Mayur S. Jain, Mayur R. Bhurat, Sunil R Bavaskar
Mr. Mayur S. Jain1*, Dr. Mayur R. Bhurat2, Mr. Sunil R Bavaskar3
1Shri. Prakashchand Jain College of Pharmacy and Research, Palaskhede, Jamner, Maharashtra, India.
2Principal, Shri. Prakashchand Jain College of Pharmacy and Research, Palaskhede, Jamner, Maharashtra, India.
3Shri. Prakashchand Jain college of Pharmacy and Research, Palaskhede, Jamner Maharashtra, India.
Volume - 11,
Issue - 4,
Year - 2021
Melphalan Flufenamide is a peptide-drug conjugate composed of a peptide conjugated, via an aminopeptidase-targeting linkage, to the alkylating agent melphalan, with potential antineoplastic and anti-angiogenic activities. Upon administration, the highly lipophilic melphalan flufenamide penetrates cell membranes and enters cells. In aminopeptidase-positive tumor cells, melphalan flufenamide is hydrolyzed by peptidases to release the hydrophilic alkylating agent melphalan. This results in the specific release and accumulation of melphalan in aminopeptidase-positive tumor cells. Melphalan alkylates DNA at the N7 position of guanine residues and induces DNA intra- and inter-strand cross-linkages. This results in the inhibition of DNA and RNA synthesis and the induction of apoptosis, thereby inhibiting tumor cell proliferation. Peptidases are overexpressed by certain cancer cells. The administration of melphalan flufenamide allows for enhanced efficacy and reduced toxicity compared to melphalan.1,2,3
Cite this article:
Mayur S. Jain, Mayur R. Bhurat, Sunil R Bavaskar. Melphalan flufenamide is an Anticancer medication used to treat multiple Myeloma: A Review. Asian Journal of Research in Pharmaceutical Sciences. 2021; 11(4):291-4. doi: 10.52711/2231-5659.2021.00045
Mayur S. Jain, Mayur R. Bhurat, Sunil R Bavaskar. Melphalan flufenamide is an Anticancer medication used to treat multiple Myeloma: A Review. Asian Journal of Research in Pharmaceutical Sciences. 2021; 11(4):291-4. doi: 10.52711/2231-5659.2021.00045 Available on: https://ajpsonline.com/AbstractView.aspx?PID=2021-11-4-5
1. www,drug bank.com
2. "FDA grants accelerated approval to melphalan flufenamide for relapsed". U.S. Food and Drug Administration (FDA). 26 February 2021. Retrieved 1 March 2021.
3. Strese, Sara; Wickström, Malin; Fuchs, Peder Fredlund; Fryknäs, Mårten; Gerwins, Pär; Dale, Tim; Larsson, Rolf; Gullbo, Joachim (2013). "The novel alkylating prodrug melflufen (J1) inhibits angiogenesis in vitro and in vivo". Biochemical Pharmacology. 86 (7): 888–95
4. "FDA Approves Oncopeptides' Pepaxto (melphalan flufenamide) for Patients with Triple-Class Refractory Multiple Myeloma" (Press release). Oncopeptides AB. 1 March 2021.
5. "Plasma Cell Neoplasms (Including Multiple Myeloma) Treatment (PDQ®)–Health Professional Version". NCI. July 29, 2016. Archived from the original on 4 July 2016. Retrieved 8 August 2016.
6. Gullbo, J; Tullberg, M; Våbenø, J; Ehrsson, H; Lewensohn, R; Nygren, P; Larsson, R; Luthman, K (2003). "Structure-activity relationship for alkylating dipeptide nitrogen mustard derivatives". Oncology Research. 14 (3): 113–32.
7. World Cancer Report 2014. World Health Organization. 2014. pp. Chapter 2.3 and 2.6.
8. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
9. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct; 5(10): 821-34.
10. Monahan SD, Subbotin VM, Budker VG, Slattum PM, Neal ZC, Herweijer H, Wolff JA: Rapidly reversible hydrophobization: an approach to high first-pass drug extraction. Chem Biol. 2007 Sep; 14(9):1065-77