.Pharmacolibrary.Drugs.L_AntineoplasticAndImmunomodulatingAgents.L04A_Immunosuppressants.L04AX03_Methotrexate.Methotrexate

Information

Methotrexate is an antimetabolite and antifolate drug, widely used in the treatment of various cancers (e.g., leukemia, lymphoma, breast cancer) and autoimmune diseases such as rheumatoid arthritis and psoriasis. It inhibits dihydrofolate reductase, blocking DNA synthesis and cell replication. Methotrexate is approved and used in clinical practice today for both oncological and non-oncological indications.

Pharmacokinetics

Pharmacokinetic parameters reported in adults, primarily cancer patients, after intravenous administration. Data based on population PK studies. Parameters represent typical values in adult patients with normal renal function.

References

1. Nader, A, et al., & Wilby, KJ (2017). Population Pharmacokinetics of Intravenous Methotrexate in Patients with Hematological Malignancies: Utilization of Routine Clinical Monitoring Parameters. European journal of drug metabolism and pharmacokinetics 42(2) 221–228. DOI:10.1007/s13318-016-0338-1 PUBMED:https://pubmed.ncbi.nlm.nih.gov/27059845

2. Medellin-Garibay, SE, et al., & Romano-Moreno, S (2020). Population pharmacokinetics of methotrexate in Mexican pediatric patients with acute lymphoblastic leukemia. Cancer chemotherapy and pharmacology 85(1) 21–31. DOI:10.1007/s00280-019-03977-1 PUBMED:https://pubmed.ncbi.nlm.nih.gov/31673826

3. Shi, ZY, et al., & Yan, D (2020). Population pharmacokinetics of high-dose methotrexate in Chinese pediatric patients with medulloblastoma. Biopharmaceutics & drug disposition 41(3) 101–110. DOI:10.1002/bdd.2221 PUBMED:https://pubmed.ncbi.nlm.nih.gov/32017134

Revisions

• 06/2025 initial generated model