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Methotrexate (tapering dose)

Hoffmann-La Roche · FDA-approved active Small molecule

Methotrexate inhibits dihydrofolate reductase, blocking the synthesis of purines and pyrimidines required for DNA replication and cell division.

Methotrexate inhibits dihydrofolate reductase, blocking folate metabolism and reducing DNA synthesis and cell proliferation. Used for Acute lymphoblastic leukemia (ALL), Osteosarcoma, Breast cancer.

At a glance

Generic nameMethotrexate (tapering dose)
SponsorHoffmann-La Roche
Drug classAntimetabolite / Folate antagonist
TargetDihydrofolate reductase (DHFR)
ModalitySmall molecule
Therapeutic areaOncology, Immunology, Rheumatology
PhaseFDA-approved

Mechanism of action

By inhibiting dihydrofolate reductase, methotrexate prevents the conversion of dihydrofolate to tetrahydrofolate, disrupting one-carbon transfer reactions essential for nucleotide synthesis. This leads to suppression of rapidly dividing cells, including cancer cells and activated immune cells. At lower doses used in autoimmune conditions, it also exerts immunosuppressive effects through adenosine release and reduced T-cell proliferation.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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