Ulipristal acetate (ULIPA) is a synthetic progesterone receptor modulator (SPRM) used in emergency hormonal contraceptives and for treatment of uterine fibroids.
DrugBank Accession Number
KEGG Entry Number
Wikipedia Entry Name
White to yellow crystalline powder
Freely soluble in CHCl3, soluble in methanol, acetone, ethanol, and insoluble in water.
Headache, abdominal pain, nausea, dysmenorrhea, fatigue, and dizziness.
"No genotoxic potential was evident in any of the test systems when tested up to appropriate concentrations and dose levels according to guidelines."
< 1250 mg/kg (rat), >1250 mg/kg (rabbit)
Progesterone Receptor Activity
Partial agonist and antagonist
Androgen Receptor Activity
Estrogen Receptor Activity
Glucocorticoid Receptor Activity
Mineralocorticoid Receptor Activity
Elimination Half-Life (t1/2)
32.4 +/- 6.3 h (from 30 mg oral dose)
Serum Protein Binding
>94% bound to plasma proteins, including high density lipoprotein, alpha-l-acid glycoprotein, and albumin
Metabolized by CYP3A4 and to a lesser extent by CYP1A2
Mostly eliminated in feces, <10% in urine. Small amounts excreted in breast milk.
176 +/- 89 ng/mL (healthy subjects, single oral dose)
556 +/- 260 ng*h/mL (0-∞, healthy subjects, single oral dose)
76.8 +/- 64.0 L/h (mean oral clearance, single oral dose, health subject)
Permeability Glycoprotein (P-gp) Binding
Does not appear to be a P-gp substrate
Not pharmacologically active. Also referred to as PGL4004. Conversion from ulipristal acetate most likely mediated by CYP3A4.
Also known as metabolite PGL4002. Pharmacologically active. Binds to human plasma proteins extensively at 96.5%. Most likely mediated by CYP3A4.