Givinostat

Structural formula
	Givinostat hydrochloride
General
Non-proprietary name	Givinostat
other names	{6 - [(Diethylamino) methyl] -2-naphthyl} methyl- [4- (hydroxycarbamoyl) phenyl] carbamate ( IUPAC ) ; N - (4 - ((Hydroxyamino) methyl) -2-naphthalenyl) methyl ester · hydrochloride ;
Molecular formula	C 24 H 27 N 3 O 4 • HCl
External identifiers / databases
EC number	823-729-3
ECHA InfoCard	100.258.524
PubChem	9804992
ChemSpider	7980752
DrugBank	DB12645
Wikidata	Q426257
Drug information
Mechanism of action	Histone deacetylase - inhibitor
properties
Molar mass	421.49 g · mol -1
safety instructions
GHS hazard labeling ; no classification available
GHS hazard labeling ; no classification available
	As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Givinostat is a potential drug in clinical development to be used in the treatment of systemic juvenile idiopathic arthritis and polycythemia . It is used medicinally as the hydrochloride and is currently in phase 2 studies.

pharmacology

Mechanism of action

Givinostat inhibits histone deacetylase (HDAC) and several pro-inflammatory cytokines, thereby reducing tumor necrosis factor -α and the release of IL-1 -α, -β and IL-6 .

Givinostat reduces the concentration of Janus Kinase 2 , which means that the abnormal growth of the erythrocytes in polycythemia is reduced and an improvement in symptoms is observed.

literature

Committee for Orphan Medicinal Products: Public summary of opinion on orphan designation: Givinostat for the treatment of polycythaemia vera , www.ema.europa.eu , EMA / COMP / 834043/2009, 3 March 2010
C. Job-Deslandre: Idiopathic juvenile-onset systemic arthritis / Summary , www.orpha.net , Orphan number: ORPHA85414, January 2007

Individual evidence

↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
↑ Clinical study on the effectiveness in polycythemia vera patients
^ Leoni F, Fossati G, Lewis EC, et al. : The histone deacetylase inhibitor ITF2357 reduces production of pro-inflammatory cytokines in vitro and systemic inflammation in vivo . In: Molecular Medicine (Cambridge, Mass.) . 11, No. 1-12, 2005, pp. 1-15. PMID 16557334 . PMC 1449516 (free full text).

[NV-1] This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.

[2] Clinical study on the effectiveness in polycythemia vera patients

[pmid16557334-3] Leoni F, Fossati G, Lewis EC, et al. : The histone deacetylase inhibitor ITF2357 reduces production of pro-inflammatory cytokines in vitro and systemic inflammation in vivo . In: Molecular Medicine (Cambridge, Mass.) . 11, No. 1-12, 2005, pp. 1-15. PMID 16557334 . PMC 1449516 (free full text).