Artemisinin-Derived Therapeutics Artemisinin endoperoxides serve as a technology platform for multiple product leads, and presently consists of the three classes of compounds below. All compounds are small, easy to synthesize, easy to deliver, non-toxic, and have demonstrated potent anti-cancer effects in vitro and in vivo.
Targeted Delivery Proprietary transferrin receptor-targeting molecules serve as a drug delivery platform for the Company's therapeutics, and may be suitable for selective delivery of other therapeutics or diagnostic agents targeting cancer cells and/or other cells with increased transferrin receptor expression.
• ART Dimers: Two artemisinin molecules linked together
• ART-Iron Chelators: Artemisinin compounds attached to iron-binding molecules
• ART-Peptides: Artemisinin compounds attached to transferrin receptor-targeting molecules
Artemisinin Dimers ART Dimers are novel compounds that consist of two artemisinin molecules attached together by a linker. These compounds are extremely stable, potent and safe. ART Dimers have shown significant growth inhibition and toxicity in vitro and in vivo against cancer cell lines and models, and are up to hundreds of times more potent than existing artemisinin compounds. ART Dimers should be suitable as an effective and safe monotherapy or adjuvant therapy for cancer and proliferative disorders.
Artemisinin-Iron Chelators (Scorpion Compounds™) ART-Iron Chelators are combination compounds that consist of artemisinin attached to small molecules called chelators that bind iron in cells. Though not delivered as selectively as ART-Peptides via cell receptors, ART-Iron Chelators have demonstrated potent cytotoxicity in vitro against multiple human cancer cell lines. These compounds are believed to act on cancer cells by two separate but synergistic mechanisms: Growth inhibition through iron chelation, and programmed cell death through artemisinin activation. With an artemisinin "Head" and an iron-binding "Tail", these are referred to as "Scorpion Compounds"™.
Artemisinin-Peptides ART-Peptides are combination compounds that consist of artemisinin molecules attached to peptides that bind to and enter cells via the cell membrane transferrin receptor. ART-Peptides do not compete with transferrin in the body for entry into cells. Rather, ART-Peptides are delivered directly into target disease cells together with iron-carrying transferrin via receptor-mediated endocytosis. These compounds employ a "Smart Drug" or "Trojan Horse" strategy to selectively destroy cancer cells with minimal effect on normal cells, and based on preclinical studies, are not anticipated to cause the adverse side-effects associated with traditional chemotherapeutic agents.