Cardio owns the intellectual property rights in a drug development program known as the ‘PCSK9’ Program.
The objective of the PCSK9 Program is the development of a drug that seeks to lower LDL cholesterol levels in patients with hypercholesterolaemia and which offers significant clinical advantage over current drug therapies.
The target of the drug is proprotein convertase subtilisin/kexin type 9 (PCSK9), and the role of the drug is to block the ability of the PCSK9 protein to bind to the low-density lipoprotein (LDL)-receptor complex. In so doing, more LDL is removed from the blood.
PCSK9 is now identified as a preferred drug target in the treatment of elevated levels of LDL cholesterol, with anti-PCSK9 therapy based on monoclonal antibodies providing better response rates and superior cardiovascular health benefits than the drugs known as ‘statin drugs’ which have dominated this field for the past 25 years.
Early attempts by pharmaceutical companies to develop a ‘statin-like’ drug (that is, an oral small molecule drug) targeting the PCSK9-LDLR interaction failed, leading to the alternative approach of monoclonal antibodies, of which two have been marketed since 2015. Both monoclonal drugs have to be administered by injection on a fortnightly or monthly basis, come at significant cost, and their use is limited to patients where other therapies have failed or are not well tolerated.
A team of Australian chemists has managed to design a small molecule that effectively blocks PCSK9’s ability to bind to the LDL-receptor complex. A provisional patent application in respect of the PCSK9 Program was lodged in Australia on 17 March 2017.
