After a pause, buckyballs make it to the big time

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Oct. 17, 2003 – Buckyballs, the soccer ball-shaped molecules that helped kick-start interest in nanoscale science and technology in the 1990s, finally made the big time. The biotech startup C Sixty announced Thursday that it is partnering with the pharmaceutical company Merck & Co. to develop drugs based on buckyballs, formally known as buckminsterfullerenes.

If they are successful, fullerenes could find a use that is both medically beneficial and lucrative, and open the door for high-volume production of fullerenes.

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“We expect to be driving the market for fullerenes and be a large consumer of fullerenes,” said Russ Lebovitz, C Sixty’s vice president of business development. C Sixty modifies fullerenes to make them biocompatible and to enhance their therapeutic properties. A handful of companies worldwide sell fullerenes, which to date have lacked a high-volume application.

C Sixty is focusing on the antioxidant properties of fullerenes. Fullerenes soak up cell-damaging free radicals, a byproduct from oxygen reacting with other chemicals in the body. Free radicals likely play a role in aging and fatal degenerative diseases such as Alzheimer’s and amyotrophic lateral sclerosis, or Lou Gehrig’s disease. 

 “This is a large opportunity in major diseases for which there is no treatment now,” Lebovitz said. “This could have an enormous impact on lots of people.”

The partnership gives Merck the rights to C Sixty’s fullerene-based drugs. A research group headed by Dennis Choi, the executive vice president for neurosciences at Merck Research Laboratories and a noted neurological researcher, will collaborate with C Sixty to conduct animal trials with the drugs. Before joining Merck, Choi led research programs at the University of Washington in St. Louis that focused on fullerenes as free radical scavengers.

Merck could begin clinical trials “in the near future” if the animal trials prove successful, said Anita Larsen, a spokesperson for Merck. Choi was traveling and unavailable for comment.   

C Sixty negotiated a three-pronged deal with Merck, said Philip Epstein, C Sixty’s chief executive. C Sixty will supply Merck with its fullerene compounds, license its research for the animal studies and give Merck an exclusive licensing option to market and sell the drugs. The commercial option will kick in only if a fullerene drug meets U.S. Food and Drug Administration standards.

C Sixty will bring its expertise in the chemistry and chemical-biological interplay of fullerenes into the partnership, while Merck will provide its experience in animal and human trials and in negotiating the federal regulatory maze. Merck intends to target its efforts toward developing drugs for two specific therapies, but did not name the diseases.

C Sixty will continue to explore potential therapeutic uses of fullerenes for applications as varied as cardiovascular drugs to skin creams. Lebowitz said the company is in contact with several institutions to begin animal studies targeting various diseases.

C Sixty’s name plays off the scientific shorthand for fullerenes, which are made of 60 linked carbon atoms, or C60. Fullerenes made a splash in the scientific world when they were unveiled in 1985 by chemists Robert Curl and Richard Smalley at Rice University and Sir Harry Kroto at the University of Sussex. The trio won the Nobel Prize in chemistry in 1996 for their discovery.

They proved that fullerenes were a third form of carbon, after graphite and diamond, and named the molecules buckminsterfullerenes because they resembled the geodesic dome invented by Buckminster Fuller. Buckyballs and another form of fullerene called carbon nanotubes are expected to become key ingredients in some nanotech products.
 
Interest in buckyballs skyrocked after 1990 when physicists Donald Huffman at Arizona State University and Wolfgang Kratschmer at Max Planck Institute in Germany reported a reasonably easy method for making quantities of the material. The method was licensed to Materials and Electrochemical Research Corp. (MER Corp.) in Arizona, one of a handful of fullerene suppliers in existence today.

Others include a joint venture in Japan among Mitsubishi Corp., Mitsubishi Chemical Corp. and Research Corporation Technologies; TDA Research in Colorado; Nano-C in Massachusetts, and CarboLex Inc. in Kentucky. Prices vary from about $45 to $190 a gram, depending on purity and other factors.

Applications have been modest. A division of the manufacturer American Bowling Service puts buckyballs in the shell of its Nanodesu bowling ball. Sony announced it was developing a fullerene-based fuel cell in 2001 but has been mostly silent since then.

Lebovitz and Epstein said they expect their suppliers will be able to ramp up production and lower costs as demand increases. They plan to work with a variety of suppliers to get their fullerenes, and anticipate the interest shown by Merck should inspire others who make, use or study buckyballs.

“From our perspective, this is the first major validation of fullerenes,” Epstein said. “It’s a major milestone.”

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