Camptothecin-peptide conjugates and pharmaceutical...

A - Human Necessities – 61 – K

Patent

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A61K 47/48 (2006.01)

Patent

CA 2658015

The present invention relates to a novel compound of use in the improved delivery of therapeutic drug agents into target cells or tissues, composition comprising the same and uses thereof. The compound is more specifically a conjugate of a peptidic moiety and a camptothecin, a derivative or analog thereof which provides numerous benefits, including enhancement in terms of aqueous solubility, pharmacokinetics and tissue distribution, enlargement of the therapeutic index, and limitation of the inter-patient metabolic variability, as well as improvement of delivery of the biologically active ingredient to the target cells or tissues.

La présente invention concerne l'utilisation d'un nouveau composé permettant une meilleure administration d'agents médicamenteux thérapeutiques à des cellules ou tissus cibles, de même que des compositions contenant ledit composé et ses utilisations. Le composé est plus spécifiquement un conjugué d'un groupement peptidique et d'une camptothécine, un dérivé, ou un analogue de celui-ci, qui offre de nombreux avantages, incluant une amélioration en termes d'hydrosolubilité, de pharmacocinétique et de distribution tissulaire, une élévation de l'indice thérapeutique, et une limitation de la variabilité métabolique parmi les patients. L'invention concerne également l'amélioration de l'administration du principe biologiquement actif aux cellules ou tissus cibles.

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