Dienestrol

Dienestrol

Cat Number
API0231509
CAS Number
84-17-3

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CAS Number
84-17-3
EINECS
201-519-7
Storage
Store at room temperature
Synonyms
Dehydrostilbestrol; Cycladiene; DienolAgaldog; 3,4-bis(4-hydroxyphenyl)-4-hexadiene; 3,4-bis(para-hydroxyphenyl)-2,4-hexadiene
Molecular Formula
C18H18O2
Molecular Weight
266.33
Smiles
C/C=C(/C(=C/C)/C1=CC=C(C=C1)O)\C2=CC=C(C=C2)O
Appearance
Faint yellow powder
Melting Point
229℃
Boiling Point
349.54℃
General Description
Dienestrol is a synthetic, non-steroidal estrogen belonging to the stilbene class, structurally related to diethylstilbestrol. It is formulated as a topical cream for intravaginal administration, designed to provide local estrogenic effects with minimal systemic absorption. This agent was developed to treat atrophic changes in the vaginal epithelium associated with estrogen deficiency.
Mechanism of Action
As an estrogen receptor agonist, dienestrol binds to and activates estrogen receptors (ERα and ERβ) in target tissues, particularly the urogenital tract. This activation promotes the transcription of estrogen-responsive genes, leading to increased proliferation and maturation of the vaginal epithelium. The result is restoration of vaginal mucosal integrity, increased glycogen deposition, and normalization of vaginal pH.
Application
It is indicated for the treatment of atrophic vaginitis and kraurosis vulvae resulting from menopausal or postmenopausal estrogen deficiency. By delivering the hormone topically, it alleviates symptoms such as vaginal dryness, pruritus, and dyspareunia without the systemic metabolic effects associated with oral estrogen therapy. Its use is typically reserved for patients who require localized symptom management.

Interventions for late‑onset vaginal side effects after radiotherapy for uterine or cervical cancers were systematically reviewed (376 patients). Hyaluronic acid combined with vitamins A and E improved multiple endpoints: dyspareunia, mucosal inflammation, vaginal dryness, bleeding, fibrosis, and cellular atypia. Alpha‑tocopherol acetate alone reduced mucosal inflammation and improved vaginal acanthosis. Dienestrol benefited dyspareunia, vaginal caliber, and bleeding. Vaginal suppositories were the clinically effective formulation. Despite limited evidence, hyaluronic acid‑based formulations appear promising for managing radiation‑induced vaginitis and vaginal atrophy, though larger randomized trials are needed.

Fig. 1 Flow chart of the databases searches on the influence of vaginal interventions on vaginitis and vaginal atrophy after brachytherapy or radiotherapy in patients with malignant endometrial or cervical tumors. (Wierzbicka A, <i>et al</i>., 2021) Fig. 1 Flow chart of the databases searches on the influence of vaginal interventions on vaginitis and vaginal atrophy after brachytherapy or radiotherapy in patients with malignant endometrial or cervical tumors. (Wierzbicka A, et al., 2021)

References

  1. Wierzbicka A, et al. Interventions Preventing Vaginitis, Vaginal Atrophy after Brachytherapy or Radiotherapy Due to Malignant Tumors of the Female Reproductive Organs-A Systematic Review. Int J Environ Res Public Health. 2021; 18(8):3932.

Does Dienestrol require protection from light during storage?

Yes, it is photosensitive. Exposure to light can cause isomerization and degradation. Store in amber glass or opaque containers in a dark environment.

What is the recommended storage temperature for Dienestrol?

Store at controlled room temperature, between 15°C and 25°C. Avoid excessive heat, which can accelerate oxidative degradation.

Is Dienestrol susceptible to oxidation, and how is this prevented?

It can undergo oxidation, forming quinone-like degradation products. Our packaging minimizes headspace and includes oxygen absorbers for long-term stability.

How is the purity of Dienestrol verified for topical and vaginal formulations?

We use a stability-indicating HPLC method to monitor related steroids and degradation products, ensuring compliance with pharmacopoeial standards for topical use.
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