AVAILABLE MEDICINE FOR Melphalan

Image	Name	Price	Action
	Alkacel Melphalan 2mg Tablets $70.00 $120.00	$70.00 $120.00
	Alkacel Melphalan 5mg Tablets $85.00 $95.00	$85.00 $95.00

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Introduction to Melphalan

Melphalan is a chemotherapy drug used to treat certain types of cancer, including multiple myeloma and ovarian cancer. Approved by the FDA in 1964, it is one of the oldest alkylating agents still widely used in oncology. Melphalan works by damaging the DNA in cancer cells, which prevents them from dividing and growing.

Unlike targeted therapies, Melphalan's mechanism broadly affects dividing cells, making it effective but also associated with significant side effects. Its primary role is in high-dose chemotherapy regimens, often accompanied by stem cell transplants for enhanced efficacy. It is sold under brand names such as Alkeran and Evomela, with generic versions also available. These provide a cost-effective option for patients worldwide, enhancing accessibility.

Mechanism of Action

Melphalan belongs to the class of alkylating agents. It exerts its anticancer effects by forming covalent bonds with DNA, leading to DNA cross-linking. This disrupts DNA replication and transcription, ultimately causing cell death.

The drug introduces alkyl groups into the DNA, targeting guanine bases. This impairs DNA strand separation, a crucial step for replication.

Although Melphalan affects both healthy and cancerous cells, its greatest impact is on rapidly dividing cells, such as cancer cells and bone marrow cells.

This non-specific mechanism is effective against various cancers but often results in significant side effects, including bone marrow suppression and gastrointestinal disturbances.

Approval

Melphalan received FDA approval in 1964 for the treatment of multiple myeloma and ovarian cancer. Over the decades, it has become a cornerstone of high-dose chemotherapy protocols, particularly in hematological malignancies.

The European Medicines Agency (EMA) approved Melphalan for similar indications, recognizing its vital role in combination therapies, such as autologous stem cell transplantation in multiple myeloma patients.

Uses of Melphalan

Melphalan is prescribed for the following conditions:

Multiple Myeloma

Often used in high-dose regimens, particularly in combination with autologous stem cell transplantation.

Ovarian Cancer

Used as part of combination chemotherapy protocols.

Amyloidosis

To manage systemic light chain amyloidosis associated with plasma cell dyscrasias.

Conditioning Agent

Administered before bone marrow transplantation to eliminate existing bone marrow.

Administration Guidelines

Oral Melphalan should be taken on an empty stomach or as directed by a healthcare provider.
Intravenous infusions are given under strict medical supervision, usually in a hospital or specialized cancer center.

Side Effects

Melphalan is associated with both common and severe side effects:

Common Side Effects

Nausea and vomiting
Diarrhea or constipation
Fatigue and weakness
Temporary hair loss
Mucosal irritation (mouth sores)

Severe Side Effects

Bone marrow suppression, leading to anemia, leukopenia, and thrombocytopenia
Secondary cancers, including acute myeloid leukemia (rare but significant risk)
Severe gastrointestinal toxicity, particularly with high-dose regimens
Allergic reactions, including anaphylaxis

Drug Interactions and Lifestyle Factors

Drug Interactions

Immunosuppressants: Increased risk of infections when combined.
Live Vaccines: Avoid due to immunosuppression.
Other Alkylating Agents: May compound toxicity, especially to the bone marrow.

Dietary or Lifestyle Considerations:

Patients should maintain good oral hygiene to minimize the risk of mucositis.
Avoid alcohol, which can exacerbate gastrointestinal and liver toxicity.
Discuss any over-the-counter medications or supplements with a healthcare provider to avoid interactions.

Pharmacokinetics

Melphalan's pharmacokinetics reflect its systemic distribution and activity:

Absorption:-

Oral Melphalan exhibits variable bioavailability (25-89%) due to inconsistent absorption in the gastrointestinal tract.
Intravenous administration ensures predictable plasma concentrations.

Distribution:-

Melphalan has moderate protein binding (~60%), primarily to albumin.
It penetrates tissues, including bone marrow, effectively targeting rapidly dividing cells.

Metabolism:

Primarily metabolized in the liver via hydrolysis.
The parent compound and its metabolites are biologically active.

Excretion:

Elimination occurs through the kidneys, with approximately 10-20% excreted unchanged in urine.
The elimination half-life ranges from 1.5 to 2 hours after intravenous administration, but this can vary with renal impairment.