Use of 3'-azido-2',3'-dideoxyuridine in combination with...

A - Human Necessities – 61 – K

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A61K 31/70 (2006.01) A61K 45/06 (2006.01)

Patent

CA 2335617

It has been discovered that 3'-azido-2',3'-dideoxyuridine (CS-87) induces a transient mutation in HIV-1 at the 70th codon (K to R, i.e., lysine to arginine) of the reverse transcriptase region of the virus. Based on this discovery, a method and composition for treating HIV is provided that includes administering CS-87 or its pharmaceutically acceptable salt or prodrug to a human in need of therapy in combination or alternation with a drug that induces a mutation in HIV-1 at a location other than the 70th codon of the reverse transcriptase region. This invention can be practiced by referring to the published mutation patterns for known anti-HIV drugs, or by determining the mutation pattern for a new drug.

Selon l'invention, 3'-azido-2',3'-didéoxyuridine (CS-87) induit une mutation transitoire dans le VIH-1 au 70ème codon (de K à R; c.-à-d. de la lysine à l'arginine) de la région transcriptase inverse du virus. Sur la base de cette découverte, un procédé et une composition sont mis au point pour traiter le VIH. Le procédé consiste à administrer à un être humain nécessitant une telle thérapie la composition de CS-87 ou son sel pharmaceutiquement acceptable ou promédicament, en association ou en alternance avec un médicament pouvant induire une mutation dans le VIH-1 à un emplacment autre que le 70ème codon de la région transcriptase inverse. Le procédé de l'invention peut être mis en oeuvre par référence aux configurations de mutation publiées pour des médicaments anti-HIV connus, ou par détermination de la configuration de mutation pour un nouveau médicament.

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