Drug intelligence / Profile preview

tacrolimus + anti-thymocyte globulin

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
Small Molecules, Antibody-Based Therapeutics
Administration
Oral, Intravenous
01

Overview

Tacrolimus + anti-thymocyte globulin is a combination immunosuppressive regimen used primarily in the management of acute graft-versus-host disease (GVHD) refractory to steroids and cyclosporine, as well as for GVHD prophylaxis in hematopoietic stem cell transplantation. Tacrolimus is a calcineurin inhibitor that suppresses T-cell activation by inhibiting the phosphatase activity of calcineurin after binding to FKBP-12, thereby blocking IL-2 transcription and other cytokines involved in T-cell activation[5]. Anti-thymocyte globulin (ATG) is a polyclonal antibody preparation targeting multiple T-cell antigens; it induces profound depletion of T lymphocytes through complement-dependent cytotoxicity, antibody-dependent cellular cytotoxicity, apoptosis via Fas-Fas ligand interactions, and modulation of adhesion molecules[6][8][10]. The combination aims to provide synergistic immunosuppression for severe or refractory immune-mediated conditions such as steroid-refractory acute GVHD. This regimen has been shown to induce responses in patients with severe GVHD but carries significant risk for infectious complications due to profound immunosuppression[1][3].

Other names
tacrolimus and ATGtacrolimus plus anti-thymocyte globulintacrolimus + ATGAMtacrolimus + Thymoglobulin
02

Targets

FKBP1ACD2 (T-cell Surface Antigen CD2)CD3 (T-cell surface glycoprotein CD3)CD4 (T lymphocyte surface antigen)CD8A (CD8 alpha/beta Coreceptor)Human leukocyte antigen class I molecule / Human leukocyte antigen class II moleculeIL-2R (Interleukin-2/interleukin-15 receptor complex)PPP3CA (Protein phosphatase 3 catalytic subunit alpha)

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