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Synonyms: Bai Zean® | BGB-A317 | BGBA317 | hu317-1/IgG4mt2 | Tevimbra® | tislelizumab-jsgr
tislelizumab is an approved drug (China (2019), EMA (2023), FDA (2024))
Compound class:
Antibody
Comment: Tislelizumab (BGB-A317) is a humanized IgG4 monoclonal antibody targeting the PD-1 immune checkpoint [5]. It contains an alternative hinge region compared to other IgG4 anti-PD-1 antibodies, and subsequently does not induce the crosslinking between PD-1 and FcγRI that is observed for existing agents and which is believed to negatively impact on anti-PD-1 antibody-mediated anti-cancer activity. This modified profile is predicted to enhance tislelizumab's clinical efficacy [5]. Like other anti-PD-1 antibodies tislelizumab acts to prevent the binding of the ligands PD-L1 and PD-L2 to PD-1. Tislelizumab is an immuno-oncology drug candidate that was originally developed by Beigene (see their patent US8735553B1 [4]), and Novartis announced that they had acquired the rights to tislelizumab in major markets outside China in January 2021.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
| References |
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1. Chen J, Zhang H, Zhu L, Zhao Y, Ding Y, Yuan Y. (2020)
Tislelizumab for the treatment of classical Hodgkin's lymphoma. Drugs Today (Barc), 56 (12): 781-785. [PMID:33332484] |
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2. Desai J, Markman B, Sandhu SK, Gan HK, Friedlander M, Tran B, Meniawy T, Boolell V, Colyer D, Norris C et al..
A phase I dose-escalation study of BGB-A317, an anti-programmed death-1 (PD-1) mAb in patients with advanced solid tumors. Accessed on 06/06/2017. Modified on 06/06/2017. http://meetinglibrary.asco.org, http://meetinglibrary.asco.org/record/125804/abstract |
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3. Lee A, Keam SJ. (2020)
Tislelizumab: First Approval. Drugs, 80 (6): 617-624. [PMID:32185681] |
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4. Li K, Zhang T, Song J, Xu L, Liu Q, Peng H. (2014)
Anti-PD1 antibodies and their use as therapeutics and diagnostics. Patent number: US8735553B1. Assignee: Beigene Ltd. Priority date: 13/09/2013. Publication date: 27/05/2014. |
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5. Zhang T, Song X, Xu L, Ma J, Zhang Y, Gong W, Zhang Y, Zhou X, Wang Z, Wang Y et al.. (2018)
The binding of an anti-PD-1 antibody to FcγRΙ has a profound impact on its biological functions. Cancer Immunol Immunother, 67 (7): 1079-1090. [PMID:29687231] |
