Table. Immunosuppressive potential of small molecule targeted therapies
| Immunosuppressant category | Drug(s) | Licensed indication(s) | Overall immunosuppressive potential | Mechanism of action | Half-life (mean) | Duration of immunosuppression | |
|---|---|---|---|---|---|---|---|
| Janus kinase (JAK) inhibitors | Baricitinib | Rheumatoid arthritis (RA), atopic dermatitis | Moderate | Inhibits JAK enzymes, which are intracellular enzymes involved in stimulating haematopoiesis and immune cell function | About 12–16 hours | Exact duration of potential immunosuppression is not well defined | |
| Tofacitinib | Ankylosing spondylitis, juvenile idiopathic arthritis (JIA), RA, psoriatic arthritis, ulcerative colitis | Moderate | Inhibits JAK enzymes, which are intracellular enzymes involved in stimulating haematopoiesis and immune cell function | About 3 hours (immediate release solution and tablet) About 6–8 hours (extended release) | Exact duration of potential immunosuppression is not well defined | ||
| Ruxolitinib | Graft-versus-host disease (GVHD), myelofibrosis, polycythaemia vera | Moderate | In myelofibrosis and polycythaemia vera, JAK enzyme activity is dysregulated. Ruxolitinib modulates the affected JAK1/2 activity. In GVHD, JAK-STAT signalling is involved with the regulation of the development, proliferation and activation of immune cell types important to GVHD pathogenesis | About 3 hours | Exact duration of potential immunosuppression is not well defined | ||
| BCR-ABL tyrosine kinase inhibitors | Imatinib Dasatinib Ponatinib | Acute lymphoblastic leukemia, chronic myeloid leukemia, aggressive systemic mastocytosis | Moderate | Inhibits BCR-ABL tyrosine kinase and induces apoptosis in BCR-ABL positive cell lines in Philadelphia chromosome–positive leukemias | 15–40 hours | Exact duration of potential immunosuppression is not well defined | |
| Bruton tyrosine kinase (BTK) inhibitors | Ibrutinib Acalabrutinib | GVHD, lymphocytic leukemia, lymphoma | Moderate | Irreversibly inhibit BTK, an integral component of the B-cell receptor and cytokine receptor pathways, reducing B-cell proliferation and survival | 1–6.5 hours | Exact duration of potential immunosuppression is not well defined | |
| Antineoplastic kinase (ALK) inhibitors | Alectinib Ceritinib | ALK-positive non-small cell lung cancer | Moderate | Inhibit proliferation of ALK-dependent cancer cells | About 41 hours | Exact duration of potential immunosuppression is not well defined | |
| Sphingosine-1-phosphate receptor modulators | Fingolimod | Multiple sclerosis | Mild | Reduces lymphocytes in the central nervous system | 6–9 days | Not generally immunosuppressive | |
| Note: This is not an exhaustive list. Licensed indications were referenced from database of the Australian Therapeutic Goods Administration (TGA). Furthermore, the underlying disease for which the medication is prescribed, and concomitant immunosuppressant use, may alter this categorisation. For further information regarding the immunosuppressive potential of underlying conditions, please also consider Table. Immunosuppressive potential of certain medical conditions. | |||||||
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