Development of an intravaginal ring delivering simultaneously anastrozole and levonorgestrel: a pharmacokinetic perspective

References

• Alexander NJ, Baker E, Kaptein M, et al. (2004). Why consider vaginal drug administration? Fertil Steril 82:1–12.
   PubMed Web of Science ®Google Scholar
• Amsterdam LL, Gentry W, Jobanputra S, et al. (2005). Anastrazole and oral contraceptives: a novel treatment for endometriosis. Fertil Steril 84:300–4.
   PubMed Web of Science ®Google Scholar
• Arimidex®. (2017). Summary of product characteristics. Available at: https://www.medicines.org.uk/emc/product/2199/smpc [last accessed 12 Feb 2019]
   Google Scholar
• Ballagh SA. (2001). Vaginal ring hormone delivery systems in contraception and menopause. Clin Obstet Gynecol 44:106–13.
   PubMed Web of Science ®Google Scholar
• Bayer Jadelle® Prescribing information “Norplant II®” Levonorgestrel Implants (Jadelle®). NDA 20-544 Supplement 003 Prescribing information. 2002. Available at: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20544se2-003_jadelle_lbl.pdf [last accessed 12 Feb 2019]
   Google Scholar
• Bayer Norgeston®. (2018). Summary of product characteristics. Available at: http://www.medicines.org.uk/emc/medicine/1834 [last accessed 12 Feb 2019]
   Google Scholar
• Bayer Study 15687. (2013). Single center, open-label study to determine the pharmacokinetics of levonorgestrel (LNG) after repeated oral administration of 0.03 mg per day for at least 28 days in 20 healthy female subjects of reproductive age (clinical study synopsis). Available at: http://trialfinder.pharma.bayer.com/omr/online/15687_Study_Synopsis_CTP.pdf. [last accessed 12 Feb 2019]
   Google Scholar
• Bayer Study 16803. (2017). Multi-center, open-label, single-arm study to assess the safety and contraceptive efficacy of a levonorgestrel-containing intravaginal ring during a treatment period of one year in healthy women 18 to 35 years of age. ClinicalTrials.gov Identifier: NCT02403401 Available at: https://clinicaltrials.gov/ct2/show/study/NCT02403401?term=16803&rank=2 [last accessed 12 Feb 2019]
   Google Scholar
• Brache V, Faundes A. (2010). Contraceptive vaginal rings: a review. Contraception 82:418–27.
   PubMed Web of Science ®Google Scholar
• Bulun SE, Zeitoun KM, Takayama K, Sasano H. (2000). Estrogen biosynthesis in endometriosis: molecular basis and clinical relevance. J Mol Endocrinol 25:35–42.
   PubMed Web of Science ®Google Scholar
• Chien YW. (1992). Vaginal drug delivery and delivery systems. In: Novel drug delivery systems. New York: Marcel Dekker Inc., 529–584.
   Google Scholar
• Dunselman GA, Vermeulen N, Becker C, et al. (2014). ESHRE guideline: management of women with endometriosis. Hum Reprod 29:400–12.
   PubMed Web of Science ®Google Scholar
• Higa GM, al Khouri N. (1998). Anastrozole: a selective aromatase inhibitor for the treatment of breast cancer. Am J Health Syst Pharm 55:445.
   PubMed Web of Science ®Google Scholar
• Hussain A, Ahsan F. (2005). The vagina as a route for systemic drug delivery. J Control Release 103:301–13.
   PubMed Web of Science ®Google Scholar
• Kennedy S, Bergqvist A, Chapron C. (2005). ESHRE special interest group for endometriosis and endometrium guideline development. ESHRE guideline for the diagnosis and treatment of endometriosis. Hum Reprod 20:2698–704.
   PubMed Web of Science ®Google Scholar
• Kerns J, Darney P. (2011). Vaginal ring contraception. Contraception 83:107–15.
   PubMed Web of Science ®Google Scholar
• Mishell DR, Talas M, Parlow AF, Moyer DL. (1970). Contraception by means of a silastic vaginal ring impregnated with medroxyprogesterone acetate. Am J Obstet Gynecol 107:100–7.
   PubMed Web of Science ®Google Scholar
• Mulders TMT, Dieben OM. (2001). Use of the novel combined contraceptive vaginal ring NuvaRing for ovulation inhibition. Fertil Steril 75:865–70.
   PubMed Web of Science ®Google Scholar
• Nave R, Jalkanen T, Talling C, et al. (2018). The effect of drug content reduction on the in vitro and in vivo properties of levonorgestrel-releasing intravaginal rings. J Pharm Sci 107:1020–7.
   PubMed Web of Science ®Google Scholar
• Nave R, Klein S, Müller A, et al. (2018). Absence of effect of intravaginal miconazole, clindamycin, nonoxynol-9, and tampons on the pharmacokinetics of an anastrozole/levonergestrel intravaginal ring. J Clin Pharmacol 58:97–106.
   PubMed Web of Science ®Google Scholar
• Nave R, Mellinger U, Klein S, et al. (2019). Absence of drug-drug-interaction of anastrozole on levonorgestrel delivered simultaneously by an intravaginal ring: results of a phase 2 trial. J Clin Pharmacol. Epub ahead of print,
   PubMed Web of Science ®Google Scholar
• Novak A, de la Loge C, Abetz L, van der Meulen EA. (2003). The combined contraceptive vaginal ring, NuvaRing: an international study of user acceptability. Contraception 67:187–94.
   PubMed Web of Science ®Google Scholar
• Plourde PV, Dyroff M, Dukes M. (1994). Arimidex: a potent and selective fourth-generation aromatase inhibitor. Breast Cancer Res Tr 30:103–11.
   PubMed Web of Science ®Google Scholar
• Plummer R, Verheul HM, De Vos F, et al. (2018). Pharmacokinetic effects and safety of olaparib administered with endocrine therapy: A phase I study in patients with advanced solid tumours. Adv Ther 35:1945–64.
   PubMed Web of Science ®Google Scholar
• Reinecke I, Hofmann B, Mesic E, et al. (2018). An integrated population pharmacokinetic analysis to characterize levonorgestrel pharmacokinetics after different administration routes. J Clin Pharmacol 58:1639–54.
   PubMed Web of Science ®Google Scholar
• Reinecke I, Schultze-Mosgau MH, Nave R, et al. (2017). Model-based dose selection for intravaginal ring formulations releasing anastrozole and levonorgestrel intended for the treatment of endometriosis symptoms. J Clin Pharmacol 57:640–51.
   PubMed Web of Science ®Google Scholar
• Richardson JL, Illum L, Thomas NW. (1992). Vaginal absorption of insulin in the rat: effect of penetration enhancers on insulin uptake and mucosal histology. Pharm Res 9:878–83.
   PubMed Web of Science ®Google Scholar
• Rotgeri A, Korolainen H, Sundholm O, et al. (2015). Characterization of anastrozole effects, delivered by an intravaginal ring in cynomolgus monkeys. Hum Reprod 30:308–14.
   PubMed Web of Science ®Google Scholar
• Schultze-Mosgau M-H, Waellnitz K, Nave R, et al. (2016). Pharmacokinetics, pharmacodynamics, safety and tolerability of an intravaginal ring releasing anastrozole and levonorgestrel in healthy premenopausal women: a Phase 1 randomized controlled trial. Hum Reprod 31:1713–22.
   PubMed Web of Science ®Google Scholar
• Schwartzberg LS, Yardley DA, Elias AD, et al. (2017). A phase I/Ib study of enzalutamide alone and in combination with endocrine therapies in women with advanced breast cancer. Clin Cancer Res 23:4046–54.
   PubMed Web of Science ®Google Scholar
• Timmer CJ, Mulders TMT. (2000). Pharmacokinetics of etonogestrel and ethinylestradiol released from a combined contraceptive vaginal ring. Clin. Pharmacokinet 39:233–42.
   PubMed Web of Science ®Google Scholar
• Trussell J. (2011). Contraceptive failure in the United States. Contraception 83:397–404.
   PubMed Web of Science ®Google Scholar
• van Laarhoven JAH, Kruft MAB, Vromans H. (2002). In vitro release properties of etonogestrel and ethinyl estradiol from a contraceptive vaginal ring. Int J Pharm 232:163–73.
   PubMed Web of Science ®Google Scholar
• Wiseman LR, Adkins JC. (1998). Anastrozole. A review of its use in the management of postmenopausal women with advanced breast cancer. Drugs Aging 13:321–2.
   PubMed Web of Science ®Google Scholar