Jiangsu Vcare's Second-Generation Selective JAK1 Inhibitor VC005 Tablet Completes First Patient Dosing in Phase II Clinical Trial for Ankylosing Spondylitis

　　The second-generation selective JAK1 inhibitor VC005 Tablet, independently developed by Jiangsu Vcare PharmaTech Co., Ltd. (Jiangsu Vcare), recently initiated its Phase II clinical study for ankylosing spondylitis (AS). On April 26th, the first patient was successfully dosed at Peking University People's Hospital. VC005 Tablet demonstrated favorable metabolic properties, safety, and tolerability in the completed Phase I clinical study. Currently, in addition to the AS trial, multiple Phase II clinical studies for VC005 Tablet in oral treatment of conditions like atopic dermatitis are also being successively initiated.

　　About VC005

　　VC005 is a novel, highly potent, and selective second-generation JAK1 inhibitor independently developed by Jiangsu Vcare. By selectively inhibiting JAK1, the drug reduces inflammatory responses and immune cell activation, thereby achieving therapeutic effects in inflammatory and autoimmune diseases. Compared to Upadacitinib(a currently marketed JAK inhibitor), VC005 exhibits lower JAK2 inhibitory activity(based on in vitro kinase assays), which may mitigate safety concerns associated with excessive JAK2 inhibition. The drug is currently being developed in two formulations: oral tablets and topical gel.

　　About JAK1

　　The JAK/STAT signaling pathway, mediated by JAK family kinases and downstream STAT transcription factors, plays a critical regulatory role in inflammatory and autoimmune diseases such as AS and AD. Current first-generation pan-JAK inhibitors non-selectively inhibit multiple JAK subtypes (e.g., JAK1, JAK2, JAK3, TYK2) at similar potency levels. Excessive JAK2 inhibition is associated with severe adverse events, prompting the U.S. FDA to issue black box warnings for these agents. Consequently, second-generation selective JAK1 inhibitors like VC005, designed for enhanced safety and efficacy, represent a necessary evolution in therapy.

　　　About AS

　　AS is a chronic inflammatory disease primarily affecting the sacroiliac joints, spine, paravertebral soft tissues, and peripheral joints, potentially causing structural damage, spinal deformity, and disability.

　　Prevalence: The Prevalence of AS in China is approximately 0.36%, affecting over 5 million individuals. Demographics: AS predominantly affects males aged between 15–40, with onset typically occur before the age of 35. Pathogenesis: The pathogenesis of AS is associated with genetic, infectious, environmental, and immunological factors. The disease progresses over time, often resulting in irreversible damage. Treatment: JAK inhibitors, which are non-immunogenic small-molecule drugs, avoid secondary failure caused by neutralizing antibodies (common with biologics), offering a promising therapeutic approach.