Abstract Topic: 13. Myeloma and other monoclonal gammopathies - Biology & Translational Research
Background: The immunomodulatory drugs (IMiDs) have made a profound difference in the treatment of multiple myeloma (MM). Lenalidomide (LND) is chiral compound with two enantiomers and one enantiomer may have different pharmacologic action than the other. For a given chiral drug, until proven otherwise, it is right to think of the two enantiomers as two different drugs with unique properties.
Aims: This study aimed to explore efficacy of lenalidomide (R) - (+) and (S) - (-) enantiomers in human multiple myeloma cell line.
Methods: H929 myeloma cell line model was designed to understand the potential differences in chirality of the R and S form of LND enantiomers and racemate in multiple myeloma cell line. We report the first biological evaluation of lenalidomide in racemic and in both (R)- and (S)-enantiomerically pure forms against (in vitro) H929 cells of multiple myeloma (MM) using an annexin V assay.
Results: It was observed that at 48 hours S-LND treated cells demonstrated significant reduction in the metabolic activity at 10 and 20 µg/mL and profound morphological changes. Cell cycle analysis showed cells in S and G2/M phase were decreased suggesting that all of the drugs can arrest cells at G1 cell cycle phase. We demonstrate (S) - (-) enantiomers of lenalidomide inhibited the growth of H929 MM cells without any in-vivo activation.
Summary/Conclusion: The study concludes that (S) - (-) enantiomers of lenalidomide noted more potent agent which could have both the anti-cancerous and immunomodulatory activity.
Keywords: Imids, Cell line, Multiple myeloma