Questions & Answers

What is BAS Technology?

BAS has discovered and developed potent spiro ortho ester-based inhibitors of human drug degradation. The magnitude and impact of human drug degradation cannot be predicted by modern drug development programs. Because fast drug degradation is not uncovered until after an IND is in place, this represents a substantial money- and time-based inefficiency of the industry.

Rapid drug degradation is primarily caused by an enzyme system known as CYP 3A (human cytochrome P450 3A), and this system is responsible for the degradation of approximately 60% of all drugs given to man. This rapid degradation of drugs by CYP 3A enzymes is known as the First Pass Effect (FPE). When the CYP 3A system is inhibited via BAS Technology, it allows many drugs to be absorbed dramatically better. BAS Technology is an anti-FPE tool.

Why is this important?

The CYP 3A enzyme system is responsible for the degradation of approximately 60% of all drugs given to man. New drug candidates fail 40% of the time because of poor bioavailability, even though the industry had made its best efforts to screen out poor candidates. Failures are a large part of development costs. BAS Technology may reduce cost to market, reduce cost per dose, revive failed drug candidates, eliminate the risk associated with CYP 3A in new drug development, and may be used to extend patent life. It may also create the potential for oral delivery of drugs that were previously restricted to intravenous dosing.

Is this technology strategy new?

No, the concept of increasing a patient’s ability to absorb medications via CYP 3A inhibition is currently used in the branded drug Kaletra™. This medication is a co-formulation of ritonavir (a CYP 3A inhibitor and antiretroviral, Norvir™) and lopinavir (the active component). Kaletra™ became the leading HIV protease inhibitor within 18 months of FDA approval. Physicians value the strategy highly, as indicated by their Kaletra™ prescribing activity. Similarly popular among physicians is the off-label “boosting” of many HIV-protease inhibitors with ritonavir. This has now resulted in label expansion of many other HIV-protease inhibitors to describe boosting with ritonavir.

Why use BAS Technology vs. other booster technologies?

BAS Technology has no known therapeutic effect, but they are remarkable inhibitors of drug degradation. All prominent drugs on the market today that inhibit drug degradation are also first-line anti-microbials. A controlling tenet of infectious disease medicine is to avoid giving anti-microbial drugs to people who do not have a well-characterized infection. Doing so causes drug-resistant microbes to emerge, and drug resistance is a major public health concern.

How do you know your Technology works?

Two U.S. human clinical trials, conducted by a non-exclusive licensee, showed an average of forty-fold enhancement of bioavailability (click here for a Summary of U.S. Clinical Trials). The boosting phenomenon was first reported in the early 1990’s when grapefruit was used in a clinical trial to mask taste. Since that time, over one hundred clinical trials have shown that grapefruit contains chemicals that boost plasma concentrations of many drugs. BAS was successful in isolating, elucidating, quantifying, patenting and clinically testing these compounds.

Is the use of BAS anti-FPE Technology limited to only a few therapeutic areas?

No, and this general applicability across all therapeutic areas is a substantial advantage of the BAS Technology. The only requirement is that the candidate is degraded by the CYP 3A system upon oral administration. The breadth of applicability is remarkable to consider, and this should prompt drug developers to enter markets that were previously considered too difficult to enter (e.g., oral protease inhibitors for hepatitis C) or re-enter (e.g., oral renin inhibitors; GpIIb/IIIa inhibitors).

How can you tell if a candidate is well matched with your technology?

There is a rather dependable in vitro – in vivo correlation for human CYP 3A inhibitor testing.

Is the BAS Technology available for licensing?

BAS is open to discussions with potential licensees for specific therapeutic applications.

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Copyright BAS 2007