Phosphodiesterase 3 (PDE3) inhibition with cilostazol does not block in vivo oocyte maturation in rhesus macaques (Macaca mulatta)

Contraception. 2015 May;91(5):418-22. doi: 10.1016/j.contraception.2015.01.017. Epub 2015 Jan 30.

Abstract

Objective: Studies in mice suggest that cilostazol, an FDA-approved phosphodiesterase 3 (PDE3) inhibitor, might have a contraceptive effect within the approved dose range. We sought to evaluate the potential contraceptive effects of cilostazol in a nonhuman primate model.

Study design: Adult female rhesus macaques were stimulated to develop multiple preovulatory follicles by administering human recombinant gonadotropins, and oocytes were collected by follicle aspiration 36 h after an ovulatory stimulus (human chorionic gonadotropin). Monkeys received no further treatment (controls) or the PDE3 inhibitor cilostazol at the maximum approved human dose of 100mg twice daily starting 6 days prior to follicle aspiration. Recovered oocytes were scored for meiotic stage [germinal vesicle (GV) intact, GV breakdown], and metaphase II stage oocytes were fertilized in vitro and observed for normal embryo development.

Results: Similar proportions of GV stage oocytes were recovered from control (27%±4%) and cilostazol (27%±9%)-treated females, and the proportion of embryos that developed into blastocysts was also similar for both groups (7%±5% control vs. 15%±8% cilostazol).

Conclusion: Oral dosing of cilostazol tablets during controlled ovarian stimulation protocols did not prevent oocyte maturation or embryo development in macaques.

Implications: Since administration of the maximum approved human dose of cilostazol (an FDA-approved PDE3 inhibitor) to macaques did not prevent oocyte maturation or fertilization, it is not likely that this dose would be contraceptive in women.

Keywords: Germinal vesicle; Meiosis; Nonhormonal contraception; Nonhuman primate; cAMP.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Blastocyst / drug effects
  • Chorionic Gonadotropin / administration & dosage*
  • Cilostazol
  • Female
  • Humans
  • Macaca mulatta
  • Meiosis
  • Mice
  • Models, Animal
  • Oocytes / drug effects*
  • Oogenesis / drug effects*
  • Phosphodiesterase 3 Inhibitors / administration & dosage*
  • Recombinant Proteins / administration & dosage
  • Tetrazoles / administration & dosage*

Substances

  • Chorionic Gonadotropin
  • Phosphodiesterase 3 Inhibitors
  • Recombinant Proteins
  • Tetrazoles
  • Cilostazol