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Table 2 Details of the drug targeting epigenetic modifiers in endothelial cells

From: Epigenetics in blood–brain barrier disruption

Name of the drug Epigenetic enzyme altered by the drug Status of the clinical study/disease or condition
Trichostatin A Inhibits class I and II HDAC enzymes Clinical trial-completed (NCT03838926)/Relapsed or Refractory Hematologic Malignancies
Valproic acid/VPA Inhibits class I and class IIa HDACs Clinical trial-completed (NCT01233609)/ Retinitis Pigmentosa
Sodium butyrate/NaB Inhibits class I and class IIa HDACs Clinical trial-completed NCT00800930/ Shigellosis
Suberoylanilide hydroxamic acid/SAHA/Vorinostat Inhibits class I and II HDACs Clinical trial-completed (NCT00106626)/ Advanced Cancer
3-Deazaneplanocin-A /DZNep Inhibits EZH2 methyltransferase
Methylthioadenosine/MTA Inhibits H3K4 methylase Clinical trial-completed (NCT03083015)/ Necrotic Pulp
Morpholino Inhibits histone acetyltransferase 7/KAT7 Clinical trial-completed (NCT03375255)/ Muscular Dystrophy, Duchenne
Resveratrol/RV Activates sirtuin1/Sirt1 Clinical trial-completed (NCT01010009)/ Cognitive and Cerebral Blood Flow Effects of Resveratrol
Panobinostat/LBH589 Inhibits ClssI, II, and IV HDACs Clinical trial-completed (NCT00840346)/ Acute Myeloblastic Leukaemia
Entinostat/SNDX-275/MS 27–275 Inhibits HDAC1/3 Clinical trial- completed (NCT02897778)/Cardiac Safety Study With Advanced Solid Tumors
Mocetinostat Inhibits HDAC1 and HDAC2 Clinical trial-completed (NCT02303262)/ Metastatic Leiomyosarcoma
Lithium Inhibits GSK3b Clinical trial-completed (NCT01259388)/ Progressive Multiple Sclerosis
5-Aza-2′-deoxycytidine (5-dAzaC) Inhibits DNMT Clinical trial-completed (NCT00744757)/ Myelodysplastic Syndrome
GSK2879552 Inhibits LSD1 Terminated clinical trials Relapsed/Refractory Small Cell Lung Carcinoma
Tazemetostat Inhibits EZH2 (PRC2 subunit) Clinical trial-completed (NCT02860286)/ Relapsed or Refractory Malignant Mesothelioma
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