Melphalan
Also known as: Phenylalanine Mustard, L- Sarcolysine
Melphalan is a cytotoxic alkylating agent that is the L-phenylanine derivative of mechlorethamine. All alkylating agent have or can form an alkyl group that becomes covalently bound to cellular constituents. Melphalan is used parentrally in the treatment of different cancers to slow or stop abnormally growing cells. Melphalan is used in combination of different anticancer drugs to obtain best therapeutic effects and to reduce side effects or toxicities.
Primary Characteristics
Melphalan is also known as Phenylalanine Mustard, L- Sarcolysine.
It is of Synthetic origin and belongs to Amino phenylalanine.
It belongs to Alkylating Agents pharmacological group on the basis of mechanism of action and also classified in Antineoplastic Agent, Alkylating Agent pharmacological group.
Molecular Weight: 305.2 · pKa: 2.1, 9.5 · Solubility in Alcohol: 1 in 50 · Non-proprietary name: Melphalan.

Pharmacokinetics
Absorption: Melphalan has an oral bioavailability is 71% (±23%).
Distribution: Melphalan has a volume of distribution is 0.62 ± 0.21 l/kg. plasma protein binding is >80%.
Elimination: plasma half-life is 90 min (oral 83min,IV 92 min), renal excretion is 30%.
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Indications
Melphalan is primarily indicated in conditions like Advanced breast cancer, Breast cancer, Ewing's sarcoma, Malignant melanoma, Myelomatosis, Neuroblastoma, Ovarian cancer, Polycythemia rubravera, Soft tissue sarcoma.
Melphalan is also indicated for secondary conditions like Multiple myeloma.
Contraindications
Melphalan is contraindicated in conditions like Neutropenia, Myelosuppression, Hypersensitivity.
Dosage
Melphalan's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 6 mg | 6 mg | — | PO | For 2-3 weeks |
| 150 ug/kg | 150 ug/kg | — | PO | For 4-7 days |
| 250 ug/kg | 250 ug/kg | — | PO | For 4 days |
| Paediatric Dosage (20kg) | ||||
| No data. | ||||
| Neonatal Dosage (3kg) | ||||
| No data. | ||||
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Melphalan in overdosage may give rise to further complications which include Hemolytic anemia , Pulmonary fibrosis , Electrolyte disturbance, Diarrhea, Myelosuppressive effect , GI symptoms, Hemolytic anemia .
Melphalan produces potentially life-threatening effects which include Anemia, Thrombocytopenia , Neutropenia , Myelosuppression , Acute leukemia. Careful monitoring is needed with proper medical management.
The signs and symptoms that are produced after acute overdosage of Melphalan are Severe myelosuppression.
Melphalan is known to cause more or less tolerable side effects which are usually transient. These include Failure of menstruation, Hair loss, Maculopapular rash, Nausea, Pruritus , Vomiting .
Warnings / Precautions
Interference in Pathology
Melphalan may interfere in the diagnosis of Periodic blood count.
Available Brands
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Single Ingredient
Storage Conditions
Drug Classification
- 1.8.2 — Cytotoxic (anti-neoplastic) drugs
Manufacturers
Manufacturers of Melphalan in Pakistan: