BioCentury
ARTICLE | Distillery Therapeutics

Therapeutics: An undetermined target

April 9, 2015 7:00 AM UTC

Cell culture and mouse studies suggest a deuterium-containing enantiomer of the racemic compound CC-122 could help treat MM and other hematologic malignancies more effectively than CC-122. Chemical synthesis and purification of deuterated versions of CC-122 - a thalidomide analog - yielded two stabilized enantiomers, (+)D2 and (-)D2. In an anti-inflammatory assay in human peripheral blood mononuclear cells, (-)D2 decreased tumor necrosis factor (TNF)-α production (IC50 = 48.5 nM) compared with (+)D2 (IC50 = 945 nM). In a mouse xenograft model of MM, oral 1.5 mg/kg doses of (-)D2 decreased tumor growth compared with 1.5 mg/kg of (+)D2 or 3 mg/kg of CC-122. Next steps include IND-enabling studies of (-)D2...