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Chronic Kidney Disease: Renin

Direct inhibition of renin offers potentially better renal protection than current therapies for the 27 million people worldwide with Chronic Kidney Disease (CKD).

Renin is the first and rate-limiting step in the renin-angiotensin system (RAS), the primary biochemical pathway for regulating blood volume, arterial pressure and vascular function. In addition to systemic activity, tissues including kidney, heart and brain, also contain RAS. This direct tissue effect of RAS appears to play a key role leading to CKD. Protection of the kidney has been demonstrated in studies with the currently marketed RAS inhibitors such as angiotensin-converting enzyme (ACE) inhibitors, angiotensin receptor blockers (ARB) and the direct renin inhibitor, Tekturna® (aliskiren). These studies showed a delay in the progression of CKD to end-stage renal disease and a reduction in the urinary biomarker albumin, which indicates the extent of kidney damage (higher levels of albumin are indicative of more severe kidney damage). Significantly, this kidney protection effect was independent of any effects the RAS inhibitors had on reducing blood pressure.

VTP-27999 Program

Although ACE inhibitors and ARBs can slow the progression of CKD, many patients still progress to end-stage renal disease (ESRD). There is still a clear need for additional strategies to block RAS effectively to provide better kidney protection or to prevent CKD.

Vitae Pharmaceuticals has developed VTP-27999, a novel, potent and selective renin inhibitor designed to offer a best-in-class therapeutic profile and, most importantly, improved kidney protection, compared to ACE inhibitors, ARBs and Tekturna®.

  • VTP-27999 has demonstrated kidney protection and survival benefits in preclinical in vivo animal studies.
  • Vitae Pharmaceuticals successfully completed both single ascending dose and multiple ascending dose studies in its Phase 1 program for VTP-27999.
  • Preliminary results have shown VTP-27999 is generally safe and well-tolerated, with pharmacokinetics supportive of once-a-day dosing and exceptional bioavailability.

Vitae Pharmaceuticals’ compound will be the second entry to market in its class with a potential best-in-class profile.

Vitae Pharmaceuticals expects to move directly into Phase 2b studies of VTP-27999 in 2012.