Givinostat - CAS 497833-27-9
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Not Intended for Therapeutic Use. For research use only.
Givinostat (INN) or gavinostat, aslo known as ITF2357,  is a histone deacetylase inhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities. It is a hydroxamate used in the form of its hydrochloride. Givinostat is in numerous phase II clinical trials (including for relapsed leukemias and myelomas), and has been granted orphan drug designation in the European Union for the treatment of systemic juvenile idiopathic arthritis and polycythaemia vera. ITF2357 was discovered at Italfarmaco of Milan, Italy. It was patented in 1997 and first described in the scientific literature in 2005.
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Givinostat; gavinostat; ITF-2357; ITF 2357; ITF2357.
Current Developer:
1.An immediate transcriptional signature associated with response to the histone deacetylase inhibitor Givinostat in T acute lymphoblastic leukemia xenografts.
Pinazza M1, Borga C2, Agnusdei V3, Minuzzo S1, Fossati G4, Paganin M2, Michielotto B2, De Paoli A5, Basso G2, Amadori A1,3, Te Kronnie G2, Indraccolo S3. Cell Death Dis. 2016 Jan 14;6:e2047. doi: 10.1038/cddis.2015.394.
Despite some success with certain hematological malignancies and in contrast with the strong pro-apoptotic effects measured in vitro, the overall response rate of acute lymphoblastic leukemia (ALL) to histone deacetylase inhibitors (HDACis) is low. With the aim to improve the understanding of how HDACis work in vivo, we investigated the therapeutic efficacy of the clinically approved HDACi Givinostat in a collection of nine pediatric human T-ALL engrafted systemically in NOD/SCID mice. We observed highly heterogeneous antileukemia responses to Givinostat, associated with reduction of the percentage of infiltrating blasts in target organs, induction of apoptosis and differentiation. These effects were not associated with the T-ALL cytogenetic subgroup. Transcriptome analysis disclosed an immediate transcriptional signature enriched in genes involved in cell-cycle regulation and DNA repair, which was validated by quantitative RT-PCR and was associated with in vivo response to this HDACi.
2.Givinostat inhibition of hepatic stellate cell proliferation and protein acetylation.
Wang YG1, Xu L1, Wang T1, Wei J1, Meng WY1, Wang N1, Shi M1. World J Gastroenterol. 2015 Jul 21;21(27):8326-39. doi: 10.3748/wjg.v21.i27.8326.
AIM: To explore the effect of the histone deacetylase inhibitor givinostat on proteins related to regulation of hepatic stellate cell proliferation.
3.Gain-of-function STAT1 mutations impair STAT3 activity in patients with chronic mucocutaneous candidiasis (CMC).
Zheng J1, van de Veerdonk FL2, Crossland KL1, Smeekens SP2, Chan CM3, Al Shehri T1, Abinun M1,4, Gennery AR1,4, Mann J5, Lendrem DW3, Netea MG2, Rowan AD3, Lilic D1,6. Eur J Immunol. 2015 Oct;45(10):2834-46. doi: 10.1002/eji.201445344. Epub 2015 Sep 1.
Signal transducer and activator of transcription 3 (STAT3) triggered production of Th-17 cytokines mediates protective immunity against fungi. Mutations affecting the STAT3/interleukin 17 (IL-17) pathway cause selective susceptibility to fungal (Candida) infections, a hallmark of chronic mucocutaneous candidiasis (CMC). In patients with autosomal dominant CMC, we and others previously reported defective Th17 responses and underlying gain-of-function (GOF) STAT1 mutations, but how this affects STAT3 function leading to decreased IL-17 is unclear. We also assessed how GOF-STAT1 mutations affect STAT3 activation, DNA binding, gene expression, cytokine production, and epigenetic modifications. We excluded impaired STAT3 phosphorylation, nuclear translocation, and sequestration of STAT3 into STAT1/STAT3 heterodimers and confirm significantly reduced transcription of STAT3-inducible genes (RORC/IL-17/IL-22/IL-10/c-Fos/SOCS3/c-Myc) as likely underlying mechanism.
4.Review article: selective histone deacetylase isoforms as potential therapeutic targets in inflammatory bowel diseases.
Felice C1, Lewis A, Armuzzi A, Lindsay JO, Silver A. Aliment Pharmacol Ther. 2015 Jan;41(1):26-38. doi: 10.1111/apt.13008. Epub 2014 Nov 4.
BACKGROUND: A link between histone deacetylases (HDACs) and intestinal inflammation has been established. HDAC inhibitors that target gut-selective inflammatory pathways represent a potential new therapeutic strategy in patients with refractory inflammatory bowel diseases (IBD).
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