Polymers containing antifibrotic agents, compositions containing

Drug – bio-affecting and body treating compositions – Solid synthetic organic polymer as designated organic active... – Aftertreated polymer

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514824, 514838, 424450, A61K 31765, A61K 31785

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active

056608225

ABSTRACT:
The present invention concerns a method for treating fibrotic conditions by administration of an effective amount of an antifibrotic agent. The antifibrotic agent is preferably a proline analog, such as cis-4-hydroxy-L-proline (cHyp). The antifibrotic agent is operatively linked to a monomer or a polymer, with or without a linking compound, e.g., lysine. Intravenous administration is preferred. The present method facilitates the delivery and release of the antifibrotic agent to inhibit collagen accumulation and thereby to treat fibrosis where collegen metabolism is implicated. A reduced quantity of the antifibrotic agent and a corresponding reduction in the potential for toxicity resulting from prolonged administration thereof may be realized.

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Ertel et al. "Copolymers of amino acids and poly(ethylene glycol): a new family of functionalized drug-carriers." Polym. mat. Sci. Eng. 66: 486-7. Proc. Am. Chem. Soc. (1991).
Papaionnou et al. "Simple synthesis of cis-4-hydroxy-L-proline and derivatives suitable for use as intermediate in peptide synthesis." Acta Chem. Scand. 44: 243-51. (1990).

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