11ß HSD-1 Inhibitor
- VTP-27999, Vitae Pharmaceuticals' wholly-owned renin inhibitor has completed Phase 1 studies and is designed to improve the treatment of patients with Chronic Kidney Disease (CKD).
- Renin is the first and rate-limiting step in the renin-angiotensin-system (RAS) pathway. RAS components are located in critical organs throughout the body (kidney, heart, brain) and RAS activity has direct effects on tissues, playing a key role in kidney damage.
- Vitae Pharmaceuticals' second program, partnered with Boehringer Ingelheim, focuses on inhibition of 11ß-hydroxysteroid dehydrogenase (HSD)-1 for the treatment of diabetes and associated metabolic diseases is currently in Phase 1 clinical trials.
- 11ß-HSD-1 is a recently validated, new diabetes target, which has demonstrated broad, potential metabolic syndrome benefit.
- Vitae Pharmaceuticals' beta-secretase (BACE) program, also partnered with Boehringer Ingelheim, has identified potent and bioavailable inhibitors that have demonstrated the ability to cross the blood-brain barrier and lower brain amyloid-beta (Aß or Abeta) peptide following a single oral dose in preclinical, in vivo models of Alzheimer's disease.
- Inhibition of BACE, an enzyme involved in the formation of amyloid-beta plaques that accumulate in the brains of patients with Alzheimer's disease, is a leading prospect for slowing or even halting disease progression.
- Vitae Pharmaceuticals has initiated a program to treat atherosclerosis by modulating LXR, an approach that increases reverse cholesterol transport (RCT), decreases inflammation and is complementary to the LDL-lowering capabilities of statins.
- In 12 months, Vitae scientists have discovered novel, small molecule compounds that induce the expression of RCT biomarkers without the induction of triglycerides in rodent and primate models.
Human genetic data show that increased amounts of Aß in the brain is a key contributor to the progression of Alzheimer’s disease and to cognitive decline. Vitae’s brain-penetrant LXRß-selective modulators increase clearance of Aß from the brain without causing plasma or liver triglyceride elevations. LXR modulation represents a novel mechanism to modify the pathogenesis of Alzheimer’s Disease.