Dienogest is a selective progesterone receptor agonist in transactivation analysis with potent oral endometrial activity due to its efficient pharmacokinetic profile
Abstract
Dienogest was introduced as an oral progestin. Yet its strong oral potency on endometrial activity is not clearly explained. To circumvent this situation, steroid hormone receptor profiling using transactivation assay and endometrial activity test in rabbits were carried out with determination of plasma drug concentration. Agonistic/antagonistic activity on human progesterone receptor (PR), androgen receptor (AR), glucocorticoid receptor (GR), mineralocorticoid receptor (MR), estrogen receptor alpha (ERalpha), or estrogen receptor beta (ERbeta) were determined. Dienogest activate PR (EC50=3.4 or 10.5 nmol/l) with antagonistic activity on AR (EC50=420.6 or 775.0 nmol/l) but not agonistic nor antagonistic action on GR, MR (3000 nmol/l). Dienogest activate neither ERalpha nor ERbeta (3000 nmol/l). Progesterone activated PR with antagonistic activity on AR and on MR. Dydrogesterone showed a similar profile to progesterone. Norethisterone activated PR, AR, and ERalpha. Medroxyprogesterone acetate activated PR, AR, and GR. Danazol activated PR and AR. Collectively, dienogest has a good specificity to PR compared with the other drugs. By oral treatment, dienogest showed the strongest endometrial activity (ED50=0.0042 mg/kg) in McPhail test among other progestins (ED50 values for MPA, DYG, NES were 0.074, 1.9, >0.05 mg/kg, respectively). Dienogest showed higher plasma concentrations than those of the other progestins with higher doses. The estimated plasma concentration of dienogest…
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Dienogest is a selective progestin that combines the pharmacological properties of 19-norprogestins and progesterone derivatives, offering a pronounced progestogenic effect at the endometrium with an absence of androgenicity and moderate suppression of ovarian activity.
“Dienogest is a selective progestin that combines the pharmacological properties of 19-norprogestins and progesterone derivatives, offering a pronounced progestogenic effect at the endometrium with an absence of androgenicity and moderate suppression of ovarian activity”
From Dienogest is as effective as leuprolide acetate in treating the painful symptoms of endometriosis: a 24-week, randomized, multicentre, open-label trial (2010) · cites this paper as Sasagawa et al., 2008
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References 55 · Cited by 177
- Authors
- Sasagawa, S., Shimizu, Y., Kami, H., Takeuchi, T., Mita, S., Imada, K., Kato, S., & Mizuguchi, K.
- Affiliations
- Mochida Pharmaceutical (Japan) (JP)
- The University of Tokyo (JP)
- Corresponding author
- Sasagawa, Shinichi
- Venue
- Steroids
- Publisher
- Elsevier BV
- Published
- 2008-02
- Volume
- 73
- Issue
- 2
- Pages
- 222-231
- ISSN
- 0039-128X (ISSN-L)
- OpenAlex
- W2032738770
- Cited by
- 177
- References
- 55
- Citations by year
- 2026: 2 · 2025: 4 · 2024: 8 · 2023: 21 · 2022: 11 · 2021: 5 · 2020: 9 · 2019: 8 · 2018: 13 · 2017: 8 · 2016: 6 · 2015: 11 · 2014: 6 · 2013: 9 · 2012: 15
- FWCI
- 4.47
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Steroids (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
- Health Sciences › Medicine › Public Health, Environmental and Occupational Health › Reproductive Health and Contraception
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Adrenal Hormones and Disorders
- Keywords
- dienogest, progesterone receptor, progestins, receptor transactivation, androgen receptor antagonism, glucocorticoid receptor, mineralocorticoid receptor, estrogen receptor, plasma pharmacokinetics, oral bioavailability, medroxyprogesterone acetate, dydrogesterone, norethisterone, danazol
- MeSH terms
- Animals, Endometrium, Female, Humans, Nandrolone, Rabbits, Receptors, Androgen, Receptors, Progesterone, Receptors, Steroid, Androgen Receptor Antagonists
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