Bulevirtide (Myrcludex B) acetate is a viral particle entry inhibitor that blocks the hepatocyte entry pathway for viral particles, the hepatic sodium/taurine co-transport polypeptide (NTCP) receptor. It can be used in HBV and HDV infection studies.

METHODS: Bulevirtide (Myrcludex B) (50-200nM) was used to treat U2OS-HA-hNTCP cells, and plasma membrane-resident NTCP was labeled with biotin- or fluorescein isothiocyanate (FITC)-labeled Bulevirtide (Myrcludex B) and hNTCP overexpressing U2OS cells were used for timely Tracking. Förster resonance energy transfer was performed using fluorescence lifetime imaging microscopy to investigate whether Bulevirtide (Myrcludex B) could be transferred to newly synthesized NTCP.
RESULTS Bulevirtide (Myrcludex B) (50-200 nM, 24 h) binds NTCP by non-covalent binding and inhibits NTCP in a time- and dose-dependent manner, while transferring to newly synthesized NTCP molecules. [1]
METHODS: LS180 cells were treated with medium containing Bulevirtide (Myrcludex B) (0.5, 1, 5, and 10 µM) for 4 consecutive times for 4 consecutive days, and fluorescent substrates were used to detect overexpression of p -glycoproteins (P-gp, ABCB1), Breast Cancer Resistance Proteins (BCRP/ABCG2), and Organic Anion Transport Polypeptides 1B1 and 1B3 (OATP1B1/SLCO1B1 and OATP1B3/SLCO1B3) in cells inhibiting p -glycoprotein (P-gp, ABCB1), breast cancer resistance protein (BCRP/ABCG2).
RESULTS Bulevirtide (Myrcludex B) inhibited two uptake transporter proteins, OATP1B1 and OATP1B3, with IC50 values of 0.5 and 8.7 µM, respectively.[2]

METHODS: Mice were treated with Bulevirtide (Myrcludex B) (2.5 mg/kg) by a single subcutaneous injection, and 20 μl of blood was withdrawn to measure plasma bile acid levels.
RESULTS Peak plasma bile salt concentration was reached 4 hours after Bulevirtide (Myrcludex B) administration, and plasma bile salt levels were completely normalized 24 hours later, consistent with NTCP-mediated restoration of bile acid transport in vitro. [1]
METHODS: Humanized uPA/SCID mice were injected subcutaneously with 2 μg/g body weight of Bulevirtide (Myrcludex B) 3 days or 3 weeks after HBV inoculation, and the treatment duration was 3 or 6 weeks.
RESULTS Bulevirtide (Myrcludex B) effectively prevented virus transmission from initially infected human hepatocytes and also effectively blocked HBV transmission. [3]