VX-222 (VCH-222, Lomibuvir)

Catalog No.S1480

VX-222 (VCH-222) is a novel, potent and selective inhibitor of HCV polymerase with IC50 of 0.94-1.2 μM, 15.3-fold less effective for mutant M423T, and 108-fold less effective for mutant I482L. Phase 2.

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VX-222 (VCH-222, Lomibuvir) Chemical Structure

VX-222 (VCH-222, Lomibuvir) Chemical Structure
Molecular Weight: 445.61

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Product Information

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Product Description

Biological Activity

Description VX-222 (VCH-222) is a novel, potent and selective inhibitor of HCV polymerase with IC50 of 0.94-1.2 μM, 15.3-fold less effective for mutant M423T, and 108-fold less effective for mutant I482L. Phase 2.
Targets HCV NS5B 1a [1] HCV NS5B 1b [1]
IC50 0.94 μM 1.2 μM
In vitro VX-222 binds to the thumb II allosteric pocket of the HCV RNA-dependent RNA polymerase. VX-222 exhibits non-competitive and selective inhibition in HCV NS5B of genotype 1a and 1b, with IC50 of 0.94 and 1.2 μM, respectively. VX-222 selectively inhibits the replication of subgenomic HCV genotype 1a and 1b with an EC50 of 22.3 and 11.2 nM, respectively. [1] Similarly, a recent study shows that VX-222 inhibits the 1b/Con1 HCV subgenomic replicon, with an EC50 of 5 nM. VX-222 preferentially inhibits primer-dependent RNA synthesis, showing only a modest or no effect on de novo-initiated RNA synthesis. [2]
In vivo In rats and dogs, VCH-222 displays fine pharmacokinetic profile, including low total body clearance and excellent oral bioavailability (greater than 30%) and good ADME properties. VCH-222 is biotransformed by several enzymes (CYP1A1, 2A6, 2B6, 2C8, CYP 3A4, UGT1A3) and is predicted to be actively transported in liver and excreted mainly intact in bile or as glucuronide adducts. [3]
Features A novel, potent and selective inhibitor of non-nucleoside polymerase, specifically the HCV RNA-dependent RNA polymerase.

Protocol(Only for Reference)

Kinase Assay: [1]

Anti-NS5B activity assay The inhibitory effect of VX-222 on HCV NS5B activity is measured by evaluating the amount of radiolabeled UTP incorporated by the C-terminal ∆21 truncated version of enzyme in a newly synthesized RNA using a homopolymeric RNA template / primer namely poly rA / oligo dT. Quantitative detection of incorporated radioactivity is done using a liquid scintillation counter. The in vitro kinetics of inhibition of HCV NS5B from genotype 1b strain BK by VX-222 are determined using the C-terminal ∆21 truncated version of NS5B. VX-222 (1 to 1.5 μM) is tested in the presence of 10 to 75 μM nonradioactive UTP mixed with 0.89 to 6.70 μCi of [α-33P]-labeled UTP. RNA-dependent-RNA polymerase reactions are allowed to proceed for 18 min at 22 °C.

Cell Assay: [2]

Cell lines Huh7.5 cells
Concentrations 0.01 nM -10 μM
Incubation Time 48 hours
Method Huh7.5 cells harboring HCV RNA replicons are trypsinized and plated into 48-well plates at a concentration of 4 × 104 cells/well. The next day the medium is changed and VX-222 is added in 200 μL of complete medium. After 48 hours, total RNA is extracted and viral RNAs are quantified by real-time reverse transcription-PCR (RT-PCR). The effective drug concentrations that reduced HCV RNA replicon levels by 50% (EC50) are calculated by nonlinear regression analysis with log curve fitting.

Animal Study: [3]

Animal Models Rats or dogs
Formulation Dissolved in 30% PEG
Dosages 5 mg/kg for rats or 10 mg/kg for dogs
Administration By oral gavage

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Bedard J, et al. J Hepatol, 2009, 50(Suppl 1), S340.

[2] Yi G, et al. Antimicrob Agents Chemother, 2012, 56(2), 830-837.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT01581138 Completed Chronic Hepatitis C Virus Vertex Pharmaceuticals Incorporated July 2012 Phase 2
NCT01516918 Completed Chronic Hepatitis C Virus Vertex Pharmaceuticals Incorporated February 2012 Phase 2
NCT01080222 Terminated Chronic Hepatitis C Virus Infection Vertex Pharmaceuticals Incorporated August 2010 Phase 2
NCT00958152 Completed Hepatitis C Vertex Pharmaceuticals Incorporated August 2009 Phase 1
NCT00911963 Completed Hepatitis C Vertex Pharmaceuticals Incorporated|ViroChem Pharma April 2009 Phase 1|Phase 2

Chemical Information

Download VX-222 (VCH-222, Lomibuvir) SDF
Molecular Weight (MW) 445.61


CAS No. 1026785-59-0
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 89 mg/mL (199.72 mM)
Ethanol 89 mg/mL (199.72 mM)
Water <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 2-Thiophenecarboxylic acid, 5-(3,3-dimethyl-1-butyn-1-yl)-3-[(cis-4-hydroxycyclohexyl)[(trans-4-methylcyclohexyl)carbonyl]amino]-

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