Felix Kratz

Summary

Affiliation: University of Freiburg
Country: Germany

Publications

  1. doi request reprint Evaluation of combination therapy schedules of doxorubicin and an acid-sensitive albumin-binding prodrug of doxorubicin in the MIA PaCa-2 pancreatic xenograft model
    Felix Kratz
    Division of Macromolecular Prodrugs, Tumor Biology Center, Breisacher Strasse 117, D 79106 Freiburg, Germany
    Int J Pharm 441:499-506. 2013
  2. doi request reprint Finding the optimal balance: challenges of improving conventional cancer chemotherapy using suitable combinations with nano-sized drug delivery systems
    Felix Kratz
    Tumor Biology Center, Division of Macromolecular Prodrugs, Breisacher Strasse 117, 79106 Freiburg, Germany
    J Control Release 164:221-35. 2012
  3. doi request reprint Clinical impact of serum proteins on drug delivery
    Felix Kratz
    Tumor Biology Center, Division of Macromolecular Prodrugs, Breisacher Strasse 117, 79106 Freiburg, Germany
    J Control Release 161:429-45. 2012
  4. ncbi request reprint Development of albumin-binding doxorubicin prodrugs that are cleaved by prostate-specific antigen
    Felix Kratz
    Tumor Biology Center, Freiburg, Germany
    Arch Pharm (Weinheim) 338:462-72. 2005
  5. doi request reprint In vitro and in vivo study of an albumin-binding prodrug of doxorubicin that is cleaved by cathepsin B
    Khalid Abu Ajaj
    Tumor Biology Center, Breisacher Strasse 117, 79106, Freiburg, Germany
    Cancer Chemother Pharmacol 64:413-8. 2009
  6. doi request reprint Zosuquidar and an albumin-binding prodrug of zosuquidar reverse multidrug resistance in breast cancer cells of doxorubicin and an albumin-binding prodrug of doxorubicin
    Khalid Abu Ajaj
    Division of Macromolecular Prodrugs, Tumor Biology Center, Breisacher Strasse 117, 79106, Freiburg, Germany
    Breast Cancer Res Treat 134:117-29. 2012
  7. doi request reprint Development of protein-binding bifunctional linkers for a new generation of dual-acting prodrugs
    Khalid Abu Ajaj
    Tumor Biology Center, Breisacher Strasse 117, 79106 Freiburg, Germany
    Bioconjug Chem 20:390-6. 2009
  8. doi request reprint In vitro and in vivo evaluation of a paclitaxel conjugate with the divalent peptide E-[c(RGDfK)2] that targets integrin alpha v beta 3
    Claudia Ryppa
    Tumor Biology Center, Breisacher Strasse 117, 79106 Freiburg, Federal Republic of Germany
    Int J Pharm 368:89-97. 2009
  9. ncbi request reprint Synthesis and biological activity of water-soluble maleimide derivatives of the anticancer drug carboplatin designed as albumin-binding prodrugs
    Andre Warnecke
    Tumor Biology Center, Breisacher Strasse 117, 79106 Freiburg, Germany, Max Delbrück Centrum, Robert Rossle Strasse 10, 13122 Berlin, Germany
    Bioconjug Chem 15:1349-59. 2004
  10. ncbi request reprint Albumin-binding prodrugs of camptothecin and doxorubicin with an Ala-Leu-Ala-Leu-linker that are cleaved by cathepsin B: synthesis and antitumor efficacy
    Björn Schmid
    Tumor Biology Center, Breisacher Strasse 117, 79106 Freiburg, Germany
    Bioconjug Chem 18:702-16. 2007

Collaborators

Detail Information

Publications29

  1. doi request reprint Evaluation of combination therapy schedules of doxorubicin and an acid-sensitive albumin-binding prodrug of doxorubicin in the MIA PaCa-2 pancreatic xenograft model
    Felix Kratz
    Division of Macromolecular Prodrugs, Tumor Biology Center, Breisacher Strasse 117, D 79106 Freiburg, Germany
    Int J Pharm 441:499-506. 2013
    ..A combination of doxorubicin and DOXO-EMCH is currently being investigated in a phase Ib study...
  2. doi request reprint Finding the optimal balance: challenges of improving conventional cancer chemotherapy using suitable combinations with nano-sized drug delivery systems
    Felix Kratz
    Tumor Biology Center, Division of Macromolecular Prodrugs, Breisacher Strasse 117, 79106 Freiburg, Germany
    J Control Release 164:221-35. 2012
    ....
  3. doi request reprint Clinical impact of serum proteins on drug delivery
    Felix Kratz
    Tumor Biology Center, Division of Macromolecular Prodrugs, Breisacher Strasse 117, 79106 Freiburg, Germany
    J Control Release 161:429-45. 2012
    ....
  4. ncbi request reprint Development of albumin-binding doxorubicin prodrugs that are cleaved by prostate-specific antigen
    Felix Kratz
    Tumor Biology Center, Freiburg, Germany
    Arch Pharm (Weinheim) 338:462-72. 2005
    ..EMC-Arg-Arg-Ser-Ser-Tyr-Tyr-Ser-Gly-DOXO showed no in vivo activity in the PSA-negative PC 3 model, but good activity in the CWR22 PSA-positive model that was comparable to Doxorubicin...
  5. doi request reprint In vitro and in vivo study of an albumin-binding prodrug of doxorubicin that is cleaved by cathepsin B
    Khalid Abu Ajaj
    Tumor Biology Center, Breisacher Strasse 117, 79106, Freiburg, Germany
    Cancer Chemother Pharmacol 64:413-8. 2009
    ....
  6. doi request reprint Zosuquidar and an albumin-binding prodrug of zosuquidar reverse multidrug resistance in breast cancer cells of doxorubicin and an albumin-binding prodrug of doxorubicin
    Khalid Abu Ajaj
    Division of Macromolecular Prodrugs, Tumor Biology Center, Breisacher Strasse 117, 79106, Freiburg, Germany
    Breast Cancer Res Treat 134:117-29. 2012
    ..Thus, a novel formulation of zosuquidar has been developed that could have the potential to improve the toxicity issues and tumor targeting properties of the original compound...
  7. doi request reprint Development of protein-binding bifunctional linkers for a new generation of dual-acting prodrugs
    Khalid Abu Ajaj
    Tumor Biology Center, Breisacher Strasse 117, 79106 Freiburg, Germany
    Bioconjug Chem 20:390-6. 2009
    ..Bound to the cysteine-34 position of albumin, it was cleaved efficiently by cathepsin B releasing the free drugs...
  8. doi request reprint In vitro and in vivo evaluation of a paclitaxel conjugate with the divalent peptide E-[c(RGDfK)2] that targets integrin alpha v beta 3
    Claudia Ryppa
    Tumor Biology Center, Breisacher Strasse 117, 79106 Freiburg, Federal Republic of Germany
    Int J Pharm 368:89-97. 2009
    ..In vivo studies in an OVCAR-3 xenograft model demonstrated no antitumor efficacy for either E-[c(RGDfK)(2)] or E-[c(RGDfK)(2)]-paclitaxel compared to moderate efficacy for paclitaxel...
  9. ncbi request reprint Synthesis and biological activity of water-soluble maleimide derivatives of the anticancer drug carboplatin designed as albumin-binding prodrugs
    Andre Warnecke
    Tumor Biology Center, Breisacher Strasse 117, 79106 Freiburg, Germany, Max Delbrück Centrum, Robert Rossle Strasse 10, 13122 Berlin, Germany
    Bioconjug Chem 15:1349-59. 2004
    ....
  10. ncbi request reprint Albumin-binding prodrugs of camptothecin and doxorubicin with an Ala-Leu-Ala-Leu-linker that are cleaved by cathepsin B: synthesis and antitumor efficacy
    Björn Schmid
    Tumor Biology Center, Breisacher Strasse 117, 79106 Freiburg, Germany
    Bioconjug Chem 18:702-16. 2007
    ..In vivo, 1 was superior to free camptothecin in an HT-29 human colon xenograft model; the antitumor efficacy of prodrug 2 was comparable to that of free doxorubicin in the M-3366 mamma carcinoma xenograft model at equimolar doses...
  11. doi request reprint Development of a novel prodrug of paclitaxel that is cleaved by prostate-specific antigen: an in vitro and in vivo evaluation study
    Bakheet Elsadek
    Tumor Biology Center, Division of Macromolecular Prodrugs, Breisacher Strasse 117, D 79106 Freiburg, Germany
    Eur J Cancer 46:3434-44. 2010
    ....
  12. ncbi request reprint Development of albumin-binding camptothecin prodrugs using a Peptide positional scanning library
    Björn Schmid
    Tumor Biology Center, Breisacher Strasse 117, 79106, Freiburg, Germany
    Bioconjug Chem 18:1786-99. 2007
    ..5 mg/kg CPT equivalents) and 40% for CPT (3 x 12.5 mg/kg)]...
  13. ncbi request reprint Development of a novel albumin-binding prodrug that is cleaved by urokinase-type-plasminogen activator (uPA)
    Da Eun Chung
    Tumor Biology Center, Breisacher Strasse 117, 79106 Freiburg, Germany
    Bioorg Med Chem Lett 16:5157-63. 2006
    ..A water-soluble albumin-binding prodrug of doxorubicin [EMC-Gly-Gly-Gly-Arg-Arg-DOXO (EMC, 6-maleimidocaproic acid)] was developed that is cleaved specifically by the tumor-associated protease urokinase-type plasminogen activator (uPA)...
  14. ncbi request reprint A new approach for the treatment of malignant melanoma: enhanced antitumor efficacy of an albumin-binding doxorubicin prodrug that is cleaved by matrix metalloproteinase 2
    Ahmed M Mansour
    Tumor Biology Center, Breisacher Strasse 117, 79106 Freiburg, Germany
    Cancer Res 63:4062-6. 2003
    ..In vivo, 1 was superior to the parent compound doxorubicin in the A375 human melanoma xenograft, which is characterized by a high expression of MMP-2...
  15. doi request reprint Development of dual-acting prodrugs for circumventing multidrug resistance
    Khalid Abu Ajaj
    Tumor Biology Center, Macromolecular Prodrugs, Breisacher Strasse 117, D 79106 Freiburg, Germany
    Bioorg Med Chem Lett 19:995-1000. 2009
    ..The prodrug, once bound through its maleimide moiety to the cysteine-34 group of human serum albumin, was cleaved by cathepsin B and in tumor homogenates demonstrating a release of the anticancer agent doxorubicin and the inhibitor...
  16. ncbi request reprint Synthesis and in vitro efficacy of acid-sensitive poly(ethylene glycol) paclitaxel conjugates
    Paula Rodrigues
    Tumor Biology Center, Department of Mecial Oncology, Clinical Research, Breisacher Strasse 117, 79106 Freiburg, FRG
    Bioorg Med Chem Lett 13:355-60. 2003
  17. doi request reprint Comparative evaluation of the biological properties of reducible and acid-sensitive folate prodrugs of a highly potent doxorubicin derivative
    Khalid Abu Ajaj
    Tumor Biology Center, Breisacher Strasse 117, 79106 Freiburg, Germany
    Eur J Cancer 48:2054-65. 2012
    ....
  18. ncbi request reprint Correlation of the acid-sensitivity of polyethylene glycol daunorubicin conjugates with their in vitro antiproliferative activity
    Paula C A Rodrigues
    Tumor Biology Center, Department of Medical Oncology, Clinical Research, Breisacher Strasse 117, D 79106 Freiburg, Germany
    Bioorg Med Chem 14:4110-7. 2006
    ..The acid-sensitivity of the link between PEG and daunorubicin is therefore an important parameter for in vitro efficacy...
  19. ncbi request reprint Maleimide-oligo(ethylene glycol) derivatives of camptothecin as albumin-binding prodrugs: synthesis and antitumor efficacy
    Andre Warnecke
    Tumor Biology Center, Breisacher Strasse 117, 79106 Freiburg, Germany
    Bioconjug Chem 14:377-87. 2003
    ..Both albumin-binding derivatives of camptothecin were well-tolerated and showed enhanced antitumor efficacy when compared to CPT...
  20. ncbi request reprint Anticancer carrier-linked prodrugs in clinical trials
    Felix Kratz
    Tumor Biology Center, Macromolecular Prodrugs, Freiburg, Germany
    Expert Opin Investig Drugs 16:1037-58. 2007
    ..This review summarizes the Phase I-III studies that have been performed with these macromolecular prodrugs...
  21. doi request reprint In vitro and in vivo evaluation of doxorubicin conjugates with the divalent peptide E-[c(RGDfK)2] that targets integrin alphavbeta3
    Claudia Ryppa
    Tumor Biology Center, Breisacher Strasse 117, 79106 Freiburg, Federal Republic of Germany
    Bioconjug Chem 19:1414-22. 2008
    ....
  22. ncbi request reprint Phase I and pharmacokinetic study of the (6-maleimidocaproyl)hydrazone derivative of doxorubicin
    Clemens Unger
    Department Medical Oncology, Tumor Biology Center, Freiburg, Germany
    Clin Cancer Res 13:4858-66. 2007
    ..The purpose of the phase I study was to characterize the toxicity profile of DOXO-EMCH, establish a recommended dose for phase II studies, and assess potential anticancer activity...
  23. ncbi request reprint Synthesis, cleavage profile, and antitumor efficacy of an albumin-binding prodrug of methotrexate that is cleaved by plasmin and cathepsin B
    Andre Warnecke
    Tumor Biology Center, Freiburg, Germany
    Arch Pharm (Weinheim) 340:389-95. 2007
    ..The data provide a further proof of concept for the development of albumin-binding, enzymatically cleavable prodrugs of anticancer drugs...
  24. ncbi request reprint Prodrug strategies in anticancer chemotherapy
    Felix Kratz
    Macromolecular Prodrugs, Tumor Biology Center, Breisacher Strasse 117, 79106 Freiburg, Germany
    ChemMedChem 3:20-53. 2008
    ..Chemical realization of prodrug approaches is illustrated by drug candidates that have or may have clinical importance...
  25. ncbi request reprint DOXO-EMCH (INNO-206): the first albumin-binding prodrug of doxorubicin to enter clinical trials
    Felix Kratz
    Macromolecular Prodrugs, Tumor Biology Center, Freiburg, Germany
    Expert Opin Investig Drugs 16:855-66. 2007
    ..e., myelotoxicity and mucositis). DOXO-EMCH was able to induce tumor regressions in anthracycline-sensitive tumors (i.e., breast cancer, small cell lung cancer and sarcoma). Phase II studies will be initiated at the beginning of 2007...
  26. doi request reprint Albumin as a drug carrier: design of prodrugs, drug conjugates and nanoparticles
    Felix Kratz
    Head of Macromolecular Prodrugs, Tumor Biology Center, Breisacher Strasse 117, D 79106 Freiburg, Germany
    J Control Release 132:171-83. 2008
    ....
  27. doi request reprint Development of novel bisphosphonate prodrugs of doxorubicin for targeting bone metastases that are cleaved pH dependently or by cathepsin B: synthesis, cleavage properties, and binding properties to hydroxyapatite as well as bone matrix
    Katrin Hochdörffer
    Division of Macromolecular Prodrugs, Tumor Biology Center, Breisacher Strasse 117, 79106 Freiburg, Germany
    J Med Chem 55:7502-15. 2012
    ..In orientating toxicity studies in nude mice, the MTD of 1 was 3-fold higher compared to conventional doxorubicin, whereas 3 showed essentially the same MTD as doxorubicin...
  28. ncbi request reprint Probing the cysteine-34 position of endogenous serum albumin with thiol-binding doxorubicin derivatives. Improved efficacy of an acid-sensitive doxorubicin derivative with specific albumin-binding properties compared to that of the parent compound
    Felix Kratz
    Tumor Biology Center, Breisacher Strasse 117, 79106 Freiburg, Germany
    J Med Chem 45:5523-33. 2002
    ..3 was distinctly superior to the parent compound doxorubicin in three animal tumor models (RENCA, MDA-MB 435, and MCF-7) with respect to antitumor efficacy and toxicity...
  29. doi request reprint 2,4-Bis(hydroxymethyl)aniline as a building block for oligomers with self-eliminating and multiple release properties
    Andre Warnecke
    Macromolecular Prodrugs, Tumor Biology Center, Breisacher Strasse 117, 79106 Freiburg, Germany
    J Org Chem 73:1546-52. 2008
    ..It was found that chain degrading 1,6-benzyl elimination occurs much faster than the effector releasing 1,4-elimination...