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DRUG:

lapatinib

i
Other names: GW572016, 572016, GW2016, GW572016F
Company:
Generic mfg.
Drug class:
EGFR inhibitor, HER2 inhibitor
Related drugs:
10d
Final Efficacy and Safety Results of Pyrotinib Combined With Trastuzumab and Chemotherapy in Pre-Treated Human Epidermal Growth Factor Receptor 2-Positive Metastatic Breast Cancer. (PubMed, Cancer Med)
Updated analyses pertaining to PFS and safety were generally aligned with data obtained from initial assessments. The OS outcomes further substantiated that the combination of pyrotinib, trastuzumab, and chemotherapy is an alternative therapeutic regimen for managing HER2-positive MBC with heavy pre-treatment in certain situations, particularly among those with non-visceral metastases.
Journal
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive • EGFR positive
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Herceptin (trastuzumab) • lapatinib • Perjeta (pertuzumab) • Irene (pyrotinib)
17d
PRKAR1B as an oncogenic biomarker for diagnostic and prognostic stratification of tumor immunity, proliferation, and migration in head and neck squamous cell carcinoma. (PubMed, Front Immunol)
Drug sensitivity analysis further suggested that Lapatinib and Erlotinib may be beneficial in HNSC patients with high PRKAR1B expression. Lastly, PRKAR1B protein expression was upregulated in clinical HNSC samples. Overall, this study thoroughly examined PRKAR1B expression and its prognostic significance in HNSC, investigated related molecular pathways and immune cell interactions, and validated its role via in vitro experiments.
Journal • IO biomarker
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PRKAR1A (Protein Kinase CAMP-Dependent Type I Regulatory Subunit Alpha)
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erlotinib • lapatinib
20d
Screening and Docking Molecular Studies of Natural Products Targeting overexpressed Receptors HER-2 in Breast Cancer. (PubMed, Arch Razi Inst)
Lapatinib (chemical compound) and quercetin (natural compound) have DeltaG of -7.58 kcal/mol and -7.28 kcal/mol, respectively, form a hydrogen bond with the same residue in the hydrophobic region. All the natural molecules seem very promising and, after in vitro/in vivo tests, could constitute good substitutes for the chemotherapies which are currently used to treat breast cancers as well as other cancers.
Journal
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2)
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lapatinib
20d
Identification and functional exploration of hub genes related to energy metabolism in acute myeloid leukemia. (PubMed, Hematology)
Consequently, lapatinib, gentamicin, etc., were predicted based on the hub genes, and we found that CDH1 was positively correlated with multiple cells, such as NK cells and T cells, and there was the highest positive correlation between CDH1 and NK cells. Correlation of CDH1 with NK cells is discussed. These hub genes offer promising targets for future individualized AML therapy.
Journal
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CDH1 (Cadherin 1) • CD44 (CD44 Molecule) • GPC3 (Glypican 3) • AGRN (Agrin) • COL4A1 (Collagen Type IV Alpha 1 Chain)
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lapatinib
20d
Cost-effectiveness analysis of tucatinib plus trastuzumab versus pertuzumab plus trastuzumab for chemotherapy-refractory, HER2-positive, RAS wild-type unresectable or metastatic colorectal cancer. (PubMed, Expert Rev Pharmacoecon Outcomes Res)
Tucatinib plus trastuzumab was cost-effective if its price was the same as lapatinib for chemotherapy-refractory, HER2-positive, RAS wild-type unresectable or metastatic CRC from the perspective of healthcare payers in China. Our exploratory result could provide a reference for clinical application of tucatinib plus trastuzumab when they are correctly interpreted.
Journal • HEOR • Cost-effectiveness
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive • RAS wild-type • RAS wild-type + HER-2 positive • HER-2 positive + RAS wild-type
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Herceptin (trastuzumab) • lapatinib • Perjeta (pertuzumab) • Tukysa (tucatinib)
24d
Benchmarking the Ligand-HER2 Interactions Using Machine Learning and Molecular Dynamics Simulations. (PubMed, ACS Omega)
Lig233 also exhibits a binding free energy of -47 kcal/mol, two times as large as that of -21 kcal/mol for the known drug lapatinib. The fresh understanding achieved in the present study can lead to the necessary adjustments in the experimental development of HER2 inhibitors.
Journal
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HER-2 (Human epidermal growth factor receptor 2)
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lapatinib
26d
EGFR/KIT-linked proliferative bias in normal breast lobules from matched non-Hispanic Black and White women is rapidly reversible by RTK inhibition. (PubMed, Am J Pathol)
Functional plausibility was assessed in pre-stasis human mammary epithelial cells (HMECs) exposed for 24 h to clinically relevant EGFR (lapatinib) or KIT (ripretinib) inhibitors. Together, matched normal tissue and primary-cell data indicate a coordinated EGFR/KIT-linked proliferative bias in NHBW epithelium that is rapidly reversible in vitro. These findings motivate composition-aware validation in larger normal-tissue cohorts and pharmacodynamic window studies to test whether short-term RTK modulation can reset proliferation-biased states in at-risk breast epithelium.
Journal
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EGFR (Epidermal growth factor receptor) • CDK4 (Cyclin-dependent kinase 4)
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lapatinib • Qinlock (ripretinib)
26d
Trial completion
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive • HER-2 expression
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lapatinib • Kadcyla (ado-trastuzumab emtansine) • Enhertu (fam-trastuzumab deruxtecan-nxki) • capecitabine
27d
Enhanced Payload Release Enables Disitamab Vedotin to Surpass Trastuzumab Emtansine and Retain Efficacy in Acquired Resistance to Clinical Anti-HER2 Therapies. (PubMed, Pharmaceutics)
Notably, RC48 retained strong activity in BT474-derived sublines resistant to T-DM1, lapatinib, or neratinib, inducing cell cycle arrest, apoptosis, and caspase activation in all resistant models. Together, these findings identify disitamab vedotin as a potent next-generation HER2-targeting ADC with the unique capacity to overcome acquired resistance to HER2-directed therapies. RC48 represents a promising therapeutic strategy for patients with refractory HER2-positive breast cancer and warrants further clinical investigation.
Preclinical • Journal
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CCNB1 (Cyclin B1)
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HER-2 positive • HER-2 overexpression • HER-2 positive + HER-2 overexpression
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lapatinib • Nerlynx (neratinib) • Kadcyla (ado-trastuzumab emtansine) • Aidixi (disitamab vedotin)
27d
In Silico Molecular Docking and Pharmacokinetic Evaluation of Cannabinoid Derivatives as Multi-Target Inhibitors for EGFR, VEGFR-1, and VEGFR-2 Proteins. (PubMed, Curr Issues Mol Biol)
Among these, 2'-Hydroxy-Delta (9)-THC and Ajulemic Acid combined favorable multi-target binding with superior predicted pharmacokinetic properties compared with other cannabinoids and reference inhibitors (lapatinib, motesanib, and sorafenib). Toxicity predictions classified all compounds as moderately toxic, with Ajulemic Acid showing a comparatively more favorable safety profile. These findings do not demonstrate biological inhibition and should be interpreted strictly as hypothesis-generating computational evidence, providing a rational framework for future in vivo and in vitro validations.
PK/PD data • Journal
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EGFR (Epidermal growth factor receptor) • KDR (Kinase insert domain receptor) • FLT1 (Fms-related tyrosine kinase 1)
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sorafenib • lapatinib • motesanib (AMG 706)
27d
A Phase 1 Dose Escalation of Lapatinib and Paclitaxel in Recurrent Ovarian Cancer. (PubMed, Cancers (Basel))
The combination of paclitaxel and lapatinib was safe and demonstrated an efficacy signal. The RP2D was weekly paclitaxel 80 mg/m2 combined with lapatinib 2000 mg twice daily two days before the paclitaxel dose. This trial was registered at ClinicalTrials.gov ID: NCT04608409.
P1 data • Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1)
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paclitaxel • lapatinib