Astex Pharmaceuticals Announces IND Candidate: ASTX727 a Potential Best-in-Class Oral Hypomethylator

On July 8, 2013 Astex Pharmaceuticals reported its plan to submit an Investigational New Drug or IND application to the Food and Drug Administration (FDA) for ASTX727, a novel oral hypomethylating agent (HMA) in the fourth quarter of this year (Press release Astex Pharmaceuticals, JUL 8, 2013, View Source [SID:1234500358]).
ASTX727 is intended as a fixed dose oral combination product consisting of decitabine and E7727, a novel cytidine deaminase inhibitor (CDAi) licensed from Eisai Inc. ASTX727 allows for an efficient oral delivery of decitabine at low doses. Relevant animal studies revealed that the product can result in therapeutic exposures of decitabine at low doses. The profile of E7727 is expected to result in low inter-patient variability across doses of decitabine with little or no gastrointestinal safety issues. Later this year, preclinical data on ASTX727 will be submitted for presentation at a scientific meeting.
Cytidine deaminase (CDA) is an enzyme that is responsible for the degradation of nucleosides, including decitabine and azacitidine. High levels of CDA in the gastrointestinal tract and liver rapidly degrade these nucleosides and prohibit or limit their oral bioavailability. E7727 is a proprietary and patented New Molecular Entity (NME) with a very wide therapeutic margin that inhibits CDA activity. Decitabine can be delivered orally and efficiently absorbed in the gut when it is combined with E7727 due to the inhibition of CDA by E7727. ASTX727 is being developed as a fixed dose oral product that combines E7727 and decitabine. This oral HMA with the potential to be best-in-class will enter clinical development in 2014. Astex has a worldwide license to E7727 from Eisai Inc.

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