Romidepsin (FK228) is a structurally unique, potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM, respectively. Romidepsin inhibits the growth of U-937, K562, and CCRF-CEM cells with IC50 of 5.92 nM, 8.36 nM, and 6.95 nM, respectively. Romidepsin exhibits concentration-dependent cytotoxicity against a panel of mantle cell lymphoma (MCL) cell lines. FK228 (Romidepsin) treatment potently inhibits the neovascularization of chick embryo and that of adult mice in the Matrigel plug assay. FK228(Romidepsin) is currently in a Phase I study in treating patients with lymphoma, chronic lymphocytic leukemia, or solid tumors with liver dysfunction.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Results from a pivotal, open-label, phase II study of romidepsin in relapsed or refractory peripheral T-cell lymphoma after prior systemic therapy.
Coiffier B, et al. J Clin Oncol. 2012 Feb 20;30(6):631-6. PMID: 22271479.
Phase 2 trial of romidepsin in patients with peripheral T-cell lymphoma.
Piekarz RL, et al. Blood. 2011 Jun 2;117(22):5827-34. PMID: 21355097.
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EDO-S101 is a pan HDAC inhibitor; inhibits HDAC1, HDAC2 and HDAC3 with IC50 values of 9, 9 and 25 nM, respectively.
Citarinostat (ACY-241) is an orally available selective HDAC6 inhibitor with IC50 of 2.6 nM and 46 nM for HDAC6 and HDAC3, respectively. It has 13 to 18-fold selectivity towards HDAC6 in comparison to HDAC1-3.
BRD73954 ia a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.
Sodium butyrate is the sodium salt of butyric acid, which has been reported to cause hyperacetylation of histones due to its role as a HDAC inhibitor with IC50 values of 0.3, 0.4, 0.3 mM for HDAC1, 2 and 7 respectively.
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