Drug intelligence / Profile preview

fludarabine + cyclophosphamide + VP-16

Development stage
Preclinical
Lead developer
Bayer
Modality
Small Molecules
Administration
Intravenous
01

Overview

This is a combination chemotherapy regimen consisting of three agents: - **Fludarabine** is a purine analog that inhibits DNA synthesis by interfering with DNA polymerase and ribonucleotide reductase, leading to inhibition of DNA replication and cell death, particularly in lymphocytes. - **Cyclophosphamide** is an alkylating agent that crosslinks DNA strands, preventing cell division and resulting in apoptosis. It is active against both resting and dividing cells. - **VP-16 (etoposide)** is a topoisomerase II inhibitor that causes double-stranded breaks in DNA during the S and G2 phases of the cell cycle, leading to apoptosis. This combination has been used as part of conditioning regimens for hematopoietic stem cell transplantation (HSCT), especially for patients with hematologic malignancies such as chronic lymphocytic leukemia (CLL), non-Hodgkin lymphoma (NHL), acute myeloid leukemia (AML), and myelodysplastic syndromes (MDS). The regimen provides immunosuppression to facilitate engraftment while exerting antitumor effects. Toxicities are primarily hematologic, including neutropenia and increased risk of infection[1][2][3].

Other names
fludarabine + cyclophosphamide + etoposide
02

Targets

DNA polymerase familyTOP2A (DNA topoisomerase II)DNARNR (Ribonucleotide reductase)

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