Methotrexate: A Pharmacological Powerhouse in Modern Therapeutics

Methotrexate (MTX), a folate antagonist, has been widely used in cancer chemotherapy and autoimmune diseases since its development in the mid-20th century. It was first used in 1948 to treat leukemia, and in 1988 the FDA approved it for use in treating rheumatoid arthritis (RA). By suppressing dihydrofolate reductase, preventing DNA and RNA synthesis, and adjusting immunological responses, MTX works. MTX has side effects such as hepatotoxicity, hematological suppression, and pulmonary problems despite its effectiveness. MTX has a limited bioavailability at large oral doses and is categorized as a BCS Class IV medication because of its poor solubility and low permeability. It is metabolized by the liver and eliminated by the kidneys. The medicine is contraindicated in pregnant individuals and those with liver, renal, or lung disorders. Drug interactions are common, particularly when using PPIs and NSAIDs. Leucovorin rescue, urine alkalinization, and hemodialysis are used to treat overdoses of MTX, which comes in a variety of oral and injectable forms. Tetra aminopyrimidine is the beginning point for a series of chemical processes that make up its production. Despite the advent of more recent treatments, MTX continues to be a mainstay medication because of its several uses in rheumatology, dermatology, and oncology.