Tislelizumab
Monoclonal antibody
From Wikipedia, the free encyclopedia
Tislelizumab, sold under the brand name Tevimbra among others, is an anti-cancer medication used for the treatment of various forms of cancer. It is a humanized monoclonal antibody directed against programmed death receptor-1.[4] It is being developed by BeOne Medicines.[7]
 Fab fragment of tislelizumab (green) binding the extracellular domain of PD-1 (pale pink). From PDB entry 7BXA | |
| Monoclonal antibody | |
|---|---|
| Type | Whole antibody |
| Source | Humanized |
| Target | PD-1 |
| Clinical data | |
| Trade names | Tevimbra |
| Other names | BGB-A317, tislelizumab-jsgr |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a624026 |
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| Routes of administration | Intravenous |
| Drug class | Antineoplastic agent |
| ATC code | |
| Legal status | |
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| Identifiers | |
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| DrugBank | |
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Tislelizumab was approved for medical use in China in December 2019,[8][9] in the European Union in September 2023,[5] in the United States in March 2024,[10][11] and in Australia in May 2024.[1]
Medical uses
In China, tislelizumab is indicated to treat people with classical Hodgkin lymphoma who have received at least two prior therapies;[9] and to treat people with locally advanced or metastatic urothelial carcinoma with PD-L1 high expression whose disease progressed during or following platinum-containing chemotherapy or within twelve months of neoadjuvant or adjuvant treatment with platinum-containing chemotherapy.[12]
In the EU, tislelizumab is indicated for the treatment of adults with unresectable, locally advanced or metastatic esophageal squamous cell carcinoma after prior platinum-based chemotherapy.[5] In November 2024, the European Commission expanded the indication of tislelizumab for use alongside platinum- and fluoropyrimidine-based chemotherapy to treat people with HER2-negative locally advanced unresectable or metastatic gastric or gastroesophageal junction adenocarcinoma; and, in combination with platinum-based chemotherapy, for those with unresectable, locally advanced or metastatic esophageal squamous cell carcinoma.[5][13]
In the US, tislelizumab is indicated for the treatment of adults with unresectable or metastatic esophageal squamous cell carcinoma after prior systemic chemotherapy that did not include a PD-(L)1 inhibitor;[4] and, in combination with platinum and fluoropyrimidine-based chemotherapy, it is indicated for the first-line treatment of adults with unresectable or metastatic HER2-negative gastric or gastroesophageal junction adenocarcinoma whose tumors express PD-L1.[4]
Adverse effects
Adverse effects include anemia, leukopenia, thrombocytopenia, nausea, increased aspartate transaminase (AST), neutropenia, fatigue, decreased appetite, vomiting, musculoskeletal pain, constipation, hypoproteinemia and rash.[14] Fatal events such as respiratory infection or failure, and hepatic injury have been reported.[15]
Adverse events are more common when combined with chemotherapy.[16]
Pharmacokinetics
Phase I clinical trial from 2016 has results suggesting an elimination half-life of 11 to 17 days.[17] A 2021 structural and functional analysis suggests a t1/2 of 238 ± 32 minutes, 30- to 80-times higher than pembrolizumab and nivolumab.[18]
History
Phase I trials began in the United States and Australia in June 2015.[19] Some early results were announced in July 2016.[20][17]
A phase II clinical trial for urothelial cancer started in China in 2017.[21]
Tislelizumab "demonstrated efficacy and tolerability" in a multicenter phase III trial for advanced hepatocellular carcinoma started in January 2018.[7][22]
In November 2024, the European Medicines Agency expanded the indication of tislelizumab as part of a first-line combination treatment for adults with advanced gastric or esophageal cancer.[5]
Society and culture
Names
Tislelizumab is the international nonproprietary name.[23]
