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DRUG:

lapatinib

i
Other names: GW572016, 572016, GW2016, GW572016F
Company:
Generic mfg.
Drug class:
EGFR inhibitor, HER2 inhibitor
Related drugs:
3d
Radiation therapy combined with tyrosine kinase inhibitors in 826 patients with HER2-positive breast cancer brain metastases: a systematic review and network meta-analysis. (PubMed, Neurosurg Rev)
Bayesian network meta-analysis (NMA) was conducted to integrate direct and indirect comparisons, addressing the lack of head-to-head trials. Eleven studies (2 RCTs, 9 retrospective; 826 patients) evaluated four treatment strategies: pyrotinib + RT, pyrotinib alone, RT alone, and lapatinib + RT. In contrast, lapatinib + RT appeared to offer limited benefit and a higher risk of SAEs. Further randomized controlled trials are needed to validate these findings.
Clinical • Retrospective data • Review • Journal
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive
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lapatinib • Irene (pyrotinib)
4d
Cost Variation and Affordability of Oral Targeted Cancer Therapy in India: Comparison of Branded and Janaushadhi Products. (PubMed, Cureus)
Percentage cost variation ranged from 8% (Bosutinib) to 14,774.74% (Midostaurin), with corresponding cost ratios up to 148.75...Absolute savings versus median branded costs ranged from ₹2,968 (Dasatinib) to ₹25,270 (Lapatinib), while percentage savings ranged from 58.89% (Dasatinib) to 91.32% (Imatinib)...However, limited PMBJP coverage restricts their overall benefit. Expanding Janaushadhi availability, improving price regulation, and encouraging rational prescribing are crucial to ensure equitable access to targeted cancer therapies in India.
Journal
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ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase) • CDK4 (Cyclin-dependent kinase 4)
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dasatinib • imatinib • lapatinib • midostaurin • bosutinib
10d
Downregulation of SLC12A5 in glioblastoma multiforme: a novel prognostic biomarker associated with brain edema and radiomic features. (PubMed, Naunyn Schmiedebergs Arch Pharmacol)
Drug sensitivity screening identified six small molecules (PD0325901, ERK-6604, paclitaxel, ribociclib, TAF1, and lapatinib) that targeted SLC12A5-related pathways. Crucially, multivariate Cox regression analysis confirmed that SLC12A5 was an independent prognostic factor (HR p = 0.04). This study established SLC12A5 as a novel biomarker for GBM, uniquely bridging molecular dysregulation, edema pathogenesis, and radiomics with implications for prognosis and targeted therapy.
Journal
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SERPINH1 (Serpin family H member 1) • LOX (Lysyl Oxidase) • MMP9 (Matrix metallopeptidase 9) • VSNL1 (Visinin Like 1) • TAF1 (TATA-Box Binding Protein Associated Factor 1)
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paclitaxel • lapatinib • Kisqali (ribociclib) • Gomekli (mirdametinib)
11d
Anti-HER2-targeted therapies: effects on human in vitro blood-brain barrier models. (PubMed, Front Drug Deliv)
Established therapies such as trastuzumab, pertuzumab, trastuzumab/pertuzumab, lapatinib and tucatinib are widely used and are selectively toxic to HER2-positive breast cancer cell line. In conclusion, we demonstrate different time- and concentration-dependent effects of anti-HER2-targeted therapies for the treatment of advanced HER2-positive breast cancer on the BBB in vitro. Further experiments are required to assess the clinical relevance of our results.
Preclinical • Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2) • CD34 (CD34 molecule) • CCL2 (Chemokine (C-C motif) ligand 2) • CLDN5 (Claudin 5) • OCLN (Occludin) • SLC2A1 (Solute Carrier Family 2 Member 1)
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HER-2 positive
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Herceptin (trastuzumab) • lapatinib • Perjeta (pertuzumab) • Tukysa (tucatinib)
15d
Efficacy and safety of pyrotinib-based regimens in patients with HER2-positive stage III/IV breast cancer: a real-world retrospective study in China. (PubMed, PeerJ)
A subgroups comparison found that significant differences were observed in patients who had not used lapatinib (P = 0.016), had a number of metastatic sites ≤ 2 (P = 0.011), were intolerant to trastuzumab (P = 0.004), and were on first-line pyrotinib treatment (P = 0.036), with these patients having median progression-free survival lengths of 13.0 months, 15.9 months, 23.5 months, and 23.5 months, respectively. In addition, a rare positive fecal occult blood profile (5.4%) was observed. Pyrotinib-based regimens have shown satisfactory clinical efficacy in HER2-positive stage III/IV BC patients, and pyrotinib is well tolerated with manageable adverse events.
Retrospective data • Journal • Real-world evidence
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive
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Herceptin (trastuzumab) • lapatinib • Irene (pyrotinib)
19d
Targeting HER2-Positive HCC1954 Breast Cancer Cells by Novel Thiazole-Dihydrobenzisoxazoles: In-Depth Design, Synthesis and Initial In Vitro Study. (PubMed, Oncol Res)
Among them, ATF-2 demonstrated antiproliferative activity comparable to HER2 inhibitor lapatinib and significantly suppressed HER2 expression and activity, epidermal growth factor receptor (EGFR) activity, and cyclin-dependent kinase 6 (CDK6) expression in HCC1954 breast cancer cells. These findings highlight ATF-2 as a promising dual HSP90-HER2 inhibitor with broader inhibitory effects on the HER2, EGFR, and CDK6 pathways.
Preclinical • Journal
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HER-2 (Human epidermal growth factor receptor 2) • CDK6 (Cyclin-dependent kinase 6) • HSP90AA1 (Heat Shock Protein 90 Alpha Family Class A Member 1Heat Shock Protein 90 Alpha Family Class A Member 1)
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HER-2 positive • HER-2 expression
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lapatinib
25d
An Updated Comprehensive Pharmacovigilance Study of Drug- Induced Breast Cancer Based on FDA Adverse Event Reporting System Data. (PubMed, Curr Med Chem)
Targeted therapies of lapatinib, fulvestrant, and endocrine agents (letrozole or ribociclib) show disproportionately high AE reporting odds ratios, necessitating vigilant monitoring. HER2-positive BC treatments (trastuzumab) and TNBC agents (sonidegib) exhibit distinct risk profiles, advocating for personalized risk-benefit assessments for BC patients.
Journal • Adverse events
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive
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Herceptin (trastuzumab) • lapatinib • Kisqali (ribociclib) • fulvestrant • letrozole • Odomzo (sonidegib)
26d
Lapatinib-Loaded ZIF‑8 Nanoparticles: A Multifunctional Drug Delivery System with Anticancer, Antibacterial, and Antioxidant Properties. (PubMed, ACS Omega)
Beyond its anticancer effects, the nanocarrier displayed broad-spectrum antibacterial activity (minimum bactericidal concentrations: 5 mg mL-1 for Staphylococcus aureus and 10 mg mL-1 for Escherichia coli) and moderate antioxidant capacity (DPPH IC50 = 666 μg mL-1). Collectively, these results position LAP@ZIF-8 as a versatile, pH-sensitive platform that combines selective anticancer efficacy with low toxicity to healthy cells alongside ancillary antibacterial and antioxidant properties suitable for multimodal therapy.
Journal
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive • HER-2 negative
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lapatinib
27d
Harnessing Ubiquitin-Proteasome System-Related Genes to Identify Subtypes of Bladder Cancer and Reveal Immune Landscape. (PubMed, Am J Mens Health)
Somatic mutations demonstrated that the mutation rate of Cluster B was higher than that of Cluster A. In addition, candidate drugs for two clusters of patients were predicted, with Lapatinib, Doramapimod, and SCH772984 may be potential drugs for Cluster A patients. Luminespib, Staurosporine, and Dasatinib may be more suitable for Cluster B patients. The study provides a reference for guiding the clinical treatment of BLCA patients.
Journal • IO biomarker
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BTLA (B And T Lymphocyte Associated)
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dasatinib • lapatinib • SCH772984 • luminespib (AUY922)
27d
HER2/CEP17 ratio is associated with pCR after HER2-directed neoadjuvant treatment in the phase III NeoALTTO trial. (PubMed, Breast)
In patients treated with HER2-based neoadjuvant therapy, quantitative analysis of the readily available pretreatment HER2/CEP17 ratio by FISH is predictive of pCR.
P3 data • Journal
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive • HER-2 overexpression • HER-2 amplification • HER-2 positive + HER-2 overexpression
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Herceptin (trastuzumab) • paclitaxel • lapatinib
2ms
Advancing liquid biopsy: whispering gallery mode laser detection of the HER2 cancer biomarker on extracellular vesicles. (PubMed, Lab Chip)
Tumors that express HER2 are susceptible to HER2-targeted therapies, which include inhibitory antibodies such as trastuzumab and pertuzumab, as well as small inhibitor molecules such as lapatinib and tucatinib. Moreover, our detection technology can discriminate between soluble HER2 and membrane-bound HER2, enabling precise identification of the latter. This advancement opens up the possibility of introducing HER2 detection as a highly accurate and quantitative liquid biopsy method for detecting HER2 in blood, in full-length forms, offering new avenues for non-invasive diagnostics, patients monitoring, and early prediction of therapy.
Journal • Liquid biopsy
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HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
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HER-2 expression
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Herceptin (trastuzumab) • lapatinib • Perjeta (pertuzumab) • Tukysa (tucatinib)