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Prodrugs

A prodrug-free technology, applied in drug combinations, antineoplastic drugs, pharmaceutical formulations, etc., can solve problems such as slow release and prodrugs that cannot induce tumor remission

Inactive Publication Date: 2014-06-18
KTB TUMORFORSCHUNGS GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Furthermore, it has been shown that albumin-binding derivatives of doxorubicin inserted with the peptide sequence Arg-Ser-Ser-Tyr-Tyr-Ser-Arg are efficiently cleaved by PSA to release the doxorubicin-dipeptide Ser-Arg-DOXO, but free Further release of doxorubicin from the dipeptide proceeds slowly, with >48 hours half-live
Furthermore, although prodrugs were superior to doxorubicin in an orthotopic PSA-positive model, prodrugs failed to induce tumor remission (Graeser et al., Int. J. Cancer, 2008, 122, 145)

Method used

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Experimental program
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Embodiment

[0046] HPLC system

[0047] Method A: Unless otherwise indicated, use a solvent delivery system (HPLC pump 422), variable wavelength UV-VIS detector (HPLC detector 430), and Nucleosil Reverse phase HPLC analysis of all compounds was performed on a Kontron system on a C-18 column (100-5, 250 x 4 mm, Macherey-Nagel). For peak integration, Geminyx software (v1.91 from Goebel Instrumentelle Analytik, FRG) was used. HPLC conditions: flow rate: 1 mL / min, gradient: 0-5 min 100% mobile phase A; 5-35 min increase to 100% mobile phase B; 35-40 min 100% mobile phase B; 40-45 min decrease to 100 % Mobile Phase A; 45-50 minutes 100% Mobile Phase A; Mobile Phase A: 30% CH 3 CN, 70% water + 0.1% TFA, mobile phase B: 70% CH 3 CN, 30% water + 0.1% TFA, injection volume: 50 μL.

[0048] Method B: Using with a Merck F-1050 spectrofluorophotometer (EX. 490nm, EM. 540nm) and a λ1000 visible detector from Bischoff Attached BioLogic Duo-Flow System from Biorad (Munich, Germany) for HPLC to st...

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Abstract

The present invention relates to a prodrug comprising at least one cytostatic agent, wherein said prodrug is cleavable by prostate-specific antigen (PSA), a process for preparing said prodrug and a pharmaceutical composition containing said prodrug in a pharmaceutically effective amount, for use in the treatment of cancer.

Description

technical field [0001] The present invention relates to a prodrug comprising at least one cytostatic agent, wherein said prodrug is cleaved by prostate specific antigen (PSA); a method for preparing said prodrug and comprising a pharmaceutically effective amount of said prodrug, Pharmaceutical compositions for cancer treatment. Background technique [0002] Most of the drugs currently used are compounds of low molecular weight and exhibit high plasma or total body clearance when administered systemically to a patient. Furthermore, the low molecular weight compounds show a high tendency to penetrate body tissues by diffusion, resulting in a homogeneous biodistribution. These are the two main reasons why only small amounts of drugs reach the site of action, and because of their distribution over healthy tissues of the body, the drugs cause problematic side effects. These disadvantages are of particular concern for those drugs with high cytotoxic potential, such as cytostatic...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K5/06A61K47/48A61P35/00
CPCC07K5/06069A61K47/48338C07K7/06C07K5/1013A61K47/65A61P35/00A61K47/50A61K31/7042A61K38/08C07K5/06
Inventor F·克拉茨A·瓦尔内克B·艾尔萨达克
Owner KTB TUMORFORSCHUNGS GMBH