2024年5月24日 · RZ402 是一种选择性口服小分子血浆激肽释放酶抑制剂（KLKB1），用于慢性治疗糖尿病性黄斑水肿（DME）， RZ-402 通过抑制激肽释放酶的形成， 阻断下游缓激肽的产生以及促炎、促凝血和漏液接触激活级联反应。 2021 年， Rezolute 报告了首次人体 1a 期单次递增剂量研究结果，表明 RZ-402 在所有测试剂量下通常是安全且耐受良好的，没有剂量限制性毒性。 在动物研究中， RZ-402 被证明可以抑制血管渗漏（高达 90%）和视网膜白细胞停滞（> 90%）。 …

2024年4月26日 · Diabetic macular edema (DME) is another area where PKa inhibitors are being extensively researched. Studies in DME patients have shown that PKa levels in the vitreous are more elevated than vascular endothelial growth factor (VEGF) levels are, and this difference is thought to contribute to the incomplete or delayed response to anti-VEGF ...

2020年9月1日 · Discover the latest findings on diabetic macular edema (DME) treatments, including the potential of a VEGF-independent pathway for preservation and recovery of vision. Learn about the emerging role of plasma kallikrein inhibition and …

Diabetic Macular Edema (DME) Announced positive topline results in May of 2024 from the Phase 2 proof-of-concept study of RZ402 in patients with DME. The study met primary endpoints, demonstrating good safety and tolerability, and a significant reduction in central subfield thickness (CST) in the Study Eye at all RZ402 dose levels compared to ...

2021年8月10日 · DME is a severe vision-threatening complication of DR characterized by swelling of the retina and thickening of the macula, the part of the eye that is responsible for high-resolution vision. Anti-vascular growth factor (anti-VEGF) injections into the eye are the current standard of care for DME, requiring continued administration over long ...

2024年10月21日 · The kallikrein-kinin system (KKS) is considered to contribute to DME in a VEGF-independent pathway, where the overactivation of plasma kallikrein ensues in inflammation and subsequent macular edema.

Diabetic Macular Edema (DME) is a severe, systemic, vision-threatening complication of diabetic retinopathy (DR) characterized by swelling of the retina and thickening of the macula, the part of the eye that is responsible for high-resolution vision.

Purpose : Excessive retinal vascular permeability (VP) is the key defining pathology underlying the development of diabetic macular edema (DME). The serine protease plasma kallikrein (PK) generates the vasoactive peptide bradykinin, a known mediator of VP.

2023年3月28日 · DR是糖尿病导致的视网膜微血管损害所引起的一系列病变；糖尿病黄斑水肿（DME）则是由于黄斑区毛细血管渗漏所致的视网膜增厚，主要影响中心视力。 DME是糖尿病患者眼睛中常见的并发症。 高血糖会导致眼部血管受损，液体渗漏到黄斑时，会发生糖尿病性黄斑水肿。 这可能导致视力丧失，在某些情况下甚至失明。 在全球范围内，目前有1.46亿人患有糖尿病视网膜病变（DR），其可发展为更严重的情况，即糖尿病黄斑水肿（DME）。 《我国糖尿病 …

2018年7月25日 · BCX7353 is a potent oral small-molecule inhibitor of plasma kallikrein with a pharmacokinetic and pharmacodynamic profile that may help prevent angioedema attacks.