Tislelizumab is an IgG4 variant monoclonal antibody against PD-1 indicated for the treatment of unresectable, locally advanced or metastatic esophageal squamous cell carcinoma

Generic Name
DrugBank Accession Number

Tislelizumab is a humanized monoclonal IgG4 antibody against PD-1. It was engineered to have a nullified Fc portion, thus minimizing binding to FcγR on macrophages and limiting treatment resistance via antibody-dependent phagocytosis.1 By blocking PD-L1/PD-L2–mediated cell signaling, tislelizumab restores T-cell function through cytokine production, resulting in immune-mediated antitumor responses.2 Tislelizumab is generally well tolerated with manageable and mild-to-moderate adverse effects.3

On September 25, 2023, tislelizumab gained EMA approval as a monotherapy for adults with esophageal cancer under the brand name TEVIMBRA. This approval was based on positive results demonstrated in the RATIONALE 302 study, where an 8.6-month median overall survival rate was observed for tislelizumab treatment compared to 6.3-month for chemotherapy.5

  • Tislelizumab
External IDs
  • BGB-A317



Tislelizumab as monotherapy is approved by the EMA for the treatment of adult patients with unresectable, locally advanced, or metastatic oesophageal squamous cell carcinoma after prior platinum-based chemotherapy.4

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Treatment ofLocally advanced unresectable esophageal squamous cell carcinoma••••••••••••••••••••••••• •••••••••••••• ••••••••••••••••••••• •••••••••••
Treatment ofUnresectable, metastatic esophageal squamous cell carcinoma (escc)••••••••••••••••••••••••• •••••••••••••• ••••••••••••••••••••• •••••••••••
Contraindications & Blackbox Warnings
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Not Available

Mechanism of action

Tislelizumab is a humanized immunoglobulin G4 (IgG4) variant monoclonal antibody against PD-1, binding to the extracellular domain of human PD-1. It competitively blocks the binding of both PD-L1 and PD-L2, inhibiting PD-1-mediated negative signaling and enhancing the functional activity in T cells in in vitro cell-based assays.4

AProgrammed cell death protein 1

The pharmacokinetics (PK) of tislelizumab were characterized using population PK analysis with concentration data from 2 596 patients with advanced malignancies who received tislelizumab doses of 0.5 to 10 mg/kg every 2 weeks, 2.0 and 5.0 mg/kg every 3 weeks, and 200 mg every 3 weeks.4

The time to reach 90% steady-state level is approximately 84 days (12 weeks) after 200 mg doses once every 3 weeks, and the steady-state accumulation ratio of tislelizumab PK exposure is approximately 2-fold.4

Tislelizumab is administered intravenously and therefore is immediately and completely bioavailable.4

Volume of distribution

A population pharmacokinetic analysis indicates that the steady-state volume of distribution is 6.42 l, which is typical of monoclonal antibodies with limited distribution.4

Protein binding

Little information is available on the protein binding of tislelizumab.


Tislelizumab is expected to be degraded into small peptides and amino acids via catabolic pathways.4

Route of elimination

Not Available


Based on population PK analysis, the geometrical mean terminal half-life of tislelizumab was approximately 23.8 days with a coefficient variation (CV) of 31%.4


Based on population PK analysis, the clearance of tislelizumab was 0.153 l/day with an interindividual variability of 26.3%.4

Adverse Effects
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There are no available data on the use of tislelizumab in pregnant women. Based on its mechanism of action, tislelizumab can cause fetal harm when administered to a pregnant woman.4

Animal reproduction studies have not been conducted with tislelizumab. However, in murine models of pregnancy, blockade of PD-1/PD-L1 signaling has been shown to disrupt tolerance to the fetus and result in increased fetal loss.4

Human IgG4 (immunoglobulins) are known to cross the placental barrier. Therefore, tislelizumab, being an IgG4 variant, has the potential to be transmitted from the mother to the developing fetus.4

Women should be advised of the potential risk to a fetus. Tislelizumab should not be used during pregnancy unless the clinical condition of the woman requires treatment with tislelizumab.4

No clinical data are available on the possible effects of tislelizumab on fertility. No reproductive and development toxicity studies have been conducted with tislelizumab. Based on a 3-month repeat-dose toxicity study, there were no notable effects in the male and female reproductive organs in cynomolgus monkeys when tislelizumab was given at doses of 3, 10, or 30 mg/kg every 2 weeks for 13 weeks (7 dose administrations).4

There is no information on overdose with tislelizumab. In case of overdose, patients should be closely monitored for signs or symptoms of adverse drug reactions, and appropriate symptomatic treatment should be instituted immediately.4

Not Available
Pharmacogenomic Effects/ADRs
Not Available


Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Tislelizumab.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Tislelizumab.
AducanumabThe risk or severity of adverse effects can be increased when Aducanumab is combined with Tislelizumab.
AlemtuzumabThe risk or severity of adverse effects can be increased when Alemtuzumab is combined with Tislelizumab.
AlirocumabThe risk or severity of adverse effects can be increased when Alirocumab is combined with Tislelizumab.
Food Interactions
No interactions found.


ATC Codes
L01FF09 — Tislelizumab
Drug Categories
Not classified
Affected organisms
Not Available

Chemical Identifiers

CAS number


General References
  1. Shen L, Kato K, Kim SB, Ajani JA, Zhao K, He Z, Yu X, Shu Y, Luo Q, Wang J, Chen Z, Niu Z, Zhang L, Yi T, Sun JM, Chen J, Yu G, Lin CY, Hara H, Bi Q, Satoh T, Pazo-Cid R, Arkenau HT, Borg C, Lordick F, Li L, Ding N, Tao A, Shi J, Van Cutsem E: Tislelizumab Versus Chemotherapy as Second-Line Treatment for Advanced or Metastatic Esophageal Squamous Cell Carcinoma (RATIONALE-302): A Randomized Phase III Study. J Clin Oncol. 2022 Sep 10;40(26):3065-3076. doi: 10.1200/JCO.21.01926. Epub 2022 Apr 20. [Article]
  2. Zhang T, Song X, Xu L, Ma J, Zhang Y, Gong W, Zhang Y, Zhou X, Wang Z, Wang Y, Shi Y, Bai H, Liu N, Yang X, Cui X, Cao Y, Liu Q, Song J, Li Y, Tang Z, Guo M, Wang L, Li K: The binding of an anti-PD-1 antibody to FcgammaRIota has a profound impact on its biological functions. Cancer Immunol Immunother. 2018 Jul;67(7):1079-1090. doi: 10.1007/s00262-018-2160-x. Epub 2018 Apr 23. [Article]
  3. Desai J, Deva S, Lee JS, Lin CC, Yen CJ, Chao Y, Keam B, Jameson M, Hou MM, Kang YK, Markman B, Lu CH, Rau KM, Lee KH, Horvath L, Friedlander M, Hill A, Sandhu S, Barlow P, Wu CY, Zhang Y, Liang L, Wu J, Paton V, Millward M: Phase IA/IB study of single-agent tislelizumab, an investigational anti-PD-1 antibody, in solid tumors. J Immunother Cancer. 2020 Jun;8(1):e000453. doi: 10.1136/jitc-2019-000453. [Article]
  4. EMA Approved Drug Products: Tevimbra (tislelizumab) concentrate for solution for intravenous infusion [Link]
  5. Anti-PD-1 antibody gains EU approval for oesophageal cancer [Link]

Clinical Trials

Clinical Trials
4Active Not RecruitingTreatmentEsophageal Squamous Cell Carcinoma (ESCC)1
4Not Yet RecruitingTreatmentNon-Muscle-invasive Bladder Cancer (NMIBC)1
4RecruitingTreatmentBreast Cancer / Neoadjuvant Therapies1
3Active Not RecruitingTreatmentEsophageal Squamous Cell Carcinoma (ESCC)2
3Active Not RecruitingTreatmentGastric and Gastroesophageal Junction (GEJ) Adenocarcinoma1


Not Available
Not Available
Dosage Forms
Not Available
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Experimental Properties
Not Available


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Pharmacological action
General Function
Signal transducer activity
Specific Function
Inhibitory cell surface receptor involved in the regulation of T-cell function during immunity and tolerance. Upon ligand binding, inhibits T-cell effector functions in an antigen-specific manner. ...
Gene Name
Uniprot ID
Uniprot Name
Programmed cell death protein 1
Molecular Weight
31646.635 Da
  1. EMA Approved Drug Products: Tevimbra (tislelizumab) concentrate for solution for intravenous infusion [Link]

Drug created at May 20, 2019 14:35 / Updated at January 03, 2024 23:22