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Astex Pharmaceuticals, Taiho Oncology, and Otsuka Pharmaceutical announce FDA and Health Canada approval of INQOVI® (decitabine and cedazuridine) tablets.

Astex Pharmaceuticals, Taiho Oncology, and Otsuka Pharmaceutical announce FDA and Health Canada approval of INQOVI® (decitabine and cedazuridine) tablets, oral hypomethylating agent (HMA) therapy for intermediate and high-risk MDS and CMML INQOVI is the first orally administered hypomethylating agent approved by the FDA and Health Canada INQOVI is a fixed-dose combination of the hypomethylating agent […]

2020 EHA: Characterization of ASTX660, an antagonist of cIAP1/2 and XIAP, in mouse models of T cell lymphoma

View Poster: Characterization of ASTX660, an antagonist of cIAP1/2 and XIAP, in mouse models of T cell lymphoma 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 a first in human phase I-II study in patients with advanced […]

2020 EHA: ASTX295, a novel small molecule MDM2 antagonist, demonstrates potent activity in AML in combination with decitabine

View Poster: ASTX295, a novel small molecule MDM2 antagonist, demonstrates potent activity in AML in combination with decitabine Abstract: Background: The tumour suppressor p53 is activated in response to various stress signals to induce transcriptional changes leading to cellular responses such as cell cycle arrest and apoptosis. Activity of p53 is tightly regulated by the […]

2020 EHA: Comparative results of azacitidine and decitabine from a large prospective Phase 3 study in treatment naïve acute myeloid leukemia (TN-AML) not eligible for intensive chemotherapy

View Presentation: Comparative results of azacitidine and decitabine from a large prospective Phase 3 study in treatment naïve acute myeloid leukemia (TN-AML) not eligible for intensive chemotherapy   Abstract: Background: Older patients with TN-AML who are ineligible for intensive chemotherapy have limited therapeutic options and poor outcomes. Hypomethylating agents (HMAs) azacitidine (AZA) and decitabine (DEC) […]

Ramsey, et al., Oral Azacitidine and Cedazuridine Approximate Parenteral Azacitidine Efficacy in Murine Model

View further details: Ramsey, H.E., Oganesian, A., Gorska, A.E. et al. Oral Azacitidine and Cedazuridine Approximate Parenteral Azacitidine Efficacy in Murine Model. Targ Oncol 15, 231–240 (2020). https://doi.org/10.1007/s11523-020-00709-x Abstract: Background: DNA methyltransferase inhibitors (DNMTis) improve survival for patients with myelodysplastic syndromes (MDS) and those with acute myeloid leukemia (AML) unable to receive standard cytotoxic chemotherapy and […]

Garcia-Manero et al., Oral cedazuridine/decitabine: a phase 2, pharmacokinetic/pharmacodynamic, randomized, crossover study in MDS and CMML

View further details: Garcia-Manero et al, “Oral cedazuridine/decitabine: a phase 2, pharmacokinetic/pharmacodynamic, randomized, crossover study in MDS and CMML”. Blood. 2020 Apr 13. pii: blood.2019004143. doi: 10.1182/blood.2019004143. [Epub ahead of print] Abstract: This phase 2 study was designed to compare systemic decitabine exposure, demethylation activity, and safety in the first 2 cycles with cedazuridine 100 […]

Ye, et al. “ASTX660, an antagonist of cIAP1/2 and XIAP, increases antigen processing machinery and can enhance radiation-induced immunogenic cell death in preclinical models of head and neck cancer”

Click link to view article https://www.tandfonline.com/doi/full/10.1080/2162402X.2019.1710398 Abstract: Inhibitor of apoptosis protein (IAP) antagonists have shown activity in preclinical models of head and neck squamous cell carcinoma (HNSCC), and work across several cancer types has demonstrated diverse immune stimulatory effects including enhancement of T cell, NK cell, and dendritic cell function. However, tumor-cell-intrinsic mechanisms for this […]

Mita, et al. “A Phase 1 Study of ASTX660, an Antagonist of Inhibitors of Apoptosis Proteins, in Adults With Advanced Cancers or Lymphoma”

Click link to view article https://clincancerres.aacrjournals.org/content/early/2020/01/03/1078-0432.CCR-19-1430.long   Abstract Purpose: This first-in-human, phase 1 study evaluated ASTX660, an oral, small-molecule antagonist of cellular/X-linked inhibitors of apoptosis proteins in patients with advanced solid tumors or lymphoma. Experimental Design: ASTX660 was administered orally once daily on a 7-day-on/7-day-off schedule in a 28-day cycle. Dose escalation followed a standard […]

Dittmann, et al. “Next-generation hypomethylating agent SGI-110 primes acute myeloid leukemia cells to IAP antagonist by activating extrinsic and intrinsic apoptosis pathways”

Clink link to view article https://www.nature.com/articles/s41418-019-0465-8 Abstract Therapeutic efficacy of first-generation hypomethylating agents (HMAs) is limited in elderly acute myeloid leukemia (AML) patients. Therefore, combination strategies with targeted therapies are urgently needed. Here, we discover that priming with SGI-110 (guadecitabine), a next-generation HMA, sensitizes AML cells to ASTX660, a novel antagonist of cellular inhibitor of […]

2019 ASH: Oral Azacitidine and Cedazuridine Approximate Azacitidine Efficacy in a Murine Model

View presentation Abstract # 1376 – Oral Azacitidine and Cedazuridine Approximate Azacitidine Efficacy in a Murine Model Authors: Haley E. Ramsey1-2, Maria P. Arrate1, Londa Fuller1, Agnieszka E. Gorska1, Kelli Boyd3-4, Melissa A. Fischer1-2, Aram Oganesian5, Mohammad Azab5, and Michael R. Savona1,2,4 1Department of Medicine, 2Cancer Biology Program, 3Department of Pathology, Microbiology and Immunology, 4Vanderbilt-Ingram Cancer Center; Vanderbilt University School of Medicine, […]