ABOUT
Endothelin-1 traps
ET-traps is a novel therapeutic for sequestering pathologically elevated endothelin-1 (ET-1) levels in the body, which is associated with a number of diseases including cardiovascular atherosclerosis, chronic kidney disease, pulmonary arterial hypertension, cancer, diabetes and neurodegenerative disorders e.g. Alzheimer's disease. Our patent has been granted in the US and EPO.
By binding only to the excess ET-1 in the body to bring it down to normal levels and not completely blocking the action of ET-1 in other physiological functions, ET-traps are efficacious in bringing different markers of kidney and heart function to non-disease levels while being non-toxic.
We have performed binding assays that confirmed the solubility of ET-trap construct (an Fc fusion protein) and that it is a very potent binder to endothelin-1, with a binding affinity in the pico molar range. Furthermore, the dissociation of ET-traps once bound to ET-1 is very slow.
We have successfully completed PoC studies in the diabetes disease space, which show that the ET-traps potently and significantly ameliorate disease pathology, including diabetic cardiomyopathy, diabetic kidney disease, and tissue fibrosis.
Furthermore, our PoC work (both in vitro and in vivo) has shown that ET-traps are non- toxic or cytotoxic at the working concentration, which gives efficacy with no side effects.
Other therapeutics targeting the endothelin system block receptors which disrupts the normal physiological functions of the endothelin system and this leads to a number of serious side effects.
ET-Traps Advantages:
- Non-toxic - Does not block the normal physiological functions of the endothelin system
- Significantly returns elevated ET-1 levels to physiological levels
- High binding affinity
- Fc-fusion protein - longer serum half life
- Non-immunogenic - FFPs can be modulated more easily so that therapy doesn't elicit any negative immune reaction
- Able to help with broad range of diseases associated with high ET-1 levels
