TPI 336, a poorly soluble compound for anti-inflammatory conditions is the active ingredient in a major marketed product with more than $2 billion in annual worldwide sales. The drug has a fairly slow onset, is only 40% bioavailable, and has a declining dose response as dose is increased. Using our CrystalMax® technology, scientists at TransForm have identified several novel crystalline forms of the compound. Our scientists then developed a novel formulation that works synergistically with this particular form to yield remarkable results. In dog studies, TransForm’s improved version of the drug attained over 90% bioavailability and much faster onset—reaching a therapeutically relevant dose within 15 minutes thereby potentially dramatically improving the effectiveness of this drug for relief of an acute indication. Furthermore, TransForm’s improved version of the drug appears to yield pharmacokinetics that vary in linear proportion to the dose administered.
Interestingly, neither our novel solid form of the active ingredient nor our novel formulation, by itself, yielded material performance enhancements over the marketed drug. Rather, significant performance improvement was only attainable as a result of a unique interaction between the novel form and the novel formulation. TransForm has filed broad patents, both on this individual discovery as well as on the principles underlying the general mechanism that we have discovered. We believe this discovery to have value for many other compounds as well.