Drug intelligence / Profile preview

tacrolimus + tocilizumab

Development stage
Preclinical
Lead developer
Genentech
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous, Subcutaneous
01

Overview

Tacrolimus + tocilizumab is a combination of two immunosuppressive agents used off-label in rare, refractory cases of autoimmune diseases such as rheumatoid arthritis (RA) and systemic lupus erythematosus (SLE). Tacrolimus is a calcineurin inhibitor that suppresses T-cell activation by inhibiting the phosphatase activity of calcineurin, thereby blocking IL-2 transcription and other cytokines involved in T-cell activation. Tocilizumab is a recombinant humanized monoclonal antibody that acts as an interleukin-6 (IL-6) receptor antagonist, blocking the pro-inflammatory effects mediated by IL-6. This combination has been reported in case studies to induce remission in patients with difficult-to-treat RA complicated by SLE who did not respond adequately to standard therapies[1][2][5]. Both drugs are potent immunosuppressants with distinct but complementary mechanisms targeting different pathways of immune activation.

02

Targets

IL-6R (Interleukin-6 receptor subunit alpha)CN (Calcineurin)

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