uproleselan sodium (APL-106) / GlycoMimetics 
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 8 Diseases   6 Trials   6 Trials   272 News 


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  • ||||||||||  GMI-1687 / GlycoMimetics, uproleselan sodium (APL-106) / GlycoMimetics, rivipansel (GMI-1070) / GlycoMimetics
    Glycomimetic drugs targeting E-selectin for inflammatory disease and as a major cause of progression and chemoresistance in cancer (Hybrid; Room 343 (Ernest N. Morial Convention Center)) -  Mar 12, 2024 - Abstract #ACSSp2024ACS_Sp_2443;    
    Rivipansel inhibits selectins by mimicking sialyl Lex and the tri-sulfated domain of PSGL-1...GMI-1687 binds E-selectin with a K D of 2.3 nM, is bioavailable through a subcutaneous route, and has recently entered Phase 1 clinical studies...As of August 2023, the reported median survival in this placebo-control blinded study with Uproleselan is over 30 months. Here, data are presented to demonstrate that E-selectin plays a major role in chemoresistance among many cancers and is susceptible to treatment with a potent glycomimetic drug.
  • ||||||||||  Venclexta (venetoclax) / Roche, AbbVie, Walter and Eliza Hall Institute, uproleselan sodium (APL-106) / GlycoMimetics
    APAL2020SC Pediatric Acute Leukemia (PedAL) Screening Trial  (Halls G-H (San Diego Convention Center)) -  Nov 3, 2023 - Abstract #ASH2023ASH_1902;    
    P2
    This protocol will promote clinical trial development by engaging industry partners and providing a single entry point to therapeutic studies with biological rationale. APAL2020SC and the EuPAL Foundation registry will generate a large, comprehensive and longitudinal dataset that will inform future trials.
  • ||||||||||  Journal, Metastases:  An overview of novel therapies in advanced clinical testing for acute myeloid leukemia. (Pubmed Central) -  Mar 9, 2023   
    Since 2017, the therapeutic armamentarium of AML has considerably expanded with the approval of midostaurin, enasidenib, ivosidenib, gilteritinib, and venetoclax in combination with hypomethylating agents and others...As a result, AML therapy is constantly evolving and so are the escape mechanisms leading to disease relapse. Therefore, it is of paramount importance to sequentially evaluate the patient during the course of AML treatment and intervene at the right time.
  • ||||||||||  uproleselan sodium (APL-106) / GlycoMimetics
    Journal:  Effects of human TFPI and CD47 expression and selectin and integrin inhibition during GalTKO.hCD46 pig lung perfusion with human blood. (Pubmed Central) -  Apr 12, 2022   
    Additionally, targeting canonical selectin and integrin adhesion pathways reduced PVR elevation associated with hTFPI.hCD47 expression, but did not significantly attenuate neutrophil or platelet sequestration. We conclude that other adhesive mechanisms mediate the residual sequestration of human formed blood elements to pig endothelium that occurs even in the context of the multiple genetic modifications and drug treatments tested here.
  • ||||||||||  uproleselan sodium (APL-106) / GlycoMimetics
    Clinical, P1/2 data, Journal:  Phase 1/2 study of uproleselan added to chemotherapy in patients with relapsed or refractory acute myeloid leukemia. (Pubmed Central) -  Mar 16, 2022   
    P1/2
    A phase 1/2 study evaluated the safety, tolerability, and antileukemic activity of uproleselan (5-20 mg/kg) with MEC (mitoxantrone, etoposide, and cytarabine) among patients with relapsed/refractory (R/R) acute myeloid leukemia (AML)...In a separate cohort, 25 newly diagnosed patients age ≥60 years received uproleselan at the RP2D plus cytarabine and idarubicin (7 + 3)...In the R/R cohort, E‑selectin expression above 10% was associated with a higher response rate and improved survival. The addition of uproleselan to chemotherapy was well tolerated with high remission rates, low-induction mortality, and low rates of mucositis, providing strong rationale for phase 3 randomized confirmatory studies.
  • ||||||||||  uproleselan sodium (APL-106) / GlycoMimetics
    Journal:  E-selectin Inhibitor is Superior to LMWH for Treatment of Experimental Venous Thrombosis. (Pubmed Central) -  Mar 4, 2022   
    Treatment results in improved vein recanalization, a decrease in vein vall inflammation and vein wall intimal thickness and fibrosis, with no changes in markers of coagulation. E-selectin inhibition with GMI-1271 alone is superior to E-selectin inhibition combined with LMWH, LMWH alone and no treatment in this DVT model of iliac vein thrombosis.
  • ||||||||||  GMI-1359 / GlycoMimetics
    Co-Targeting E-Selectin/CXCR4 with GMI-1359 Facilitates AML Stem Cell Mobilization and Protects BM Niches from Anti-Leukemia Therapy (GWCC - Hall B5, Level 1) -  Nov 5, 2021 - Abstract #ASH2021ASH_5026;    
    P1
    We previously demonstrated (Chang et al., ASH 2020) that E-selectin blockade by the pharmacological antagonist, GMI-1271 (uproleselan; GlycoMimetics, Inc) sensitized therapy-resistant LSC to Bcl-2 targeted therapy...Hence, we hypothesized that co-targeting E-selectin/CXCR4 more efficiently mobilizes AML cells from BM niches and synergizes with the anti-leukemia activity of venetoclax/hypomethylating agent (Ven/HMA)...We also observed upregulated pro-survival signaling pathways such as phosphorylation of AKT-MAPK-ERK along with increased Bcl-xL, Bcl-2, and Idu expression in MSC from the GMI-1359 + Ven/HMA treated PDX mice compared to Ven/HMA single treatment cohorts. Collectively, our results provide strong evidence that co-targeting E-selectin/CXCR4 with GMI-1359 profoundly reduces BM retention of LSC as well as protects BM niche component cells from apoptosis induced by targeted therapy, resulting in improving the anti-leukemia activity of Ven/HMA therapy in AML.