Core Viewpoint - Crystal Technology (晶泰科技) announced a significant milestone in clinical research for the next-generation PRMT5 inhibitor PEP08, which has received clinical trial approvals from regulatory bodies in Australia and Taiwan, marking the initiation of Phase I clinical trials [1][3]. Group 1: Clinical Development - PEP08 has been approved for clinical trials by the Human Research Ethics Committee (HREC) in Australia, the Therapeutic Goods Administration (TGA), and the Taiwan Food and Drug Administration (TFDA) [1]. - The approval signifies a major step forward in the collaboration between Crystal Technology and PharmaEngine, leading to milestone payments for Crystal Technology [1][3]. Group 2: Drug Characteristics - PRMT5 is a key enzyme overexpressed in various cancers, and inhibiting its activity can lead to a "synthetic lethality" effect in tumors with homozygous deletion of MTAP, which accounts for approximately 10-15% of human cancers [1]. - PEP08, as a second-generation PRMT5 inhibitor, exhibits high activity and selectivity, forming a stable ternary complex with PRMT5, specifically targeting MTAP-deficient tumor cells while minimizing effects on normal cells [2][3]. Group 3: Preclinical Research - Preclinical data indicate that PEP08 shows significant advantages in toxicity and safety compared to first-generation non-selective PRMT5 inhibitors, with good blood-brain barrier penetration and ideal overall drug-like properties [3]. - PEP08 demonstrates strong in vivo efficacy at lower doses in multiple animal efficacy models, suggesting potential best-in-class effects and broad potential for combination with other therapies [3].
晶泰科技(02228)助力智擎生技新一代“合成致死”新药获临床实验审批 AI制药再迎里程碑