HBVPRES/2-48CONS-MYR (known as Bulevirtide or Myrcludex B) was developed as an agent bind and inactivate the hepatocyte surface protein sodium taurocholate cotransporting polypeptide (SLC10A1 or NTCP). By blocking NTCP, the drug misdirects hepatitis B virus (HBV) and co-infecting hepatitis D virus (HDV) to an unproductive pathway and thereby prevents infection of the cell. Because NTCP is involved in the bile acid transport cycle, the blockade of this target by myrcludex B can potentially be used for the treatment of various metabolic and inflammatory diseases. Myrcludex B is going to participate in phase 3 trial for patients with chronic hepatitis D, however, the study is not yet recruited. The drug successfully completed phase II clinical trial for the patients with chronic hepatitis B and D. In addition, myrcludex B has been studied during preclinical research as a potential treatment of dyslipidemias, non-alcoholic steatohepatitis; primary biliary cirrhosis.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| The NTCP-inhibitor Myrcludex B: Effects on Bile Acid Disposition and Tenofovir Pharmacokinetics. | 2018-02 |
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| First-in-human application of the novel hepatitis B and hepatitis D virus entry inhibitor myrcludex B. | 2016-09 |
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| Treatment of chronic hepatitis D with the entry inhibitor myrcludex B: First results of a phase Ib/IIa study. | 2016-09 |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT03852719
subcutaneously for 48 weeks at a dose of 2 mg or 10 mg once daily
Route of Administration:
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FDA ORPHAN DRUG |
470915
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MYRCLUDEX B
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admin on Tue Apr 01 19:26:30 GMT 2025 , Edited by admin on Tue Apr 01 19:26:30 GMT 2025
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PRIMARY | Myrcludex B is an experimental drug for the treatment of hepatitis B and D. The first Phase IIa clinical trials with 40 patients concluded in 2014, finding that the drug was well tolerated and, as far as can be said with the limited data, effective against hepatitis B.Mechanism of action:The hepatitis B virus uses its surface lipopeptide pre-S1 for docking to mature liver cells via their sodium/bile acid co-transporter (NTCP) and subsequently entering the cells. Myrcludex B is a synthetic N-acetylated pre-S1 that can also dock to NTCP, blocking the virus's entry mechanism.The drug is also effective against hepatitis D because the hepatitis D virus is only infective in the presence of a hepatitis B virus infection. | ||
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ACTIVE MOIETY