Estramustine
- CAS NO.:2998-57-4
- Empirical Formula: C23H31Cl2NO3
- Molecular Weight: 440.4
- MDL number: MFCD00866377
- EINECS: 221-076-3
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-04 20:04:50
What is Estramustine?
The Uses of Estramustine
Antineoplastic.
The Uses of Estramustine
Estradiol 3-[N,N-Bis(2-chloroethyl)carbamate] is used treatment of breast cancer. Also used in the treatment of prostate cancer.
Background
A nitrogen mustard linked to estradiol, usually as phosphate; used to treat prostatic neoplasms; also has radiation protective properties.
Indications
For the palliative treatment of patients with metastatic and/or progressive carcinoma of the prostate
What are the applications of Application
Estramustine is an estrogen derivative
Definition
ChEBI: A carbamate ester obtained by the formal condensation of the hydroxy group of 17beta-estradiol with the carboxy group of bis(2-chloroethyl)carbamic acid.
Indications
Estramustine phosphate sodium (Emcyt) is a hybrid structure combining estradiol and a nitrogen mustard in a single molecule. The drug has been approved for use in prostatic carcinomas and will produce clinical remissions in one-third of patients who have failed to respond to previous estrogen therapy. The mechanism of action of estramustine is not well defined, but it does not appear to require either alkylation of DNA or the presence of estrogen receptors in tumor cells. Nonetheless, the toxicities of the drug are similar to those of estrogen therapy: breast tenderness and enlargement (gynecomastia), fluid retention, mild nausea, and an increased risk of thrombophlebitis and pulmonary embolism.The drug is not myelosuppressive.
Biological Functions
Estramustine has a low affinity for the βm tubulin isotype, which often is overexpressed in estramustineresistant prostatic neoplasms as one defense against this therapeutic intervention.
Mechanism of action
Because this anticancer agent contains a carbamylated nitrogen mustard moiety, it is most commonly classified as a DNA alkylator; however, it is now known that its primary mechanism of antineoplastic action is inhibition of mitosis.
Pharmacokinetics
Estramustine is an antineoplastic agent indicated in the palliative treatment of patients with metastatic and/or progressive carcinoma of the prostate. Estramustine is a combination of estradiol with nitrogen mustard. In vivo, the nitrogen-mustard moiety becomes active and participates in alkylation of DNA or other cellular components.. This causes DNA damage in rapidly dividing cancerous cells leading to cell death and ideally, tumor shrinkage.
Metabolism
Not Available
Properties of Estramustine
Melting point: | 104-105° |
Boiling point: | 565.8±50.0 °C(Predicted) |
alpha | D20 +50° (in dioxane) |
Density | 1.253±0.06 g/cm3(Predicted) |
storage temp. | Store at -20°C |
pka | 15.05±0.40(Predicted) |
form | Solid |
color | White to off-white |
Water Solubility | 1mg/L(30 ºC) |
CAS DataBase Reference | 2998-57-4(CAS DataBase Reference) |
Safety information for Estramustine
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for Estramustine
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