alcestobart (LBL-007) / Leads Biolabs - LARVOL DELTA

Phase 2 Study of Investigational Agents Plus Tislelizumab ± Chemotherapy in Untreated Locally Advanced/Metastatic NSCLC (IASLC-WCLC 2026) - P2 | "Investigational agents were BGB-A445 (OX40 agonist), LBL-007 (anti-LAG-3), and BGB-15025 (HPK1 inhibitor). Conclusions : Novel investigational agents in combination with tislelizumab ± chemotherapy were generally tolerable but did not improve efficacy in untreated, locally advanced/metastatic NSCLC. No new safety signals were identified."

IO biomarker • Metastases • P2 data • Lung Cancer • Non Small Cell Lung Cancer • Solid Tumor • PD-1 • PD-L1

BGB-A317-290-LTE1: Study of Tislelizumab, Pamiparib, and Other Investigational Agents in Participants With Advanced Malignancies (clinicaltrials.gov) - P3 | N=404 | Completed | Sponsor: BeOne Medicines | Active, not recruiting ➔ Completed

Trial completion • Oncology • Solid Tumor

BGB-A317-LBL-007-202: A Study to Evaluate LBL-007 in Combination With Tislelizumab Plus Chemotherapy in Participants With Unresectable Locally Advanced or Metastatic Esophageal Squamous Cell Carcinoma (clinicaltrials.gov) - P2 | N=118 | Completed | Sponsor: BeiGene | Active, not recruiting ➔ Completed

Trial completion • Esophageal Cancer • Esophageal Squamous Cell Carcinoma • Oncology • Squamous Cell Carcinoma

BGB-HNSCC-201: A Study of Tislelizumab in Combination With Investigational Agents in Participants With Head and Neck Squamous Cell Carcinoma (clinicaltrials.gov) - P2 | N=160 | Active, not recruiting | Sponsor: BeiGene | Completed ➔ Active, not recruiting

Enrollment closed • Head and Neck Cancer • Oncology • Solid Tumor • Squamous Cell Carcinoma • Squamous Cell Carcinoma of Head and Neck • PD-L1

A phase 2 study of tislelizumab (TIS) + investigational agents as first-line (1L) treatment in recurrent and/or metastatic head and neck squamous cell carcinoma (R/M HNSCC) (AACR 2026) - P2 | "Here, we present results from a phase 2, open-label, international study of TIS with or without the anti-TIM-3 mAb surzebiclimab (SUR) and/or the anti-LAG-3 mAb alcestobart (LBL-007 hereafter) as 1L treatment in pts with R/M HNSCC (NCT05909904). Eligible pts were ≥18 years with histologically/cytologically confirmed R/M HNSCC and positive PD-L1 expression CPS ≥1. Overall, efficacy was comparable between treatment arms. Safety profiles were consistent with previous reports. No additional benefit accrued from adding SUR, LBL-007, or SUR and LBL-007 to TIS as 1L treatment in pts with R/M HNSCC."

Clinical • IO biomarker • Metastases • P2 data • Head and Neck Cancer • Oncology • Solid Tumor • Squamous Cell Carcinoma • Squamous Cell Carcinoma of Head and Neck

Anti-LAG-3 antibody LBL-007 in combination with anti-PD-1 antibody toripalimab, in patients with advanced malignant tumors: A phase Ib/II, open-label, multicenter, dose escalation/expansion study (AACR 2024) - P1/2 | "LBL-007 in combination with toripalimab is well tolerated in patients with advanced malignant tumors and has demonstrated encouraging preliminary efficacy in patients with advanced NPC with or without prior anti-PD-(L)1 therapy. Clinical trial information: NCT05102006."

Clinical • Combination therapy • Metastases • P1/2 data • Esophageal Cancer • Esophageal Squamous Cell Carcinoma • Head and Neck Cancer • Lung Cancer • Nasopharyngeal Carcinoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Squamous Cell Carcinoma • Squamous Cell Carcinoma of Head and Neck

BGB‑A317‑LBL‑007‑202: A phase 2, randomized, active-controlled, open-label study to evaluate the efficacy and safety of LBL‑007 (anti-LAG-3) in combination with tislelizumab (TIS; anti-PD-1) plus chemotherapy (chemo) as first-line (1L) treatment in patients with unresectable locally advanced/metastatic esophageal squamous cell carcinoma (ESCC) (AACR 2024) - P2 | "The chemo doublet will consist of either cisplatin (60-80 mg/m2 IV Q3W) + 5-fluorouracil (750-800 mg/m2 IV daily on Days 1-5 Q3W), or cisplatin + paclitaxel (175 mg/m2 IV Q3W), determined by the investigator before randomization. Exploratory endpoints include comparison of overall survival, assessment of predictive, prognostic, and pharmacodynamic biomarkers, pharmacokinetic evaluation of LBL-007 and TIS, and immunogenicity. The study is currently recruiting at approximately 46 sites across Asia, including Taiwan, mainland China, South Korea, and Thailand."

Clinical • Combination therapy • IO biomarker • Metastases • P2 data • Esophageal Cancer • Esophageal Squamous Cell Carcinoma • Oncology • Squamous Cell Carcinoma • LAG3

Liberty-201: Maintenance fluoropyrimidine and bevacizumab with or without anti-lymphocyte activation gene-3 (LAG-3) antibody LBL-007 plus anti-programmed cell death protein-1 (PD-1) antibody tislelizumab (TIS) for patients (pts) with metastatic or unresectable microsatellite stable (MSS)/mismatch repair proficient (pMMR) colorectal cancer (CRC) (AACR 2024) - P1/2 | "Secondary endpoints include overall survival, PFS2, overall response rate, duration of response, safety, pharmacokinetics, and immunogenicity. Exploratory endpoints include potential biomarkers (including but not limited to PD-L1 and LAG-3)."

Clinical • IO biomarker • Metastases • Mismatch repair • pMMR • Colorectal Cancer • Gastrointestinal Cancer • Microsatellite Instability • Oncology • Solid Tumor • MSI • PD-L1

BGB-LC-201 (NCT05635708): A phase 2, open-label, multi-arm study of tislelizumab (TIS; anti-PD-1) in combination with investigational agents +/- chemotherapy as first-line treatment for patients with locally advanced, unresectable, or metastatic non-small cell lung cancer (NSCLC) (AACR 2024) - P2 | "This phase 2 study will determine whether adding investigational agents BGB-A445 (OX40 agonistic monoclonal antibody [mAb]), LBL-007 (anti-lymphocyte activation gene-3 mAb), or BGB-15025 (hematopoietic progenitor kinase 1 [HPK1] inhibitor) improves the therapeutic benefit of TIS (anti-PD-1 mAb) +/- chemo in patients with locally advanced, unresectable, or metastatic NSCLC. The umbrella design allows for the use of multiple investigational drugs, administered alone or in combination, in patients with untreated locally advanced, unresectable, or metastatic NSCLC without actionable driver mutations. Exploratory endpoints include overall survival, time to response, and relevant biomarker associations with response or resistance to study treatments. Enrollment is ongoing at 66 sites in China, Asia-Pacific, the United States, and the European Union."

Clinical • Combination therapy • IO biomarker • Metastases • P2 data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Translational assessment of triple combination with Tislelizumab (anti-PD-1), LBL-007 (anti-LAG-3) and Surzebiclimab (anti-TIM-3) highlights its strong anti-tumor activity and clinical potential in solid tumors such as HNSCC (AACR 2024) - P2 | "The concurrent blockade of PD-1/LAG-3/TIM-3 represents a promising strategy to enhance T cell function and anti-tumor activity. The results demonstrated the therapeutic potential of the triple combination. A Ph2 study evaluating Tisle in combination with LBL-007 and/or Surze in first-line treatment of recurrent or metastatic HNSCC (NCT05909904) is recruiting."

Clinical • IO biomarker • Colon Cancer • Colorectal Cancer • Head and Neck Cancer • Oncology • Solid Tumor • Squamous Cell Carcinoma • Squamous Cell Carcinoma of Head and Neck • IFNG

LBL-007-CN-004: A Phase Ib/II Clinical Trial of LBL-007 Combined With Tislelizumab in the Treatment of Malignant Tumors (clinicaltrials.gov) - P1/2 | N=98 | Completed | Sponsor: Nanjing Leads Biolabs Co.,Ltd | Recruiting ➔ Completed | N=490 ➔ 98 | Trial completion date: Jul 2026 ➔ Jan 2026 | Trial primary completion date: May 2026 ➔ Jan 2026

Enrollment change • Trial completion • Trial completion date • Trial primary completion date • Oncology • Solid Tumor

BGB-A317-290-LTE1: Study of Tislelizumab, Pamiparib, and Other Investigational Agents in Participants With Advanced Malignancies (clinicaltrials.gov) - P3 | N=404 | Active, not recruiting | Sponsor: BeOne Medicines | Enrolling by invitation ➔ Active, not recruiting

Enrollment closed • Oncology • Solid Tumor

BGB-HNSCC-201: A Study of Tislelizumab in Combination With Investigational Agents in Participants With Head and Neck Squamous Cell Carcinoma (clinicaltrials.gov) - P2 | N=160 | Completed | Sponsor: BeOne Medicines AG | Active, not recruiting ➔ Completed

Trial completion • Head and Neck Cancer • Oncology • Solid Tumor • Squamous Cell Carcinoma • Squamous Cell Carcinoma of Head and Neck • PD-L1

BGB-A317-290-LTE1: Study of Tislelizumab, Pamiparib, and Other Investigational Agents in Participants With Advanced Malignancies (clinicaltrials.gov) - P3 | N=430 | Enrolling by invitation | Sponsor: BeOne Medicines | Trial completion date: Dec 2026 ➔ Jul 2026 | Trial primary completion date: Dec 2026 ➔ Jul 2026

Trial completion date • Trial primary completion date • Oncology • Solid Tumor

A phase 2 study of LBL-007 (anti-LAG-3) plus tislelizumab (anti-PD-1) and chemotherapy as first-line treatment in patients with unresectable locally advanced/metastatic esophageal squamous cell carcinoma. (ASCO-GI 2026) - P2 | " In this phase 2, randomized, active-controlled, open-label trial (NCT06010303), pts ≥18 years with ECOG PS ≤1 and no prior systemic therapy were randomized 2:1 to LBL-007 (600 mg IV Q3W) + TIS (200 mg IV Q3W) + CT (Arm A; A) or TIS (200 mg IV Q3W) + CT (Arm B; B); CT was 60-80 mg/m2 cisplatin + 750‑800 mg/m2 5-FU or 175 mg/m2 paclitaxel IV Q3W... In pts with advanced/metastatic ESCC, adding LBL-007 to TIS + CT did not improve ORR versus TIS + CT alone, which was consistent with historical data in this population. PFS was numerically longer with LBL-007 but not statistically significant. The safety profile of the triplet was manageable and consistent with the known profiles of the individual agents."

Clinical • Metastases • P2 data • Esophageal Cancer • Esophageal Squamous Cell Carcinoma • Gastrointestinal Cancer • Oncology • PD-L1

Phase II Clinical Results of Leads Biolabs' Alcestobart in Treating Nasopharyngeal Carcinoma Published in Clinical Cancer Research (Leads Biolabs Press Release) - "With a median follow-up of 19.0 months, ORR was 83.3%, and DCR was 97.6%. Median PFS reached 15.8 months, Median DoR was 14.6 months, median OS was not reached."

P2 data • Nasopharyngeal Carcinoma

BGB-LC-201: A Study of Tislelizumab in Combination With Investigational Agents in Participants With Non-Small Cell Lung Cancer (clinicaltrials.gov) - P2 | N=400 | Active, not recruiting | Sponsor: BeiGene | Trial completion date: Oct 2025 ➔ Oct 2026 | Trial primary completion date: Oct 2025 ➔ Dec 2025

Trial completion date • Trial primary completion date • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • PD-L1

Anti-LAG-3 Antibody LBL-007 Plus Tislelizumab and Chemotherapy as First-Line Therapy for Advanced Nasopharyngeal Carcinoma: A Multicenter Phase 2 Trial. (PubMed, Clin Cancer Res) - "LBL-007 plus tislelizumab and chemotherapy shows promising clinical benefits and manageable toxicity as first-line therapy for RM-NPC. Dual-positive LAG-3/PD-L1 expression was associated with improved outcomes, supporting further exploration of this biomarker-defined subpopulation in randomized trials."

IO biomarker • Journal • P2 data • Nasopharyngeal Carcinoma • Oncology • Solid Tumor • PD-L1

BGB-A317-LBL-007-202: A Study to Evaluate LBL-007 in Combination With Tislelizumab Plus Chemotherapy in Participants With Unresectable Locally Advanced or Metastatic Esophageal Squamous Cell Carcinoma (clinicaltrials.gov) - P2 | N=118 | Active, not recruiting | Sponsor: BeiGene | Trial primary completion date: Sep 2024 ➔ May 2025

Trial primary completion date • Esophageal Cancer • Esophageal Squamous Cell Carcinoma • Oncology • Squamous Cell Carcinoma

LBL-007-CN-004: A Phase Ib/II Clinical Trial of LBL-007 Combined With Tislelizumab in the Treatment of Malignant Tumors (clinicaltrials.gov) - P1/2 | N=490 | Recruiting | Sponsor: Nanjing Leads Biolabs Co.,Ltd | Trial completion date: Dec 2025 ➔ Jul 2026 | Trial primary completion date: Oct 2025 ➔ May 2026

Trial completion date • Trial primary completion date • Oncology • Solid Tumor

Novel anti-LAG-3 antibody LBL-007 with anti-PD-1 blockade enhances antitumor immunity by promoting T cell-induced apoptosis. (PubMed, Sci Rep) - "The combination of LBL-007 and anti-PD-1 antibodies delayed tumor growth and promoted tumor cell apoptosis compared with monotherapy in human LAG-3 transgenic mice subjected to transplantation with colorectal tumor cells. Taken together, the combination of LBL-007 and anti-PD-1 antibodies plays an enhanced antitumor role by improving T cell viability and activity as well as by promoting T cell-induced apoptosis, thereby suggesting this combination as a potential effective strategy for cancer immunotherapy."

IO biomarker • Journal • Colorectal Cancer • Melanoma • Oncology • Solid Tumor • Transplantation • IL10 • IL2 • LAG3

A Phase 2 Multicenter Umbrella Trial Assessing Tislelizumab ± Anti-TIGIT or Anti-LAG-3 mAb ± Chemotherapy in Resectable NSCLC (IASLC-WCLC 2025) - P2 | "Patients with PD-L1 TC ≥50% were assigned to Substudy 1 and randomized to TIS (anti-PD-1; Arm 1A), TIS plus ociperlimab (anti-TIGIT; Arm 1B), or TIS plus LBL-007 (anti-LAG-3; Arm 1C); patients with PD-L1 TC <50% were assigned to Substudy 2 and randomized to TIS and chemotherapy (Arm 2A) or TIS plus LBL-007 and chemotherapy (Arm 2C). Conclusions : Neoadjuvant TIS as monotherapy or TIS-based immunotherapy combinations in PD-L1 TC ≥50% NSCLC had promising MPR/pCR; the addition of other immunotherapy to neoadjuvant TIS and chemotherapy in PD-L1 TC <50% did not provide additional efficacy benefit. Treatment guided by histology and PD-L1 expression is suggested for future exploration."

Clinical • IO biomarker • P2 data • Anemia • Hematological Disorders • Lung Cancer • Lung Non-Small Cell Squamous Cancer • Lung Non-Squamous Non-Small Cell Cancer • Non Small Cell Lung Cancer • Solid Tumor • ALK • EGFR • TIGIT

A Study to Assess LBL-007 in Combination With Toripalimab and Axitinib Tablets Subjects With Advanced Melanoma (clinicaltrials.gov) - P1 | N=79 | Completed | Sponsor: Nanjing Leads Biolabs Co.,Ltd | Recruiting ➔ Completed

Trial completion • Melanoma • Oncology • Solid Tumor

A Trial of LBL-024 Monotherapy, LBL-024 Combined With LBL-007 or Toripalimab in Patients With Advanced Melanoma (clinicaltrials.gov) - P1/2 | N=200 | Recruiting | Sponsor: Nanjing Leads Biolabs Co.,Ltd | Not yet recruiting ➔ Recruiting

Enrollment open • Monotherapy • Melanoma • Oncology • Solid Tumor

A Trial of LBL-024 Monotherapy, LBL-024 Combined With LBL-007 or Toripalimab in Patients With Advanced Melanoma (clinicaltrials.gov) - P1/2 | N=200 | Not yet recruiting | Sponsor: Nanjing Leads Biolabs Co.,Ltd

Monotherapy • New P1/2 trial • Melanoma • Oncology • Solid Tumor