^
Contact us  to learn more about
our Premium Content:  News alerts, weekly reports and conference planners
DRUG:

lapatinib

i
Other names: GW572016, 572016, GW2016, GW572016F
Company:
Generic mfg.
Drug class:
EGFR inhibitor, HER2 inhibitor
Related drugs:
9d
Amiloride sensitizes prostate cancer cells to the reversible tyrosine kinase inhibitor lapatinib by modulating Erbb3 subcellular localization. (PubMed, Cell Mol Life Sci)
Amiloride combined with lapatinib significantly increased apoptosis at relatively low doses of both drugs but did not affect AR transcriptional activity. Thus, our data indicate that a combination of amiloride and lapatinib could target HSPC tumors without problems associated with using ADT as NAT in HSPC.
Journal
|
EGFR (Epidermal growth factor receptor) • AR (Androgen receptor) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
|
lapatinib
13d
HER-2 SMASH. (PubMed, Cancer Chemother Pharmacol)
We named this method the smash method, which is the volleyball term. In volleyball, the ball is raised while low and quickly hits the ground again, just like we do with the HER-2 receptor. The smash method can switch HER-2 negative or HER-2 low tumors into HER-2 overexpressed, iatrogenically. Thus, we can use her2-targeted therapies in all cancer patients instead of a small portion.
Journal
|
HER-2 (Human epidermal growth factor receptor 2)
|
HER-2 overexpression • HER-2 negative
|
lapatinib • Kadcyla (ado-trastuzumab emtansine)
15d
Prognostic value of residual disease (RD) biology and gene expression changes during the neoadjuvant treatment in patients with HER2+ early breast cancer (EBC). (PubMed, Ann Oncol)
In patients with HER2+ EBC and RD, tumor biomarkers provide more prognostic information at baseline. In contrast, immune biomarkers perform better for EFS prognosis in RD.
Journal
|
HER-2 (Human epidermal growth factor receptor 2) • CD8 (cluster of differentiation 8)
|
Herceptin (trastuzumab) • lapatinib
17d
Screening and identification of potential target of 1'-acetoxychavicol acetate (ACA) in acquired lapatinib-resistant breast cancer. (PubMed, Heliyon)
Overall, ACA might counteract breast cancer resistance to lapatinib by targeting BCL2, SSTR3, PLAU, ICAM1, IGF1R, and MET. Further in vitro studies involving gene silencing could provide more detailed insights into the mechanism by which ACA combats lapatinib resistance.
Journal • IO biomarker
|
HER-2 (Human epidermal growth factor receptor 2) • MET (MET proto-oncogene, receptor tyrosine kinase) • BCL2 (B-cell CLL/lymphoma 2) • IGF1R (Insulin-like growth factor 1 receptor) • ICAM1 (Intercellular adhesion molecule 1) • CDC42 (Cell Division Cycle 42) • CXCR2 (Chemokine (C-X-C motif) receptor 2) • PLAU (Plasminogen Activator)
|
lapatinib
17d
Lapatinib in Combination With Trastuzumab in Patients With HER2-Positive, Metastatic Breast Cancer (clinicaltrials.gov)
P2, N=87, Completed, Nancy Lin, MD | Active, not recruiting --> Completed | Trial completion date: Dec 2024 --> Aug 2024
Trial completion • Trial completion date • Metastases
|
HER-2 positive
|
Herceptin (trastuzumab) • lapatinib
18d
Uncovering key genes and molecular mechanisms of dendritic cell dysfunction in Esophageal Cancer: implications for Novel Diagnostic and therapeutic strategies. (PubMed, Discov Oncol)
Drug sensitivity analysis suggested that Metformin, Gefitinib, and Lapatinib may be more effective in the low-risk group, while Pyrimethamine, Axitinib, and Rapamycin may be more beneficial for high-risk patients. In summary, we identified a 6-gene signature related to dendritic cell dysfunction that can predict prognosis in esophageal cancer, offering valuable insights for personalized therapeutic strategies.
Journal • PD(L)-1 Biomarker • IO biomarker
|
PD-L1 (Programmed death ligand 1) • PD-1 (Programmed cell death 1) • GDF15 (Growth differentiation factor 15) • SLC5A1 (Solute Carrier Family 5 Member 1)
|
PD-1 expression • 6-gene signature
|
gefitinib • lapatinib • Inlyta (axitinib) • sirolimus • metformin
18d
TRPC6 is a Biomarker for Prognosis and Immunotherapy of Stomach Adenocarcinoma Based on Bioinformatic Analysis and Experimental Validation. (PubMed, Immunotargets Ther)
TRPC6 expression correlated strongly with immune cell infiltration, immune checkpoint genes, and sensitivity to therapies such as Lapatinib, anti-CTLA4, and anti-PD1 treatments...This study highlights the prognostic significance of TRPC6 in STAD and its potential as a therapeutic target. TRPC6's involvement in immune regulation and cancer cell progression underscores its dual role in STAD pathogenesis and treatment, offering new avenues for targeted therapy development.
Journal • PD(L)-1 Biomarker • IO biomarker
|
TRPC6 (Transient Receptor Potential Cation Channel Subfamily C Member 6)
|
lapatinib
19d
Cardiovascular toxicity risk assessment of tyrosine kinase inhibitors: a pharmacovigilance study using the VigiBase database. (PubMed, Front Pharmacol)
Significant cardiovascular signals were identified for 17 TKIs, including erlotinib, gefitinib, and imatinib...Heatmaps indicated significant signals for drugs such as lapatinib in males and gefitinib in younger patients...These results underscore the importance of individualized risk assessment and management of TKI-treated patients. In conclusion, this study provides valuable insights into the cardiotoxic risk of TKIs, which is essential for developing tailored treatment plans.
Journal • Adverse events
|
EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • ALK (Anaplastic lymphoma kinase) • ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
|
erlotinib • gefitinib • imatinib • lapatinib
19d
Potential Drug Synergy Through the ERBB2 Pathway in HER2+ Breast Tumors. (PubMed, Int J Mol Sci)
We visualized these interactions using Cytoscape to generate individual and combined drug-gene networks, focusing on frequently used drugs such as Erlotinib, Gefitinib, Lapatinib, and Cetuximab...Combined drug networks, such as those for Cetuximab with Lapatinib, Cetuximab with Erlotinib, and Erlotinib with Lapatinib, revealed potential synergies that could enhance therapeutic efficacy by simultaneously influencing multiple genes and pathways. Our findings suggest that a network-based approach to analyzing drug combinations provides valuable insights into the molecular mechanisms of HER2+ breast cancer and offers promising strategies for overcoming drug resistance and improving treatment outcomes.
Journal
|
EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2)
|
HER-2 positive • HER-2 overexpression
|
Herceptin (trastuzumab) • Erbitux (cetuximab) • erlotinib • gefitinib • lapatinib
20d
Study of TRAF3IP3 for prognosis and immune infiltration in hepatocellular carcinoma. (PubMed, PeerJ)
Notably, the half-maximal inhibitory concentration (IC50) of commonly used chemotherapeutic drugs, such as lapatinib and mitomycin, was inversely associated with TRAF3IP3 expression in HCC patients. TRAF3IP3 may be as a novel and promising biomarker for prognosis prediction and immunological evaluation of HCC.
Journal
|
CD8 (cluster of differentiation 8) • TNFA (Tumor Necrosis Factor-Alpha)
|
lapatinib • mitomycin
1m
Structure-based pharmacophore modelling for ErbB4-kinase inhibition: a systematic computational approach for small molecule drug discovery for breast cancer. (PubMed, SAR QSAR Environ Res)
Critical pharmacophoric features were extracted from the crystal structures of ErbB4-lapatinib, followed by virtual screening of the Chembl database to discover potential small molecule candidates. Furthermore, the ADMET profiles of 11 shortlisted candidates were assessed to verify their pharmacokinetic and toxicity properties, identifying Chembl310724, Chembl521284, and Chembl4168686 as promising inhibitors of ErbB4 kinase activity with the binding free energy (ΔGbind) values of -99.84, -89.42 and -86.06 kcal/mol, respectively. This integrated methodology not only enhances our understanding of ErbB4 inhibition but also sets a foundation for the rational design of targeted therapies addressing breast cancer with ErbB4 dependency.
Journal
|
ERBB4 (erb-b2 receptor tyrosine kinase 4)
|
HER-2 positive
|
lapatinib
1m
Combination therapy of Lapatinib/Letrozole-based protein-vitamin nanoparticles to enhance the therapeutic effectiveness in drug-resistant breast cancer. (PubMed, Colloids Surf B Biointerfaces)
Both in vitro and in vivo studies demonstrated that a combination of Lapa@HSA(VE) NPs and Let@HSA(VE) NPs in the ratio 75:25 inhibited tumor development and enhanced apoptosis significantly compared to individual NP treatment and free drug. The combination NPs therapy exhibited significant efficacy even in Lapa-resistant cell lines.
Journal • Combination therapy • IO biomarker
|
HER-2 (Human epidermal growth factor receptor 2)
|
HER-2 positive • HER-2 expression
|
lapatinib • letrozole
1m
The novel BCL-2/BCL-XL inhibitor APG-1252-mediated cleavage of GSDME enhances the antitumor efficacy of HER2-targeted therapy in HER2-positive gastric cancer. (PubMed, Acta Pharmacol Sin)
Mechanistically, APG-1252 combined with lapatinib synergistically induced GSDME-mediated pyroptosis in HER2-positive gastric cancer by activating caspase-dependent pathways and blocking the phospho-AKT/GSK-3β/MCL-1 signaling pathway. Our data indicated that the combination of lapatinib and APG-1252 had a synergistic antitumor effect on HER2-positive gastric cancer through the induction of caspase-3/GSDME-mediated apoptosis and pyroptosis.
Journal • IO biomarker
|
BCL2 (B-cell CLL/lymphoma 2) • BCL2L1 (BCL2-like 1) • CASP3 (Caspase 3) • GSDME (Gasdermin E)
|
HER-2 positive • HER-2 overexpression
|
lapatinib • pelcitoclax (APG-1252)
2ms
Dual inhibition of HERs and PD-1 counteract resistance in KRASG12C-mutant head and neck cancer. (PubMed, J Exp Clin Cancer Res)
Our study highlights the critical need for blocking both intrinsic and extrinsic mechanisms of resistance for the prolonged response and shows that such treatment is ineffective in KRASG12Ci-AcR tumors.
Journal • PD(L)-1 Biomarker • IO biomarker
|
EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • CD8 (cluster of differentiation 8)
|
KRAS mutation • PD-L1 overexpression • KRAS G12C • KRAS G12
|
lapatinib • Lumakras (sotorasib) • Krazati (adagrasib)
2ms
Precision Nanomedicine: Lapatinib-Loaded Chitosan-Gold Nanoparticles Targeting LINC01615 for Lung Cancer Therapy. (PubMed, AAPS J)
Chitosan-gold nanoparticles conjugated with Lapatinib significantly reduced LINC01615 expression in lung cancer cell lines while enhancing apoptosis rates. Therefore, these nanoparticles could be considered a promising therapeutic candidate for treating cancers with overexpression of LINC01615.
Journal
|
LINC01615 (Long Intergenic Non-Protein Coding RNA 1615)
|
lapatinib
2ms
Case report: Efficacy of later-line fam-trastuzumab deruxtecan in a patient with triple-positive breast cancer with brain metastases. (PubMed, Front Oncol)
After receiving capecitabine, lapatinib, gonadotropin-releasing hormone (GnRH) agonist, and tamoxifen, multiple new lesions appeared in the brain after 14 months. The patient then received capecitabine, neratinib, GnRH agonist, and letrozole; however, her brain metastases still progressed after 7 months...Now aged 30, the patient is continuing to receive T-DXd treatment to prevent recurrence. We conclude that T-DXd was effective for the treatment of brain metastases in this young patient with triple-positive metastatic breast cancer who had multiple risk factors and had received several anti-HER2 therapies prior to T-DXd.
Journal
|
MUC1 (Mucin 1)
|
EGFR positive
|
lapatinib • tamoxifen • Nerlynx (neratinib) • Enhertu (fam-trastuzumab deruxtecan-nxki) • capecitabine • letrozole
2ms
Characterizing PANoptosis gene signature in prognosis and chemosensitivity of colorectal cancer. (PubMed, J Gastrointest Oncol)
Particularly, patients in high-risk group exhibited higher sensitivity to fluorouracil, oxaliplatin and lapatinib compared to the low-risk group. This study highlights the prognostic potential of PANoptosis-related features in CRC, demonstrating their role as key biomarkers significantly associated with patient survival and aiding in the identification of high-risk patients, thereby advancing immunotherapy approaches.
Journal • Gene Signature • IO biomarker
|
CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • TIMP1 (Tissue inhibitor of metalloproteinases 1) • TLR3 (Toll Like Receptor 3)
|
5-fluorouracil • lapatinib • oxaliplatin
2ms
Quantum DFT analysis and molecular docking investigation of various potential breast cancer drugs. (PubMed, J Mater Chem B)
In contrast, anastrozole and letrozole show lower binding affinities for HER2 and EGFR due to their simpler structures but are potent aromatase inhibitors, making them effective in treating estrogen receptor-positive (ER-positive) breast cancers. In conclusion, DFT and molecular docking studies affirm the suitability of lapatinib, tucatinib, and neratinib for HER2-positive cancers, while anastrozole and letrozole are effective in ER-positive cancers, emphasizing the role of molecular structure and binding affinity in optimizing cancer treatment strategies.
Journal
|
EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
|
HER-2 positive • ER positive
|
lapatinib • Nerlynx (neratinib) • Tukysa (tucatinib) • letrozole • anastrozole
2ms
Rational Design of HER2-Targeted Combination Therapies to Reverse Drug Resistance in Fibroblast-Protected HER2+ Breast Cancer Cells. (PubMed, Cell Mol Bioeng)
Drug sensitivity to the HER2 kinase inhibitor lapatinib was characterized under conditions of monoculture and exposure to breast fibroblast-conditioned medium...Combination therapies targeting HER2 kinase and these fibroblast-induced signaling adaptations eliminates fibroblast-protected HER2+ breast cancer cells. The online version contains supplementary material available at 10.1007/s12195-024-00823-0.
Journal • Combination therapy
|
HER-2 (Human epidermal growth factor receptor 2) • PLK1 (Polo Like Kinase 1)
|
HER-2 expression • PAI1 expression
|
lapatinib
2ms
Reactivation of MAPK-SOX2 pathway confers ferroptosis sensitivity in KRASG12C inhibitor resistant tumors. (PubMed, Redox Biol)
The clinical success of KRASG12C inhibitors (G12Ci) including AMG510 and MRTX849 is limited by the eventual development of acquired resistance...We found the ferroptosis inducers including sorafenib and lapatinib stood out with an obvious growth inhibition in the G12Ci resistant cells...Ferroptosis induced by sulfasalazine (SAS) achieved obvious inhibition on the tumor growth of xenografts derived from AMG510-resistant KRASG12C-mutant cells. Collectively, our results suggest a novel therapeutic strategy to treat patients bearing G12Ci resistant cancers with ferroptosis inducers.
Journal
|
KRAS (KRAS proto-oncogene GTPase) • SOX2 • SLC7A11 (Solute Carrier Family 7 Member 11) • SLC40A1 (Solute Carrier Family 40 Member 1)
|
KRAS mutation • SOX2 overexpression • SOX2 expression
|
sorafenib • lapatinib • Lumakras (sotorasib) • Krazati (adagrasib)
2ms
Lapatinib Ditosylate Before Surgery in Treating Patients With Recurrent High-Grade Glioma (clinicaltrials.gov)
P1, N=29, Completed, National Cancer Institute (NCI) | Active, not recruiting --> Completed | Trial completion date: Oct 2025 --> Oct 2024
Trial completion • Trial completion date • Surgery
|
EGFR (Epidermal growth factor receptor)
|
EGFR amplification
|
lapatinib
2ms
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, Daiichi Sankyo | Trial completion date: May 2025 --> Jul 2025
Trial completion date • Metastases
|
HER-2 (Human epidermal growth factor receptor 2)
|
HER-2 positive • HER-2 expression
|
lapatinib • Kadcyla (ado-trastuzumab emtansine) • Enhertu (fam-trastuzumab deruxtecan-nxki) • capecitabine
2ms
Design, in silico studies and biological evaluation of novel chalcones tethered triazolo[3,4-a]isoquinoline as EGFR inhibitors targeting resistance in non-small cell lung cancer. (PubMed, Sci Rep)
The selectivity index of 3f for EGFRT790M was 1.81 times more selective than that of lapatinib. In addition, 3e and 3f initiated cell cycle arrest at the G2/M and pre-G1 phases along with the downregulation of anti-apoptotic protein Bcl2 and the upregulation of pro-apoptotic proteins: p53, Bax, and caspases 3, 8, and 9. Further studies are recommended to evaluate animal models' promising anticancer activity and molecular mechanism of triazolo[3,4-a]isoquinoline derivatives 3e and 3f.
Journal
|
BCL2 (B-cell CLL/lymphoma 2) • CASP8 (Caspase 8) • CASP9 (Caspase 9)
|
EGFR T790M
|
lapatinib
2ms
Targeting HER2 in breast cancer with brain metastases: a pharmacological point of view with special focus on the permeability of blood-brain barrier to targeted treatments. (PubMed, Eur J Pharmacol)
The National Comprehensive Cancer Network (NCCN) guidelines recommend the use of tyrosine kinase inhibitors (TKIs) lapatinib, neratinib, and tucatinib in co-administration with monoclonal antibodies or chemotherapy drugs and the antibody-drug conjugates (ADCs) trastuzumab-deruxtecan and trastuzumab-emtansine. In this review article, we discuss about the molecular and cellular features of the barriers located in the central nervous system and the pharmacological parameters found to be important in predicting BBB permeability in human normal brain and in the presence of brain metastases. Finally, we reported the clinical outcomes and intracranial response of patients with HER2-positive breast cancer with brain metastases treated with targeted TKIs and ADCs.
Review • Journal
|
HER-2 (Human epidermal growth factor receptor 2)
|
HER-2 positive • EGFR positive
|
lapatinib • Nerlynx (neratinib) • Kadcyla (ado-trastuzumab emtansine) • Enhertu (fam-trastuzumab deruxtecan-nxki) • Tukysa (tucatinib)
2ms
Annexin A6 modulates the secretion of pro-inflammatory cytokines and exosomes via interaction with SNAP23 in triple negative breast cancer cells. (PubMed, bioRxiv)
Moreover, cholesterol content in EVs was significantly higher in AnxA6-expressing cells than in AnxA6 downregulated cells and following chronic lapatinib induced upregulation of AnxA6...AnxA6 neutralizing antibodies strongly diminished the survival of AnxA6 low TNBC cells but had minimal effects on the survival of TNBC cells expressing relatively high levels of the protein. Together, these data suggest that AnxA6 facilitates the secretion of EVs and proinflammatory cytokines that may be critical for TNBC progression.
Journal
|
CXCL8 (Chemokine (C-X-C motif) ligand 8) • DKK1 (dickkopf WNT signaling pathway inhibitor 1) • SPP1 (Secreted Phosphoprotein 1) • CCL2 (Chemokine (C-C motif) ligand 2) • ANXA6 (Annexin A6)
|
lapatinib
2ms
Lapatinib Ditosylate Before Surgery in Treating Patients With Recurrent High-Grade Glioma (clinicaltrials.gov)
P1, N=29, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Oct 2024 --> Oct 2025
Trial completion date
|
EGFR (Epidermal growth factor receptor)
|
EGFR amplification
|
lapatinib
2ms
Trial completion • Metastases
|
HER-2 (Human epidermal growth factor receptor 2)
|
HER-2 positive
|
lapatinib • capecitabine • oxaliplatin
2ms
Design and synthesis of novel 2-(2-(4-bromophenyl)quinolin-4-yl)-1,3,4-oxadiazole derivatives as anticancer and antimicrobial candidates: in vitro and in silico studies. (PubMed, RSC Adv)
The assessed compounds 7-17e showed considerable cytotoxic activity activities against HepG2 and MCF-7 with IC50 values of 0.137-0.332 and 0.164-0.583 μg mL-1, respectively, in comparison to erlotinib as the positive control, which showed an IC50 value of 0.308 and 0.512 μg mL-1, respectively...The results showed good IC50 values of 0.14 and 0.18 μM for compounds 8c and 12d, respectively, compared to lapatinib (IC50 value of 0.12 μM)...Compounds 17b, 17d and 17e displayed the most potent inhibitory activity, exhibiting 4-, 16- and 8-fold more activity, respectively, than the reference neomycin. Hence, we can conclude that the afforded compounds can be used as lead dual anticancer and antimicrobial candidates for future optimization.
Preclinical • Journal
|
EGFR (Epidermal growth factor receptor)
|
erlotinib • lapatinib
2ms
LC-HRMS-based global metabolomics profiling unravels the distinct metabolic signature of lapatinib-resistant and trastuzumab-resistant HER2+ breast cancer cells. (PubMed, J Pharm Biomed Anal)
Joint pathway enrichment analysis of LAP-resistant DEMs and differentially expressed genes (DEGs) showed enrichment in glutathione metabolism, while that of TRZ-resistance and DEGs showed enrichment in carbohydrate metabolism, namely pentose and glucuronate interconversions, starch and sucrose metabolism, and galactose metabolism. The findings from this study indicate considerable metabolic changes in LAP- and TRZ-resistant HCC1954 cells, which are crucial for understanding the resistance mechanisms and developing strategies to overcome these problems.
Journal • Metabolomic study
|
HER-2 (Human epidermal growth factor receptor 2)
|
Herceptin (trastuzumab) • lapatinib
2ms
Enhanced antitumor activity of lapatinib against triple-negative breast cancer via loading in human serum albumin. (PubMed, Int J Biol Macromol)
Biodistribution studies using technetium-99 m (99mTc) labeling revealed enhanced tumor targeting. These findings highlight the potential of HSA as a delivery vehicle for LAP, particularly in combination with anti-angiogenic agents like VGB3, offering a promising therapeutic strategy for TNBC.
Journal
|
FLT1 (Fms-related tyrosine kinase 1)
|
lapatinib
3ms
Design, synthesis, and biological evaluation of novel quinoline-based EGFR/HER-2 dual-target inhibitors as potential anti-tumor agents. (PubMed, RSC Adv)
With inhibitory (IC50) values of 71 and 31 nM, respectively, compound 5a proved to be the most effective dual-target inhibitor of EGFR and HER-2, outperforming the reference erlotinib (IC50 = 80 nM) as an EGFR inhibitor but falling short of the clinically used agent lapatinib (IC50 = 26 nM) as a HER2 inhibitor. The apoptotic potential activity of 5a was examined, and the findings demonstrated that 5a promotes apoptosis by activating caspase-3, 8, and Bax while simultaneously reducing the expression of the anti-apoptotic protein Bcl-2. The docking studies provided valuable insights into the binding interactions of compounds 3e and 5a with EGFR, effectively rationalizing the observed SAR trends.
Journal • IO biomarker
|
EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • BCL2 (B-cell CLL/lymphoma 2) • CASP3 (Caspase 3) • CASP8 (Caspase 8)
|
BCL2 expression
|
erlotinib • lapatinib
3ms
Her2 positive metastatic breast cancer treated with low dose lapatinib in a resource-constrained setting in South India: a retrospective audit. (PubMed, Ecancermedicalscience)
In our institution, consecutive patients with Her2 positive metastatic breast cancer from 1 January 2014 to 31 December 2020 who could not afford trastuzumab, lapatinib or any other anti-Her2 agent were offered low-dose lapatinib, 500 mg daily with meal. Low-dose lapatinib is a regimen that offers an acceptable disease control rate. This strategy requires further exploration, particularly for the benefit of resource-limited areas.
Retrospective data • Journal • Metastases
|
HER-2 (Human epidermal growth factor receptor 2)
|
HER-2 positive
|
Herceptin (trastuzumab) • lapatinib
3ms
Final analysis of the ALTTO trial: adjuvant trastuzumab in sequence or in combination with lapatinib in patients with HER2-positive early breast cancer [BIG 2-06/NCCTG N063D (Alliance)]. (PubMed, ESMO Open)
With a longer follow-up, no significant improvement was observed in DFS in patients treated with dual anti-HER2 blockade with lapatinib + trastuzumab compared to trastuzumab alone. The 10-year survival rates for the combination group are consistent with other studies that have explored dual anti-HER2 therapy.
Clinical • Journal • Combination therapy
|
HER-2 (Human epidermal growth factor receptor 2)
|
HER-2 positive
|
Herceptin (trastuzumab) • lapatinib
3ms
Lapatinib-induced enhancement of mitochondrial respiration in HER2-positive SK-BR-3 cells: mechanism revealed by analysis of proteomic but not transcriptomic data. (PubMed, Front Mol Biosci)
However, it is consistent with the results of the resazurin test, which showed a 1.8-fold increase in SK-BR-3 cellular respiration upon exposure to lapatinib. Thus, we conclude that enhanced cellular respiration is a novel additional mechanism of action of lapatinib on HER2-positive cancer cells.
Journal
|
EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2)
|
HER-2 positive
|
lapatinib
3ms
The Prospective Role of Lapatinib as an Adjuvant Therapy in Prevalent Cancers: Insights from In Silico Analysis Targeting EGFR and HER2. (PubMed, Mol Cell Probes)
Our results indicate an upregulation in the expression levels of HER2 and EGFR in certain common cancers, suggesting that lapatinib, in addition to breast cancer, could be considered for the treatment of these cancers. Furthermore, we demonstrated that some genes with increased expression in prevalent cancers and associated with poor prognosis have the potential to be modulated by lapatinib.
Journal
|
EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • CCND1 (Cyclin D1) • METTL1 (Methyltransferase 1, TRNA Methylguanosine) • NOP2 (NOP2 Nucleolar Protein)
|
HER-2 expression
|
lapatinib
3ms
Molecular Profiling and Targeted Therapy for Advanced Non-Small Cell Lung Cancer, Small Cell Lung Cancer, and Thymic Malignancies (clinicaltrials.gov)
P2, N=647, Completed, National Cancer Institute (NCI) | Active, not recruiting --> Completed | Trial completion date: Dec 2024 --> Jul 2024
Trial completion • Trial completion date
|
EGFR (Epidermal growth factor receptor) • BRAF (B-raf proto-oncogene)
|
EGFR mutation
|
erlotinib • sunitinib • lapatinib • Koselugo (selumetinib) • MK-2206
3ms
Trial completion date • Metastases
|
HER-2 (Human epidermal growth factor receptor 2)
|
HER-2 positive
|
lapatinib • capecitabine • oxaliplatin
3ms
A review on tyrosine kinase inhibitors for targeted breast cancer therapy. (PubMed, Pathol Res Pract)
Several TKIs, including lapatinib, neratinib, and tucatinib, have been developed and are currently used in clinical settings, often in combination with chemotherapy, endocrine therapy, or other targeted agents. TKIs have emerged as a promising therapeutic option for patients with breast cancer and hold potential for treating other breast cancer subtypes. The development of new TKIs and their integration into personalized treatment strategies will continue to shape the future of breast cancer therapy.
Review • Journal
|
HER-2 (Human epidermal growth factor receptor 2) • ALK (Anaplastic lymphoma kinase) • RET (Ret Proto-Oncogene) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • FGFR (Fibroblast Growth Factor Receptor)
|
lapatinib • Nerlynx (neratinib) • Tukysa (tucatinib)
3ms
Fibroblast growth factor 20 ameliorates cardiac hypertrophy via activation ErbB2. (PubMed, Heliyon)
Lapatinib largely abrogated the anti-hypertrophic effect of FGF20, accompanied by increases in cardiomyocyte apoptosis and oxidative stress. In summary, this study reveals that FGF20 prevents cardiac hypertrophy by inhibiting apoptosis and oxidative stress via activating ErbB2 and may be a promising therapeutic strategy for cardiac hypertrophy.
Journal
|
HER-2 (Human epidermal growth factor receptor 2) • NPPB (Natriuretic Peptide B)
|
lapatinib
4ms
Long-Term Success With a TDM-1 Biosimilar in Recurrent HER2-Positive Breast Cancer With Multisite Metastases: A Comprehensive Case Study. (PubMed, Cureus)
A 54-year-old postmenopausal female patient with recurrent breast cancer and metastasis was treated with trastuzumab and paclitaxel (12 cycles), followed by trastuzumab maintenance therapy (71 cycles)...Oral therapy with lapatinib and letrozole was prescribed for a year to treat the breast cancer, along with the lesions and enhanced nodules observed in the patient's lungs, liver, and bones...This case report demonstrates the long-term efficacy of T-DM1 and its satisfactory safety profile. Overall, it provides valuable insights into the management of and challenges faced during the treatment of recurrent breast cancer with metastasis.
Journal
|
HER-2 (Human epidermal growth factor receptor 2)
|
HER-2 positive
|
paclitaxel • lapatinib • Kadcyla (ado-trastuzumab emtansine) • letrozole
4ms
Proteomic assessment of SKBR3/HER2+ breast cancer cellular response to Lapatinib and investigational Ipatasertib kinase inhibitors. (PubMed, Front Pharmacol)
Furthermore, over fifty of the impacted proteins represent approved or investigational targets in the DrugBank database, which through their protein-protein interaction networks can inform the selection of effective therapeutic partners. Altogether, the exposure of SKBR3/HER2+ cells to Lapatinib and Ipatasertib kinase inhibitors uncovered a broad plethora of yet untapped opportunities that can be further explored for enhancing the anti-cancer effects of each drug as well as of many other multi-drug therapies that target the EGFR/ERBB2 and PI3K/AKT pathways.
Journal
|
HER-2 (Human epidermal growth factor receptor 2)
|
lapatinib • ipatasertib (RG7440)
4ms
Amiloride Sensitizes Prostate Cancer Cells to the Reversible Tyrosine Kinase Inhibitor Lapatinib by Modulating ERBB3 Subcellular Localization. (PubMed, Res Sq)
Amiloride combined with lapatinib significantly increased apoptosis but did not affect AR transcriptional activity. Thus, our data indicate that a combination of amiloride and lapatinib could target HSPC tumors without problems associated with androgen deprivation therapy in localized PCa.
Journal
|
EGFR (Epidermal growth factor receptor) • AR (Androgen receptor) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
|
lapatinib