Drug intelligence / Profile preview

carmustine + etoposide + thiotepa

Development stage
Unknown
Modality
Small Molecules
Administration
Intravenous
01

Overview

This is a combination chemotherapy regimen consisting of carmustine (also known as BCNU), etoposide (also known as VP-16), and thiotepa. All three are alkylating or DNA-damaging agents used primarily in high-dose conditioning regimens prior to autologous stem cell transplantation, especially for central nervous system (CNS) malignancies such as primary CNS lymphoma and recurrent malignant brain tumors. - Carmustine is a nitrosourea alkylating agent that cross-links DNA and RNA, inhibiting replication and transcription. - Etoposide is a topoisomerase II inhibitor that induces double-strand DNA breaks, leading to apoptosis in rapidly dividing cells. - Thiotepa is an alkylating agent that cross-links DNA strands, preventing cell division and leading to cell death. The combination exploits synergistic cytotoxicity against tumor cells while providing broad coverage against various cancer cell populations within the CNS. This regimen has been used in myeloablative therapy followed by autologous bone marrow or stem cell rescue[1][2][4]. The main indications are high-risk or relapsed/refractory CNS tumors including aggressive lymphomas and pediatric brain tumors[1][2][4].

Other names
BCNU + VP-16 + thiotepa
02

Targets

DNATOP2A (DNA topoisomerase II)

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