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. 2020 Sep 27;9(10):3120. doi: 10.3390/jcm9103120

Table 1.

Comparison between melflufen and the known alkylator melphalan [30,33,40].

Characteristic Melflufen Melphalan
Chemical structure graphic file with name jcm-09-03120-i001.jpg graphic file with name jcm-09-03120-i002.jpg
Peak intracellular melphalan concentration * Relative concentration: ≈80 (achieved after 15 min exposure) Relative concentration: ≈4 (achieved after 60 min exposure)
Mean IC50, μM 0.05 1.5
Lipophilicity (LogP) 4.0 −0.97

* Evaluated in U1810 cells after up to 120 min of exposure with 10 μM melflufen and 10 μM melphalan. Mean IC50 value was obtained from 15 primary cultures from patients with hematologic malignancies. The partition coefficient, LogP, is a measure of the propensity for a compound to dissolve in lipids and water. A positive value indicates a higher concentration in the lipid phase, whereas a negative value indicates a higher concentration in water.