Conjugates useful in the treatment of prostate cancer

A - Human Necessities – 61 – K

Patent

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Details

A61K 38/14 (2006.01) C07K 5/09 (2006.01) C07K 5/103 (2006.01) C07K 5/107 (2006.01) C07K 14/47 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2321171

Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA) and known cytotoxic agents are disclosed. The conjugates of the invention are characterized by a hydroxylalkylamino linker between the oligopeptide and vinblastine. Such conjugates are useful in the treatment of prostatic cancer and benign prostatic hypertrophy (BPH). Also disclosed are novel cytotoxic agents that are derivatives of vinca alkaloid drugs.

L'invention concerne des conjugués qui comprennent des oligopeptides portant des séquences d'acides aminés subissant sélectivement un clivage protéolytique sous l'effet d'un antigène libre spécifique de la prostate et d'agents cytotoxiques connus. Les conjugués de l'invention se caractérisent par une liaison hydroxylalkylamino entre l'oligopeptide et la vinblastine. De tels conjugués contiennent au traitement du cancer de la prostate et de l'hypertrophie prostatique bénigne. L'invention concerne également des agents cytotoxiques dérivés des alcaloïdes de la pervenche.

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