Thiopurines such as thioguanine are used to treat acute leukemias and remissions in acute granulocytic leukemias.
Azathioprine is the main immunosuppressive cytotoxic substance. A prodrug, it is widely used in transplantation to control rejection reactions. It is nonenzymatically cleaved to mercaptopurine, a purine analogue that inhibits DNA synthesis. By preventing the clonal expansion of lymphocytes in the induction phase of the immune response, it affects both cell immunity and humoral immunity. It also successfully suppresses autoimmunity.