Tìm theo
SB939
Thuốc điều trị ung thư
Thuốc Gốc
Small Molecule
SB939 is a novel HDAC inhibitor with improved in vivo properties compared to other HDAC inhibitors currently in clinical trials, allowing oral dosing. Data demonstrate that SB939 is a potent and effective anti-tumor drug with potential as an oral therapy for a variety of human hematological and solid tumors.
Dược Lực Học : SB939 is a novel compound with superior pharmaceutical, metabolic and pharmacokinetic properties. SB939 has demonstrated excellent in vivo anti-tumour activity in various animal models with dose proportional pharmacodynamic effects. The pharmacokinetics and pharmacodynamic attributes of SB939 explain and differentiate it as the best in class HDAC inhibitor.
Cơ Chế Tác Dụng : SB939 is a novel HDAC inhibitor with improved in vivo properties compared to other HDAC inhibitors currently in clinical trials, allowing oral dosing. Data demonstrate that SB939 is a potent and effective anti-tumor drug with potential as an oral therapy for a variety of human hematological and solid tumors. Inhibition of HDAC activity allows for the accumulation of acetyl groups on the histone lysine residues resulting in an open chromatin structure and transcriptional activation. In vitro, SB939 causes the accumulation of acetylated histones and induces cell cycle arrest and/or apoptosis of some transformed cells. The mechanism of the antineoplastic effect of SB939 has not been fully characterized.
Dược Động Học :
▧ Absorption :
Oral bioavailability in mice is 34%.
Chỉ Định : For the treatment of various forms of cancer.
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