Veloxis CEO says Envarsus XR is unique product for kidney transplant patients

After waiting a year and a half for approval in the United States, Veloxis recently announced that the Food and Drug Administration has approved its once-daily Envarsus XR tablets for the prophylaxis of rejection in kidney transplant patients.

The product features the active ingredient called tacrolimus, which is also found in the twice-daily oral tablets currently available on the market.

"Tacrolimus is a remarkable drug that revolutionized transplant medicine as a result of its remarkable pharmacology in preventing rejection; the drug however is pharmacokinetic nightmare and is prone to significant fluctuations and variability," Veloxis President and CEO Bill Polvino told American Pharmacy News recently. "This variability is particularly problematic for a drug that has a narrow therapeutic index, like tacrolimus does. If the drug level is too low, the organ is at risk of rejection; if the drug level is too high, there are significant toxicities including tremor, infections, malignancy and ironically kidney toxicity. And the drug itself displays a great deal of variability in the bloodstream."

Polvino said Envarsus XR is unique in what it offers as a transplant product.

"We used our proprietary formulation technology, MeltDose, to re-engineer tacrolimus delivery and significantly alter the blood profile," Polvino said. "Envarsus XR provides significantly greater oral absorption, and consequently a lower dose requirement; the kinetics are made to be much 'flatter' with a very significant prolongation in time to peak concentrations, and a marked reduction in peak concentration and peak-to-trough variability. The result for a patient is once-daily dosing, a lower total daily dose, and a blood level that fluctuates much less during the day than is seen with any other tacrolimus oral product."

Polvino did point that that while Envarsus does present great potential benefits, it also has significant side effects.

"Just like other transplant therapies, these side effects include the risks of serious infections, malignancies, diabetes, tremors, kidney damage, and other adverse reactions," he said. "There are also other available transplant (therapies) that are quite good for transplant patients. The choice of the transplant therapy, the management of the drug, and the monitoring for side effects are important decisions that really need to be made on an individual basis between the patient and his/her treating clinician."

While future studies are planned to reduce side effects and determine the risk and benefits of Envarsus XR, initial studies have shown that the lower-dose drug immunosuppressive regimen has resulted in no reduction in efficacy. In some subgroups, such as African Americans, there has even been a suggestion of improved efficacy.

Envarsus XR is expected to be available to kidney transplant recipients during the fourth quarter of this year.

"We hope that Envarsus XR offers kidney transplant patients and their clinicians a new therapeutic option," Polvino said. "We have demonstrated the appropriate regimen for converting patients to this new therapeutic, specifically by reducing the total dose by 20 percent, administering it once a day, and by rechecking a blood level to ensure that the final dose is tweaked appropriately by the treating clinician to ensure blood levels are in the correct range. We have clearly changed the blood profile of tacrolimus into an oral delivery pattern that has never been achieved by any other oral tacrolimus product."