Research
Overview
Antyra has invested over $25M to generate an integrated set of Technology Modules for drug discovery that allows the Company to move from target to drug lead in an expeditious manner. Specifically, Antyra can define the essential pharmacological domains of any protein interaction (referred to as HotSpots) in order to identify and validate targets while at the same time generating novel drug candidates. The strength and robustness of the platform is underlined by the fact that these Technology Modules have a common basis that allows them to be integrated seamlessly into one continuous discovery platform. This is accomplished by the generation of proprietary, biologically active entities called HotSpot Pharmacophores (HPs). Antyra has conclusively established that HPs can bind the individual contact sites through which proteins interact and that they possess biological properties that facilitate subsequent manipulation of these sites. Most importantly, the Company has shown that HP themselves are drug leads in their own right.
Antyra strongly believes that its HPs are a new generation of biologicals and can be used for the treatment of cancer as well as other unmet medical needs. HPs are competitive and viable alternatives to biopharmaceuticals such as antibodies and oligonucleotide-based reagents as well as traditional small molecules. Most of the past limitations of peptides have been removed by new technologies, so that HPs can be developed, manufactured and moved into clinical trials more rapidly than antibodies. HPs offer several decided advantages over monoclonal antibodies as drug candidates including: (a) lower manufacturing costs (chemical synthetic versus fermentation), (b) greater batch to batch consistency, (c) lower royalty stacking vs. antibodies (licensing and patent issues for MAbs compared to Antyra’s Intellectual Property and Freedom-to-Operate for HPs), (d) better organ or tumor penetration. In addition, HPs have excellent pharmaceutical properties including high affinity, low immunogenicity and target specificity. HP-based drugs for cancer and other disease indications represent the hope of providing a new class of therapeutics that is highly specific, precision-targeted, safe and affordable.
Novel Targets, Technologies and Pipeline
Antyra has identified well over 150 additional oncology and non-cancer targets together with the generation of bioactive HPs modulating these proteins. These targets provide a diverse array of therapeutic opportunities that include receptors involved in angiogenesis and cell signaling. Moreover, each of these targets has been analyzed with its respective HP. Antyra believes that its integrated, modular drug discovery paradigm affords the Company a powerful and rapid approach for the identification, characterization and validation of additional oncology targets at the same time providing a unique set of reagents since HPs can act as pharmacophores for continued analysis or future drug discovery using other drug discovery modalities. HPs provide opportunities for the Company to develop a sustainable product pipeline in oncology and the Company believes that its future growth can be assured by the identification of these targets with their attendant HPs.
Bi-specific HPs. Antyra has recently developed an array of second generation drug leads that simultaneously bind to and regulate multiple targets, termed Bi-specific HPs (BHPs). The rationale behind this approach lies in the observation that many proteins such as tyrosine kinase receptors “cooperate” in disease indications. In its first iteration, the Company has generated BHPs which bind to and inhibit the activity of two validated oncology targets, the IGF-1 and the EGF receptors. Both have been shown to be over-expressed in many cancers. These leads have shown efficacy in the appropriate in vitro cell models and the Company will pursue animal studies in the near future. Antyra intends to generate a number of BHPs in cancer and other disease indications such as Rheumatoid Arthritis.
Delivery and Cell Penetrating Peptides (CPP). Because of their exquisite target specificity, Antyra has initiated programs to develop HPs as delivery vehicles for therapeutics such as conventional chemotherapeutics and siRNA. Several candidates have been identified and are currently being tested in the appropriate in vitro models.
Intellectual Property
Antyra has 6 issued patents based on its HP libraries and their use in drug discovery. In addition, there are several pending patents covering the Company’s technology platform, individual targets, HPs and lead products. The Company believes that it has Freedom-to-Operate in its areas of focus. In addition, the Company is committed to pursuing worldwide composition of matter patent coverage for all its internal lead HPs and collaboration programs.
