Venomics Pty Ltd, PO Box 1810, North Sydney, NSW 2059, Australia.
Toxicon. 2012 Mar 15;59(4):456-63. doi: 10.1016/j.toxicon.2010.12.010. Epub 2010 Dec 22.
Snake venoms are attractive for drug discovery and development, with a number of therapeutics derived from snake venom either in clinical use or in development. Recognising this opportunity, Australian biopharmaceutical company QRxPharma Ltd and its subsidiary Venomics Pty Ltd (VPL) has partnered with the University of Queensland (UQ) to screen and develop drug candidates from Australian elapid snake venoms. VPL has three haemostasis candidates in early preclinical development. Textilinin-1 (Q8008) is a 7 kDa potent and selective plasmin inhibitor that has application as an anti-fibrinolytic agent to reduce blood loss associated with complex surgeries. Haempatch™ (Q8009) is a Factor Xa-like protein that displays potent procoagulant effects and is being developed as a topical haemostatic agent to reduce blood loss resulting from surgery or trauma. CoVase™ (V0801) is a procoagulant cofactor that may have application as a systemic anti-bleeding agent in the treatment of internal bleeding and non-compressible haemorrhage. This review focuses on drug discovery from Australian elapid snake venoms, with emphasis on the QRxPharma/VPL drug discovery project undertaken in collaboration with UQ and candidates at further stages of development.
蛇毒在药物发现和开发方面具有吸引力,许多治疗药物源自蛇毒,无论是在临床应用中还是在开发中。澳大利亚生物制药公司 QRxPharma Ltd 及其子公司 Venomics Pty Ltd (VPL) 意识到这一机会,与昆士兰大学 (UQ) 合作,从澳大利亚的眼镜蛇毒液中筛选和开发候选药物。VPL 有三个处于早期临床前开发阶段的止血候选药物。Textilinin-1(Q8008)是一种 7 kDa 的有效且选择性的纤溶酶抑制剂,可用作抗纤维蛋白溶解剂,以减少与复杂手术相关的失血。Haempatch™(Q8009)是一种类似于因子 Xa 的蛋白质,具有很强的促凝作用,正在开发作为一种局部止血剂,以减少手术或创伤引起的失血。CoVase™(V0801)是一种促凝辅因子,可作为治疗内部出血和不可压缩性出血的全身性止血剂应用。本文重点介绍澳大利亚眼镜蛇毒液的药物发现,重点介绍 QRxPharma/VPL 与 UQ 合作开展的药物发现项目以及处于进一步开发阶段的候选药物。