A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 47/48 (2006.01) A61K 38/08 (2006.01) A61K 47/20 (2006.01)
Patent
CA 2323784
A carrier for in vivo delivery of a therapeutic agent comprising a thiol group is provided, wherein the therapeutic agent is conjugated to the carrier via a biodegradable disulfide bond. Since extracellular fluids in vivo do not provide the appropriate environment to efficiently reduce a disulfide bond, while cellular cytosol does provide an appropriate environment, the agent will remain substantially coupled to the carrier while circulating through the body until the carrier crosses a cell membrane. As a result, the therapeutic agent is protected from degradation and renal clearance, and the potential for the therapeutic agent to elicit an immune response is limited.
L'invention porte sur un excipient destiné à l'administration in vivo d'un agent thérapeutique et comprenant un groupe thiol, l'agent thérapeutique étant conjugué à l'excipient par une liaison disulfure biodégradable. Du fait que, contrairement au cytosol cellulaire, les fluides extracellulaires in vivo ne créent pas l'environnement approprié pour réduire de manière efficace une liaison disulfure, l'agent reste alors pratiquement couplé à l'excipient tout en circulant dans le corps jusqu'à ce que l'excipient traverse une membrane cellulaire. En conséquence, l'agent thérapeutique est protégé de la dégradation et de la clairance rénale, mais son potentiel pour déclencher une réponse immune est limité.
Leibowitz Michael J.
Stein Stanley
Ogilvy Renault Llp/s.e.n.c.r.l.,s.r.l.
University Of Medecine And Dentistry Of New Jersey
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