Limerick BioPharma Announces Positive Phase 1a Data for LIM-0705
SOUTH SAN FRANCISCO, Calif.--(BUSINESS WIRE)--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.
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.
LIM-0705 is an orally administered small molecule. It is being developed for adjunctive use with the calcineurin inhibitor drug, tacrolimus that suppresses immune rejection after transplant surgery. LIM-0705 is designed to activate ATP-binding cassette (ABC) transporters to chaperone tacrolimus away from vulnerable organs and back into the bloodstream.
About Limerick BioPharma
Limerick BioPharma (http://www.limerickbio.com) is developing small molecule modulators of cell membrane-bound transporters to rid cells of unwanted toxins. By activating cellular transport pumps to redistribute drugs away from organs and tissues where they have adverse effects, the company's proprietary Activators minimize toxic side effects at non-targeted vulnerable organs and tissues while maintaining or enhancing a drug's desired effects. Limerick Activators are applicable to a broad range of therapeutic drug classes including immunosuppressants, opioids, immunomodulators, selective estrogens receptor modulators, and psychotropics. In the monotherapy setting, Limerick is developing Activators that target the treatment of metabolic diseases such as hypercholesteremia and hyperglycemia via a novel mechanism related to reverse cholesterol transport.
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Posted: March 2010