Ulipristal Acetate-d6 (Synonyms: CDB-2914-d6)

Ulipristal acetate-d₆ is intended for use as an internal standard for the quantification of ulipristal acetate by GC- or LC-MS. Ulipristal acetate is a selective progesterone receptor modulator (SPRM) that binds to the human progesterone receptors PR-A and PR-B (EC₅₀s = 8.5 and 7.7 nM, respectively), rabbit uterine PR (EC₅₀ = 13.6 nM), and rabbit thymic glucocorticoid receptor (GR; EC₅₀ = 15.4 nM).¹ It is selective for human progesterone receptors over the human estrogen receptor (ER; EC₅₀ = >10,000 nM). It inhibits growth of IGROV-1 and SK-OV-3 human ovarian cancer cells (IC₅₀s = 15.5 and 31.5 μM, respectively) even after resistance to combined cisplatin and paclitaxel treatment has developed.² Ulipristal acetate reverses the proliferative effect of progesterone on patient-derived germline mutant BRCA1 breast tissue xenografts in ovariectomized athymic mice.³ Ulipristal acetate (40 mg/kg, i.p.) administered to female mice within 6 hours of human chorionic gonadotropin (hCG) treatment inhibits ovulation.⁴ Formulations containing ulipristal acetate have been used as emergency contraceptives and to treat uterine fibroids.

1.Attardi, B.J., Burgenson, J., Hild, S.A., et al.In vitro antiprogestational/antiglucocorticoid activity and progestin and glucocorticoid receptor binding of the putative metabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristoneJ. Steroid Biochem. Mol. Biol.88(3)277-288(2004) 2.Gamarra-Luques, C.D., Hapon, M.B., Goyeneche, A., et al.Resistance to cisplatin and paclitaxel does not affect the sensitivity of human ovarian cancer cells to antiprogestin-induced cytotoxicityJ. Ovarian Res.7:45(2014) 3.Communcal, L., Vilasco, M., Hugon-Rodin, J., et al.Proliferation and ovarian hormone signaling are impaired in normal breast tissues from women with BRCA1 mutations: Benefit of a progesterone receptor modulator treatment as a breast cancer preventive strategy in women with inherited BRCA1 mutationsOncotarget7(29)45317-45330(2016) 4.Nallasamy, S., Kim, J., Sitruk-Ware, R., et al.Ulipristal blocks ovulation by inhibiting progesterone receptor-dependent pathways intrinsic to the ovaryReprod. Sci.20(4)371-381(2013)