Drug intelligence / Profile preview

dexamethasone + cisplatin + cytarabine + cyclophosphamide + etoposide

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

Overview

This is a combination chemotherapy regimen consisting of five agents: dexamethasone (a synthetic corticosteroid), cisplatin (a platinum-based DNA crosslinking agent), cytarabine (a nucleoside metabolic inhibitor), cyclophosphamide (an alkylating agent), and etoposide (a topoisomerase II inhibitor). This combination may be used in salvage or high-dose chemotherapy regimens for patients with aggressive hematologic malignancies, such as non-Hodgkin lymphoma, particularly as part of preparatory regimens before stem cell transplantation. The combination leverages distinct, non-overlapping mechanisms of action to maximize cytotoxicity against rapidly dividing cancer cells. Mechanistically, dexamethasone reduces inflammation and immune responses, cisplatin crosslinks and damages DNA, cytarabine inhibits DNA synthesis, cyclophosphamide induces DNA alkylation and breakage, and etoposide inhibits topoisomerase II to cause DNA strand breaks. Each drug contributes to the overall antineoplastic effect through disruption of different stages of the cell cycle or DNA integrity.[4][9][3][7]

02

Targets

GR (Glucocorticoid receptor)TOP2A (DNA topoisomerase II)DNA polymerase familyDNA

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