Tislelizumab
 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 | |
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Tislelizumab, sold under the brand name Tevimbra among others, is a humanized monoclonal antibody directed against programmed death receptor-1.[3] It is being developed by BeiGene.[6]
Tislelizumab was approved for medical use in China in December 2019,[7] in the European Union in September 2023,[4] and in the United States in March 2024.[8]
Medical uses
In China, tislelizumab is indicated to treat people with classical Hodgkin lymphoma who have received at least two prior therapies;[7] 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.[9]
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.[4]
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.[3]
Adverse effects
Adverse effects include anemia, leukopenia, thrombocytopenia, nausea, increased aspartate transaminase (AST), neutropenia, fatigue, decreased appetite, vomiting, musculoskeletal pain, constipation, hypoproteinemia and rash.[10] Fatal events such as respiratory infection or failure, and hepatic injury have been reported.[11]
Adverse events are more common when combined with chemotherapy.[12]
Pharmacokinetics
Phase I clinical trial from 2016 has results suggesting an elimination half-life of 11 to 17 days.[13] A 2021 structural and functional analysis suggests a t1/2 of 238 ± 32 minutes, 30- to 80-times higher than pembrolizumab and nivolumab.[14]
History
Phase I trials began in the US and Australia in June 2015.[15] Some early results were announced in July 2016.[16][13]
A phase II clinical trial for urothelial cancer started in China in 2017.[17]
Tislelizumab "demonstrated efficacy and tolerability" in a multicenter phase III trial for advanced hepatocellular carcinoma started in January 2018.[6][18]
Society and culture
Names
Tislelizumab is the international nonproprietary name.[19]
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