Fullerenes for the Treatment of Osteoporosis

In the treatment of osteoporosis and other bone disorders, it is desirable to deliver therapeutic compounds to the bone. However, it is known that certain substances, although therapeutic, are too toxic to be transported in the human body in free form. For example, fluoride anion (F–) is known to be an active therapeutic agent for osteoporosis, and the only known agent that can generate new bone matrix and new mineral from previously inactive areas. It both improves bone strength and helps prevent fractures. Yet it is too toxic to be administered in free form, such as by injecting NaF in aqueous solution intraveneously. One recently approved treatment for bone disease is a class of chemicals known as biphosphonates. Bisphosphonates bind to bone, slowing osetoporosis and allowing new bone to be formed. However, because this effect is temporary, bone mass is not substantially increased in the long term. Because new bone is not formed, bones are left weakened and prone to later injury. Hence, bisphosphonates alone are not entirely satisfactory. There remains a need for a suitable compound that inhibits bone resorption and promotes new bone formation so as to produce a net bone gain without adversely affecting the patient. Further, such a compound would be targeted to bone, permitting the release of a therapeutic agent at the site of the bone, and hindering any, potentially harmful release of the agent to the rest of the body. Professor Lon Wilson in the Dept. of Chemistry has pioneered a new class of drugs for the treatment of osteoporosis and possibly other bone disorders. This medical advancement provides a non-toxic, biologically active composition that is capable of promoting bone growth while simultaneously inhibiting bone resorption, so as to produce a net bone gain. In its most essential design, the drug is comprised of a bisphosphonate group linked to a fullerene molecule. Alternatively, the bisphosphonate group can form chemical bonds directly with the fullerene, or between a linking molecule. A preferred method of synthesis of a fullerene-based bisphosphonated drug includes attachment of a water-solubilizing group, and attachment of a therapeutic agent. A plurality of fluorine atoms, as a therapeutic agent, are bound to one hemisphere the fullerene, thus hindering toxicity. Further it is believed that fluorine anion is released over time at the surface of the bone, due partly to the basic and nucleophilic environment of bone’s surface. It is known that fluorine anion generates new bone matrix and new mineral from previously inactive areas. It is envisioned that polyfluorobisphosphonated fullerenes, as bimodal drugs, can deliver the two bisphosphonate and F– components to bone in a single, non-toxic “package” that is easily absorbed in the gastrointestinal tract.

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