SUZHOU, China, May 22, 2024 /PRNewswire/ -- Alphamab Oncology (stock code: 9966.HK) announced 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.

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.

About Alphamab Oncology

Alphamab Oncology is a leading biopharmaceutical company committed to the discovery, development, manufacturing, and commercialization of cutting-edge biotherapeutics for the treatment of cancer. On December 12, 2019, the company was successfully listed on the Main Board of the Hong Kong Stock Exchange, trading under the stock code 9966.