The Speed and Development of New Drugs

There are hundreds of new drugs appearing on the market today at an amazingly fast rate. People are able to create new drugs in a more informed manner, and with the invention of new technology, analyze and test the drugs more rapidly than ever before. Rather than taking "the conventional 10-14 years there is now a reduced the discovery-to-market time of only 5-8 years" (Revolution, Beeley). This is due in great part to the many processing developments that have been made.

Synthetic organic chemistry is crucial in any drug discovery program. To help clarify what this is, it can be compared to Lego building blocks. “Chemical building blocks are assembled according to precise rules, creating molecules of increasing complexity. Some of these blocks hold others in position, while others are capable of interacting with a biochemical target ... Some blocks are there to modify the metabolism of molecules and others modify the overall structure to improve drug delivery” (Revolution, Beeley). Combinatorial Chemistry is a major factor in the ability to test drugs more quickly. “Combinatorial Chemistry is the process by which millions of molecular constructions can be created and tested simultaneously.”(Revolution, Beeley).

One of the first examples of combinatorial chemistry, was in 1985. Richard Houghten synthesized millions of peptides as mixtures. Once this was done, he screened for biological activity. Having identified those that showed positive activity, he was able to figure out which components of the mixtures were responsible for this activity.

Traditionally, medicinal chemists had to synthesize a handful of different molecules at one time, and then wait for the results. Once these came through, they were then able to modify the design and retest. Due to recent advances, this time has been significantly compressed. “Genomics has improved the identification of useful points of therapeutic intervention; combinatorial chemistry has generated massive numbers of molecules for testing; and screening using high throughput techniques has automated the process of doing large numbers of biological assays” (Revolution, Beeley).

The work of Bruce Merrifield in devising “a methodology that allowed peptide synthesis to be performed on a solid support using ... beads of polystyrene ... and resulting in an almost instant purification of molecules ...”(Revolution, Beeley) allowed for a single operator to synthesize biologically active peptides in a 24 hour period. This methodology gave way to Mario Geysen’s discovery in the early 1980’s of synthesizing many peptides in parallel. “Geysen’s matrix was used to identify useful epitopes” (Revolution, Beeley). His 8x12 matrix of polystyrene pins, corresponds to today’s 96-well microtitre plate.

Many companies in the pharmaceutical and biotechnology industries are now using some form of combinatorial chemistry in their laboratories. With its invention, companies are now able to use only a single chemist to synthesize thousands of different molecules in the time-span of only one week. “The promise of a considerably shortened discovery-to-market time has become a reality” (Revolution, Beeley).

One major driver behind this need for advancement and speed in discovery-to-market is the ever-present HIV virus. More than 50 million people have become infected with the HIV virus in the past two decades, and about 17 million have died from it. “In some countries, as many as one in four adults are HIV positive ...” (Study, Henderson).

The situation of HIV/AIDS is most dismal in developing countries. Patients’ life-spans in sub-Saharan Africa are expected to decline to age 30 within a decade. Despite this fact, it has been stated that India is currently the most at-risk nation. With nary a health-care plan in place, and the second largest population leader, “the ingredients exist in India for an epidemic of unprecedented magnitude” (Study, Henderson).

Another, possibly more transmissible and lethal strain of HIV may be responsible for more than half of the HIV infections in the world. This strain is known as HIV-1C, (the more common strain being HIV-1B.) It has not yet made much of an impact on the major-market countries, (“these countries are the United States, France, Germany, Italy, Spain, the United Kingdom, and Japan”) (Study, Henderson).

Drugs that will most likely be used to help combat the HIV/AIDS problem are didanosine plus hydroxyurea, or lamivudine and zidovudine with nevirapine. These will “most likely be the therapeutic interventions of choice in the developing world because of their cost-effectiveness and simplified administration schedules” (Study, Henderson).

Because of epidemics and other wide-spread diseases such as HIV/AIDS, the need for the development of new drugs to combat them is absolutely essential. With the help of modern technology, faster discovery-to-market rates are possible, and the ability to more effectively fight these illnesses is possible.