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Advances in development of “lipidoid” formulations for systemic delivery of RNAi therapeutics

Published on December 30, 2009 at 12:54 AM · No Comments

Alnylam Pharmaceuticals, Inc. (Nasdaq: ALNY), a leading RNAi therapeutics company, and collaborators from the David H. Koch Institute for Integrative Research at the Massachusetts Institute of Technology (MIT) today announced the publication of new data in the journal Proceedings of the National Academy of Sciences (PNAS) describing further advancements in discovery and development of novel “lipidoid” formulations for the systemic delivery of RNAi therapeutics. Lipidoids are lipid-like materials discovered for the delivery of RNAi therapeutics, and were originally described by Alnylam and MIT collaborators (Akinc et al., Nature Biotechnology, 26: 561-569, 2008). In particular, the new research findings demonstrate the discovery of new lipidoid materials that facilitate significantly improved in vivo potency for RNAi therapeutics.

“We are excited by the delivery performance of these new formulations”

“We are very encouraged with the substantial progress we and our collaborators have made with lipid nanoparticles (LNPs) based on novel lipid-like materials such as lipidoids,” said Victor Kotelianski, M.D., Ph.D., D.Sc., Senior Vice President, Distinguished Alnylam Fellow. “To our knowledge, these new LNP formulations facilitate endogenous liver gene silencing at doses that are orders-of-magnitude lower than those required by previously described siRNA delivery approaches, thereby setting a new standard in potency for the systemic delivery of RNAi therapeutics. In addition, the current study is the first to report on the simultaneous and highly specific RNAi-mediated silencing of as many as five liver targets in vivo, serving as proof of principle that multiple genes involved in similar or divergent biological pathways can be silenced with a single administration of a single drug product. From a therapeutic standpoint, this could enable novel pharmaceutical strategies, where silencing of multiple targets could achieve an enhanced level of efficacy.”

The new pre-clinical data describe a formulation based on a lipidoid known as “C12-200” that was shown to:

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