Drug intelligence / Profile preview

abatacept + tacrolimus

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Intravenous, Subcutaneous, Oral, Topical
01

Overview

Abatacept + tacrolimus is a combination of two immunosuppressive agents used primarily in the management of autoimmune diseases such as rheumatoid arthritis and for the prevention of graft-versus-host disease (GVHD) following hematopoietic stem cell transplantation. Abatacept is a selective co-stimulation modulator that inhibits T-cell activation by binding to CD80 and CD86 on antigen-presenting cells, thereby blocking their interaction with CD28 on T cells. This prevents the delivery of the second co-stimulatory signal required for full T-cell activation[6][10]. Tacrolimus is a calcineurin inhibitor that suppresses immune responses by inhibiting T-lymphocyte signal transduction and interleukin-2 transcription through binding to FKBP-12, ultimately preventing dephosphorylation and nuclear translocation of NF-AT, which initiates gene transcription for lymphokines[8]. The combination has been studied in rheumatoid arthritis patients who are refractory or intolerant to other therapies, as well as in transplant settings to reduce acute GVHD incidence. Clinical studies indicate that this combination can be effective without significantly increasing adverse events compared to monotherapy[1][2][3].

Other names
TAC + ABTabatacept and tacrolimus
02

Targets

CD80 (T-lymphocyte activation antigen CD80)FKBP1ACD86 (T-lymphocyte activation antigen CD86)CN (Calcineurin)

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