methotrexate + human serum albumin

Methotrexate + human serum albumin is a conjugate or non-covalent complex of methotrexate, a well-established antimetabolite and immunosuppressant, with human serum albumin (HSA), used as a drug delivery carrier. Methotrexate exerts its anti-proliferative and anti-inflammatory effects primarily by inhibition of dihydrofolate reductase, disrupting DNA synthesis in rapidly dividing cells. Conjugation to human serum albumin enhances drug delivery and targeting due to albumin’s natural accumulation in tumors and inflamed tissue, leveraging the "Trojan horse" effect for selective uptake. This approach prolongs the circulation time of methotrexate up to several weeks (versus hours for free methotrexate) and greatly reduces systemic toxicity and off-target side effects. It is being evaluated for solid tumors, metastases, and inflammatory diseases such as rheumatoid arthritis and atherosclerosis, with evidence of increased efficacy and lower toxicity compared to free methotrexate. The compound may be prepared pharmaceutically or engineered into carrier systems such as liposomes for advanced drug delivery applications[1][4][6].

Brand names

MTX-HSA

Other names

methotrexate-albumin conjugatealbumin-coupled methotrexatemethotrexate-human serum albumin complexHSA-methotrexate