Entries by Renee Hansen

Savona et al., An oral fixed-dose combination of decitabine and cedazuridine in myelodysplastic syndromes: a multicentre, open-label, dose-escalation, phase 1 study

View further details Savona et al, “Savona et al., An oral fixed-dose combination of decitabine and cedazuridine in myelodysplastic syndromes: a multicentre, open-label, dose-escalation, phase 1 study”, The Lancet Haematology, Volume 6, Issue 4, e194 – e203  DOI:10.1016/S2352-3026(19)30030-4 Abstract BACKGROUND: Decitabine, a DNA methyltransferase 1 inhibitor or DNA hypomethylating compound, is not readily orally bioavailable […]

de Witte, Effective oral hypomethylating drugs in intermediate-risk or high-risk myelodysplasia: a breakthrough?

Click for link to article: “Effective oral hypomethylating drugs in intermediate-risk or high-risk myelodysplasia: a breakthrough?” The Lancet Haematology, Volume 6, Issue 4, PE170-E171, DOI 10.1016/S2352-3026(19)30025-0•   Curative treatment options for patients with intermediate-risk or high-risk myelodysplasia are intensive chemotherapy and allogeneic stem cell transplantation, but most patients with myelodysplasia are too frail to be […]

2019 ICTXV: Nonclinical Development of Cedazuridine, a Novel Cytidine Deaminase Inhibitor for use in Combination with Decitabine to Enable Oral Administration to Patients with Myelodysplastic Syndromes (MDS)

Click here to view presentation: Nonclinical Development of Cedazuridine, a Novel Cytidine Deaminase Inhibitor for use in Combination with Decitabine to Enable Oral Administration to Patients with Myelodysplastic Syndromes (MDS) Abstract: Cedazuridine (E7727) is a synthetic nucleoside analog derived from tetrahydrouridine (THU) and designed as a potent inhibitor of cytidine deaminase (CDA) with improved stability […]

2019 EHA: RESULTS OF ASTRAL-1 STUDY, A PHASE 3 RANDOMIZED TRIAL OF GUADECITABINE (G) VS TREATMENT CHOICE (TC) IN TREATMENT NAÏVE ACUTE MYELOID LEUKEMIA (TN-AML) NOT ELIGIBLE FOR INTENSIVE CHEMOTHERAPY (IC)

Click to view presentation: RESULTS OF ASTRAL-1 STUDY, A PHASE 3 RANDOMIZED TRIAL OF GUADECITABINE (G) VS TREATMENT CHOICE (TC) IN TREATMENT NAÏVE ACUTE MYELOID LEUKEMIA (TN-AML) NOT ELIGIBLE FOR INTENSIVE CHEMOTHERAPY (IC)   Background: Guadecitabine is a next generation hypomethylating agent (HMA) given subcutaneously (SC) which provides prolonged in vivo exposure to its active […]

2019 EHA: ASTX660, a non-peptidomimetic antagonist of cIAP1/2 and XIAP, induces apoptosis in T cell lymphoma by enhancing immune mediated and death receptor dependent killing

Click here to view presentation: ASTX660, a non-peptidomimetic antagonist of cIAP1/2 and XIAP, induces apoptosis in T cell lymphoma by enhancing immune mediated and death receptor dependent killing   Abstract: Background: ASTX660 is a potent, non-peptidomimetic antagonist of the cellular and X-linked inhibitors of apoptosis proteins (cIAP1/2 and XIAP), which is currently being tested in […]

2019 EHA: Preliminary Results of ASTX660, a Novel Non-Peptidomimetic cIAP1/2 and XIAP Antagonist, in Relapsed/Refractory Peripheral T-Cell Lymphoma and Cutaneous T-Cell Lymphoma

Background: ASTX660 is an oral, novel nonpeptidomimetic, small-molecule antagonist of cellular/X-linked inhibitors of apoptosis proteins (cIAP1/2 and XIAP). ASTX660 is currently being evaluated in a first-in-human phase 1‒2 study in patients (pts) with advanced solid tumors and lymphoma (ClinicalTrials.gov NCT02503423). In the phase 1 part of the study, the recommended phase 2 dose (RP2D) was […]

2019 EHA: Characterization of a novel, potent small molecule MDM2 antagonist which activates wild-type p53 and induces apoptosis in AML

Background: In the presence of various stress signals, p53 acts as a tumor suppressor by regulating the expression of a multitude of genes to elicit cellular responses such as cell cycle arrest and apoptosis. The activity of p53 is tightly regulated by MDM2, an E3 ubiquitin ligase that acts as a primary inhibitor of p53 […]

2019 MDSF: Long Term Survival Results and Prognostic Factors Results of Higher Risk MDS and CMML treated with guadecitabine

Click here to view Publication: Long Term Survival Results and Prognostic Factors Results of Higher Risk MDS and CMML treated with guadecitabine   Abstract: Background: Guadecitabine SC (SGI-110) is a dinucleotide next generation hypomethylating agent (HMA) resistant to degradation by cytidine deaminase resulting in extended in vivo exposure to its active metabolite decitabine.  Methods: Int, […]

2018 EBF: Development and validation of an LC-MS/MS method for the simultaneous quantitation of cedazuridine (E7727), epimer of cedazuridine and decitabine in THU-stabilized K2EDTA human Plasma

Summary Abstract: Cedazuridine is a novel cytidine deaminase inhibitor that inhibits the in vivo metabolic degradation of decitabine when administered orally in combination with decitabine (known as ASTX727) in clinical trials. Cedazuridine inhibits degradation of decitabine by inhibiting cytidine deaminase in the gut and liver thereby increasing oral bioavailability of decitabine. To support clinical trial […]

2019 MDSF: Development of an oral hypomethylating agent (HMA) as a fixed dose combination (FDC) of decitabine and CDA inhibitor cedazuridine

Summary: Background: Hypomethylating agents azacitidine and decitabine are not readily bioavailable orally due to their degradation in the gut and liver by CDA. We developed a selective, potent, and safe CDA inhibitor cedazuridine. The combination of cedazuridine with decitabine delivered orally as an FDC tablet is developed to achieve an equivalent AUC exposure to IV […]