Safety and efficacy of the CD95-ligand inhibitor asunercept in transfusion-dependent patients with low and intermediate risk MDS

Leuk Res. 2018 May:68:62-69. doi: 10.1016/j.leukres.2018.03.007. Epub 2018 Mar 10.

Abstract

In low risk MDS, increased apoptosis of erythroid progenitors mediated via CD95 (Fas) activation has been described to result in peripheral cytopenia. Blockade of the CD95 system can improve erythropoiesis in MDS. Asunercept (APG101) is a fusion protein consisting of the extracellular domain of human CD95 and the Fc domain of human IgG1 blocking the interaction between CD95 and its ligand. Here we report on results from a phase I study in 20 transfusion-dependent low and intermediate risk MDS patients treated with intravenous asunercept (EudraCT 2012-003027-37). Primary objectives were safety and tolerability as well as pharmacodynamic effects. Secondary objectives were hematologic improvement, incidence and time to leukemic progression as well as overall survival. Frequency and severity of adverse events were in range of what could be expected in a patient cohort comprising of elderly MDS patients. Two patients experienced a serious adverse event with a suspected relationship to asunercept. The incidence of disease progression was low. In the 20 patients a decrease of the transfusion need from a mean of 10,8 (±5,1) pRBCs during the 12 weeks treatment phase to a mean of 10,0 (±4,2) pRBCs at the end of the study was observed. In conclusion, asunercept was well tolerated and showed efficacy in transfusion-dependent low and intermediate risk MDS patients. Further clinical investigation is warranted, particularly in combination with erythropoiesis stimulating agents (ESAs).

Keywords: Apoptosis; CD 95; Clinical trial; Erythropoiesis; Fas ligand; Myelodysplastic syndromes.

Publication types

  • Clinical Trial, Phase I

MeSH terms

  • Aged
  • Aged, 80 and over
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / adverse effects*
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Blood Transfusion*
  • Disease Progression
  • Dose-Response Relationship, Drug
  • Fas Ligand Protein / antagonists & inhibitors
  • Female
  • Humans
  • Immunoglobulin G / administration & dosage
  • Immunoglobulin G / adverse effects*
  • Immunoglobulin G / pharmacology
  • Immunoglobulin G / therapeutic use*
  • Male
  • Middle Aged
  • Myelodysplastic Syndromes / drug therapy*
  • Myelodysplastic Syndromes / pathology
  • Prospective Studies
  • Recombinant Fusion Proteins / administration & dosage
  • Recombinant Fusion Proteins / adverse effects*
  • Recombinant Fusion Proteins / pharmacology
  • Recombinant Fusion Proteins / therapeutic use*
  • Risk
  • fas Receptor / administration & dosage
  • fas Receptor / therapeutic use*

Substances

  • Antineoplastic Agents
  • Fas Ligand Protein
  • Immunoglobulin G
  • Recombinant Fusion Proteins
  • fas Receptor
  • APG101