5-Fluorouracil / Doxorubicin / Gemcitabine based Prodrugs Targeting Hypoxia

Protection of active site by 2-nitroimidazole is released in hypoxia

Advantage & Core Benefits

  • Much higher concentrations are well tolerated due to reduced toxicity.
  • Prodrugs are synthesized by one step reaction from commercialized GMP compounds.
  • Prodrugs of three chemotherapy compounds are registered-patent protected.

Background & Technology

Although 5-Fluorouracil(5-FU), Doxorubicin(DOX) and Gemcitabine(GEM) are commonly prescribed to kinds of tumors, severe adverse effects owing to the toxicity to normal dividing cells limit the dose and efficacies.     Moreover, those drugs cannot reach hypoxic regions of tumor, and that could be one of the reasons that cancers acquire drug resistance and abilities of invasion and metastasis.

The novel hypoxia-activated prodrugs have been engineered based on nitro-imidazole derivative conjugated with 5-FU, DOX and GEM (Fig). The drugs are designed to seal the toxicity in normoxic condition.


 5Fluo 1

Data & Publication

Prodrug was selectively distributed to hypoxic region of tumor after intraperitoneal administration of DOX / or prodrug to tumor-bearing mice (Fig). Body weights of mice treated with the prodrug with high dose continued to increase, while those in low dose DOX treated group were declined and most of these mice were dead by toxicity of DOX. Survival rates treated with prodrug were drastically improved(Fig).

5Fluo 2


5Fluo 3


Registered: 9655975(US), 5676020 (JP)

Pending: 2816036 (EP)


Dr. Yutaka Ikeda and Dr. Yukio Nagasaki (Tsukuba University)


We are seeking a company who are interested in commercializing this technology.

Product No:TP-00786



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