Prodrugs and drugs for selective ADC tumor therapy

Antibody tumor therapies have provided therapeutic benefit to patients with cancer, autoimmune diseases and other serious medical conditions. However, many antibodies lack sufficient intrinsic anti-tumor activity to be used as therapeutics. Scientists at the University of Göttingen developed new highly potent drugs (with an IC50 in the pico-molar range) as well as selective antibody tumor therapeutical approaches through their prodrugs.

The IP has been successfully licensed to the British ADC company Iksuda Therapeutics.

Challenge

While a prodrug needs to have low cytotoxicity, the activated drug must on the other hand show a very high cytotoxicity in the pico-molar range. Thus, there is a high medical unmet need to have prodrugs/drugs with a big therapeutic window and extremely high and selective cytotoxicity.

Our Solution

Scientists at the University of Göttingen developed new highly potent drugs (with an IC50 in the pico-molar range) as well as a selective tumor therapy through their prodrugs.

Advantages

  • New highly soluble prodrugs with low cytotoxicity.
  • Prodrug has low cytotoxicity (IC50 = 146.000 pmol/l), whereas drug is highly cytotoxic in low pico-molar range (IC50 = 0,11 pmol/l).
  • Higher cytotoxicity than actually used Doxorubicin.
  • Even less side-effects expected due to QIC50 Prodrug/Drug = 1.000.000
  • Expected improvement in safety through bigger therapeutical dosage range.
  • Specific tumor targeting through available antibodies.
  • Activation of the prodrug into cytotoxic drug occurs through the enzyme at the tumor site only (ADEPT or ADC).
  • NEW: Now including innovative linker technology to directly couple to antibody!

CBI moiety of Duocarmycin. Our prodrug technology is based on Duocarmycin analoga.

Applications

Tumor Therapy:

  • Use of Prodrugs for an Antibody Directed Enzyme Prodrug Therapy (ADEPT) or Antibody Drug Conjugate (ADC).
  • Use of Drugs for a direct cancer therapy possible.

Development Status

The out-licensed ADC payload platform, termed as Protein Alkylating (ProAlk) tumour-activated payload platform, is now under Iksuda's development.

Contact

Dr. Stefan Uhle
Patent Manager Life Science
E-Mail: This email address is being protected from spambots. You need JavaScript enabled to view it.
Tel.: +49 551 30724 154
Reference: BioT-0706+BioT-1248+BioC-1848-SUG+BioC-2012-SUG

Tags: Therapy, Life science

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