MedKoo product information:

 Pracinostat

Description of Pracinostat: Pracinostat (SB939) is an orally bioavailable, small-molecule histone deacetylase (HDAC) inhibitor with potential antineoplastic activity. Pracinostat inhibits HDACs, which may result in the accumulation of highly acetylated histones, followed by the induction of chromatin remodeling; the selective transcription of tumor suppressor genes; the tumor suppressor protein-mediated inhibition of tumor cell division; and, finally, the induction of tumor cell apoptosis. This agent may possess improved metabolic, pharmacokinetic and pharmacological properties compared to other HDAC inhibitors. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).  

Current developer:    S*Bio.

1: Jayaraman R, Pilla Reddy V, Khalid Pasha M, Wang H, Sangthongpitag K, Yeo P, Yong Hu C, Wu X, Xin L, Goh E, Sun New L, Ethirajulu K. Preclinical Metabolism and Disposition of SB939 (Pracinostat), an Orally Active Histone Deacetylase Inhibitor, and Prediction of Human Pharmacokinetics. Drug Metab Dispos. 2011 Dec;39(12):2219-32. Epub 2011 Aug 26. PubMed PMID: 21873472.

2: Wang H, Yu N, Chen D, Lee KC, Lye PL, Chang JW, Deng W, Ng MC, Lu T, Khoo ML, Poulsen A, Sangthongpitag K, Wu X, Hu C, Goh KC, Wang X, Fang L, Goh KL, Khng HH, Goh SK, Yeo P, Liu X, Bonday Z, Wood JM, Dymock BW, Kantharaj E, Sun ET. Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylami de (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. J Med Chem. 2011 Jul 14;54(13):4694-720. Epub 2011 Jun 16. PubMed PMID: 21634430.

3: Novotny-Diermayr V, Sausgruber N, Loh YK, Pasha MK, Jayaraman R, Hentze H, Yong WP, Goh BC, Toh HC, Ethirajulu K, Zhu J, Wood JM. Pharmacodynamic evaluation of the target efficacy of SB939, an oral HDAC inhibitor with selectivity for tumor tissue. Mol Cancer Ther. 2011 Jul;10(7):1207-17. Epub 2011 May 17. PubMed PMID: 21586629.

4: Yong WP, Goh BC, Soo RA, Toh HC, Ethirajulu K, Wood J, Novotny-Diermayr V, Lee SC, Yeo WL, Chan D, Lim D, Seah E, Lim R, Zhu J. Phase I and pharmacodynamic study of an orally administered novel inhibitor of histone deacetylases, SB939, in patients with refractory solid malignancies. Ann Oncol. 2011 Nov;22(11):2516-22. Epub 2011 Mar 8. PubMed PMID: 21385886.

5: Razak AR, Hotte SJ, Siu LL, Chen EX, Hirte HW, Powers J, Walsh W, Stayner LA, Laughlin A, Novotny-Diermayr V, Zhu J, Eisenhauer EA. Phase I clinical, pharmacokinetic and pharmacodynamic study of SB939, an oral histone deacetylase (HDAC) inhibitor, in patients with advanced solid tumours. Br J Cancer. 2011 Mar 1;104(5):756-62. Epub 2011 Feb 1. PubMed PMID: 21285985; PubMed Central PMCID: PMC3048208.

6: Novotny-Diermayr V, Sangthongpitag K, Hu CY, Wu X, Sausgruber N, Yeo P, Greicius G, Pettersson S, Liang AL, Loh YK, Bonday Z, Goh KC, Hentze H, Hart S, Wang H, Ethirajulu K, Wood JM. SB939, a novel potent and orally active histone deacetylase inhibitor with high tumor exposure and efficacy in mouse models of colorectal cancer. Mol Cancer Ther. 2010 Mar;9(3):642-52. Epub 2010 Mar 2. PubMed PMID: 20197387.