GenSci139 / GeneScience - LARVOL DELTA

Dual Targeting of EGFR and HER2 by a Bispecific Antibody-Drug Conjugate Demonstrates Broad Antitumor Activity in Multiple Solid Tumors. (PubMed, Mol Cancer Ther) - "While HER2-directed antibody-drug conjugates (ADCs), such as ENHERTU® (DS-8201), represent a major therapeutic advance, treatment options for tumors with low HER2 expression remain limited, and acquired resistance continues to pose a significant clinical challenge. Mechanistic studies revealed that GenSci139 induced DNA damage, apoptosis, and hallmarks of immunogenic cell death, suggesting potential for synergistic combination with immunotherapies. Collectively, our preclinical data position GenSci139 as a promising novel therapeutic candidate with the potential to address the unmet medical need in a broad spectrum of solid tumors, including those of the lung, breast and stomach."

IO biomarker • Journal • Oncology • Solid Tumor • EGFR • HER-2

A phase I, first-in-human study to evaluate the safety, tolerability, pharmacokinetics, and preliminary anti-tumor activities of GenSci139 in patients with solid tumors. (ASCO 2026) - P1 | "In preclinical studies, GenSci139 demonstrated broad-spectrum efficacy, surpassing ENHERTU in HER2-low tumor models. After determination of the MTD/RDE, Part 2 will evaluate the preliminary anti-tumor activity of GenSci139, with primary endpoints including objective response rate (ORR), disease control rate (DCR) and Duration of response (DoR). The study initiated in December 2025 and is currently recruiting."

Clinical • First-in-human • P1 data • PK/PD data • Breast Cancer • Gastric Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • Urothelial Cancer • EGFR • HER-2

Towards a platform PBPK-QSP model for first-in-human dose selection of GenSci139, a potential best-in-class EGFR×HER2 bispecific ADC, in patients with cancer (AACR 2026) - P1 | "Monkey PBPK model of GenSci139 and clinical PBPK models of trastuzumab (mAb targeting HER2) and cetuximab (mAb targeting EGFR) were developed to enable the estimation of human EGFR/HER2 expression across tissues. The whole-body PBPK-QSP model was developed to mechanistically elucidate the dose-exposure-efficacy relationship of GenSci139. This model will incorporate toxicity predictions for a comprehensive dose-exposure-efficacy/toxicity profile as clinical data emerging. It represents a step toward an integrated platform PBPK-QSP model capable of facilitating ADC design, lead candidate selection, and clinical dose optimization."

ADC • Bispecific • Clinical • First-in-human • Late-breaking abstract • P1 data • Bladder Cancer • Genito-urinary Cancer • Oncology • Solid Tumor • EGFR • HER-2

GenSci139, a highly differentiated EGFR×HER2 bispecific ADC, for the treatment of multiple solid tumors (AACR 2025) - "These data suggest the potential of GenSci139 as a novel and effective therapy across a variety of tumor types, including urothelial cancer, lung cancer, gastric cancer, colorectal cancer, ovarian cancer, breast cancer, etc., and support its further evaluation in IND-enabling studies."

ADC • Bispecific • IO biomarker • Breast Cancer • Colorectal Cancer • Gastric Cancer • Genito-urinary Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Solid Tumor • Urothelial Cancer • EGFR • HER-2

GenSci139-101: GenSci139 in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=280 | Recruiting | Sponsor: Changchun GeneScience Pharmaceutical Co., Ltd. | Not yet recruiting ➔ Recruiting

Enrollment open • First-in-human • Oncology • Solid Tumor

GenSci139 in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=280 | Not yet recruiting | Sponsor: Changchun GeneScience Pharmaceutical Co., Ltd.

First-in-human • New P1 trial • Oncology • Solid Tumor

GenSci139: A highly differentiated and potential best-in-class EGFRxHER2 bispecific ADC, in multiple solid tumors (ESMO 2025) - "Background ENHERTU®, a HER2-targeting ADC, has been approved for the treatment in multiple indications, yet significant unmet needs persist in HER2-low settings beyond breast cancer. These results position GenSci139 as a promising therapeutic candidate for further clinical development in NSCLC, GC, TNBC and other EGFR/HER2-driven malignancies. Legal entity responsible for the study GeneScience Pharmaceutical Co., Ltd."

IO biomarker • Breast Cancer • Gastric Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • EGFR • HER-2