tislelizumab

Overview

Tislelizumab (BGB-A317) is a humanized monoclonal antibody that targets programmed death 1 (PD-1), a key immune checkpoint receptor expressed on T cells. By blocking the interaction between PD-1 and its ligands PD-L1 and PD-L2, tislelizumab restores antitumor immune activity that cancer cells exploit to evade immune surveillance. Engineered with a modified Fc region to minimize Fc gamma receptor binding on macrophages — a mechanism thought to reduce antibody-dependent cellular phagocytosis of T cells — tislelizumab is designed to preserve effector T cell function more effectively than earlier generation PD-1 inhibitors. Developed by BeiGene, the drug has received regulatory approval in China and select global markets for multiple indications including non-small cell lung cancer, hepatocellular carcinoma (HCC), and esophageal squamous cell carcinoma (ESCC).

As a PD-1 checkpoint inhibitor, tislelizumab belongs to the broader class of immune oncology agents that have transformed the treatment landscape for solid tumors over the past decade. Its clinical development has expanded across gastrointestinal malignancies, thoracic cancers, and combination strategies with chemotherapy, radiotherapy, and targeted biologics — reflecting a growing emphasis on harnessing immunotherapy within multimodal treatment regimens.

Focus of Latest Publications

Recent publications on tislelizumab have focused on its use in combination regimens across several solid tumors, with particular attention to neoadjuvant, first-line, and multimodal treatment strategies. In advanced epithelial ovarian cancer, the exploratory NAIVE phase II trial compared neoadjuvant platinum-based chemotherapy plus tislelizumab with chemotherapy alone in FIGO IIIC-IV disease. The combination showed numerically longer progression-free survival, higher 1-year and 2-year PFS rates, improved objective response and R0 resection rates, and more complete pathological responses, while maintaining manageable immune-related adverse events and no unexpected safety signals. Immune profiling suggested that response may be linked to a CXCL13+Th1-GC B-cell-tertiary lymphoid structure axis, with responders showing greater CD8+ T-cell-mediated toxicity and metabolic fitness.

In non-small cell lung cancer, recent work has included both clinical outcome analyses and formulation development. A model-informed phase 1 study evaluated subcutaneous tislelizumab in treatment-naïve patients with locally advanced or metastatic NSCLC, using population pharmacokinetic modeling to compare thigh and abdominal administration with intravenous dosing. Subcutaneous thigh administration showed greater bioavailability and lower variability than abdominal administration, and simulations supported 300 mg every 3 weeks as providing exposure comparable to intravenous 200 mg every 3 weeks, supporting phase 3 selection. Separately, the RATIONALE-307 trial was revisited to examine associations between patient-reported outcomes and overall survival in advanced squamous NSCLC, building on prior findings that tislelizumab plus chemotherapy improved survival and symptoms. In advanced squamous NSCLC, the HARMONi-6 trial also compared ivonescimab plus chemotherapy with tislelizumab plus chemotherapy, with the latter serving as the active comparator in an interim overall survival analysis.

Other studies have examined tislelizumab in gastrointestinal and hepatobiliary malignancies and in bladder cancer. In HER2-positive gastroesophageal cancer, zanidatamab with chemotherapy was studied with and without tislelizumab, with the abstract noting encouraging efficacy and safety for the broader first-line phase 2 strategy. In advanced oesophageal squamous cell carcinoma, a Markov modeling study assessed the value-based price range at which tislelizumab plus chemotherapy would be cost-effective versus chemotherapy alone. In hepatocellular carcinoma, the AdvanTIG-206 phase II trial investigated ociperlimab plus tislelizumab and BAT1706 versus tislelizumab and BAT1706 in first-line disease. In locally advanced esophageal squamous cell carcinoma, tislelizumab has also been studied with induction chemotherapy and concurrent chemoradiotherapy, including PET/CT-guided neoadjuvant approaches in resectable disease and a multicenter randomized phase II trial in unresectable disease.

Additional publications highlight tislelizumab combinations in less common thoracic and urologic settings. A single-arm phase II study evaluated tislelizumab plus anlotinib as first-line therapy in advanced pulmonary sarcomatoid carcinoma. In very high-risk nonmuscle-invasive bladder cancer, a study examined MRI-derived radiomic phenotypes to stratify response and define immune states in patients treated with tislelizumab plus nanoparticle albumin-bound paclitaxel, aiming to improve biomarker-guided selection for checkpoint inhibitor-based therapy. Across these reports, tislelizumab is being explored as a programmed cell death 1-targeting backbone for combination treatment, with ongoing efforts to refine efficacy, safety, delivery, and predictive biomarkers.

Key Publications

• NEWJul Neoadjuvant tislelizumab (anti-PD-1 antibody) plus chemotherapy in patients with advanced epithelial ovarian cancer: the exploratory NAIVE trial. (Signal transduction and targeted therapy, 2026, PMID 42399240): "To clarify these effects, the NAIVE trial (NCT04815408), a prospective phase II study, evaluated the efficacy of neoadjuvant platinum-based chemotherapy with tislelizumab (NACI) in comparison with chemotherapy alone (NAC) in patients with FIGO IIIC-IV EOC."
• NEWJul Model-Informed Development of a Subcutaneous Formulation of Tislelizumab: Phase 1 Pharmacokinetics in Patients With Cancer. (Clinical and translational science, 2026, PMID 42337921): "Although tislelizumab is approved across multiple malignancies and dosing schedules, intravenous administration imposes logistical burdens."
• NEWJul Magnetic resonance imaging radiomic phenotypes stratify response and define immune states in very high-risk, nonmuscle-invasive bladder cancer treated with tislelizumab plus nanoparticle albumin-bound paclitaxel. (Cancer, 2026, PMID 42339693): "...response to immune checkpoint inhibitor-based therapy."
• NEWJun Prognostic associations between patient-reported outcomes and overall survival among patients with advanced squamous non-small cell lung cancer: results from the RATIONALE-307 trial. (Quality of life research : an international journal of quality of life aspects of treatment, care and rehabilitation, 2026, PMID 42319531): "In the RATIONALE-307 trial, favorable overall survival (OS) outcomes with tislelizumab plus chemotherapy versus chemotherapy alone have been reported, along with improvements in patient-reported outcomes (PROs), including global health status/quality of life (GHS/QoL) and lung cancer-specific symptoms such as cough and dyspnea."
• May Ivonescimab plus chemotherapy versus tislelizumab plus chemotherapy in advanced squamous non-small-cell lung cancer (HARMONi-6): interim overall survival analysis of a randomised, double-blind, phase 3 trial in China. (Lancet (London, England), 2026, PMID 42218899): "In our previous report of the HARMONi-6 study, we aimed to evaluate the efficacy and safety of ivonescimab plus chemotherapy versus tislelizumab plus chemotherapy as a first-line therapy for patients with advanced squamous NSCLC."
• May Zanidatamab with and without Tislelizumab in HER2-Positive Gastroesophageal Cancer. (The New England journal of medicine, 2026, PMID 42202319): "Zanidatamab, a dual human epidermal growth factor receptor 2 (HER2)-targeted bispecific antibody, plus chemotherapy both with and without tislelizumab (anti-programmed death 1), showed encouraging efficacy and safety as first-line therapy in phase 2 studies involving patients with HER2-positive gastroesophageal adenocarcinoma."
• May Value-based pricing of tislelizumab plus chemotherapy versus chemotherapy alone for advanced oesophageal squamous cell carcinoma: a Markov modelling study from the US payer perspective. (BMJ open, 2026, PMID 42203284): "This study aimed to determine the value-based price range at which tislelizumab combined with chemotherapy becomes cost-effective compared with chemotherapy alone for treating advanced oesophageal squamous cell carcinoma."
• Apr AdvanTIG-206: a phase II, randomized study of ociperlimab plus tislelizumab and BAT1706 (bevacizumab biosimilar) versus tislelizumab and BAT1706 in first-line hepatocellular carcinoma. (Cancer immunology, immunotherapy : CII, 2026, PMID 42047833): "This phase II trial investigated the efficacy and safety of ociperlimab and tislelizumab plus BAT1706 (a bevacizumab biosimilar) in patients with first-line HCC."
• Apr Tislelizumab Combined With Induction Chemotherapy and Concurrent Chemoradiotherapy in Locally Advanced Esophageal Squamous Cell Carcinoma: A Multicenter, Randomized, Phase II Trial (EC-CRT-002). (Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 2026, PMID 41962116): "To evaluate the efficacy and safety of adding tislelizumab to induction chemotherapy and concurrent chemoradiotherapy (CRT), with or without maintenance immunotherapy, in patients with unresectable locally advanced esophageal squamous cell carcinoma (ESCC)."
• Jun The Efficacy and Safety of Tislelizumab plus Anlotinib as First-line Treatment in Advanced Pulmonary Sarcomatoid Carcinoma: A Single-Arm Phase II Trial. (Clinical cancer research : an official journal of the American Association for Cancer Research, 2026, PMID 41894181): "to evaluate the efficacy and safety of tislelizumab in combination with anlotinib as first-line therapy in patients with advanced PSC."