Decitabine and cedazuridine (Inqovi)

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Mechanism of action

From the NCI Drug Dictionary: An orally available combination agent containing the cytidine deaminase (CDA) inhibitor E7727 and the cytidine antimetabolite decitabine, with potential antineoplastic activity. Upon oral administration of decitabine and cedazuridine, the CDA inhibitor E7727 binds to and inhibits CDA, an enzyme primarily found in the gastrointestinal (GI) tract and liver that catalyzes the deamination of cytidine and cytidine analogs. This prevents the breakdown of decitabine, increasing its bioavailability and efficacy while decreasing GI toxicity due to the administration of lower doses of decitabine. Decitabine exerts its antineoplastic activity through the incorporation of its triphosphate form into DNA, which inhibits DNA methyltransferase and results in hypomethylation of DNA. This interferes with DNA replication and decreases tumor cell growth.

Diseases for which it is used

History of changes in FDA indication

  • 7/7/2020: Initial approval for adult patients with myelodysplastic syndromes (MDS) including the following:
    • Previously treated and untreated, de novo and secondary MDS with the following French-American-British subtypes (refractory anemia, refractory anemia with ringed sideroblasts, refractory anemia with excess blasts, and chronic myelomonocytic leukemia [CMML]) and
    • Intermediate-1, intermediate-2, and high-risk International Prognostic Scoring System groups.

Also known as

  • Code name: ASTX727
  • Brand name: Inqovi