Table 1.

Inhibitors targeting HBV transcription.

Substance	Property	Target	Clinical Status	IC50 HBV Transcription	Inventor	Reference
IFN-α	Cytokine	STAT1/2,histones	Approved	180 μg/week 1500 IU/mL	Merck 2	[110,111]
rIL-6	Cytokine	STAT3,HNF1α/4α	Preclinical	20 ng/mL	n/a	[112,113]
TGF-β	Cytokine	HNF4α,AID	Preclinical	10 ng/mL	n/a	[114,115,116]
Tazarotene(Tazorac)	Small molecule	RARβ/γ	Approved 3	20–75 nM	Allergan	[117]
Tamibarotene(Am80)	Small molecule	RARα	Approved 3	≈1 nM	Nippon Shinyaku	[118]
Isotretinoin(Accutane)	Small molecule	RAR/RXR	Approved 3	1.2 μM	Roche	[119]
Bexarotene(Targretin)	Small molecule	RXRα	Approved 3	1–5 μM	Ligand Pharma	[120]
GW4064	Small molecule	FXRα	Preclinical	0.2 μM	GSK	[121,122]
EYP001	Small molecule	FXR	Phase II	1.25–2.5 μM	Enyo Pharma	[123]
T0901317	Small molecule	LXRα/β	Preclinical	0.3–3 μM	Merck	[124]
GW3965	Small molecule	LXRα/β	Preclinical	0.3–3 μM	GSK	[124]
MLN4924	Small molecule	NAE1	Phase II/III 3	290 nM	Takeda	[125,126,127]
Nitazoxanide	Small molecule	HBx-DDB1	Approved 3	20 μM	Romark Lab.	[128,129]

¹ Dose for patients according to the AASLD guideline in 2016. ² Referring to in particular Intron A (IFN-α-2b). ³ Approved for administrations other than chronic HBV infection. IC₅₀: half maximal inhibitory concentration in in vitro models; IFN: interferon; IL: interleukin; STAT: signal transducer and activator of transcription; TGF: tumor growth factor; HNF: hepatic nuclear factor; AID: activation-induced cytidine deaminase; RAR: retinoic acid receptor; RXR: retinoid X receptor; FXR: farnesoid X receptor; LXR: liver X receptor; NAE1: NEDD8-activating enzyme 1; DDB1: DNA-damage binding protein 1. GSK: GlaxoSmithKline. n/a: not applicable.