Which of my compounds are Bioavailable?

The main prerequisite for the development of a successful drug is that it must be bioavailable, to be able to access and remain in the circulation for long enough to generate a therapeutic effect.

Two criteria must be fulfilled for an orally-administered drug to have good bioavailability, the drug must be absorbed efficiently from the GI tract, and it must not undergo extensive first pass metabolism in the liver. The major determinants of bioavailability are therefore drug transport across the intestinal epithelium and drug metabolism in the liver.

The CXR approach

CXR Biosciences has developed screens that provide an early determination of bioavailability. Our staged approach ranges from high throughput in vitro screens to determine the metabolism and absorption of a large number of test compounds, to detailed in vivo / in vitro analyses for selected lead compounds. The use of human liver microsomes, recombinant human drug metabolising enzymes, cell line models of drug transport, and MDR-1 knockout mice contribute to a full understanding of the role of metabolism and drug transport in bioavailability.

Studies can also be designed to evaluate species differences and likely drug /drug interactions, providing data which is directly relevant to man and which is useful in the design and interpretation of subsequent preclinical studies.