Products
Lead Programs
Antyra has positioned itself to generate and develop a new generation of precisely targeted, disease-specific therapeutics. The Company has shown that its HPs act as targeted therapeutics and represent the next generation of biological therapeutics. HP antagonists have been identified for a range of cancers with several already tested in animal models. In addition, the Company has identified and is developing TNFR1 antagonists which may have utility in the treatment of Rheumatoid Arthritis and related disease indications. On this basis, Antyra’s present strategy is to move one lead candidate into the development pipeline and complete one clinical trial within 24 months of closing the present round.
Antyra has several potential lead clinical candidates in its pipeline. The Company has completed definitive animal studies for ANT-429 (pancreatic cancer) and ANT-G12 (prostate and breast cancers and the data indicate that both HPs significantly inhibit the growth of established human tumors in mice xenograft models. Additional animal studies are ongoing with the goal of moving the Company’s lead oncology candidate into formal preclinical pharmacology/toxicology evaluation in 2008.
Oncology Leads
IGF-1R Antagonist: ANT-429. The Company has generated some exciting data with its IGF-1R antagonist, ANT-429, which 
represents a novel and potentially effective clinical strategy for the treatment of pancreatic and other cancers. Pancreatic cancer is the fifth leading cause of cancer deaths following breast cancer, lung cancer, colon cancer, and prostate cancer and as such, cancers of the pancreas are a very serious health issue in the United States where approximately 27,000 patients are diagnosed annually with the same number dying from this disease. The disease is extremely difficult to treat and due to difficulties in diagnosis, the intrinsic aggressive nature of pancreatic cancers and the poor treatment options available, 5 year survival remains only 3-5%. For these and other reasons, pancreatic cancer continues to be a serious unmet medical need and has been called “the challenge of the twenty-first century."
As shown in the accompanying figure, ANT-429 inhibits the growth of pancreatic tumors in nude mice in a dose responsive manner. At the highest dose, there was a 100% response rate with one complete remission. In addition, 40% of the animals in the low dose group responded to ANT-429. Overall these data confirm earlier studies regarding the efficacy of ANT-429 in vivo and solidify it as a lead candidate for further clinical development.
CSTa-derived HP: ANT-G12. Antyra’s proprietary technology, Cell Surface Targets (CSTa), has been designed and developed with the intent to isolate specific, cytotoxic HPs that bind to cell surface targets expressed in a disease-specific context such as cancer. In addition, CSTa can also be used to identify HPs which bind to GPCRs expressed in their native state and HPs which are internalized as Cell Penetrating Peptides (CPP) and can be used as drug delivery modules. CSTa offers a profoundly versatile approach since it can generate HPs independently of whether the target is known or not. The HP can not only be used to identify the target to which it binds but in addition it can serve as a therapeutic agent for downstream clinical development. Antyra has used CSTa to identify one of its lead therapeutic candidates, ANT-G12, for the treatment of prostate cancer as well as to develop a pipeline of pharmaceutical leads for other cancers including pancreatic, gastric, lung, colorectal and breast.
To establish the potential clinical relevance of ANT-G12, the Company evaluated the in vivo efficacy of ANT-G12 in a series of tumor xenograft studies. Animals with established prostate tumors from the human prostate cancer cell line, DU145, were treated with ANT-G12 with multiple doses. The animal studies indicated that ANT-G12 significantly inhibited the growth of established human prostate tumor xenografts in nude mice in a dose responsive manner. In addition, a second CSTa-derived HP, ANT-C7, was also efficacious in inhibiting tumor growth in relation to the controls . These data indicate that CSTa can be used to identify biologically active HPs and establish ANT-G12 as a strong lead candidate for further development. Moreover, in follow-up analyses, Antyra has identified the putative target for ANT-G12 and, in so doing, has exemplified the Company’s capability for identifying and validating a novel “druggable” targets.
Non-Oncology Leads
Although Antyra is focused principally on developing target-specific therapeutics for cancer, the versatility and breadth of application of its technology affords it the ability to work on selective application of its HPs as potential drug leads for non-oncology indications such as Rheumatoid Arthritis (RA).
TNFR1 Antagonists. Although Antyra is focused principally on developing target-specific therapeutics for cancer, the versatility and breadth of application of its technology affords it the ability to work on selective application of its HPs as potential drug leads for non-oncology indications such as Rheumatoid Arthritis (RA). Overall, RA is an extremely large market affecting about 1% of all Americans, greater than 2 million people, with, until recently, current treatment options using traditional drugs such as NSAIDS and corticosteroids. However, more recent drug development efforts have focused on inhibiting the effect of TNF-α. TNF-a is a validated target for RA, with a new generation of biologicals targeting this growth factor. In fact, the combined sales of two biologicals targeting TNF-a (Enbrel [Amgen] and Remicade [J&J]) were over $6 billion in 2005, Antyra has developed several HPs which are specific TNFR1 (Tumor Necrosis Factor Receptor 1) antagonists and inhibit its biological function. Antyra believes that this novel approach and its HPs represent a new class of pharmaceuticals for RA and even modest penetration of the marketplace would represent a significant opportunity for the Company.
EPO Mimetics. More recently Antyra has examined the opportunity of developing a novel EPO mimetic. These HP-derived EPO mimetics may work by a different mechanism that the products already on the market with a concomitant decrease in their cost and perceived clinical toxicity. This is currently a work-in-progress but the Company is confident of building such an agonist since it has already successfully accomplished the construction of an agonist for Insulin with biological and pharmacodynamic properties equal or better than the natural ligand. In addition, an EPO mimetic may have novel clinical utility in protecting against neurodegeneration.
