Emerging drugs for the treatment of paroxysmal nocturnal hemoglobinuria

Expert Opin Emerg Drugs. 2022 Mar;27(1):33-43. doi: 10.1080/14728214.2022.2031973. Epub 2022 Jan 31.

Abstract

Introduction: Eculizumab, the first anti-C5 monoclonal antibody approved for patients with paroxysmal nocturnal hemoglobinuria (PNH), has revolutionized the natural history of this disease, blocking intravascular hemolysis, reducing the risk of thromboembolic events, resulting in a significant improvement in survival and quality of life. However, the hematological response to eculizumab is extremely heterogeneous, with only one-third of PNH patients reaching normal hemoglobin levels.

Areas covered: This article reviews the current new drugs being investigated in phase II and III trials for adult PNH patients. Literature search was performed using Medline and Clinicaltrials.org databases.

Expert opinion: The new molecules have been classified according to the target of the complement system on which they act; we have novel terminal complement inhibitors, which target C5, and proximal complement inhibitors, which interfere with C3 or even further upstream (factor B and D). Ravulizumab is the first next-generation C5 inhibitor, approved by FDA and EMA, which reproduced the excellent results achieved with eculizumab, trying to improve the convenience of patients. However, unresolved issues remain, such as C3-mediated extravascular hemolysis, on which novel proximal complement inhibitors are showing their efficacy. Pegcetacoplan is the first C3-inihibitor approved by FDA. Long-term safety data for novel complement inhibitors are needed.

Keywords: Paroxysmal nocturnal hemoglobinuria; intravascular and extravascular hemolysis; novels complement inhibitors.

Publication types

  • Review

MeSH terms

  • Adult
  • Complement Inactivating Agents / adverse effects
  • Hemoglobinuria, Paroxysmal* / drug therapy
  • Hemolysis
  • Humans
  • Peptides, Cyclic / therapeutic use
  • Quality of Life

Substances

  • Complement Inactivating Agents
  • Peptides, Cyclic
  • pegcetacoplan