Mechanism of Action

Azathioprine is a phase-specific drug that is toxic to cells during nucleic acid synthesis. Phase-specific drugs are toxic during a specific phase of the mitotic cycle, usually the S-phase, when DNA synthesis is occurring, as opposed to cycle-specific drugs that kill both cycling and intermitotic cells.

Azathioprine is converted in vivo to thioinosinic acid, which competitively inhibits the synthesis of in-osinic acid, the precursor to adenylic acid and guanylic acid. In this way, azathioprine inhibits DNA synthesis and therefore suppresses lymphocyte proliferation. This effectively inhibits both humoral and cell-mediated immune responses.

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