors. These single-cell quantitative measurements provide new insight into the role of membrane transporters in the uptake of TKI drugs in living cells.
  • ||||||||||  lapatinib / Generic mfg., cisplatin / Generic mfg.
    Journal:  Mapping the Anti-Cancer Activity of ?-Connexin Carboxyl-Terminal (aCT1) Peptide in Resistant HER2+ Breast Cancer. (Pubmed Central) -  Jan 26, 2024   
    Findings from this study show a dynamic range of binding partners for aCT1, many of which regulate gene expression and RNA biology. nCounter analysis shows that a number of pathways are significantly impacted by aCT1, including upregulation of apoptotic factors, leading to the prediction and demonstration that aCT1 can boost the cell death effects of cisplatin and lapatinib in HER2+ breast cancer cells that have become resistant to HER2-targeted agents.
  • ||||||||||  Enhertu (fam-trastuzumab deruxtecan-nxki) / Daiichi Sankyo, AstraZeneca
    Trastuzumab deruxtecan versus treatment of physician () -  Jan 22, 2024 - Abstract #YIR2024YIR_125;    
    P3
    nCounter analysis shows that a number of pathways are significantly impacted by aCT1, including upregulation of apoptotic factors, leading to the prediction and demonstration that aCT1 can boost the cell death effects of cisplatin and lapatinib in HER2+ breast cancer cells that have become resistant to HER2-targeted agents. Background: In the single-arm, phase 2 DESTINY-Breast01 trial, trastuzumab deruxtecan showed robust activity in patients with HER2-positive metastatic breast cancer who were refractory or resistant to trastuzumab emtansine; a population with scarce effective treatments...Treatment of physician
  • ||||||||||  lapatinib / Generic mfg.
    Preclinical, Journal:  The effect of shikonin on the metabolism of lapatinib in vitro, and in vivo. (Pubmed Central) -  Jan 17, 2024   
    It could be successfully applied to the study of pharmacokinetic interaction of shikonin on the inhibition of lapatinib metabolism in vivo and in vitro. In the end, further studies are needed to determine if such interactions are indeed valid in humans and if the interaction is clinically relevant.