Munich, Germany
Munich, Germany
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Heinemann V.,Ludwig Maximilians University of Munich | Ebert M.P.,University of Heidelberg | Laubender R.P.,Ludwig Maximilians University of Munich | Bevan P.,WILEX | And 2 more authors.
British Journal of Cancer | Year: 2013

Background:To evaluate the efficacy and tolerability of the urokinase plasminogen activator (uPA) inhibitor upamostat in combination with gemcitabine in locally advanced pancreatic adenocarcinoma (LAPC).Methods:Within a prospective multicenter study, LAPC patients were randomly assigned to receive 1000 mg m-2 of gemcitabine IV weekly either alone (arm A) or in combination with 200 mg (arm B) or 400 mg (arm C) oral upamostat daily. Efficacy endpoints of this proof-of-concept study included response rate, time to first metastasis, progression-free and overall survival (OS).Results:Of the 95 enroled patients, 85 were evaluable for response and 93 for safety. Median OS was 12.5 months (95% CI 8.2-18.2) in arm C, 9.7 months (95% CI 8.4-17.1) in arm B and 9.9 months (95% CI 7.4-12.1) in arm A; corresponding 1-year survival rates were 50.6%, 40.7% and 33.9%, respectively. More patients achieved a partial remission (confirmed responses by RECIST) with upamostat combination therapy (arm C: 12.9%; arm B: 7.1%; arm A: 3.8%). Overall, only 12 patients progressed by developing detectable distant metastasis (arm A: 4, arm B: 6, arm C: 2). The most common adverse events considered to be related to upamostat were asthenia, fever and nausea.Conclusion:In this proof-of-concept study targeting the uPA system in LAPC, the addition of upamostat to gemcitabine was tolerated well; similar survival results were observed for the three treatment arms. © 2013 Cancer Research UK.


Patent
Wilex | Date: 2013-07-01

The invention relates to specific amino acid sequences which have been determined to be target epitope for antibodies, in particular, for a G250 antibody.


The present invention refers to the detection of bone metastases in renal cell carcinoma (RCC) and suitable reagents therefore using a ^(12)4 I-labelled antibody or antigen-binding fragment thereof directed against carbonic anhydrase IX.


Patent
Wilex | Date: 2012-09-12

The invention relates to a method for the treatment of G250-antigen-expressing tumors, in particular renal clear cell carcinoma comprising the administration of G250-antigen-specific antibodies to high-risk patients diagnosed with non-metastasising disease.


The present invention relates to a combined treatment of cancer using a urokinase inhibitor and a cytotoxic or a cytostatic agent.


A method for enhancing the therapeutic effect of cytokine treatment is disclosed. More specifically the present invention relates to a method for administering to a tumor patient a therapeutic dose of cytokine in combination with antibodies directed against the tumor associated antigen carbonic anhydrase IX (CAIX/G250/MN). The improved treatment method is characterized in a significantly reduced cytokine-related toxicity combined with potentiated effectiveness of anti-G250 antibody alone, resulting in a positive therapeutic response with respect to that observed with single anti-tumor agents alone.


The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidino-phenylalanine derivatives under gentle conditions (H_(2 )or ammonium formiate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H_(2), Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.


The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidino-phenylalanine derivatives under gentle conditions (H_(2 )or ammonium formiate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H_(2), Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.


Patent
Wilex | Date: 2014-02-21

The present invention relates to a carbonic anhydrase IX targeting compound for the use in the treatment of cancer, wherein the use comprises quantifying CAIX expression as well as the determination of a CAIX score based on the CAIX expression. The present invention relates further to a method for diagnosing, predicting and/or classifying a cancer disease comprising quantifying CAIX expression, and the determination of a CAIX score.


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