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Littérature scientifique sur le sujet « Lapatinib: Chemistry »

Auteur : Grafiati

Publié le 2 juin 2025

Mis à jour le 31 juillet 2025

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Articles de revues sur le sujet "Lapatinib: Chemistry"

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Akash, Darekar* Dr. V. M. Satpute Ghodake S. R. "Overview of Lapatinib: Chemistry, Pharmacology, and Clinical Applications." International Journal of Pharmaceutical Sciences 3, no. 5 (2025): 3774–87. https://doi.org/10.5281/zenodo.15489237.

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The present study focuses on the development and validation of a sensitive, accurate, and reproducible bioanalytical method for the estimation of Lapatinib in active pharmaceutical ingredient (API) form and marketed formulations using human plasma. Lapatinib, a dual tyrosine kinase inhibitor used in the treatment of HER2-positive breast cancer, requires precise quantification in biological matrices for effective pharmacokinetic and bioequivalence studies. A high-performance liquid chromatography (HPLC) method coupled with UV detection was developed for the extraction and quantification of Lapa

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Huynh, Thanh Kieu, Chien-Yi Ho, Chi-Hua Tsai, et al. "Proteasome Inhibitors Suppress ErbB Family Expression through HSP90-Mediated Lysosomal Degradation." International Journal of Molecular Sciences 20, no. 19 (2019): 4812. http://dx.doi.org/10.3390/ijms20194812.

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Although dual EGFR/HER2 tyrosine kinase inhibitor lapatinib has provided effective clinical benefits for HER2-positive breast cancer patients, acquired resistance to this drug remains a major concern. Thus, the development of alternative therapeutic strategies is urgently needed for patients who failed lapatinib treatment. Proteasome inhibitors have been reported to possess high anti-tumor activity to breast cancer cells. Therefore, this study aims to examine whether and how proteasome inhibitor bortezomib can overcome lapatinib resistance. Treatments with several proteasome inhibitors, includ

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January, Jaymi Leigh, Ziyanda Zamaswazi Tshobeni, Nokwanda Precious Pearl Ngema, et al. "Novel Cytochrome P450-3A4 Enzymatic Nanobiosensor for Lapatinib (a Breast Cancer Drug) Developed on a Poly(anilino-co-4-aminobenzoic Acid-Green-Synthesised Indium Nanoparticle) Platform." Biosensors 13, no. 9 (2023): 897. http://dx.doi.org/10.3390/bios13090897.

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Breast cancer (BC) is one of the most common types of cancer disease worldwide and it accounts for thousands of deaths annually. Lapatinib is among the preferred drugs for the treatment of breast cancer. Possible drug toxicity effects of lapatinib can be controlled by real-time determination of the appropriate dose for a patient at the point of care. In this study, a novel highly sensitive polymeric nanobiosensor for lapatinib is presented. A composite of poly(anilino-co-4-aminobenzoic acid) co-polymer {poly(ANI-co-4-ABA)} and coffee extract-based green-synthesized indium nanoparticles (InNPs)

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Walker, Rashidra R., Jankiben R. Patel, Akash Gupta, et al. "Glyceollins Trigger Anti-Proliferative Effects in Hormone-Dependent Aromatase-Inhibitor-Resistant Breast Cancer Cells through the Induction of Apoptosis." International Journal of Molecular Sciences 23, no. 5 (2022): 2887. http://dx.doi.org/10.3390/ijms23052887.

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Aromatase inhibitors (AIs) are standard treatment for estrogen-dependent postmenopausal breast tumors; however, resistance develops leading to tumor relapse and metastasis. We previously demonstrated that glyceollin inhibits proliferation, survival, and migration of hormone-independent letrozole-resistant breast cancer. Since many AI-resistant tumors remain hormone-dependent, identifying distinctions between estrogen-receptor-positive (ER+) and ER-negative (ER-) AI-resistant tumor response to therapy is critical. We hypothesize that treating ER+ letrozole-resistant T47D breast cancer cells (T4

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Behera, Ranjan, Sarah M. Thomas, and Kojo Mensa-Wilmot. "New Chemical Scaffolds for Human African Trypanosomiasis Lead Discovery from a Screen of Tyrosine Kinase Inhibitor Drugs." Antimicrobial Agents and Chemotherapy 58, no. 4 (2014): 2202–10. http://dx.doi.org/10.1128/aac.01691-13.

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ABSTRACTHuman African trypanosomiasis (HAT) is caused by the protozoanTrypanosoma brucei. New drugs are needed to treat HAT because of undesirable side effects and difficulties in the administration of the antiquated drugs that are currently used. In human proliferative diseases, protein tyrosine kinase (PTK) inhibitors (PTKIs) have been developed into drugs (e.g., lapatinib and erlotinib) by optimization of a 4-anilinoquinazoline scaffold. Two sets of facts raise a possibility that drugs targeted against human PTKs could be “hits” for antitrypanosomal lead discoveries. First, trypanosome prot

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Kang, Jia, Zanzan Guo, Haoqi Zhang, Rongqi Guo, Xiaofei Zhu, and Xiaofang Guo. "Dual Inhibition of EGFR and IGF-1R Signaling Leads to Enhanced Antitumor Efficacy against Esophageal Squamous Cancer." International Journal of Molecular Sciences 23, no. 18 (2022): 10382. http://dx.doi.org/10.3390/ijms231810382.

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Both the epidermal growth factor receptor (EGFR) and insulin-like growth factor 1 receptor (IGF-1R) have been implicated in the development of cancers, and the increased expression of both receptors has been observed in esophageal cancer. However, the tyrosine kinase inhibitors of both receptors have thus far failed to provide clinical benefits for esophageal cancer patients. Studies have confirmed the complicated crosstalks that exist between the EGFR and IGF-1R pathways. The EGFR and IGF-1R signals act as mutual compensation pathways, thereby conveying resistance to EGFR or IGF-1R inhibitors

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Achounna, Angèle Sorel, David Ordaz-Rosado, Janice García-Quiroz, et al. "EB1089 Increases the Antiproliferative Response of Lapatinib in Combination with Antiestrogens in HER2-Positive Breast Cancer Cells." International Journal of Molecular Sciences 25, no. 6 (2024): 3165. http://dx.doi.org/10.3390/ijms25063165.

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HER2-positive breast cancer is associated with aggressive behavior and reduced survival rates. Calcitriol restores the antiproliferative activity of antiestrogens in estrogen receptor (ER)-negative breast cancer cells by re-expressing ERα. Furthermore, calcitriol and its analog, EB1089, enhance responses to standard anti-cancer drugs. Therefore, we aimed to investigate EB1089 effects when added to the combined treatment of lapatinib and antiestrogens on the proliferation of HER2-positive breast cancer cells. BT-474 (ER-positive/HER2-positive) and SK-BR-3 (ER-negative/HER2-positive) cells were

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Yamaura, Kei, Keiko Kuwata, Tomonori Tamura, et al. "Live cell off-target identification of lapatinib using ligand-directed tosyl chemistry." Chem. Commun. 50, no. 91 (2014): 14097–100. http://dx.doi.org/10.1039/c4cc05885b.

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Clayton, Natasha S., Edward P. Carter, Abbie E. Fearon, et al. "HDAC Inhibition Restores Response to HER2-Targeted Therapy in Breast Cancer via PHLDA1 Induction." International Journal of Molecular Sciences 24, no. 7 (2023): 6228. http://dx.doi.org/10.3390/ijms24076228.

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The downregulation of Pleckstrin Homology-Like Domain family A member 1 (PHLDA1) expression mediates resistance to targeted therapies in receptor tyrosine kinase-driven cancers. The restoration and maintenance of PHLDA1 levels in cancer cells thus constitutes a potential strategy to circumvent resistance to inhibitors of receptor tyrosine kinases. Through a pharmacological approach, we identify the inhibition of MAPK signalling as a crucial step in PHLDA1 downregulation. Further ChIP-qPCR analysis revealed that MEK1/2 inhibition produces significant epigenetic changes at the PHLDA1 locus, spec

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de Sousa, Ana Carolina C., Keletso Maepa, Jill M. Combrinck, and Timothy J. Egan. "Lapatinib, Nilotinib and Lomitapide Inhibit Haemozoin Formation in Malaria Parasites." Molecules 25, no. 7 (2020): 1571. http://dx.doi.org/10.3390/molecules25071571.

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With the continued loss of antimalarials to resistance, drug repositioning may have a role in maximising efficiency and accelerating the discovery of new antimalarial drugs. Bayesian statistics was previously used as a tool to virtually screen USFDA approved drugs for predicted β-haematin (synthetic haemozoin) inhibition and in vitro antimalarial activity. Here, we report the experimental evaluation of nine of the highest ranked drugs, confirming the accuracy of the model by showing an overall 93% hit rate. Lapatinib, nilotinib, and lomitapide showed the best activity for inhibition of β-haema

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Chapitres de livres sur le sujet "Lapatinib: Chemistry"

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Stuart Cockerill, G., and Karen E. Lackey. "CHAPTER 27. Lessons Learned From the Discovery and Development of Lapatinib/Tykerb." In The Handbook of Medicinal Chemistry. Royal Society of Chemistry, 2015. http://dx.doi.org/10.1039/9781782621836-00676.

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