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Typical immunosuppressive drug
| Product name | Common name | Molecular formula | Feature |
|---|---|---|---|
| Imuran (Azanin) |
Azathioprine (AZT) |
 C6H7N7O2S |
Purine base antagonist ・AZT is converted to active 6-MP and inhibits purine (adenine and guanine) synthesis process (inhibitis DNA synthesis). AZT works on T, B cells and macrophages. AZT supress cell-mediated immune response through the inhibition of T cells, NK activity, antibody production. |
| Endoxan |
Cyclophosphamide (CPA) |
 C7H15Cl2N2O2P・H2O |
Alkylating agent ・CPA alkylates guanine in DNA and crosslinks to impair DNA replication. CPA decrease number of T and B cells, and then B cell antibody production. |
| Methotrexate Rheumatrex |
Methotrexate (MTX) |
 C20H22N8O5 |
Folic acid derivative (antagonist) ・MTX, by binding to dihydrofolate reductase, inhibits synthesis from dihydrofolic acid to tetrahydrofolic acid. This action inhibits the synthesis of inosinic acid, a purine precursor. (inhibits DNA and RNA synthesis). MTX suppresses the proliferation and activity of lymphocytes and macrophages. As a result, that suppresses the amount of cytokine's production is decreased. |
| Bredinin |
Mizoribine (MZR) |
 C9H13N3O6 |
Purine antagonist (antimetabolite) ・MZR inhibits the metabolic pathway from inosinic acid to guanylic acid in the purine synthesis system (nucleic acid synthesis is suppressed). MZR suppresses the proliferation of lymphocytes, strongly on T cells and macrophages. |
| Cellcept | Mycophenolate mofetil (MMF) |
 C23H31NO7 |
MMF inhibits the lymphocyte DNA synthesis (de novo's purine biosynthesis pathway) As a result, MMF suppresses lymphocyte activation and proliferation. |
| Sandimmun (Neoral) |
Ciclosporin (CPA) |
 C62H111N11O12 |
Inhibition of T cell calcineurin activity. ・CPA inhibits the enzymatic activity of calcineurin by binding to immunophilins (cyclophilins) (inhibits the translocation of NF-AT into the mucleus). As a result, cytokine gene expression is inhibited, and suppresses the activation of lymphocytes. (especially on T cells) |
| Prograf | Ttacrolimus (FK506) |
 C44H69NO12 |
Inhibition of T cell calcineurin activity. ・FK506 inhibits the enzymatic activity of calcineurin by binding to immunophilins (FKBP) (inhibits the translocation of NF-AT into the mucleus). As a result, cytokine gene expression is inhibited, and suppresses the activation of lymphocytes. (especially on T cells) |
The upper listed medicines are commonly used in Japanese clinical practice.