Drug intelligence / Profile preview

etoposide + lomustine

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Etoposide + lomustine is a combination chemotherapy regimen consisting of two small molecule antineoplastic agents. Etoposide is a semisynthetic derivative of podophyllotoxin that acts primarily as a DNA topoisomerase II inhibitor, leading to DNA strand breaks and inhibition of cell division, particularly affecting the S and G2 phases of the cell cycle[4]. Lomustine (also known as CCNU) is an alkylating agent from the nitrosourea class that exerts its cytotoxic effect by causing cross-linking of DNA strands, thereby inhibiting DNA replication and transcription[5]. This combination has been used in various regimens for treating relapsed or refractory cancers such as small cell lung cancer (SCLC), aggressive lymphomas, brain tumors including glioblastoma multiforme, and other malignancies[1][3][5]. The regimen may be administered orally and is sometimes chosen for patients who are not candidates for intensive intravenous chemotherapy due to frailty or comorbidities. Both drugs have significant hematologic toxicity risks.

Other names
etoposide and lomustineCCNU + VP-16
02

Targets

TOP2B (DNA topoisomerase II beta)DNATOP2A (DNA topoisomerase II)

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