Co-crystals Yield 30-50X Better Solubility

Itraconazole is a very poorly soluble drug for treatment of anti-fungal infections, with 2002 worldwide annual sales of over $500MM. Its most stable crystalline form is virtually insoluble and, in part because of its very poor solubility, the drug has significant food effects. It has not proven to be possible to make pharmaceutically acceptable salts from this compound. With our CrystalMax® technology, TransForm was able to identify several stable, pharmaceutically acceptable co-crystals of TPI-315. The in vitro performance of these co-crystals is similar to that which might be expected of a salt: namely, they are roughly 30X – 50X more soluble in simulated gastric fluid than the crystalline form of the free base.

In less than 2 months, TransForm discovered:

Novel, stable co-crystal forms with 30X-50X better solubility
Liquid formulations with >3X solubility over marketed oral solution