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    DRUG CLASS:

    E-selectin inhibitor

    Related drugs:
    over1year
    Analogues of the pan-selectin antagonist rivipansel (GMI-1070). (PubMed, Eur J Med Chem)
    The aim of this contribution was to improve the pan-selectin affinity of rivipansel (3) by leveraging a new class of sLex mimetics in combination with an optimized linker length to the sulfate bearing group. As a result, the pan-selectin antagonist 11b exhibits an approximatively 5-fold improved affinity for E-, as well as P-selectin.
    Journal
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    SELP (Selectin P)
    2years
    The Heparinoid Sevuparin Improves Anemia and Kidney Status in a Mouse Model of Chronic Kidney Disease (ASH 2023)
    Our data in this mouse CKD model add new insights to the role of hepcidin in the development of CKD anemia over time. Furthermore, the results are promising and support further mechanistic and clinical studies to elucidate the therapeutic role for sevuparin as a treatment in anemia of inflammatory and/or chronic diseases in monotherapy or in combination with EPO and to explore its role in kidney protection.
    Preclinical
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    IL6 (Interleukin 6) • BMP6 (Bone Morphogenetic Protein 6)
    |
    IL6 expression
    |
    Aranesp (darbepoetin alfa)
    almost3years
    An overview of novel therapies in advanced clinical testing for acute myeloid leukemia. (PubMed, Expert Rev Hematol)
    The year 2017 marks a cornerstone in the treatment landscape of AML with the approval of midostaurin in the United States for newly diagnosed fit adults with FLT3 mutated AML. Subsequently, the therapeutic armamentarium of AML considerably expanded with the approval of 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.
    Journal • Metastases
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    FLT3 (Fms-related tyrosine kinase 3)
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    FLT3 mutation
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    Venclexta (venetoclax) • Xospata (gilteritinib) • midostaurin • Vanflyta (quizartinib) • Tibsovo (ivosidenib) • Idhifa (enasidenib) • magrolimab (ONO-7913) • uproleselan (APL-106)
    3years
    Uproleselan (GMI-1271) for GI Toxicity Prophylaxis During Melphalan-Conditioned Autologous Hematopoietic Cell Transplantation (Auto-HCT) for Multiple Myeloma (MM) (clinicaltrials.gov)
    P2, N=51, Completed, Washington University School of Medicine | Active, not recruiting --> Completed
    Trial completion
    |
    CD34 (CD34 molecule)
    |
    melphalan • uproleselan (APL-106)
    3years
    A Phase I Study of Uproleselan Combined with Azacitidine and Venetoclax for the Treatment of Older or Unfit Patients with Treatment Naïve Acute Myeloid Leukemia (ASH 2022)
    Preliminary results from this Phase I study reveals a tolerable safety profile of UPRO with AZA/VEN in pts with untreated AML ineligible for IC. No DLTs were observed, and the most common Grade 3-4 AE and SAE were hematologic. The combination shows promising preliminary efficacy, including a 50% rate of MRD-ve CR/CRi.
    Clinical • P1 data
    |
    TP53 (Tumor protein P53) • FLT3 (Fms-related tyrosine kinase 3) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2) • NPM1 (Nucleophosmin 1) • RUNX1 (RUNX Family Transcription Factor 1) • TET2 (Tet Methylcytosine Dioxygenase 2) • BCOR (BCL6 Corepressor)
    |
    TP53 mutation • FLT3-ITD mutation • IDH2 mutation
    |
    Venclexta (venetoclax) • azacitidine • uproleselan (APL-106)
    3years
    Uproleselan Added to Cladribine Plus Low Dose Cytarabine (LDAC) in Patients with Treated Secondary Acute Myeloid Leukemia (TS-AML) (ASH 2022)
    The combination produced an ORR of 62% in a high-risk, refractory population whose prognosis is very dismal. The relationship of E-selectin ligand expression, response to treatment, and outcomes is being analyzed.
    Clinical
    |
    TP53 (Tumor protein P53) • NRAS (Neuroblastoma RAS viral oncogene homolog) • RUNX1 (RUNX Family Transcription Factor 1) • TET2 (Tet Methylcytosine Dioxygenase 2) • SRSF2 (Serine and arginine rich splicing factor 2) • SETBP1 (SET Binding Protein 1) • SELL (Selectin L)
    |
    TP53 mutation • TET2 mutation • SRSF2 mutation
    |
    cytarabine • cladribine • uproleselan (APL-106)
    3years
    Uproleselan (GMI-1271) for GI Toxicity Prophylaxis During Melphalan-Conditioned Autologous Hematopoietic Cell Transplantation (Auto-HCT) for Multiple Myeloma (MM) (clinicaltrials.gov)
    P2, N=51, Active, not recruiting, Washington University School of Medicine | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    CD34 (CD34 molecule)
    |
    melphalan • uproleselan (APL-106)
    3years
    Uproleselan With Pre-Transplant Conditioning in Hematopoietic Stem Cell Transplantation for AML (clinicaltrials.gov)
    P1/2, N=28, Recruiting, John Horan, MD | Not yet recruiting --> Recruiting
    Enrollment open • Pre-transplantation
    |
    RUNX1 (RUNX Family Transcription Factor 1) • HLA-DRB1 (Major Histocompatibility Complex, Class II, DR Beta 1)
    |
    RUNX1 mutation
    |
    clofarabine • fludarabine IV • busulfan • uproleselan (APL-106)
    3years
    Uproleselan With Pre-Transplant Conditioning in Hematopoietic Stem Cell Transplantation for AML (clinicaltrials.gov)
    P1/2, N=28, Not yet recruiting, John Horan, MD
    New P1/2 trial • Pre-transplantation
    |
    RUNX1 (RUNX Family Transcription Factor 1) • HLA-DRB1 (Major Histocompatibility Complex, Class II, DR Beta 1)
    |
    RUNX1 mutation
    |
    clofarabine • fludarabine IV • busulfan • uproleselan (APL-106)
    3years
    NCI-2021-10020: Highest Dose of Uproleselan in Combination With Fludarabine and Cytarabine for Patients With Acute Myeloid Leukemia, Myelodysplastic Syndrome, or Mixed Phenotype Acute Leukemia Relapsed or Refractory and That Expresses E-selectin Ligand on the Cell Membrane (clinicaltrials.gov)
    P1, N=18, Suspended, National Cancer Institute (NCI) | Recruiting --> Suspended
    Trial suspension • Combination therapy
    |
    SELL (Selectin L)
    |
    cytarabine • leucovorin calcium • fludarabine IV • uproleselan (APL-106) • Starasid (cytarabine ocfosfate)