Tinostamustine (EDO-S101)

Elodie_Espesset · November 22, 2017, 7:14pm

A new phase 1/2 trial is recruiting patients with soft tissue sarcoma (including synovial sarcoma) in California and Arizona:

Elodie_Espesset · November 22, 2017, 8:18pm

EDO-S101 is a mix of bendamustine and HDAC inhibitor vorinostat:

ncbi.nlm.nih.gov

The Alkylating-HDAC Inhibition Fusion Principle: Taking Chemotherapy to the Next Level with the First in Class Molecule EDO-S101.

T Mehrling and Y Chen, Anti-cancer agents in medicinal chemistry, 2016

Chemotherapy may still be an essential component to treat cancer in combination with new targeted therapies. But chemotherapy needs to get smarter in order to make those combination regimens more effective and also more tolerable, particularly for an aging population. We describe the first time the synthesis and pharmacological testing of a fusion molecule comprising of the alkylator bendamustine and the HDAC-inhibitor vorinostat. The drug was designed to allow for the exploitation of both mechanisms of action simultaneously with the goal to provide a molecule with superior efficacy over the single agents. The pharmacological testing confirms the full functional capacity of both moieties and encouraging pharmacological data raises the hope that the drug may turn out to be a great addition to the armentarium of anticancer agents.

A phase 2 study of bendamustine in patients with refractory soft tissue sarcoma from Germany gave the following results in 2007:
http://onlinelibrary.wiley.com/doi/10.1002/cncr.22846/full

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Tinostamustine (EDO-S101)

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