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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › ALKYLATING AGENTS › Nitrogen mustard analogues
melphalan flufenamide
L01AA10
Forms & Strengths
- Powder for reconstitution: 20 mg melphalan flufenamide (as 21.6 mg melphalan flufenamide hydrochloride) in a single-dose vial
Adult Dosing
- 40 mg intravenously once every 28 days
- Administer in combination with dexamethasone (40 mg orally once weekly, or 20 mg for patients >75 years)
- Pre-medication with antiemetics recommended
- Modify dose based on hematologic toxicity during treatment
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of adult patients with relapsed or refractory multiple myeloma who have received at least four prior lines of therapy and whose disease is refractory to at least one proteasome inhibitor, one immunomodulatory agent, and one anti-CD38 monoclonal antibody
Mechanism of Action
- Peptide-drug conjugate that lipophilically crosses cell membranes
- Substrate for aminopeptidases, which are overexpressed in myeloma cells
- Rapidly hydrolyzed inside cells to release alkylating agents (melphalan), causing DNA crosslinking and cell death
Contraindications
- Known hypersensitivity to melphalan flufenamide or melphalan
Adverse Reactions
- Thrombocytopenia
- Neutropenia
- Anemia
- Fatigue
- Nausea
- Diarrhea
- Pyrexia
- Respiratory tract infections
- Hemorrhage
- Secondary primary malignancies
Drug Interactions
- Strong OATP1B1/3 inhibitors may increase systemic exposure of melphalan flufenamide
- Concomitant myelosuppressive agents may exacerbate bone marrow suppression
- Vaccination with live vaccines is not recommended during treatment
Curated Content: Needs Vetting Before Put to Clinical Use