Drug intelligence / Profile preview

abatacept + azathioprine + cyclophosphamide + prednisone

Development stage
Unknown
Lead developer
Bristol Myers Squibb
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, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Intravenous, Subcutaneous, Oral
01

Overview

This is a combination regimen consisting of four immunosuppressive and anti-inflammatory agents—abatacept, azathioprine, cyclophosphamide, and prednisone—used in the management of severe autoimmune diseases such as lupus nephritis. - **Abatacept** is a biologic fusion protein that inhibits T-cell activation by binding to CD80/CD86 on antigen-presenting cells, thereby blocking the co-stimulatory signal required for full T-cell activation. - **Azathioprine** is an antimetabolite immunosuppressant that interferes with purine synthesis, inhibiting DNA replication in proliferating immune cells. - **Cyclophosphamide** is an alkylating agent that suppresses immune function by cross-linking DNA strands and inducing apoptosis in rapidly dividing lymphocytes. - **Prednisone** is a synthetic glucocorticoid corticosteroid with potent anti-inflammatory and immunosuppressive effects through modulation of gene expression and suppression of multiple inflammatory pathways. This specific combination has been studied primarily for induction therapy in active lupus nephritis (notably in the ACCESS trial), where abatacept was added to standard-of-care low-dose cyclophosphamide followed by azathioprine maintenance plus background prednisone[1][2][6]. The addition of abatacept did not significantly improve clinical outcomes compared to standard therapy alone but was generally well tolerated[1][2][6].

02

Targets

CD80 (T-lymphocyte activation antigen CD80)CD86 (T-lymphocyte activation antigen CD86)GR (Glucocorticoid receptor)DNARAC1 (Rac family small GTPase 1)

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