Comparative inhibitory effects of bepotastine and diphenhydramine on rituximab-induced infusion reactions

Int J Hematol. 2025 Sep;122(3):413-420. doi: 10.1007/s12185-025-03990-6. Epub 2025 Apr 29.

Abstract

Purpose: Infusion-related reaction (IRR) is a common adverse event induced by rituximab. Although first-generation histamine 1 receptor antagonists (H1RAs) are commonly used to prevent IRR, evidence on IRR suppression by the second-generation H1RA bepotastine is scarce. In this study, we assessed the inhibitory effects of bepotastine on rituximab-induced IRR and compared them with those of the first-generation H1RA diphenhydramine.

Methods: We retrospectively evaluated IRR incidence in patients with B-cell non-Hodgkin lymphoma who received their first dose of rituximab.

Results: The incidence of any grade IRR was 9.8% in the bepotastine group (n = 92), which was significantly lower than the 30.2% rate in the diphenhydramine group (n = 96; p < 0.001). The incidence of grade 2 or higher IRR was similar between the two groups (6.5% vs. 12.5%; p = 0.16). Multivariable logistic regression analysis revealed that the risk of any grade IRR incidence was higher in patients with B symptoms and bulky disease. Premedication with bepotastine was an independent factor in reducing the risk of any grade IRR incidence (odds ratio = 0.19, 95% confidence interval: 0.08-0.47).

Conclusion: Bepotastine may be more effective than diphenhydramine in reducing the incidence of rituximab-induced IRR, particularly low-grade reactions.

Keywords: Bepotastine; Diphenhydramine; Infusion reaction; Rituximab.

Publication types

  • Comparative Study

MeSH terms

  • Adult
  • Aged
  • Diphenhydramine* / administration & dosage
  • Diphenhydramine* / therapeutic use
  • Female
  • Histamine H1 Antagonists* / therapeutic use
  • Humans
  • Incidence
  • Infusions, Intravenous
  • Lymphoma, B-Cell* / drug therapy
  • Male
  • Middle Aged
  • Piperidines* / administration & dosage
  • Piperidines* / therapeutic use
  • Pyridines* / administration & dosage
  • Pyridines* / therapeutic use
  • Retrospective Studies
  • Rituximab* / administration & dosage
  • Rituximab* / adverse effects

Substances

  • Diphenhydramine
  • Rituximab
  • Piperidines
  • Pyridines
  • bepotastine besilate
  • Histamine H1 Antagonists