TSN222 / Tyligand Bioscience - LARVOL DELTA

Dual action tumor immune agonist (DATIA) ADCs activating STING pathway and subsequently inducing cytotoxicity of tumor cells exhibits potent and lasting in vivo tumor growth inhibition in multiple preclinical tumor antigen positive cancer models (AACR 2025) - "Introduction : TSN222, currently in Phase 1 clinical development for solid tumors, is a novel dual action tumor immune agonist (DATIA) via intratumoral administration...The dual action of STING pathway activation and subsequent induction of apoptotic signals in tumor cells by the moderately toxic metabolite renders timely presentation of antigens to bridge the innate and adaptive immune system. With the preclinical proof-of-concept studies and ongoing clinical trial data of the payload to inform on safety and tolerability, the DATIA ADC platform is positioned to serve as a distinctly different approach for better safety and efficacy."

ADC • Preclinical • Tumor cell • Breast Cancer • Colorectal Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • CLDN18

Safety and efficacy results of phase I/II first-in-human study of TSN222 in patients with advanced malignancies (ESMO 2025) - P1/2 | "Conclusions TSN222 was well tolerated with favorable PK and efficacy profile in pts with heavily pretreated malignant tumors, differentiating from previous STING agonists by mechanism of action and clinical outcomes. These data warrant the further investigation of TSN222 via i.t. injection and inform its tolerance and efficacy potential as a payload for ADC development."

Clinical • First-in-human • IO biomarker • Metastases • P1/2 data • Breast Cancer • Melanoma • Oncology • Sarcoma • Solid Tumor • CD4 • CD8 • PD-L1

Phase 1/2 study of TSN222, a novel dual action tumor immune agonist (DATIA), in patients with advanced malignancies. (ASCO 2025) - P1/2 | "TSN222 was well tolerated with favorable PK profile and promising antitumor activity in patients with heavily pretreated advanced tumors. In addition to monotherapy, the differentiated safety profile of TSN222 supports the exploration of diverse combination therapies in clinical trials. Current data also informs the tolerance and efficacy potential of TSN222 as a promising payload for antibody drug conjugates (ADCs) development."

Clinical • IO biomarker • Metastases • P1/2 data • Fibrosarcoma • Hematological Malignancies • Liposarcoma • Lymphoma • Melanoma • Oncology • Pain • Sarcoma • Soft Tissue Sarcoma • Solid Tumor • CD4 • CD8 • PD-L1 • STING

TSN222 in Subjects With Advanced Solid Tumors or Lymphomas (clinicaltrials.gov) - P1/2 | N=162 | Recruiting | Sponsor: Tyligand Bioscience (Shanghai) Limited | Not yet recruiting ➔ Recruiting

Enrollment open • Metastases • Head and Neck Cancer • Hematological Malignancies • Lymphoma • Melanoma • Oncology • Solid Tumor • Squamous Cell Carcinoma of Head and Neck • BRAF

TSN222 in Subjects With Advanced Solid Tumors or Lymphomas (clinicaltrials.gov) - P1/2 | N=162 | Not yet recruiting | Sponsor: Tyligand Bioscience (Shanghai) Limited

New P1/2 trial • Head and Neck Cancer • Hematological Malignancies • Lymphoma • Melanoma • Oncology • Solid Tumor • Squamous Cell Carcinoma of Head and Neck • BRAF