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Molecular Mechanisms and Efficacy of Tislelizumab, a PD-1 Inhibitor Developed in China, in Non-Small Cell Lung Cancer.

Chemical biology & drug design 2026 Vol.107(2) p. e70252

Liu Y, Meng W, Pan L, Zhang H, He Q

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Lung cancer remains the leading cause of cancer incidence and mortality worldwide, with non-small cell lung cancer (NSCLC) accounting for approximately 85% of all lung cancer cases.

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  • 95% CI 1.19-1.65
  • HR 0.59
  • RR 1.40

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BibTeX ↓ RIS ↓
APA Liu Y, Meng W, et al. (2026). Molecular Mechanisms and Efficacy of Tislelizumab, a PD-1 Inhibitor Developed in China, in Non-Small Cell Lung Cancer.. Chemical biology & drug design, 107(2), e70252. https://doi.org/10.1111/cbdd.70252
MLA Liu Y, et al.. "Molecular Mechanisms and Efficacy of Tislelizumab, a PD-1 Inhibitor Developed in China, in Non-Small Cell Lung Cancer.." Chemical biology & drug design, vol. 107, no. 2, 2026, pp. e70252.
PMID 41606434
DOI 10.1111/cbdd.70252

Abstract

Lung cancer remains the leading cause of cancer incidence and mortality worldwide, with non-small cell lung cancer (NSCLC) accounting for approximately 85% of all lung cancer cases. Tislelizumab, a PD-1 inhibitor developed in China, has shown promising efficacy as a monotherapy and in combination with chemotherapy. This study examines the molecular structure of tislelizumab and its interaction with PD-1, along with its therapeutic effects and adverse reactions in NSCLC patients. Using GRAMM (Global Range Molecular Matching), protein-protein docking was conducted to analyze the binding affinity of tislelizumab with PD-1. A comprehensive search in PubMed, Embase, Cochrane Library, and Web of Science identified eligible studies, including randomized controlled trials (RCTs) and single-arm studies reporting survival outcomes, tumor responses, or adverse events. Tislelizumab significantly improved event-free survival (RR = 1.40, 95% CI: 1.19-1.65) and median progression-free survival (mPFS) by 1.77 months in RCTs, and reduced the risk of disease progression or death by 41% (HR = 0.59, 95% CI: 0.52-0.67). The overall survival risk was reduced by 35% (HR = 0.65, 95% CI: 0.59-0.73). The overall response rate (ORR) was higher in the tislelizumab group (RR = 1.86). In single-arm studies, the 1-year overall survival rate was 73.8%, with an ORR of 59.5%. AEs were generally manageable, with more frequent elevated ALT/AST, hypothyroidism, and rash, but fewer cases of anemia and neutropenia compared to chemotherapy. Tislelizumab significantly improves survival outcomes and tumor response rates in NSCLC patients, with an overall acceptable safety profile. For patients with suboptimal responses, dose adjustments or combination strategies may help improve efficacy.

MeSH Terms

Humans; Carcinoma, Non-Small-Cell Lung; Lung Neoplasms; Antibodies, Monoclonal, Humanized; Programmed Cell Death 1 Receptor; China; Molecular Docking Simulation; Antineoplastic Agents

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