Challenges and future perspectives for the use of temozolomide in the treatment of SCLC

Cancer Treat Rev. 2024 Sep:129:102798. doi: 10.1016/j.ctrv.2024.102798. Epub 2024 Jul 3.

Abstract

Small-cell lung cancer (SCLC), accounting for 10-20 % of all lung tumors, represents the most aggressive high-grade neuroendocrine carcinoma. Most patients are diagnosed with extensive-stage SCLC (ES-SCLC), with brian metastases identified in ∼ 80 % of cases during the disease cours, and the prognosis is dismal, with a 5-year survival rate of less than 5 %. Current available treatments in the second-line setting are limited, and topotecan has long been the only FDA-approved drug in relapsed or refractory ES-SCLC, until the recent approval of lurbinectedin, a selective inhibitor of RNA polymerase II. Temozolomide (TMZ) is an oral alkylating agent, which showed single-agent activity in SCLC, particularly among patients with O6-methylguanine-DNA methyltransferase (MGMT) promoter methylation. Several studies have revealed the synergistic activity of temozolomide with poly-ADP-ribose polymerase (PARP) inhibitors, that prevent repair of TMZ-induced DNA damage. This review focuses on the rationale for the use of TMZ in ES-SCLC and provides an overview of the main trials that have evaluated and are currently investigating its role, both as a single-agent and in combinations, in relapse or refractory disease.

Keywords: Chemotherapy combinations; MGMT; PARP inhibitors; SCLC; Temozolomide.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents, Alkylating* / therapeutic use
  • Humans
  • Lung Neoplasms* / drug therapy
  • Poly(ADP-ribose) Polymerase Inhibitors / therapeutic use
  • Small Cell Lung Carcinoma* / drug therapy
  • Small Cell Lung Carcinoma* / pathology
  • Temozolomide* / therapeutic use

Substances

  • Temozolomide
  • Antineoplastic Agents, Alkylating
  • Poly(ADP-ribose) Polymerase Inhibitors