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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