Version May 2024
Prostate cancer, metastatic, castration-resistant: While estramustine is approved for palliative treatment of progressive or metastatic prostate cancer, guidelines from the American Society of Clinical Oncology (ASCO) and Cancer Care Ontario for systemic therapy in men with metastatic castration-resistant prostate cancer recommend that estramustine not be offered in patients with metastatic castration-resistant prostate cancer due to a lack of benefit in survival or quality of life and an increased risk of toxicity (Ref). Therefore, dosing is not included.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
Frequency not always defined.
>10%:
Cardiovascular: Edema (20%)
Endocrine & metabolic: Gynecomastia (75%), increased lactate dehydrogenase (2% to 33%), decreased libido
Gastrointestinal: Nausea (16%), diarrhea (13%), gastrointestinal irritation (12%)
Genitourinary: Breast tenderness (71%)
Hepatic: Increased serum AST (2% to 33%)
Respiratory: Dyspnea (12%)
1% to 10%:
Cardiovascular: Cardiac failure (3%), local thrombophlebitis (3%), myocardial infarction (3%), cerebrovascular accident (2%), pulmonary embolism (2%), chest pain (1%), flushing (1%)
Central nervous system: Lethargy (4%), insomnia (3%), emotional lability (2%), anxiety (1%), headache (1%)
Dermatologic: Pruritus (2%), xeroderma (2%), exfoliation of skin (1%), skin rash (1%), thinning hair (1%)
Endocrine & metabolic: Increased thirst (1%)
Gastrointestinal: Anorexia (4%), flatulence (2%), gastrointestinal hemorrhage (1%), sore throat (1%), vomiting (1%)
Hematologic & oncologic: Leukopenia (4%), bruise (3%), thrombocytopenia (1%)
Hepatic: Increased serum bilirubin (1% to 2%)
Neuromuscular & skeletal: Leg cramps (9%)
Ophthalmic: Lacrimation (1%)
Respiratory: Hoarseness (1%), rhinorrhea (1%)
<1%, postmarketing, and/or case reports: Anemia, angina pectoris, angioedema, cerebral ischemia, confusion, depression, decreased glucose tolerance, hypercalcemia, hypocalcemia, hypersensitivity reaction, hypertension, impotence, ischemic heart disease, myasthenia, venous thrombosis
Known hypersensitivity to estramustine, estradiol, nitrogen mustard, or any component of the formulation; active thrombophlebitis or thromboembolic disorders (except where tumor mass is the cause of thromboembolic disorder and benefits may outweigh risks).
Canadian labeling: Additional contraindications (not in the US labeling): Severe hepatic or cardiac disease.
Concerns related to adverse effects:
• Cardiovascular effects: Elevated blood pressure or heart failure may occur. Estrogen treatment for prostate cancer is associated with an increased risk of thrombosis or myocardial infarction (including fatalities). Use with caution in patients with a history of thrombophlebitis, thrombosis, or thromboembolic disease, especially if associated with estrogen therapy. Use with caution in patients with cerebrovascular disease or coronary artery disease.
• Endocrine effects: Estrogenic effects may decrease testosterone levels; may cause gynecomastia and/or impotence.
• Fluid retention: Exacerbation of new or preexisting peripheral edema or heart failure has been observed. Use with caution in patients where fluid accumulation may be poorly tolerated, including heart failure, hypertension, migraine, seizure disorder or kidney dysfunction.
• Glucose tolerance: Glucose tolerance may be decreased; patients with diabetes should be carefully monitored.
• Hepatic effects: Liver enzyme and bilirubin abnormalities may occur.
• Hypersensitivity: Allergic reactions and angioedema, including airway involvement, have been reported.
Disease-related concerns:
• Metabolic bone disease: Use with caution in patients with metabolic bone diseases associated with hypercalcemia (due to effects on calcium and phosphorus homeostasis).
• Osteoblastic metastases: Patients with osteoblastic metastases are at risk for hypocalcemia; monitor calcium regularly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, Oral, as phosphate sodium:
Emcyt: 140 mg
No
Capsules (Emcyt Oral)
140 mg (per each): $20.11
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Capsule, Oral, as phosphate sodium:
Emcyt: 140 mg [DSC]
Oral: Administer on an empty stomach, at least 1 hour before or 2 hours after eating. Administer with water; do not administer with milk, milk-based products, or calcium products.
Hazardous agent (NIOSH 2016 [group 1]).
Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2016; USP-NF 2020).
Prostate cancer, metastatic, castration-resistant: While estramustine is approved for palliative treatment of progressive or metastatic prostate cancer, guidelines from the American Society of Clinical Oncology (ASCO) and Cancer Care Ontario for systemic therapy in men with metastatic castration-resistant prostate cancer recommend that estramustine not be offered in patients with metastatic castration-resistant prostate cancer due to a lack of benefit in survival or quality of life and an increased risk of toxicity (ASCO [Basch 2014]).
Emcyt may be confused with Eryc
Estramustine may be confused with carmustine, enzalutamide, exemestane.
This medication is in a class the Institute for Safe Medication Practices (ISMP) includes among its list of drug classes which have a heightened risk of causing significant patient harm when used in error.
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Calcium Salts: May decrease the absorption of Estramustine. Management: Administer estramustine on an empty stomach, at least 1 hour before or 2 hours after the dose of an oral calcium supplement. If coadministered with calcium salts, monitor for decreased estramustine therapeutic effects. Risk D: Consider therapy modification
Clodronate: May increase the serum concentration of Estramustine. Risk C: Monitor therapy
Lenograstim: Antineoplastic Agents may diminish the therapeutic effect of Lenograstim. Management: Avoid the use of lenograstim 24 hours before until 24 hours after the completion of myelosuppressive cytotoxic chemotherapy. Risk D: Consider therapy modification
Lipegfilgrastim: Antineoplastic Agents may diminish the therapeutic effect of Lipegfilgrastim. Management: Avoid concomitant use of lipegfilgrastim and myelosuppressive cytotoxic chemotherapy. Lipegfilgrastim should be administered at least 24 hours after the completion of myelosuppressive cytotoxic chemotherapy. Risk D: Consider therapy modification
Palifermin: May enhance the adverse/toxic effect of Antineoplastic Agents. Specifically, the duration and severity of oral mucositis may be increased. Management: Do not administer palifermin within 24 hours before, during infusion of, or within 24 hours after administration of myelotoxic chemotherapy. Risk D: Consider therapy modification
Estramustine serum levels may be decreased if taken with milk or other dairy products, calcium supplements, and vitamins containing calcium. Management: Take on an empty stomach at least 1 hour before or 2 hours after eating.
Some males who were impotent on estrogen therapy have regained potency while taking estramustine; effective contraception should be used for patients with partners who could become pregnant.
Estramustine is not indicated for use in females.
Estramustine is not indicated for use in females.
Milk products and calcium-rich foods or supplements may impair the oral absorption of estramustine phosphate sodium.
Monitor serum calcium, endocrine function tests (eg, testosterone; during therapy and for 2 months following therapy), liver function tests (during therapy and for 2 months following therapy), and serum glucose (in patients with diabetes). Monitor blood pressure and fluid status. Monitor for signs/symptoms of hypersensitivity, endocrine adverse effects, and/or thromboembolic events. Monitor adherence.
The American Society of Clinical Oncology hepatitis B virus (HBV) screening and management provisional clinical opinion (ASCO [Hwang 2020]) recommends HBV screening with hepatitis B surface antigen, hepatitis B core antibody, total Ig or IgG, and antibody to hepatitis B surface antigen prior to beginning (or at the beginning of) systemic anticancer therapy; do not delay treatment for screening/results. Detection of chronic or past HBV infection requires a risk assessment to determine antiviral prophylaxis requirements, monitoring, and follow-up.
Estramustine is an estradiol and nornitrogen mustard carbamate-linked combination which has antiandrogen effects (due to estradiol) and antimicrotubule effects (due to nornitrogen mustard); it causes a marked decrease in plasma testosterone and an increase in estrogen levels.
Absorption: Incomplete (Bergenheim 1998)
Metabolism: Initially dephosphorylated in the GI tract, then hepatically oxidated and hydrolyzed to estramustine, estromustine (oxidized isomer of estramustine), estrone, and estradiol.
Bioavailability: Oral: 44% to 75% (Bergenheim 1998)
Half-life elimination: Estromustine: 13.6 hours (range: 9 to 23 hours); Estrone: 16.5 hours (Bergenheim 1998)
Time to peak: 2 to 3 hours (Bergenheim 1998)
Excretion: Feces (primarily); urine (trace amounts) (Bergenheim 1998)
Hepatic function impairment: Estramustine may be poorly metabolized in patients with hepatic impairment.
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