Plasma Kallikrein/KLKB1 Overview
Molecule Name
Plasma kallikrein
Synonyms
Fletcher factor,kallikrein B, plasma (Fletcher factor) 1,kininogenin,KLK3 plasma kallikrein,KLKB1,plasma kallikrein heavy chain,plasma kallikrein light chain,Plasma Kallikrein,Plasma Prekallikrein,PPK,KLKB1
Drug Development Progress
Drugs in Clinical Trials13
Approved Drugs4
Highest Development StageApproved
Target Synonym
EC:3.4.21.34，EC 3.4.21，Fletcher factor，Plasma prekallikrein，KLKB1，Kallikrein B1，Kallikrein B， Plasma (Fletcher Factor) 1，Kininogenin，KLK3，PKK，Plasma Kallikrein，EC 3.4.21.34，PKKD，PPK，PKal，pKAL
Background
Human Plasma Kallikrein, a serine protease, is synthesized in the liver and circulates in the plasma by binding to high molecular weight (HMW) kininogen or as a free zymogen. The enzyme cleaves Lys-Arg and Arg-Ser bonds. It activates, in a reciprocal reaction, factor XII after its binding to a negatively charged surface. It also releases bradykinin from HMW kininogen and may also play a role in the renin-angiotensin system by converting prorenin into renin.
Plasma Kallikrein/KLKB1 Product List
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Clinical Drug Information
| English Name | Research Code | Highest Development Stage | Company | Indication | Clinical Trial |
|---|---|---|---|---|---|
| Navenibart | QLS-215; STAR-0215 | Phase 3 Clinical | Quellis Biosciences Inc | Angioedemas, Hereditary | Details |
| ADX-324 | ADX-324; ADX324 | Phase 3 Clinical | ADARx Pharmaceuticals Inc | Angioedemas, Hereditary | Details |
| Lonvoguran Ziclumeran | NTLA-2002 | Phase 3 Clinical | Intellia Therapeutics Inc | Angioedemas, Hereditary | Details |
| THR-149 | TG-758; THR-149 | Phase 2 Clinical | Bicycle Therapeutics, Thrombogenics Inc | Diabetes Mellitus; Diabetic macular oedema; Diabetic Retinopathy | Details |
| BW-20805 | BW-20805; BW20805 | Phase 2 Clinical | Hangzhou Bolin Pharmaceutical Technology Co Ltd | Angioedemas, Hereditary | Details |
| MDPK-67b | DM-107; MDPK-67; MDPK-67b; MDKP 67b; RIK-7 | Phase 1 Clinical | Med Discovery | Prostatic Neoplasms | Details |
| MSB-03 | MSB-03 | Phase 1 Clinical | MatriSys Bioscience Inc | Rosacea | Details |
| Avoralstat | BCX-V; BCX-4161 | Phase 1 Clinical | Biocryst Pharmaceuticals Inc | Angioedemas, Hereditary; Diabetic macular oedema | Details |
| ADX-324(Tenacia) | ADX324; ADX-324 | Phase 1 Clinical | Yuanyi Biotechnology (Shanghai) Co., Ltd. | Angioedemas, Hereditary | Details |
| ZKLJ-02 | Phase 1 Clinical | Kunming Longjin Pharmaceutical Co Ltd | Cardiovascular Diseases; Ischemic Stroke; Nervous System Diseases; Stroke | Details | |
| ATN-249 | ATN-249 | Phase 1 Clinical | Attune Pharmaceuticals | Angioedemas, Hereditary | Details |
| BI-Z | Clinical | Boehringer Ingelheim Pharma Gmbh & Co Kg | Wet Macular Degeneration | Details | |
| mRNA encoded Cas9 targeting human KLKB 1 gene therapy (Pharma Gateway) | Clinical | Pharma Gateway AB | Angioedemas, Hereditary | Details |
Marketed Drug Information
| English Name | Research Code | Highest Development Stage | Company | First Brand Name | First Approved Country | First Indication | First Approved Company | First Approved Date | Indication | Clinical Trial |
|---|---|---|---|---|---|---|---|---|---|---|
| Lanadelumab | 2372V1TKXK (UNII code); X124-G01; SHP-643; DX-2930; TAK-743 | Approved | Dyax Pharma | Takhzyro, 达泽优 | United States | Angioedemas, Hereditary | Dyax Corp | 2018-08-23 | Angioedema; Angioedemas, Hereditary; Coronavirus Disease 2019 (COVID-19); Hereditary Autoinflammatory Diseases; Lung Injury | Details |
| Berotralstat | BCX-7353 | Approved | Biocryst Pharmaceuticals Inc | ORLADEYO | United States | Angioedemas, Hereditary | Biocryst Pharmaceuticals Inc | 2020-12-03 | Angioedemas, Hereditary | Details |
| Ecallantide | DX-88; EPI-KAL2; FOV-2302; CB-500929 | Approved | Dyax Pharma | Kalbitor | United States | Angioedema | Dyax Corp | 2009-12-01 | Angioedema; Angioedemas, Hereditary; Blood Loss, Surgical; Hemorrhage; Hereditary Angioedema Types I and II; Macular Edema; Retinal Vein Occlusion | Details |
| Sebetralstat | KVD-900 | Approved | Vantia Therapeutics Ltd. | Ekterly | United States | Angioedemas, Hereditary | Kalvista Pharmaceuticals Ltd, Kalvista Pharmaceuticals Inc | 2025-07-03 | Angioedemas, Hereditary | Details |