Drug reference

Estramustine

Taxane · Anticancer

Also known as Estramustine phosphate, Estramustine sodium phosphate, Estracyt

TaxaneAnticancerATC null

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

2 major

SEVERE in our sources

PREGNANCY

and reproductive function in Cytotoxic drugs

FDA category + note

Top interactionssee all 3 →

ThalidomideSevereDatabaseDDInter
Tranexamic AcidSevereDatabaseDDInter

Mechanism

Estramustine inhibits microtubule function, acting as an antimicrotubule agent. This action disrupts cellular processes dependent on microtubules, such as cell division.

Indications

Malignant diseaseHormone-refractory prostate cancerPalliative treatment of progressive or metastatic prostate cancerAdvanced or metastatic prostate cancer (nonresponsive to hormone therapy)

Dosing

Adult: adults for the treatment of recurrent glioblastoma multiforme as an adjunct to surgery. Carmustine implants are also licensed for high-grade malignant glioma as adjunctive treatment to surgery and radiotherapy. Estramustine phosphate p. 946 is a combination of an oestrogen and chlormethine used predominantly in prostate cancer.…

Pharmacokinetics

Half-life

10 h (estramustine); 14 h (estromustine, active metabolite)

Bioavailability

At least 75% of a dose is absorbed after oral administration.

Metabolism

Extensive first-pass metabolism by hepatic CYPs to an active 17-keto derivative (estromustine) and multiple inactive products. Some hydrolysis of the carbamate linkage occurs in the liver, releasing estradiol, estrone, and the normustine group. The active drug forms accumulate in the prostate.

Excretion

Inactive metabolites, mainly in the feces.

Contraindications

Concomitant administration of spironolactone

Side effects

Common

Anaemiacongestive heart failurediarrhoeaembolismfluid retentiongynaecomastiaheadachehepatic function abnormallethargyleucopeniamyocardial infarctionnauseathrombocytopeniavomitingMyelosuppressionGynecomastiaImpotenceHypercalcemiaImpaired glucose toleranceAnorexiaSomnolenceDermatitisAngioedemaHypersensitivity reactions

Serious