Drug reference

Diethylstilbestrol

Estrogen · Hormone responsive malignancy

Also known as Stilboestrol

EstrogenHormone responsive malignancy

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

8 major

SEVERE in our sources

PREGNANCY

In first trimester, high doses associated with vaginal carcinoma, urogenital abnormalities, and reduced fertility in female offspring. Increased risk of hypospadias in male offspring.

FDA category + note

Top interactionssee all 8 →

BexaroteneSevereDatabaseDDInter
CarfilzomibSevereDatabaseDDInter
DantroleneSevereDatabaseDDInter
LenalidomideSevereDatabaseDDInter

Mechanism

Diethylstilbestrol is a nonsteroidal estrogen that functions as an agonist, binding to and activating intracellular estrogen receptors (ERα and ERβ) within target cells. This activation modulates gene transcription and protein synthesis, mimicking the physiological effects of natural estrogens. Its widespread estrogenic activity influences cellular differentiation and development, which, when present during critical developmental stages, can result in adverse long-term clinical consequences like an increased risk of vaginal adenocarcinoma.

Indications

Breast cancer in postmenopausal womenProstate cancer

Dosing

Adult: Breast cancer in postmenopausal women: 10–20 mg daily by mouth. Prostate cancer: 1–3 mg daily by mouth.
Hepatic adjustment: Manufacturer advises caution in mild to moderate impairment; avoid in severe or active impairment.

Contraindications

Pregnancy (especially during first trimester, due to increased risk of carcinoma in offspring)

Side effects

Common

breast abnormalitiescervical mucus increasedcontact lens intolerancedepressionerectile dysfunctionerythema nodosumfeminisationfluid retentiongynaecomastiaheadachesmood alterednauseaskin reactionssodium retentiontesticular atrophyuterine disordersvomitingweight changeswithdrawal bleed

Serious

Cardiovascular disease
Bone pain (in breast cancer)
cholelithiasis
hypercalcaemia (in breast cancer)
hypertension
increased risk of thrombosis
jaundice cholestatic
neoplasms
Increased incidence of vaginal and cervical carcinoma in the female offspring in childhood or early adulthood
Other genital abnormalities in female and male offspring

Pregnancy & lactation

Pregnancy

In first trimester, high doses associated with vaginal carcinoma, urogenital abnormalities, and reduced fertility in female offspring. Increased risk of hypospadias in male offspring.