Investigational new drug (IND) application of SC-102 was approved by CDE of NMPA

On August 8, 2024, Conjustar Biologics announced that the investigational new drug (IND) application for the company's second peptide-drug conjugate (PDC), SC-102 for Injection, for the treatment of advanced malignant solid tumors expressing EphA2, was approved by the Center for Drug Evaluation (CDE) of the Chinese National Medical Products Administration. SC-102 is a peptide-drug conjugate (PDC) consisting of a peptide targeting the EphA2 protein and a microtubule inhibitor, MMAE, conjugated by a protease-cleavable linker.

EphA2 (Ephrin receptor A2) belongs to the ephrin receptor protein family and is a type of receptor tyrosine kinase (RTK). EphA2 is highly expressed in various cancer cells, such as prostate cancer, lung cancer, esophageal cancer, colorectal cancer, cervical cancer, ovarian cancer, breast cancer, and skin cancer. Upregulation of EphA2 expression is closely related to malignant transformation of cells, proliferation, motility, invasion, and metastasis of tumor cells, angiogenesis in the tumor microenvironment, and poor prognosis in patients. In addition, EphA2 is also involved in mediating the acquired resistance of tumor cells to various antitumor therapeutic drugs. EphA2 provides a new research direction and potential therapeutic target for antitumor treatment. Currently, most EphA2-targeted drug candidates are in the preclinical stage, and SC-102 is the first EphA2-targeted drug approved for clinical trials in China.

Preclinical studies results have shown that SC-102 can bind the target, EphA2, with high affinity and selectivity. Moreover, in vivo tumor models have demonstrated that SC-102 rapidly accumulates at the tumor site after administration and releases toxins within tumor cells, with toxins maintaining high concentrations in the tumor for an extended period, supporting a once-weekly dosing frequency for SC-102 in clinical settings. SC-102 has exhibited strong antitumor effects in multiple CDX and PDX tumor models. Furthermore, DMPK and toxicology studies have shown that SC-102 has favorable distribution and metabolic properties in vivo, with good safety. In addition, SC-102 is synthesized by solid-phase synthesis, resulting in uniform components, and controllable production costs. Conjustar Biologics will initiate the clinical trial of SC-102 to verify the antitumor efficacy in patients this year, ultimately providing more effective and safe innovative therapy for patients with advanced tumors that express EphA2