Melphalan is a nitrogen mustard alkylating agent belonging to the class of bifunctional alkylating compounds. It is an aromatic derivative of nitrogen mustard and is used as an antineoplastic pharmaceutical active ingredient.
Melphalan exerts its anticancer activity primarily by alkylating DNA, resulting in DNA cross-linking and inhibition of DNA replication and transcription. This mechanism affects rapidly dividing malignant cells and contributes to its cytotoxic activity.
Melphalan has the molecular formula C13H18Cl2N2O2 and a molecular weight of approximately 305.20 g/mol. Its CAS Number is 148-82-3.
Melphalan contains a nitrogen mustard functional group and is chemically related to the amino acid phenylalanine. The molecule contains a stereogenic center and is commonly handled as the L-isomer in pharmaceutical applications.
Melphalan is a DNA-alkylating agent. Its reactive nitrogen mustard group forms covalent bonds with nucleophilic sites on DNA, particularly DNA bases.
This can result in interstrand and intrastrand DNA cross-links, interfering with DNA replication and transcription and ultimately causing cellular damage and death.
Melphalan is used in pharmaceutical formulations for the treatment of selected hematological malignancies and solid tumors.
It has established applications in conditions including:
The approved indications vary according to formulation, dosage, treatment protocol and regulatory jurisdiction.
Melphalan API can be evaluated using validated analytical procedures for identification, assay, related substances, stereochemical purity, water content, residual solvents, elemental impurities and other applicable quality attributes.
HPLC, infrared spectroscopy and other validated analytical techniques may be used for identity, assay and purity determination. Because melphalan is a chemically reactive cytotoxic API, appropriate controls for degradation products and process-related impurities are important.
Final acceptance criteria should follow the applicable manufacturer's approved drug-substance specification and Certificate of Analysis.
Melphalan should be stored in a tightly closed pharmaceutical-grade container under controlled conditions and protected from excessive heat, moisture and light.
Because melphalan is a cytotoxic pharmaceutical substance, handling, storage and transportation should follow appropriate occupational safety and hazardous-drug procedures.
Melphalan API may be supplied for qualified pharmaceutical manufacturing, formulation development, analytical and research applications, subject to applicable regulatory, quality and occupational-safety requirements.
Melphalan API is available for qualified pharmaceutical development and manufacturing requirements. Customers can request product specifications, Certificate of Analysis, analytical documentation, packaging information and commercial details according to their requirements.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 2.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 10 ppm |
| pH (1% Solution) | 4.0 – 7.0 |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 2.0% |
| Water Content | NMT 2.0% |