Drug intelligence / Profile preview

mifepristone + misoprostol

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

Overview

Mifepristone + misoprostol is a pharmaceutical combination used primarily for the medical termination of intrauterine pregnancy through ten weeks gestation. Mifepristone is a synthetic steroid that acts as a competitive antagonist at the progesterone receptor, blocking the action of progesterone, which is necessary to sustain pregnancy. This leads to detachment of the gestational sac and softening of the cervix. Misoprostol, a prostaglandin E1 analog, induces uterine contractions and cervical dilation to expel pregnancy tissue. The regimen typically involves oral administration of mifepristone followed by buccal or vaginal administration of misoprostol 24–48 hours later. The combination is highly effective for early medical abortion and also used in management of early pregnancy loss (miscarriage). Mifepristone was developed by Roussel Uclaf (hence code name RU‑486) and first approved in 2000 in the US as Mifeprex; generic versions are now available[1][2][3][4][5].

Brand names
Mifégyne + MisoOneMedabonMifegyne Combikit
Other names
mifepristone and misoprostol combinationmedical abortion pill (colloquial)abortion pill (colloquial)
02

Targets

PR (Progesterone receptor)ORM1 (Alpha-1-acid glycoprotein 1)PTGER4 (Prostaglandin E2 receptor EP4 subtype)GR (Glucocorticoid receptor)PTGER2 (Prostaglandin E2 receptor EP2)AR (Adrenergic receptors)PTGER3 (Prostaglandin E2 receptor EP3 subtype)

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