Bioavailability enhancements, a long-standing problem for drug developers

After a series of scientific breakthroughs, the pharmaceutical industry is edging closer to developing treatments for many devastating diseases. But the newfound optimism is offset by a big, common barrier: bioavailability. With as much as 95% of the drug development pipeline suffering from low solubility or permeability, the conversion of cutting-edge science into life-saving treatments is wholly reliant on the advancement and application of bioavailability enhancement techniques.

Bioavailability is a long-standing problem for drug developers. At the start of the 1990s, adverse pharmacokinetic and bioavailability characteristics accounted for 40% of clinical-stage pipeline failures. Over the next 10 years, drug developers got much better at spotting drugs with these traits during preclinical research — culminating in bioavailability being a causal factor in less than 10% of failures by 2000 — but the underlying challenge of turning poorly soluble active ingredients into viable therapeutics never went away.

The challenge is now greater than ever. Some estimates suggest around 90% of pipeline candidates are categorized as poorly soluble under the Biopharmaceutical Classification System (BCS), with a further 5% presenting bioavailability challenges because of their low permeability. Just one-third of approved drugs are classed as poorly soluble. The growing prevalence of pipeline products with poor bioavailability has intensified demand for technologies and methods that can overcome these traits, as well as for companies that understand how and when they should be applied.

In this paper we look at the process CoreRx goes through when given an active ingredient with low bioavailability and four approaches that may be applied to increase the amount of the therapeutic that enters systemic circulation.

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