Drug intelligence / Profile preview

melphalan + etoposide + lomustine + thiotepa

Development stage
Preclinical
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

**melphalan + etoposide + lomustine + thiotepa** is a high-dose chemotherapy combination regimen comprised of four chemotherapeutic agents: melphalan (an alkylating nitrogen mustard), etoposide (a topoisomerase II inhibitor), lomustine (a nitrosourea alkylating agent), and thiotepa (an alkylating agent from the polyfunctional aziridine group). This combination is designed as a conditioning regimen for hematopoietic stem cell transplantation, most commonly in the treatment of lymphomas, and sometimes other refractory or relapsed solid tumors. Each agent interferes with cancer cell growth and division through distinct mechanisms, collectively producing synergistic cytotoxicity. - **Melphalan** cross-links DNA, leading to apoptosis in proliferating cells. - **Etoposide** induces DNA strand breaks by inhibiting topoisomerase II. - **Lomustine** alkylates DNA and RNA, inhibiting replication and transcription. - **Thiotepa** alkylates DNA, preventing cell division and triggering apoptosis. This regimen is used in preparative or conditioning protocols prior to autologous hematopoietic stem cell transplantation, aiming to eradicate residual malignant cells. The combination may not have a unique brand name and is often identified in literature by its constituent agents[1][3][7]. Relevant toxicities are profound myelosuppression, mucositis, hepatic and renal dysfunction, and risk of infection.

Other names
melphalan + etoposide + lomustine + thiotepa
02

Targets

DNA

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