【HER2 inhibitors】Trastuzumab(Herceptin®), Pertuzumab, Lapatinib, Antibody-drug conjugates (KADCYLA®)

Learn about Trastuzumab (Herceptin®), Pertuzumab (PERJETA®), Lapatinib (TYKERB®), and Antibody-drug conjugates (ADCs) (KADCYLA®).
Plus, find out about serious side effects.
【Additional explanation】
Trastuzumab deruxtecan (Enhertu®): trastuzumab +deruxtecan (a topoisomerase I inhibitor).
Similar to the video's description of trastuzumab-emtansine, it gets taken into cells through endocytosis.
However, Trastuzumab deruxtecan (Enhertu®) contains the topoisomerase I inhibitor deruxtecan, which blocks DNA replication.
#cancertreatment #her2positive #pharmacologymadeeasy
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【Notes】
▹This video was created based on data as of April 2024, with the purpose of supporting medical students in their exam preparations.
▹Please note that thanks to the tireless efforts of researchers worldwide, this data is updated daily. ▹Unauthorized reproduction is prohibited.
【Contents】
00:00 What is HER2?
00:36 Beast cancer and HER2?
01:02 constitutive signaling?
01:29 HER2 inhibitors: blocks HER2 pathway
01:46 monoclonal antibody drugs, Mechanism
02:23 Tyrosin kinase inhibitors, Mechanism
03:17 Clinical Use
03:40 Antibody-drug conjugates (ADCs), Mechanism
05:19 Adverse Effect
【Reference and figure】 I express my gratitude and respect for your wonderful achievements.
1. NCI (National Cancer Institute) Dictionary of Cancer Terms, “HER2-neu”.
www.cancer.gov/publications/d...
2. Arteaga, C., Sliwkowski, M., Osborne, C. et al. Treatment of HER2-positive breast cancer: current status and future perspectives. Nat Rev Clin Oncol 9, 16-32 (2012). doi.org/10.1038/nrclinonc.201...
3. Moasser MM. The oncogene HER2: its signaling and transforming functions and its role in human cancer pathogenesis. Oncogene. 2007 Oct 4;26(45):6469-87. doi: 10.1038/sj.onc.1210477. Epub 2007 Apr 30. PMID: 17471238; PMCID: PMC3021475.
4. Iqbal N, Iqbal N. Human Epidermal Growth Factor Receptor 2 (HER2) in Cancers: Overexpression and Therapeutic Implications. Mol Biol Int. 2014;2014:852748. doi: 10.1155/2014/852748. Epub 2014 Sep 7. PMID: 25276427; PMCID: PMC4170925.
5. Qi, X., Shi, Q., Xuhong, J. et al. Pyrotinib-based therapeutic approaches for HER2-positive breast cancer: the time is now. Breast Cancer Res 25, 113 (2023). doi.org/10.1186/s13058-023-01...
6. Greenblatt K, Khaddour K. Trastuzumab. [Updated 2022 Nov 28]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2024 Jan-. Available from: www.ncbi.nlm.nih.gov/books/NB...
7. M. Capelan, L. Pugliano, E. De Azambuja, I. Bozovic, K.S. Saini, C. Sotiriou, S. Loi, M.J. Piccart-Gebhart, Pertuzumab: new hope for patients with HER2-positive breast cancer, Annals of Oncology, volume 24, Issue 2, 2013, Pages 273-282, ISSN 0923-7534,
doi.org/10.1093/annonc/mds328.
(www.sciencedirect.com/science...)
8. DRUGBANK online, “Lapatinib”, DB01259.
go.drugbank.com/drugs/DB01259
9. Cooper GM. The Cell: A Molecular Approach. 2nd edition. Sunderland (MA): Sinauer Associates; 2000. Endocytosis. Available from: www.ncbi.nlm.nih.gov/books/NB...
10. Barok, M., Joensuu, H. & Isola, J. Trastuzumab emtansine: mechanisms of action and drug resistance. Breast Cancer Res 16, 209 (2014). doi.org/10.1186/bcr3621
11. Marei, H.E., Cenciarelli, C. & Hasan, A. Potential of antibody-drug conjugates (ADCs) for cancer therapy. Cancer Cell Int 22, 255 (2022). doi.org/10.1186/s12935-022-02...
12. Copeland-Halperin RS, Liu JE, Yu AF. Cardiotoxicity of HER2-targeted therapies. Curr Opin Cardiol. 2019 Jul;34(4):451-458. doi: 10.1097/HCO.0000000000000637. PMID: 31082851; PMCID: PMC7313632.

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