Print Page  Close Window

SEC Filings

S-1
VITAE PHARMACEUTICALS, INC filed this Form S-1 on 08/12/2014
Entire Document
 

Table of Contents

that further contribute to the disease. Amyloid production begins with an enzyme in the brain known as b-Site Amyloid Precursor Protein Cleaving Enzyme 1, or BACE. There are significant genetic data that implicate BACE as playing a direct role in the disease process itself. We discovered and are developing VTP-37948, a BACE inhibitor, in collaboration with BI. In preclinical studies, VTP-37948 demonstrated highly potent and selective inhibition of BACE in the brain, with up to 95% lowering of brain amyloid beta levels. VTP-37948 is currently in two Phase 1 clinical trials involving a total of 68 healthy volunteers. The first trial includes endpoints of safety, tolerability and pharmacokinetics. The second study looks at the effects of VTP-37948 on a key biomarker of activity, amyloid beta concentration in the cerebrospinal fluid, or CSF. Results from both of these studies are expected in the second half of 2014.

VTP-43742

        We are developing VTP-43742 for autoimmune disorders. Autoimmune disorders include commonly known diseases such as psoriasis, multiple sclerosis, or MS, and rheumatoid arthritis, or RA, as well as rarer conditions such as Behcet's disease, an inflammatory disease of blood vessels, and autoimmune uveitis, an inflammatory disease of the eye. Increased activity of a class of lymphocytes, which are a type of white blood cells called Th17 cells, is a critical part of the pathophysiology of many human autoimmune disorders. RAR-Related Orphan Receptor gamma-t, or RORgt, is a protein that is essential for the formation and function of Th17 cells. Preclinical studies in animal models have demonstrated that inhibition of RORgt activity is beneficial for the treatment of multiple autoimmune disorders. In preclinical studies, VTP-43742 has been shown to inhibit the secretion of Interleukin 17, or IL-17, and other inflammatory proteins from Th17 cells, and has been demonstrated to be therapeutically beneficial in an animal model of MS. These studies also show that VTP-43742 is well absorbed after oral administration in multiple animal species and has a long half-life in plasma, which we believe is consistent with once-a-day dosing in humans. We plan to file an Investigational New Drug application, or IND, with the U.S. Food and Drug Administration, or FDA, for VTP-43742 in the first half of 2015, with Phase 1 clinical trials commencing thereafter. We expect to have Phase 1 proof-of-concept data demonstrating clinical efficacy by the end of 2015.

VTP-38443

        We are developing VTP-38443 for acute coronary syndrome, or ACS. Liver X receptors, or LXRs, which include, LXRa and LXRb, stimulate the production of proteins to transport cholesterol out of cells and inhibit the production of inflammatory proteins. Several studies have demonstrated that LXR agonists promote reverse cholesterol transport, or RCT, in vivo in mice and prevent the development of atherosclerosis. VTP-38443, an orally active LXRb selective agonist, works by augmenting RCT, helping remove cholesterol from the plaque in vessel walls and by inhibiting the production of pro-inflammatory proteins around the plaque. Both of these mechanisms make the plaque less inflamed and more stable, which we believe lowers the risk of plaque rupture and blood clot formation that may lead to a heart attack, and could make VTP-38443 a potential complement to current therapies for ACS. In preclinical studies, VTP-38443 decreased cholesteryl ester formation in plaques by more than 90% and lowered the plaque's inflammatory state. We anticipate completing the necessary preclinical studies and filing an IND for VTP-38443 in the first half of 2016, with Phase 1 clinical trials commencing thereafter.

VTP-38543

        We are developing VTP-38543 topically for atopic dermatitis, also known as eczema. Atopic dermatitis is characterized by a loss of barrier function of the skin and skin inflammation. Similar to VTP-38443, VTP-38543 transports lipids out of cells and decreases inflammation, in this case in damaged skin tissue. VTP-38543, an LXRb selective agonist, has been shown in preclinical studies to stimulate mature skin cells to synthesize and secrete lipids to improve its barrier function, while also decreasing skin inflammation. In an animal model of skin inflammation, VTP-38543 has demonstrated equal or superior efficacy versus a

 

3