1. Anti-infection Epigenetics
  2. Small Interfering RNA (siRNA) HBV
  3. Elebsiran

Elebsiran (VIR-2218) is a siRNA that targets and degrades hepatitis B virus (HBV) and hepatitis D virus (HDV) RNA transcripts. Elebsiran leads to a significant decrease in HBV surface antigen (HBsAg) and a reduction in viral load. Elebsiran binds to the sialic acid-depleted glycoprotein receptor (ASGPR) on the surface of liver cells through the GalNAc ligand, achieving liver-targeted delivery and demonstrating improved liver safety. Elebsiran can be used for the study of chronic HBV/HDV infections.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Elebsiran sodium) that retains the same biological activity.

For research use only. We do not sell to patients.

Elebsiran

Elebsiran Chemical Structure

CAS No. : 2648009-64-5

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Description

Elebsiran (VIR-2218) is a siRNA that targets and degrades hepatitis B virus (HBV) and hepatitis D virus (HDV) RNA transcripts. Elebsiran leads to a significant decrease in HBV surface antigen (HBsAg) and a reduction in viral load. Elebsiran binds to the sialic acid-depleted glycoprotein receptor (ASGPR) on the surface of liver cells through the GalNAc ligand, achieving liver-targeted delivery and demonstrating improved liver safety. Elebsiran can be used for the study of chronic HBV/HDV infections[1][2][3].

In Vitro

Elebsiran (0.1 pM-100 nM) effectively reduces HBsAg and the infectivity of HDV, and when combined with Tobevibart (HY-P990015) for treatment, it shows an additive effect[1].
Elebsiran exhibits comparable antiviral activity to ALN-HBV in HepG2.2.15 cells but its cytotoxicity is significantly reduced[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics[2]
Species Dose Route Indicator value
Monkey 10 mg/kg s.c. Tmax 24 h
Rat 10 mg/kg s.c. Tmax 7 h
Monkey 10 mg/kg s.c. Cmax 135000 ng/g
Rat 10 mg/kg s.c. Cmax 97000 ng/g
Monkey 10 mg/kg s.c. AUClast 37200000 h·ng/g
Rat 10 mg/kg s.c. AUClast 6610000 h·ng/g
Monkey 10 mg/kg s.c. T1/2 160 h
Rat 10 mg/kg s.c. T1/2 93.1 h
In Vivo

Elebsiran (9 mg/kg, s.c., single dose) possess antiviral activity against HBV and HDV in mice[1].
Elebsiran (12-100 mg/kg, s.c., 5 doses on Days 0, 21, 28, 35, and 42) does not cause a significant increase in ALT in all dosage groups and demonstrates high liver safety in mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: HBV/HDV-coinfected liver-chimeric model established in liver-chimeric mice[1]
Dosage: 9 mg/kg alone or with 15 mg/kg muHBC34 (the murinized version of Tobevibart)
Administration: Subcutaneous injection (s.c.), single dose
Result: Significant decreased of 0.6 log for HBsAg, 0.5 log for HBV DNA and 0.7 log for HDV RNA compared to the vehicle control on day 14 post-treatment.
Led to the strongest reductions in HBsAg, HBV DNA and HDV RNA levels relative to the vehicle group with muHBC34.
Animal Model: Chimeric mouse model established male PXB mice at 12 to 18 weeks[3]
Dosage: 12 mg/kg, 36 mg/kg, and 100 mg/kg
Administration: Subcutaneous injection (s.c.), on Days 0, 21, 28, 35, and 42
Result: Observed a clear dose-dependent increase in hALT1 levels, whereas no relationship between hALT1 and dose level.
Clinical Trial
Molecular Weight

14976.67

Formula

C485H618F9N158Na40O294P39S6

CAS No.
SMILES

[Elebsiran]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Elebsiran
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