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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ACY-738 is a potent, selective and orally-bioavailable HDAC6 inhibitor, with an IC50s of 1.7 nM.
HPOB is a highly potent and selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 of 56 nM, >30 fold less potent against other HDACs.
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