CHEMICAL AND PHYSICAL PROPERTIES
| LogP | 4.04 |
|---|---|
| Dissociation Constants | 7.13 |
COMPUTED DESCRIPTORS
| Molecular Weight | 498.4 g/mol |
|---|---|
| XLogP3 | 3.2 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 6 |
| Rotatable Bond Count | 14 |
| Exact Mass | 497.1648254 g/mol |
| Monoisotopic Mass | 497.1648254 g/mol |
| Topological Polar Surface Area | 84.7 Ų |
| Heavy Atom Count | 33 |
| Formal Charge | 0 |
| Complexity | 579 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 2 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently-Bonded Unit Count | 1 |
| Compound Is Canonicalized | Yes |
PRODUCT INTRODUCTION
description
Melphalan flufenamide, also known as melflufen or J1, is a prodrug of [melphalan]. Melphalan flufenamide is more readily uptaken by cells than melphalan, and is cleaved to the active metabolite by aminopeptidases. In vitro models show that melphalan is 10 to hundreds of times more potent than melphalan. The increased potency makes melphalan flufenamide a treatment option for patients with relapsed or refractory multiple myeloma who have attempted at least 4 lines of therapy already. Melphalan flufenamide was granted FDA approval on 26 February 2021.. It has since been withdrawn from the market in the wake of the phase 3 OCEAN trial which showed a decrease in overall survival in comparison to standard treatment with [pomalidomide] and [dexamethasone] despite superior progression-free survival.