Positive results from Limerick BioPharma's LIM-0705 Phase 1a trial

Mar 10 2010

Limerick BioPharma, Inc., a developer of innovative therapies that help cells pump unwanted or toxic substances away from vulnerable tissues, has announced positive results of a Phase 1a trial for its lead compound, LIM-0705, which has completed its first in man study.

“Not only is the safety data compelling, but we are encouraged by the data demonstrating an effect of LIM-0705 on the pharmacokinetics of Tacrolimus.”

LIM-0705 is a small-molecule compound being developed to administer alongside tacrolimus, a calcineurin inhibitor widely used to block the body from rejecting transplanted organs. Because tacrolimus produces toxicities in the pancreas, brain and kidneys, LIM-0705 is designed to activate specific ATP-binding cassette (ABC) transporters in these organs to pump tacrolimus out of vulnerable cells while preserving its effect against tissue rejection.

The Phase 1a trial consisted of two studies. In a single ascending dose study involving 48 subjects, LIM-0705 was evaluated pharmacologically at a variety of doses. Three dose levels of LIM-0705 were then selected for a multiple ascending dose study. In this study, 28 normal volunteers received LIM-0705 twice daily for 5 days. Pharmacokinetic parameters were again evaluated. On the final day of dosing LIM-0705, a single dose of tacrolimus was also administered. Subjects then returned two weeks later for an additional dose of tacrolimus before exiting the study.

No serious adverse side effects of LIM-0705 or tacrolimus were noted in this trial. Pharmacokinetic analysis revealed that LIM-0705 favorably altered tacrolimus tissue distribution in a majority of subjects (P<0.001) compared to dosing tacrolimus alone. Neither GI uptake nor elimination was adversely affected.

“We are pleased by these results from the first completed human trial of our Activator technology,” said Michael Chang, Limerick’s Vice President of Research and Development. “Not only is the safety data compelling, but we are encouraged by the data demonstrating an effect of LIM-0705 on the pharmacokinetics of Tacrolimus.”

Limerick recently initiated a multi day Phase 1b study with LIM-0705 and tacrolimus. Safety and efficacy parameters including tacrolimus-induced immune suppression will be measured in this next trial.