[Pharmacological characteristics and clinical outcomes of Epcoritamab (recombinant) (Epkinly® subcutaneous injection ) for malignant lymphoma]

Nihon Yakurigaku Zasshi. 2024;159(1):61-68. doi: 10.1254/fpj.23076.
[Article in Japanese]

Abstract

The prognosis of patients with B-cell non-Hodgkin lymphoma (B-NHL) has improved with the use of anti-CD20 based immunochemotherapy. However, management of relapsed or refractory disease remains a challenge, indicating a high unmet need for novel treatments. Epcoritamab (recombinant) is a humanized immunoglobulin G1 (IgG1) bispecific antibody that simultaneously binds to CD3 on T cells and CD20 on B cells or tumor cells inducing T-cell mediated cytotoxicity against CD20-positive B cells. It demonstrated consistent cytotoxic effects in B-cell lymphoma cell line-derived xenograft models, patient-derived xenograft models, and cynomolgus monkey studies. Pharmacological studies in cynomolgus monkeys showed peak plasma concentrations of cytokines were lower with subcutaneous versus intravenous administration. To reduce the risk of cytokine release syndrome (CRS) and improve convenience, Epcoritamab has been developed as a subcutaneous formulation.To further reduce the risk of CRS, clinical trials utilized a priming dose and incremental dose increases. In Phase I/II overseas trials with relapsed, progressive, or refractory B-NHL patients, the recommended Phase II trial dose was determined based on safety, efficacy, and pharmacokinetic model simulation results. The Phase II dose-expansion part demonstrated the efficacy and high tolerability of epcoritamab monotherapy at the recommended dose. Similar efficacy and tolerability were observed in Japanese Phase I/II trials in relapsed or refractory B-NHL patients. Based on these results, epcoritamab received the approval in September 2023 for the treatment of "relapsed or refractory large B-cell lymphoma (DLBCL, HGBCL, PMBCL)" and "relapsed or refractory follicular lymphoma (Grade 3B)" in Japan.

Publication types

  • Clinical Trial, Phase I
  • English Abstract

MeSH terms

  • Animals
  • Antineoplastic Agents* / adverse effects
  • Humans
  • Injections, Subcutaneous
  • Lymphoma* / drug therapy
  • Lymphoma, B-Cell* / drug therapy
  • Lymphoma, B-Cell* / pathology
  • Macaca fascicularis

Substances

  • Antineoplastic Agents