SUBA™itraconazole

Itraconazole, a synthetic broad-spectrum triazole antifungal agent discovered in 1984, is used for with the treatment of fungal infections. It is a prescription drug that may be given orally or intravenously.
 
Itraconazole is marketed worldwide by Johnson & Johnson companies under a number of brand names, the most common of which is Sporanox®. In 2000, the US patent for the itraconazole molecule in Sporanox® Capsules expired. For the year ending 2009, global sales of Sporanox® and other generic itraconazole products was approximately 550M USD.

Itraconazole is difficult to formulate as an oral product because of its low solubility in water.  As such, most formulations have relatively low bioavailability (that is a high dose must be administered to ensure sufficiently high blood levels).  Currently available itraconazole formulations, including Sporanox® Capsules exhibit a significant food effect and carry an “administer with food” label.

SUBA technology uses a molecular dispersion to improve the bioavailability of poorly soluble drugs.  This dispersion improves the dissolution of poorly soluble drugs compared to their normal crystalline form.

Matrix core of active
(x600)	(x400)
Itraconazole crystals microcapsule cross section

SUBA™-itraconazole has been developed using patented technology to overcome the inherent difficulties in formulating itraconazole (i.e. to improve the oral bioavailability of itraconazole).

Pharmacokinetic studies to date highlight the superior bioavailability of SUBA™-Itraconazole to the market leading antifungal product, Sporanox®.

Itraconazole Bioavailability Study CM4799
Itraconazole, Mean plasma concentration (n=8)
Treatment A (blue): 1x100mg test itraconazole capsule, fasted
Treatment B (red): 1x100mg Sporanox capsule, fasted

Source: Pilot study to compare the bioavailability of a test itraconazole formulation with the reference Sporanox®. Report of Itraconazole Bioavailability Study Number CM4799. 24 Nov 1999.

Please note this information is intended for potential licensees.

The product is currently under clinical study.