Drug intelligence / Profile preview

methotrexate + misoprostol

Development stage
Unknown
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Intramuscular, Oral, Vaginal, Buccal, Sublingual
01

Overview

Methotrexate + misoprostol is a combination regimen used primarily for the medical termination of early intrauterine pregnancy (medical abortion), typically up to 8 weeks gestation. Methotrexate is an antimetabolite and antifolate agent that inhibits dihydrofolate reductase, thereby blocking DNA synthesis and cell replication, particularly affecting rapidly dividing trophoblastic tissue in early pregnancy. Misoprostol is a synthetic prostaglandin E1 analog that induces uterine contractions and cervical softening, leading to expulsion of uterine contents. This combination offers an alternative to surgical abortion methods and has also been used off-label for the management of ectopic pregnancies and non-viable pregnancies[1][2][3][6][8]. Both drugs are approved by regulatory agencies for other indications—methotrexate for certain cancers, rheumatoid arthritis, psoriasis; misoprostol for prevention of NSAID-induced gastric ulcers—but their use together in abortion is off-label[1][5][6]. The regimen's efficacy decreases with increasing gestational age beyond 50 days[1].

02

Targets

DHFR (Dihydrofolate reductase)

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