First Dosing of Participant in the First Clinical Trial of Jiangsu Vcare's Highly Selective JAK1 Inhibitor VC005 Tablets

　　On November 19, 2021, the first clinical trial participant was dosed with VC005 tablets, a highly selective JAK1 inhibitor independently developed by Jiangsu Vcare PharmaTech Co., Ltd. (Jiangsu Vcare). The dosing was completed at the Phase I Clinical Research Center of the First Hospital of Jilin University, and the participant has now successfully completed the safety observation period.

　　About VC005

　　VC005 tablets is a novel, potent, and highly selective JAK1 inhibitor independently developed by Jiangsu Vcare. The drug selectively inhibits JAK1, thereby suppressing immune cell-mediated cytotoxicity and immune responses, while exhibiting weaker inhibitory activity against JAK2 and JAK3. VC005 tablets received clinical trial implied permission from the NMPA on August 31st, 2021, for the indication of inflammatory bowel disease (IBD).

　　About JAK1

　　The JAK-STAT pathway plays a crucial role in the pathogenesis of diseases such as IBD. Currently marketed oral JAK inhibitors, due to their low selectivity, inhibit JAK1 while also affecting targets like JAK2 and JAK3. This has resulted in significant adverse reactions in clinical settings, including anemia, infections, dyslipidemia, and malignancies, leading to FDA boxed warnings. Since the first half of 2021, the FDA has repeatedly delayed review decisions for pan-JAK inhibitor drugs, drawing intense attention from the biopharmaceutical industry. Consequently, the development of highly selective JAK1 inhibitors has become an key trend. Notably, no JAK inhibitors are currently approved in China for IBD, highlighting a critical unmet clinical need.

　　VC005's development strategy is rooted in differentiation, specifically addressing the aforementioned issues from the project initiation and design stages. Preclinical studies have confirmed that compared to drugs targeting the same pathway, VC005 demonstrates a lower effective dose, higher tolerated dose, and fewer side effects in animal models, suggesting potential dual advantages in both safety and efficacy. It holds promise to become a globally leading therapeutic option for autoimmune and inflammatory diseases.

　　About IBD

　　IBD is a group of non-specific, chronic inflammatory intestinal disorders, primarily classified clinically as ulcerative colitis (UC) and Crohn's disease (CD). Key manifestations include abdominal pain/diarrhea, bloody stool, and weight loss, characterized by being difficult to cure, prone to relapse, and carrying a potential risk of malignant transformation. Epidemiologically, there are significant regional disparities globally. Western countries are in a compounded epidemic phase, with an incidence rate of 12-16 per 100,000 population. China is currently in an accelerating phase of the disease; owing to its large population base, the total number of cases reached 350,000 between 2005 and 2014, and is projected to reach 1.5 million by 2025, indicating a rapidly increasing prevalence. Regarding therapeutic drugs, small-molecule JAK inhibitors, unlike biologics, are non-immunogenic. This characteristic enables them to effectively avoid secondary failure caused by neutralizing antibodies in humans.