Estramustine is an antineoplastic pharmaceutical compound used primarily in the treatment of advanced prostate cancer. It is a nitrogen mustard derivative linked to an estrogen component, giving it a distinctive dual mechanism involving both cytotoxic and microtubule-targeting activity.
Estramustine is used as an active pharmaceutical ingredient in oncology formulations, where it is commonly administered in the form of estramustine phosphate, a water-soluble prodrug.
Estramustine is an antineoplastic agent structurally related to both nitrogen mustard compounds and estrogenic steroids. Its pharmacological activity is associated with disruption of microtubule function and inhibition of cancer-cell proliferation.
CAS Number: 2998-57-4
Molecular Formula: C₂₃H₃₁Cl₂NO₃
Molecular Weight: 456.40 g/mol
Estramustine and its active metabolites interfere with microtubule-associated proteins and microtubule assembly, disrupting cell division and inhibiting proliferation of tumor cells.
Its mechanism is associated with:
Estramustine is primarily associated with pharmaceutical formulations for:
The exact indication depends on the specific pharmaceutical formulation and applicable regulatory approval.
Estramustine is an oncology API with defined chemical and stereochemical characteristics. Pharmaceutical-grade material requires appropriate control of identity, assay, related substances, residual solvents and other quality attributes.
Typical analytical evaluation may include:
Pharmaceutical-grade Estramustine should comply with the applicable approved specification and relevant regulatory requirements.
A qualified supplier should provide Certificate of Analysis (CoA), specification sheet, SDS/MSDS, batch traceability and applicable regulatory documentation.
Store Estramustine in a tightly closed container, protected from excessive moisture, heat and direct light, according to the approved storage and stability requirements.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.2% |
| Heavy Metals | NMT 20 ppm |
| pH (1% Solution) | 2.0 – 4.0 |