lapatinib / Generic mfg. - LARVOL DELTA

Efficacy and safety of lapatinib in comparison with trastuzumab therapy for HER2-positive advanced and metastatic breast cancer (ESMO Asia 2025) - "This meta-analysis indicates that Trastuzumab remains superior to Lapatinib in terms of OS and PFS for patients with advanced and metastatic HER2-positive breast cancer. Although Lapatinib shows a comparable safety profile with no significant increase in severe adverse events, its efficacy is inferior to Trastuzumab. These findings support the continued use of Trastuzumab as the preferred first-line therapy in this setting."

Clinical • Metastases • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • HER-2

Efficacy and safety of trastuzumab deruxtecan (T-DXd) in HER2-positive (HER2+) advanced breast cancer (ABC) with CNS progression after local treatment: Real-world data (ESMO Asia 2025) - "Median lines of previous treatment in ABC was four (1-8), 47 (84%) pts have received pertuzumab, T-DM1 – 45 (80%) pts, lapatinib – 22 (39%) pts; all 3 anti-HER2 Rx received 15 (27%)pts. T-DXd is effective even in pts with CNS progression previously treated with radiation therapy. No new safety signals were recorded."

Clinical • Metastases • Real-world • Real-world evidence • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • HER-2

Real-world evaluation of a trastuzumab emtansine biosimilar in metastatic HER2-positive breast cancer: A single-centre retrospective analysis from India (ESMO Asia 2025) - "All patients had prior trastuzumab exposure; many were heavily pretreated (taxanes 84.3%, anthracyclines 62.7%, pertuzumab 19.6%, lapatinib 39.2%). This analysis supports the trastuzumab emtansine biosimilar as an effective, well-tolerated option for metastatic HER2-positive breast cancer, demonstrating a meaningful ORR and manageable toxicity profile, with PFS broadly consistent across subgroups. Confirmation in larger studies is warranted."

HEOR • Metastases • Real-world • Real-world evidence • Retrospective data • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • ER • HER-2 • PGR

MULTISARC: Molecular Profiling of Advanced Soft-tissue Sarcomas (clinicaltrials.gov) - P3 | N=603 | Active, not recruiting | Sponsor: Institut National de la Santé Et de la Recherche Médicale, France | Trial completion date: Oct 2025 ➔ Jan 2026

IO biomarker • Trial completion date • Oncology • Sarcoma • Soft Tissue Sarcoma • Solid Tumor

Simultaneous targeting of multiple etiological using a nanosized strategy for psoriasis management. (PubMed, Mater Today Bio) - "In this study, we developed a bilirubin-conjugated hyaluronic acid-assembled, lapatinib/rosiglitazone-coloaded nanoparticle (LR@HBn) to target both peroxisome proliferator-activated receptor γ (PPARγ) and epidermal growth factor receptor (EGFR) as well as intervene nuclear factor kappa B (NF-κB) signaling to effectively alleviate the progression of psoriasis by suppressing inflammatory microenvironment, preventing abnormal cellular growth, scavenging reactive oxygen species (ROS), and inhibiting interleukin-17A secretion. In vitro and in vivo experiments revealed excellent antioxidative, anti-inflammatory, anti-proliferative features and safety of LR@HBn, with resultant attenuation of psoriatic disease progression and suppression of recurrence. Taken collectively, these results point to LR@HBn as a promising and advanced strategy for treating psoriasis by administering topically."

Journal • Dermatology • Immunology • Inflammation • Psoriasis • EGFR • IL17A • PPARG

Construction of a survival prognosis model for epithelial-mesenchymal transition-related genes in gastric cancer. (PubMed, Eur J Med Res) - "Our study provides a prognostic assessment tool for GC based on EMT-related genes and offers novel insights into understanding the roles of EMT in GC progression and treatment resistance. These findings may aid in the development of precision therapy strategies for GC."

Journal • Gastric Cancer • Oncology • Solid Tumor • NPR3 • OLFML2B

Novel benzoxazole-based hybrids as multi-target inhibitors of aromatase, EGFR, and PI3K with potential anti-breast cancer activity. (PubMed, Bioorg Med Chem) - "MTT assay showed that 6 and 9b were 4.5 and 2 times more potent than doxorubicin against MCF-7 cells, while 9a and 13b were 10 and 7.5 times more effective against MDA-MB-231 cells, respectively...Compound 13b exhibited comparable EGFRL858R inhibition to lapatinib and outperformed pictilisib against PI3Kα, PI3Kβ, and PI3Kδ. Compound 6 showed greater ARO inhibition than letrozole, while being slightly less potent than pictilisib against PI3Kα and PI3Kβ...Docking studies supported the in vitro enzymatic inhibition assays results. Thus, 9b and 13d are potent anti-breast cancer benzoxazoles with selective ARO and PI3kα inhibition activity, respectively, while 6, 9a, and 13b are multi-target inhibitors exhibiting other anticancer synergistic mechanisms."

Journal • Breast Cancer • Oncology • Solid Tumor • ANXA5 • BECN1 • CASP9 • EGFR • PIK3CA • PIK3CB • PIK3CD

Efficacy of cross-line therapy with anti-HER2 TKI in HER2-positive MBC: a multicenter real-world study (SABCS 2025) - "Importantly, patients who switched from lapatinib to pyrotinib had a significantly longer PFS2 compared to those who continued pyrotinib in the second-line setting (mPFS: 7.0 vs. 4.1 months, HR 0.523, 95%CI 0.298 - 0.917, P < 0.001). This study indicated that cross-line anti-HER2 TKI therapy confers sustained PFS benefits in HER2-positive MBC. Notably, patients with longer frontline PFS and those who switched TKI agents exhibited superior survival outcomes in subsequent treatment lines. Further prospective studies are warranted to confirm these findings."

Clinical • Real-world • Real-world evidence • Breast Cancer • HER2 Positive Breast Cancer

Adjuvant aromatase inhibitor or tamoxifen in patients with hormone receptor-positive/HER2-positive early breast cancer: An exploratory analysis from the ALTTO (BIG 2-06) trial (SABCS 2025) - "The present analysis investigated the efficacy of different types of ET in pts with centrally tested HR+/HER2+ EBC treated with modern chemotherapy (CT) and trastuzumab (T)-based regimens at 10-year follow-up.Patients and ALTTO (BIG 2-06) is an international phase 3 trial in pts with HER2+ EBC randomized to 4 adjuvant anti-HER2 treatments with CT: T alone, lapatinib (L) alone, their sequence (T->L) or their combination (T+L). In this large 10-year follow-up analysis of pts with centrally tested HR+/HER2+ EBC treated with modern CT+anti-HER2-based therapy in the ALTTO trial, the use of AI was associated with significantly improved DFS and TTDR without differences in OS. The DFS benefit of AI was observed in both premenopausal and postmenopausal pts. These data may help optimizing adjuvant ET choices in pts with HR+/HER2+ EBC and shed light on the need of designing ad hoc clinical trials in this setting."

Clinical • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • HER-2

Cytotoxic Effects of Sorafenib, Lapatinib, and Bevacizumab, Alone and in Combination, on Medullary Thyroid Carcinoma Cells. (PubMed, Curr Oncol) - "The Lapatinib-Bevacizumab combination produced the most potent inhibition of cell viability, comparable to high-dose monotherapy. These findings suggest that combining kinase inhibitors with Bevacizumab may enhance antitumor activity, allow the use of lower drug doses, and overcome resistance, representing a promising therapeutic strategy for medullary thyroid carcinoma that warrants further investigation in clinical settings."

Journal • Neuroendocrine Tumor • Oncology • Solid Tumor • Thyroid Gland Carcinoma • Thyroid Gland Medullary Carcinoma • RET

Computational profiling of flavonoids against key breast cancer targets: an in-silico exploration. (PubMed, In Silico Pharmacol) - "Comparative docking with five reference drugs (Alpelisib, Buparlisib, Lapatinib, Gefitinib, and Afatinib) identified nine flavonoids; Sphaerobioside, Avicularin, Nicotiflorin, Myricetin, Quercitrin, Rutin, Isoquercetin, Didymin, and Robinin as promising candidates with favorable binding affinities and stable receptor interactions...Collectively, these findings highlight the multitarget inhibitory potential of selected flavonoids and demonstrate how integrated computational profiling can accelerate the discovery and optimization of natural product-based anticancer agents. The online version contains supplementary material available at 10.1007/s40203-025-00489-0."

Journal • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • EGFR • HER-2

Evaluation of lapatinib ditosylate nanoparticles for enhanced dissolution rate, oral bioavailability and effective oral carcinoma treatment. (PubMed, Pharm Dev Technol) - "LDNP showed complete remission of xenografted oral cancer in a C57BL/6 mouse model after seven doses of 100 mg/kg LDNP. The LDNP formulation can be developed to enhance the oral bioavailability of LD for effective oral cancer treatment."

Journal • Head and Neck Cancer • Oncology • Oral Cancer • Solid Tumor

Keratin 80 serves as a potential biomarker in metastatic breast cancer. (PubMed, Discov Oncol) - "Collectively, KRT80 may be linked with metastasis of BC, and it may serve as a potential therapeutic target for mBC treatment."

Biomarker • Journal • Breast Cancer • Oncology • Solid Tumor • CD8 • KRT80

Combination of iron chelator deferoxamine and ABCG2 transporter inhibitor lapatinib for therapeutic enhancement of 5-aminolevulinic acid. (PubMed, Photochem Photobiol) - "Not just increasing ALA-PpIX levels, Lap enhanced PpIX localization in the mitochondria and promoted mitochondria-mediated apoptosis after PDT in the H4 cell line with strong ABCG2 activities. Our results demonstrate that blocking ABCG2-mediated PpIX efflux is critical for the enhancement of ALA and, in tumor cells with ABCG2 activities, inhibiting PpIX bioconversion by DFO needs to be combined with PpIX efflux suppression for effective enhancement of ALA."

Journal • Brain Cancer • Glioblastoma • Oncology • Solid Tumor • ABCG2

DS-8201a in Pre-treated HER2 Breast Cancer That Cannot be Surgically Removed or Has Spread [DESTINY-Breast02] (clinicaltrials.gov) - P3 | N=608 | Active, not recruiting | Sponsor: Daiichi Sankyo | Trial completion date: Jul 2025 ➔ Jan 2026

Trial completion date • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • HER-2

Disrupting DDB2-DNA Interaction by Lapatinib Enhances Chemotherapy Sensitivity. (PubMed, Int J Biol Sci) - "Co-treatment with lapatinib and doxorubicin exhibited synergistic cytotoxicity in both cancer cell lines and patient-derived organoids. These findings reveal a previously unrecognized role for lapatinib in targeting DNA repair machinery, supporting its repurposing as a chemosensitizing agent. Our study highlights DDB2 as a critical mediator of chemoresistance and proposes disruption of DDB2-dependent DNA repair as a novel strategy for chemosensitization."

Journal • Biliary Cancer • Cholangiocarcinoma • Lung Cancer • Oncology • Solid Tumor • DDB2

Drug Repurposing in a Zebrafish AML Model (ASH 2023) - "In comparison, treatment with decitabine resulted in a decrease in the number of lyz expressing cells in both the MA9/lyz-EGFP and the control embryos. Treatment with doxorubicin, zoledronic and arsenic trioxide did not have an effect on the number of lyz-expressing population in the transgenic nor in the control embryos. These results were confirmed by qPCR, which showed that expression of lyz was reduced by 33% to 51% in the erlotinib, lapatinib, cytarabine, and gefitinib treated MA9 transgenic embryos (Figure 2)...Our results provide strong evidence for the successful establishment of a zebrafish model of KMT2A-rearranged AML that can be used for low to medium-throughput drug screening by employing the expression level of an endogenous gene (lyz) as a read-out. This model is a valuable tool to assess the drug's specificity in targeting oncogene-expressing cells and normal hematopoietic cells and, therefore, to identify novel therapeutic agents that can target the..."

Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Oncology • KMT2A • KRAS • LYZ • MLLT3 • RUNX1 • TP53

Deciphering the Role of KIF18A in Osteosarcoma Progression: An Integrative Analysis and Experimental Validation. (PubMed, Front Biosci (Landmark Ed)) - "This study reveals that KIF18A is upregulated in OS, particularly in metastatic cases, and is linked to poor clinical outcomes. Functional experiments confirm that KIF18A promotes proliferation, migration, and invasion of OS cells while suppressing apoptosis. In vivo experiments reveal that KIF18A knockdown strongly inhibits tumor growth. KIF18A expression correlates with dysregulation of key oncogenic pathways, an immunosuppressive microenvironment, and potential immunotherapy resistance. These results highlight KIF18A's role as a pivotal oncogene in OS progression and suggest its promise as both a prognostic biomarker and a therapeutic target."

IO biomarker • Journal • Oncology • Osteosarcoma • Sarcoma • Solid Tumor • KIF18A

Targeted colon cancer therapy using lapatinib-encapsulated chitosan nanoparticles conjugated with lactoferrin and melatonin with integrated in silico in vitro and in vivo evaluation. (PubMed, J Drug Target) - "Pharmacokinetic studies in Wistar rats showed a longer half-life (9.69 vs. 5.28 h), higher AUC0-∞ (452.880 vs. 159.715 µg/mL·h), and improved MRT (15.260 vs. 7.696 h). Focused colon retention (8.20 ± 1.38 µg/g), minimal toxicity, and confirmed safety and stability underscore its potential as an accurate, efficient treatment for colon cancer."

Journal • Preclinical • Colon Cancer • Colorectal Cancer • Oncology • Solid Tumor • EGFR • MAPK14

Drug-Induced Senescence in Liver Cells Promotes M2 Macrophage Polarization: Implications for Tyrosine Kinase Inhibitor-Associated Hepatotoxicity. (PubMed, J Vis Exp) - "Lapatinib and neratinib are tyrosine kinase inhibitors (TKIs) approved for treating HER2-positive metastatic breast cancer, but their clinical use is limited by hepatotoxicity. This underscores the importance of targeting senescent cells or SASP factors to reduce liver toxicity and improve treatment outcomes, making the identification of effective senotherapeutics a vital research focus. There hasn't been any literature report demonstrating the effect of TKI-induced liver cell secretome on macrophage polarization."

Journal • Breast Cancer • Fibrosis • HER2 Breast Cancer • HER2 Positive Breast Cancer • Immunology • Metabolic Disorders • Oncology • Solid Tumor • HER-2

Integrating deep generative model with active learning for predicting immunotherapy responses in gastric cancer. (PubMed, Comput Methods Programs Biomed) - "The proposed framework effectively addresses data insufficiency in ICT response prediction and demonstrates high accuracy in identifying GC patients likely to benefit from immunotherapy. The identified key genes and candidate compounds provide mechanistic insights and potential strategies for combinatorial therapies. This approach could enhance the accuracy of ICT response predictions and reveal novel insights for potential therapeutic interventions."

IO biomarker • Journal • Gastric Cancer • Oncology • Solid Tumor

Lower Incidence of Pancreatic Cancer in Patients on HER2-Targeted Therapy: Potential Implications in Pancreatic Cancer Prevention (ACG 2025) - "Cohort 1 comprised patients who received HER2-targeted agents (trastuzumab, pertuzumab, margetuximab, neratinib, lapatinib, tucatinib, trastuzumab deruxtecan); Cohort 2 included patients with a cancer diagnosis but no exposure to HER2-targeted agents. After matching, 54,338 patients were included in each cohort. The incidence of PC was lower in the HER2-targeted group compared to the control group (276 vs. 329)."

Clinical • Addiction (Opioid and Alcohol) • Bladder Cancer • Diabetes • Gastric Cancer • Genetic Disorders • Hepatology • HER2 Positive Breast Cancer • Metabolic Disorders • Nicotine Addiction • Non Small Cell Lung Cancer • Obesity • Oncology • Ovarian Cancer • Pancreatic Cancer • Pancreatitis • Solid Tumor

Multi-omic analysis reveals elevated BRI3BP expression associated with hepatocellular carcinoma progression and poor prognosis. (PubMed, Sci Rep) - "Drug sensitivity assays confirmed lower lapatinib IC50 in overexpression models. High BRI3BP expression correlates with aggressive HCC phenotypes, poorer survival, and dysregulated oncogenic pathways, supporting its role as a prognostic biomarker and candidate therapeutic target."

Biomarker • Journal • Hepatocellular Cancer • Oncology • Solid Tumor • CD68 • CD8

Design, Synthesis, and Evaluation of a Novel 99mTc-Labeled Small Molecule Inhibitor (Lapatinib)-Based SPECT Tracer Targeting HER2. (PubMed, J Med Chem) - "SPECT images of [99mTc]Tc-Lapa-HYNIC-TPPTS in HER2-positive model mice revealed that it can effectively locate tumors. This study is the first attempt at a 99mTc-labeled small-molecule inhibitor tracer targeting HER2, showing great potential for applications in the diagnosis of HER2-positive cancers."

Journal • Oncology • HER-2

Retrospective database analysis to assess treatment patterns, clinical outcomes, and healthcare resource utilization in metastatic or recurrent HER2-positive breast cancer in Alberta. (PubMed, Cancer Treat Res Commun) - "Uptake of guideline-recommended regimens in each line of therapy was lower in recurrent patients although survival was similar to de novo patients. These findings highlight the need for consensus on treatment regimens for de novo and recurrent HER2+ patients, effective first-and second-line management, and novel therapies to improve outcomes. MICROABSTRACT Our study evaluated real-world treatment patterns, clinical outcomes, and healthcare utilization in HER2-positive metastatic breast cancer (mBC) in Alberta, Canada. Among 758 patients, survival was similar between new diagnoses and recurrent cases, despite lower uptake of guideline-recommended therapies in recurrent patients. Our findings highlight the need for consensus on treatment strategies and novel therapies to improve mBC outcomes."

Clinical data • HEOR • Journal • Retrospective data • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • HER-2