Advertisement

Nano World: Nano to speed drug discovery

By CHARLES Q. CHOI

NEW YORK, March 4 (UPI) -- Nanotechnology soon could speed the discovery of blockbuster drugs, cutting down the roughly eight to 12 years and $900 million it takes currently to develop a new pharmaceutical, experts told UPI's Nano World.

"A new drug addressing a disease previously without an effective remedy has the potential to generate a revenue of $1 billion per year. It is a classic winner-take-all industry, as the first mover with a revolutionary new drug usually takes over 75 percent of the market -- even years after initial discovery," said Nelesh Patel, an associate analyst with NanoMarkets, a research firm in Sterling, Va.

Advertisement

In addition to the constant pressure pharmaceutical giants face to deliver a drug to market as fast as possible, the industry needs new technologies of all sorts to help replace the 42 of 52 blockbuster drugs on the market in 2001 that will lose patent protection by 2007, noted a February report from analyst firm Lux Research in New York. Those 42 drugs will represent $87 billion in combined worldwide sales that year.

Advertisement

One solution may be nanotechnology, which could help more candidate drugs make it to market through clinical trials. NanoBusiness Alliance executive director Sean Murdock told UPI's Nano World the chances today of a candidate drug making its way to market, through both clinical trials and regulatory approval, was a dismal 8 percent.

"Companies like OpGen (in Madison, Wis.) or U.S. Genomics (in Woburn, Mass.) or Nanofluidics (in Menlo Park, Calif.) are taking nanotech-based approaches for whole-genome sequencing that could enable understanding of individual genetic predispositions to certain illnesses," said Murdock, a one-time consultant to the pharmaceutical industry. "By having a richer set of information on how populations might respond to drugs, you can appropriately target your use of therapies and increase the success rate of drugs in the pipeline."

Nanotechnology could offer pharmaceutical researchers a critical further miniaturization of drug-discovery technology, Patel said.

The common procedure for researching a new drug involves first testing promising molecules on proteins and other compounds found on the surfaces of bacteria or other targets linked to a disease, then selecting out the most effective and safest-looking candidates.

Using current microarray technologies, researchers can analyze thousands of microscopic quantities of drugs at once.

Advertisement

"Where it once took the effort of a single chemist to view anything from one to 12 gene variations at a time, microarrays can view thousands in the same time frame," Patel told Nano World. "Now nanotechnology promises to exponentially increase even the volume of microarrays by working at a level far smaller than conventional microarrays."

BioForce NanoSciences in Ames, Iowa, for instance, has developed a nanoarray "that can actually measure interactions between individual molecules, down to resolutions of as little as 1 nanometer," or billionth of a meter, Patel said. "The nanometer-scale resolution capabilities of the technology offer many advantages in the emerging field of functional proteomics" -- the study of proteins.

"Unlike nucleic acids, which can easily be multiplied by amplification methods," Patel continued, "individual proteins cannot be easily increased in quantity. Using nanoarray technology, very small quantities of individual proteins can be effectively screened against a large set of drug targets."

BioForce's device actually recognizes when a chemical interaction has occurred by measuring the change in height of a molecule when it bonds to the protein in question. This eliminates the need that other arrays have to see what's going on by using fluorescent dyes or other intermediates that could interfere with the reaction scientists want to measure in the first place, Patel said.

Advertisement

Along the same line as nanoarrays are nanofluidic devices, which act as infinitesimal labs-on-a-chip. Current microfluidic devices mix microscopic amounts of fluids together, just as a chemist would mix chemicals in a beaker, with the aim of creating often-precious enzymes or other valuable molecules. Microfluidic devices automate mixing and scale it down so it happens thousands of times simultaneously, for tasks such as finding the best growth conditions for a crystalline drug.

"In a similar manner to microarrays, microfluidic systems offer several advantages," Patel said, including "decreased sample volumes, reduction in the amount of required reagents, reduction in waste, easy automation, and potentially massive parallel processing of laboratory samples.

The increase in automation that nanoarrays and nanofluidic devices allow should speed drug discovery and also reduce the need for an expert lab staff, he added.

Novel discs made of the same kind of material as cell membranes could help present the molecules that drugs target in a more lifelike way -- instead of unnaturally splaying them on a glass plate -- "and thus more (would) likely behave as you would expect in a clinical trial," Murdock said. "If we can improve the likelihood that candidate molecules entering clinical trials make it out as efficacious drugs, we improve the returns of drug discovery."

Advertisement

The company Nanodisc in Chicago is offering such a product.

Nanotechnology also can improve one of the workhorse technologies the pharma industry uses to identify molecules: mass spectrometry. Advion Biosciences, in Ithaca, N.Y.; BioTrove of Woburn, Mass., and NanoHorizons of State College, Pa., each offers nano-mass-spectrometry techniques with boosts in speed, increases in sensitivity and cuts in the amount of sample needed, Patel noted.

Moreover, Quantum Dot, of Hayward, Calif., offers nanometer-sized semiconductor crystals that are improvements over current fluorescent labels used for tracking molecules and identifying their interactions. The crystals can help scientists follow many different kinds of molecules simultaneously over long periods with just one laser, while existing fluorescent labels require multiple lasers to track multiple targets and often wear out quickly.

Patel said Quantum Dot already is collaborating with industry giants Genentech, Roche, and GlaxoSmithKline.

Nano-delivery techniques might aid drug discovery, Murdock added. Elan Pharmaceuticals in Dublin, Ireland, estimates as much as half of all drug candidates show promise against their targets, but cannot be used in the human body because of poor solubility and therefore are rejected in the early stages of the drug discovery process.

Reformulating such molecules using nanotech to make them more soluble "can take compounds that were on the margins before and push them over the fence so they become viable candidates again," Murdock said.

Advertisement

Murdock said he thinks big pharma companies are "only beginning to turn their eyes towards the possibilities nanotech offers in drug discovery."

Patel agreed. "I feel that in the next two to three years, all the major pharma and biotech companies will make substantial investments in nanotechnology to facilitate the drug discovery process," he said.

--

Nano World is a weekly series examining the exploding field of nanotechnology, by Charles Choi, who covers research and technology for UPI Science News. E-mail: [email protected]

Latest Headlines