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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. ✖ |
| No information available. |
Summary of Clinical Use  |
| The first worldwide approval of tislelizumab (BGB-A317) for clinical use was granted in China in late 2019 [1,3]. The initial approval was as a third-line treatment for classical Hodgkin lymphoma, and this was later expanded to include previously treated, PD-L1high bladder cancer. Clinical trials to support approvals outside of China are ongoing. Tislelizumab is being investigated in hematological malignancies and solid tumours, as a monotherapy, and in combination with existing anti-cancer drugs, and small molecules such as the BTK inhibitors zanubrutinib (an already approved drug) and tirabrutinib (GS-4059; investigational). Click here to link to ClinicalTrials.gov's full list of BGB-A317 studies. The EMA approved tislelizumab as a therapy for advanced esophageal squamous cell carcinoma (ESCC) at the end of 2023. FDA approval for this indication was issued in March 2024. |
| Clinical Trials | |||||
| Clinical Trial ID | Title | Type | Source | Comment | References |
| NCT02407990 | Study of the Safety, Pharmacokinetics and Antitumor Activities of BGB-A317 in Participants With Advanced Tumors | Phase 1 Interventional | BeiGene | ||
| NCT02795182 | Zanubrutinib (BGB-3111) in Combination With Tislelizumab (BGB-A317) in Participants With B-cell Malignancies | Phase 1 Interventional | BeiGene | ||
