On May 22, 2024 Alphamab Oncology (stock code: 9966.HK) reported that the first patient has been successfully dosed in the phase I clinical study (JSKN016-101) of JSKN016, a novel bispecific antibody-drug conjugate (ADC) targeting HER3 and TROP2, in the treatment of Chinese patients with advanced malignant solid tumors.
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Trophoblast cell surface antigen 2 (TROP2) is widely expressed in solid tumors, and its up-regulation can stimulate tumor growth, proliferation and invasion. Studies have showed that high TROP2 expression was observed in 64% of lung adenocarcinomas, 75% of lung squamous cell carcinoma, and up to 78% of breast cancer. Overexpression of Human epidermal growth factor receptor 3 (HER3) may be associated with poor prognosis of a variety of solid tumors such as lung cancer, breast cancer, gastric cancer, ovarian cancer, and melanoma. Therefore, molecules targeting TROP2 or HER3 may play anti-tumor activity in solid tumors.
JSKN016 is a bispecific antibody-drug conjugate (ADC) simultaneously targeting HER3 and TROP2, which is independently developed by Alphamab. After binding with TROP2 and/or HER3 on the surface of tumor cells, JSKN016 enters the lysosome through target-mediated endocytosis, releasing cytotoxic topoisomerase I inhibitor (TOPIi), and then inducing apoptosis of TROP2 and/or HER3 positive tumor cells. In addition, the inhibitor can penetrate the cell membrane and enter the antigen-negative tumor cells to exert bystander effect. These effects can effectively inhibit the growth of tumor cells.
JSKN016-101 is an open-label, multi-center, first-in-human (FIH) phase I clinical trial of JSKN016, including dose-escalating and dose-expansion phases. The primary endpoint is to evaluate the safety, tolerability, pharmacokinetics (PK)/pharmacodynamics, and antitumor activity of JSKN016 in Chinese patients with advanced malignant solid tumors, as well as to determine the maximum tolerated dose (MTD) and/or the recommended phase II dose (RP2D).
About JSKN016
JSKN016 is a bispecific antibody-drug conjugate (ADC) targeting HER3 and TROP2, which is developed inhouse with proprietary Glycan-specific conjugation platform. JSKN016 can induce apoptosis of TROP2 or HER3 positive tumor cells, and penetrate the cell membrane into antigen-negative tumor cells to exert bystander effect, thus effectively inhibiting the growth of tumor cells. The phase I clinical study of JSKN016 for the treatment of advanced malignant solid tumors is currently being conducted in China.
(Press release, Alphamab, MAY 22, 2024, View Source [SID1234657013])