Drug intelligence / Profile preview

cyclophosphamide + prednisone + azathioprine

Development stage
Unknown
Lead developer
Takeda
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination therapy consisting of three immunosuppressive drugs—cyclophosphamide, prednisone, and azathioprine. Each component has a distinct mechanism of action but all contribute to immunosuppression. Cyclophosphamide is an alkylating agent that crosslinks DNA, leading to cell death, particularly in rapidly dividing immune cells. Prednisone is a synthetic glucocorticoid corticosteroid that suppresses inflammation and modulates the immune response by altering gene expression. Azathioprine is a purine analogue antimetabolite that inhibits DNA synthesis in proliferating cells, especially lymphocytes. This combination has been used for the treatment of severe autoimmune diseases (such as lupus nephritis and glomerulonephritis) and as part of immunosuppressive regimens following organ transplantation[1][2][5]. The rationale for combining these agents lies in their complementary mechanisms targeting different aspects or phases of the immune response.

Other names
cyclophosphamide-prednisone-azathioprineCyclophosphamide Regimens in Juvenile SLE Nephritis
02

Targets

DNAGR (Glucocorticoid receptor)IMPDH (Inosine-5'-monophosphate dehydrogenase 1)HPRT1 (Hypoxanthine-guanine phosphoribosyltransferase)

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