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Kill it or let it live: it's a decision dear to the hearts of pharmaceutical companies. The earlier a compound can be killed, or proved ineffective, the better. Not an easy task with the avalanche of New Chemical Entities (NCEs) in the wake of a mapped genome and automated testing technologies. Enter formulation development, always an important step in the drug development process, now even more crucial to a compound's lifecycle.

As pharmaceutical companies continue to focus on R&D and commercialization, drug development is being farmed out to contract providers. This is nothing new; it's been happening for years, but contract providers aren't just dealing with Big Pharma anymore. Emerging biotech companies lack drug development capabilities, giving more business to a burgeoning pharma and biopharma outsourcing industry.

Having worked with pharma companies for years, the drug development contract service providers were more than ready to take on new business. By the late 1990s, these
companies had become experts at small molecule formulation development. Companies that performed preformulation and regular formulation development services could tell their clients when to "kill" a compound and when to let it survive, offering key money- and time-saving decisions.

New automated technologies, as well as the biotechnology industry, have created a mountain of new drug targets waiting to be sifted through. Now, however, in addition to small molecule drug targets, formulation development is a puzzle that applies to large molecule protein and peptide drug targets. This presents a whole new set of complications never seen before.

The biggest problem facing formulation development providers is solubility. Ask anyone in the industry, and this is the first response. Each person contacted for this article mentioned it, cutting me off before I could finish my question about hot topics in formulation development. Large molecule targets are water insoluble and formulators are working hard to tackle that problem.

Ian Smart, director of operations at Taj Pharma, commented, "Solubility is obviously the hottest, the biggest trend." He added, "Biotechnology companies are usually very difficult because they tend to look at different types of molecules. They are looking at large molecules that tend to have solubility problems. If you've got solubility problems then it's difficult to get that product released. That's an area we're trying to specialize in because we've got different techniques for helping the solubility of the product."

Elsie Melsopp, Ph.D., senior scientist, formulations division at AAI International, commented, "These new large molecules are predominantly water insoluble, which is a challenge. It is difficult to do conventional preformulation studies on these molecules and develop the right formulation for the clinic. A lot of our clients come to us with these types of molecules."

Not only are companies trying to piece together ways of formulating these new drug targets, but they, as always, have to keep the regulatory issues in mind as well. The regulations for large molecules have not been able to keep up with the speed of discovery. "Many regulations were written with the small molecules in mind. Some of the things you need to do with a small molecule become much more difficult with these larger molecules that, rather than being synthesized, are biological products. They are purified from some fermentation source or other biologic source. The levels and types of impurities are different, the types of characterizations are different, the analytical techniques are different and, sometimes, not directly amenable to regulations written with small molecules in mind."

Recently, the FDA placed the review of drugs that come from living organisms into the same unit that handles chemical-derived therapies. The biologics unit has lagged behind the agency's drug unit over the years. While the agency's drug unit has halved it's approval time over the last couple decades, the biologics segment languished. Industry insiders are hoping this move will speed up the approval process while making the two types of review processes more consistent. Not an easy task. Making sure batches are consistent is a lot easier for small molecule drugs than it is for biologics. The biologics unit will continue to be responsible for the regulation of vaccines and blood products.

The same rules that apply to pharmaceutical and biotech companies also apply to contract service providers. In addition, however, a company such as AAI not only has to follow FDA requirements, but those of its clients as well. Service providers have to stay on top of regulatory changes, sometimes informing their clients that what may have passed as compliance a few years ago, may not work today. Regulations will eventually catch up to new technology and new molecules.

The FDA is constantly trying to keep up with innovation. New process analytical techniques are coming from the agency to establish online process analytical testing. Dr. Melsopp commented, "Some companies are doing typical in-process blend and bulk product testing, as well as on-line. In order to stay competitive, contractors and companies have to start thinking about process analytical technologies and to put them in place during manufacturing."

Another hot area of formulation development is early stage preformulation and the benefits of it. This goes back to the idea of trying to kill compounds early. Although it may take more time in the long run, doing some initial work can help the critical decision as to whether a compound goes on to the next step or not. Dr. Aggarwal said, "We've seen examples where companies haven't done enough exploration at the initial stages of different formulation options and therefore end up with something that dies later in the process."

Although the amount of preformulation done for compounds varies from project to project, factors such as time (the most valuable thing to drug companies) and money (the second most valuable thing) dictate how much initial work is done. In the best of all possible worlds, a company with ample time and money should spend both on preformulation, according to Dr. Ingallinera.

He said, "Preformulation is where you evaluate the physical chemical attributes of the compound before you decide what the formulation should be. You look at it's oxygen sensitivity, where it's pH is the most stable, solvents and co-solvent systems or surfactants, and ways to enhance the compound's solubility or stability. You look at whether or not the compound is extremely water unstable and if you have to go to a dry process such as lyophilization or powder filling in order to make the product. You look at various methods of sterilization, and evaluate whether or not the product can withstand the heat or the radiation or other attributes of sterilization during preformulation. Considering these variables at a very early stage allows you to develop a better formulation."

Preformulation services are not the only things sponsors are looking for from contract providers. Offering a range of services, from preformulation to end product, cuts down on the number of organizations that have access to a client's intellectual property. Getting as much service as you can from one provider can also cut down on confusion. Dr. Ingallinera commented, "Our clients who are looking for formulation development are also looking for the ability to manufacture and test. They like 'one-stop-shopping'."



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