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ChemTech Expertise

Novel PELORUSIDE analogues with microtubule-stabilizing activity

The current broad spectrum antitumor drugs, paclitaxel (Taxol ®) and docetaxel (Taxotere ®), are chemotherapeutics that stabilise the microtubules. As they interfere with the dynamics of the microtubules, they inhibit the formation of the mitotic spindle and consequently arrest the proliferation of fast dividing cells, such as cancer cells. However multidrug resistance, complex pharmaceutical formulations and toxicity limit their pharmaceutical use. 

Researchers at Ghent University have designed a novel simplified peloruside analogue, nicknamed Pelofen. Our proprietary technology has multiple advantages such as:

• Novel peloruside analogue with a unique binding site on tubulin maintains its activity in paclitaxel-resistant cancers
• Unique binding site on tubulin allows combination therapies with current chemotherapeutics which suppresses development resistance upon treatment of cancer cells
• Synergetic effect with paclitaxel permits lower doses of chemotherapeutics during treatment and consequently reduces side effects
• Hydrophilic nature of Pelofen makes it less susceptible for MDR via overexpression of the P-gp efflux system and allows easy formulations of the drug
• Simplified structure of Pelofen allows shorter synthesis and makes it more economically feasible as synthetic drug
• Modular synthesis makes a broad range of diverse Pelofen analogues accessible

Read more in our Technology Offer: "Pelofen: enabling the treatment of resistant cancers" , our poster or contact us
 

UGent VITAMIN D ANALOGUE (Inecalcitol) licensed to HYBRIGENICS

Identified for its major role in regulating calcium absorption from the gut, storage in mineral form in the bones, and excretion by the kidneys, vitamin D can influence the regulation of a very broad range of biological functions linked with cell proliferation, cell differentiation, cell death, inflammation or immune reactions. Therefore, vitamin D's role has been investigated in multiple diseases.  A Vitamin D analogue (Inecalcitol), designed and synthesized at Ghent University has been licensed to HYBRIGENICS. It has been shown that Inecalcitol also acts by binding to the vitamin D receptor but some of its properties differ from calcitriol's. Inecalcitol does not bind to the vitamin D binding protein which means that it readily penetrates into cells without accumulating in the bloodstream, allowing it to have a more manageable half-life. Inecalcitol's binding to VDR is performed in a different conformation to that of calcitriol, which leads to an inecalcitol/VDR/RXR complex that not bind to the same VDREs or binds with different affinities than those of calcitriol's complex.  

Hybrigenics' current development program is based on Inecalcitol, our vitamin D receptor agonist being studied in clinical trials for several potential indications:

  • alone in chronic lymphocytic leukaemia
  • in combination with imatinib in chronic myeloid leukaemia
  • in combination with daratumumab in multiple myeloma 
  • in prostate cancer, for use with current standards of care

“Five out of six human multiple myeloma cell lines and all four human acute myeloid leukemia
cell lines tested have responded within 2 to 3 days by a strong and reproducible increase in the
expression of the CD38 surface antigen to in vitro treatment by inecalcitol. These results
strongly support the idea to test in the clinics the combination of inecalcitol with an anti-CD38
therapy such as daratumumab. Inecalcitol may strengthen the use of daratumumab in multiple
myeloma and could also open acute myeloid leukemia as a new therapeutic indication for
daratumumab,” said Remi Delansorne, Hybrigenics’ CEO. 


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