Drug intelligence / Profile preview

temozolomide + epirubicin

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

Temozolomide + epirubicin is a combination chemotherapy regimen consisting of two small molecule drugs, temozolomide and epirubicin. Temozolomide is an oral alkylating agent of the imidazotetrazine class that induces DNA damage by methylating guanine residues, leading to cell cycle arrest and apoptosis. Epirubicin is an anthracycline topoisomerase II inhibitor that intercalates into DNA, inhibiting nucleic acid synthesis and causing cytotoxicity through free radical formation and DNA strand breaks. This combination has been investigated for the treatment of advanced leiomyosarcoma (LMS), where it demonstrated promising efficacy with a median progression-free survival of 10 months and an overall response rate of 53% in retrospective studies. The most common adverse effects include myelosuppression (leukopenia, neutropenia, thrombocytopenia), anemia, nausea, vomiting, fatigue, and oral mucositis[1][2][5]. Both agents are approved individually for various cancers; their combination represents an off-label or investigational approach in soft tissue sarcomas.

Other names
EPI-TMZ
02

Targets

TOP2A (DNA topoisomerase II)DNA

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