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ACY-241 is a new, selective and orally available inhibitor of HDAC6 [1][2].

Histone deacetylase 6 (HDAC6) is an enzyme that removes acetyl groups from an ε-N-acetyl lysine on a histone, allowing the histones to wrap the DNA more tightly. HDAC6 plays an important role in transcriptional regulation and cell cycle progression.

ACY-241 is a new, selective and orally available HDAC6 inhibitor. In MM and MCL cells, the addition of ACY-241 to either lenalidomide (len) or pomalidomide (pom) resulted in synergistic increases in apoptosis and further reduced the expression of transcription factors MYC and IRF4 [1]. In multiple solid tumor cell lines, combination treatment with ACY-241 and paclitaxel resulted in enhanced inhibition of cell proliferation and increased cell death, compared with either single agent alone [2].

In MM xenograft model, combination treatment with ACY-241 and pomalidomide was well tolerated with no overt toxicity and significantly extended survival [1]. In xenograft models of pancreatic and ovarian cancer, combination treatment with ACY-241 and paclitaxel significantly increased mitotic cells with multipolar spindles. ACY-241 dose-dependently increased α-tubulin hyperacetylation [2].

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