Product Programs

Envarsus® has been developed as a once-daily dosage tablet version of tacrolimus for the treatment of kidney transplant patients. Compared with Astellas Pharma Inc’s. Prograf, a twice-daily dosage capsule version of tacrolimus, Veloxis believes that Envarsus® has the following potential benefits:

  • once-daily dosing;
  • improved systemic absorption;
  • improved bioavailability and thus a lower dose of tacrolimus; and
  • limited variability in the concentration of tacrolimus in the blood (“peak-to-trough” fluctuation).

Veloxis believes that physicians will have a preference for the once-daily dosing of Envarsus® given the potential for positive impact on compliance for patients, and based on physicians’ preference for non-generic products for molecules with a narrow therapeutic index.

Advagraf, Astellas Pharma Inc.’s once-daily dosage form of Prograf, was approved by the EMA in mid-2007 and commercialized in the European Union and other regions. In July 2013, Advagraf was approved for commercialization in the U.S. as Astagraf XL.

Transplant patients need to maintain a minimum level of tacrolimus in the blood in order to prevent organ rejection. On the other hand, if too much tacrolimus is administered, there is an increased risk of serious side effects such as kidney damage.

Since tacrolimus is a “narrow therapeutic index” drug, its concentration and dosing must be carefully managed, typically requiring transplant patients to visit the hospital for monitoring and dose adjustments after receiving a new organ. In Phase I, II and III clinical studies, Envarsus® has demonstrated improved and higher bioavailability when compared with Prograf.

Envarsus® is formulated using Veloxis’ MeltDose technology, and through this technology Veloxis has aimed to optimize the delivery kinetics of Envarsus® to provide “flat” pharmacokinetics, reducing the peak concentrations associated with standard tacrolimus formulations. The benefits of these flatter, less variable blood levels may potentially include a reduction in side effects, an improvement in efficacy and/or greater convenience to patients, including a less frequent need for dose adjustments. The development programme at Veloxis seeks to demonstrate data to support some or all of these potential benefits.