These compounds are the first to be invented by Speedel Experimenta, the company’s late-stage research unit, which was established in 2002.
SPP630 and SPP635 have now been successfully tested in micro-dosing studies with human volunteers and in preclinical studies with transgenic rats that express the human genes for renin and angiotensinogen.
These studies show that this next generation of renin inhibitors offer potential improvements over currently available therapies, and specifically show that both compounds demonstrate bioavailability in humans of up to 30% and in rats of 70% to 90%, figures far greater than have been obtained with any previous renin inhibitor.
The compounds have also shown larger tissue distribution than previous renin inhibitors, indicating their incremental potential for end-organ protection, and not only reduce blood pressure in transgenic rats over 24 hours, but also slow down the progression of renal damage after oral treatment.
Dr Alice Huxley, CEO, commented: “This significant milestone further strengthens Speedel’s leadership in renin inhibition and demonstrates our ability to generate our own drug candidates. Our innovative approach with the use of human micro-dosing has allowed us to fast-track these compounds to a stage where we expect to select the best candidate(s) to continue classical phase I studies in Q3 2005.”
The microdosing studies were performed in collaboration with Xceleron Ltd. Both SPP630 and SPP635, together with other compounds from the SPP600 series, will be evaluated in toxicology studies before a decision is made about which compound(s) will continue in classical phase I studies with single ascending and multiple ascending doses.