Data confirms the once daily profile of LCP's extended release tablet formulation of tacrolimus when compared to twice daily Prograf(R) capsules (Astellas Pharma)

HØRSHOLM, Denmark--(BUSINESS WIRE)--Apr. 30, 2009-- LifeCycle Pharma A/S (CSE:LCP), today announced positive interim results from a Phase 2 clinical trial involving 63 patients comparing LCP-Tacro™ tablets administered once daily versus Prograf® capsules, administered twice daily in de novo kidney transplant patients. These data confirm the previous experience with LCP-Tacro™ in stable kidney and liver transplant patients announced in March and July 2008, respectively. The results demonstrate that over the first 14 days of the pharmacokinetic study stage within the early post-operative period following a kidney transplant, LCP-Tacro™ tablets can be safely and efficaciously administered once-daily to de novo kidney transplant patients. These findings are further supported by interim preliminary 6-month follow-up data as the randomized transplant patients have progressed into the 1-year maintenance stage of the study.

“These results provide a very important milestone for LCP’s development activities in the Transplantation therapeutic area. The unique potential benefits of LCP’s MeltDose® formulation technology as applied to LCP-Tacro™ are clearly highlighted in the safety, efficacy, and controlled-release properties of this product,” said Dr. Jim New, President and CEO of LCP. “It’s also an important step forward for our transplantation franchise and our plan to commercialize LCP-Tacro™ within the U.S. and European pharmaceutical markets.”

LCP will draw on these emerging data to form the basis for LCP’s planning and preparation of the pivotal phase 3 study in de novo kidney transplant patients and will consult with the U.S. Food and Drug Administration (FDA) with the goal to submit a final Phase 3 protocol in the second half of 2009. The Phase 3 program will evaluate the use of LCP-Tacro™ with mycophenolate mofetil and corticosteroids compared to the FDA-approved standard treatment of mycophenolate mofetil in combination with cyclosporine and corticosteroids in de novo kidney transplant patients. The upcoming phase 3 studies in de novo kidney transplants will run in parallel with LCP’s currently ongoing phase 3 studies in stable kidney transplant patients.

“From a clinical perspective, these results are very encouraging and show a gentle, but robust pharmacokinetic profile that are supported by interim efficacy and safety data from up to 6-months follow-up period of the ongoing 1-year maintenance stage of the study. LCP-Tacro™ could become the first tacrolimus product to be approved for use with mycophenolate mofetil (MMF; CellCept®, Roche) with the potential to be the only once-daily tacrolimus product on the U.S. market,” said Anderson Gaweco, M.D., Ph.D, Chief Medical Officer at LCP. MMF is FDA-approved for the prevention of transplant allograft rejection when used in combination with cyclosporine and corticosteroids.

“Currently, mycophenolate mofetil in combination with tacrolimus and corticosteroids remains the cornerstone immunosuppressive regimen in kidney transplantation. However, patient compliance is a major issue under this immunosuppressive modality over the long-term. Failure to adhere to the prescribed regimen leads to suboptimal immunosuppression, an increased risk of chronic rejection, and thereafter graft loss. LCP-Tacro™ is a tacrolimus extended release formulation. Because LCP-Tacro™ formulation allows only one intake a day, this might enhance patient compliance and thereby reduce the risk of graft damage, and protect patient quality of life,” said Lionel Rostaing, M.D., Ph.D., Professor of Medicine, Chief of Multiorgan Transplantation Unit, Toulouse University Hospital, Toulouse, France.

About the LCP-Tacro (de novo Kidney) Phase 2 Clinical Trial Design

The Phase 2 clinical trial, which commenced enrollment in October 2008, is an open-label, multi-center, prospective, parallel group dose-finding study in de novo kidney transplant patients. The objectives of the study are to determine the pharmacokinetic profile (AUC0-24, Cmax, Cmin, and Tmax), safety and efficacy of LCP-Tacro™ (tacrolimus) tablets once daily versus Prograf® (tacrolimus) capsules twice daily. De novo kidney transplant candidates who fulfill all inclusion/exclusion criteria are randomized to receive either LCP-Tacro™ or Prograf® within 12 hours following their kidney transplantation. The first dose of LCP-Tacro™ is administered at a 30% lower daily dose than Prograf® and subsequently, doses of both drugs are adjusted based on target whole blood therapeutic tacrolimus levels. A 24-hour pharmacokinetic (PK) profile assessment is performed on Study Days 1, 7 and 14. Patients will continue in the 1 year maintenance stage of the study to evaluate the long-term safety and efficacy of LCP-Tacro™ versus Prograf®.

About LCP-Tacro™ and tacrolimus

Tacrolimus is a leading immunosuppression drug used for the prevention of transplant allograft rejection after organ transplantation. LCP-Tacro™ is being developed as a once daily tablet version of tacrolimus, with improved bioavailability and reduced peak-to-trough variability when compared to Astellas Pharma’s Prograf®, a twice daily version of tacrolimus, marketed worldwide, and it’s once daily version of tacrolimus, Advagraf®, marketed in some European countries.

Transplant patients need to maintain a minimum blood level of tacrolimus for the prevention of transplant allograft rejection, but excessive levels may increase the risk of serious side effects such as nephrotoxicity and opportunistic infections. Therefore, tacrolimus levels need to be managed carefully and transplant patients typically are obliged to make frequent visits to the hospital for monitoring and dose adjustments for months after receiving a new organ.

About Solid Organ Transplant Rejection

The prophylactic treatment of transplant allograft rejection is a major significant segment of the worldwide immunosuppressive market for which sales of Prograf® in 2008 were approximately USD 1.9 billion (IMS; all rights reserved).

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