High Quality USP/EP Standard Yellow Powder Methotrexate CAS 59-05-2 Anti-cancer

Methotrexate More Info

Methotrexate is a widely used antimetabolite and immunosuppressant medication with applications in oncology, rheumatology, and dermatology.

Mechanism of Action

Methotrexate acts primarily by inhibiting several key enzymes involved in nucleotide synthesis, leading to impaired DNA and RNA synthesis and thus inhibiting cell division. Its main mechanisms include:
Inhibition of dihydrofolate reductase (DHFR): This prevents the reduction of dihydrofolate to tetrahydrofolate, a necessary cofactor for purine and thymidylate synthesis, thereby blocking DNA synthesis and cell replication, especially in rapidly dividing cells such as cancer cells.
Inhibition of thymidylate synthase and aminoimidazole carboxamide ribonucleotide transformylase (AICART): Methotrexate polyglutamates inhibit AICART, causing accumulation of aminoimidazole carboxamide ribonucleotide (AICAR), which leads to increased extracellular adenosine. Adenosine binds to cell surface receptors (notably adenosine receptor A2a), producing potent anti-inflammatory effects by suppressing immune cell activation.
Inhibition of nuclear factor-κB (NF-κB) activation: Through increased adenosine signaling and inhibition of BH2 to BH4 reduction, methotrexate reduces pro-inflammatory gene expression.
Modulation of immune cell functions: Methotrexate affects T cells, macrophages, endothelial cells, and fibroblast-like synoviocytes, reducing inflammation in autoimmune diseases like rheumatoid arthritis.

Applications

Oncology: Treatment of various cancers including acute lymphoblastic leukemia (ALL), non-Hodgkin's lymphoma, breast cancer, head and neck cancers, lung cancer, and mycosis fungoides (cutaneous T-cell lymphoma).
Autoimmune and inflammatory diseases: Rheumatoid arthritis (RA), polyarticular juvenile idiopathic arthritis (PJIA), severe psoriasis, systemic lupus erythematosus, inflammatory bowel disease, vasculitis, and other connective tissue diseases.
Other uses: Adjunct in organ transplantation, treatment of graft-versus-host disease, and in combination with other therapies for enhanced immunosuppression.

Routes of Administration and Dosage

Oral: Preferred for rheumatoid arthritis and psoriasis, with typical doses starting at 10 mg once weekly, escalating up to 15-25 mg weekly depending on response and tolerance.
Subcutaneous or intramuscular injection: Used especially when oral bioavailability is insufficient or gastrointestinal side effects occur; parenteral administration can improve efficacy and reduce GI toxicity.
Intravenous: Mainly used in oncology for high-dose methotrexate therapy.
Dose adjustments are made based on disease, patient response, and side effects. Methotrexate is typically administered once weekly for autoimmune conditions, never daily due to toxicity risk.

Safety and Side Effects

Common side effects: Nausea, vomiting, mouth sores, fatigue, low blood cell counts (anemia, leukopenia), abnormal liver function tests.
Serious adverse effects:
Hepatotoxicity, including severe or life-threatening liver damage with long-term use.
Bone marrow suppression leading to pancytopenia.
Pulmonary toxicity including pneumonitis.
Severe skin reactions and hypersensitivity.
Renal impairment, which can impair methotrexate clearance and increase toxicity.
Increased risk of infections due to immunosuppression.
Monitoring: Regular blood tests for liver function, renal function, and blood counts are essential. Folic acid supplementation is often used to reduce side effects.
Contraindications: Pregnancy (teratogenic), breastfeeding, severe renal or hepatic impairment, blood dyscrasias, active infections.

Pharmacokinetics

Absorption: Oral bioavailability is approximately 60% at doses ≤30 mg/m² but decreases at higher doses. Peak plasma concentrations occur between 45 minutes and 6 hours after administration.
Distribution: About 50% protein-bound (mainly albumin). Methotrexate distributes into synovial fluid and other tissues.
Metabolism: Partially metabolized in liver and cells to active polyglutamated forms that prolong intracellular effects. Also converted to 7-hydroxymethotrexate, a less soluble metabolite.
Elimination: Primarily renal excretion via glomerular filtration and active tubular secretion. Half-life varies but generally ranges from 3 to 10 hours depending on dose and renal function.

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