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Description

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.

Originator

Approval Year

Unknown
139594
PubMed

PubMed

TitleDatePubMed
First-in-human application of the novel hepatitis B and hepatitis D virus entry inhibitor myrcludex B.
2016 Sep
Treatment of chronic hepatitis D with the entry inhibitor myrcludex B: First results of a phase Ib/IIa study.
2016 Sep
The NTCP-inhibitor Myrcludex B: Effects on Bile Acid Disposition and Tenofovir Pharmacokinetics.
2018 Feb

Sample Use Guides

In Vivo Use Guide
subcutaneously for 48 weeks at a dose of 2 mg or 10 mg once daily
Route of Administration: Other
Name Type Language
MYRCLUDEX B
Common Name English
GLYCINE, N-(1-OXOTETRADECYL)GLYCYL-L-GLUTAMINYL-L-ASPARAGINYL-L-LEUCYL-L-SERYL-L-THREONYL-L-SERYL-L-ASPARAGINYL-L-PROLYL-L-LEUCYLGLYCYL-L-PHENYLALANYL-L-PHENYLALANYL-L-PROLYL-L-.ALPHA.-ASPARTYL-L-HISTIDYL-L-GLUTAMINYL-L-LEUCYL-L-.ALPHA.-ASPARTYL-L-PROLYL
Systematic Name English
HBVPRES/2-48MYR(C)
Common Name English
HBVPRES2-48MYR
Common Name English
HBVPRES/2-48CONS-MYR
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 470915
Created by admin on Sat Dec 16 12:34:18 GMT 2023 , Edited by admin on Sat Dec 16 12:34:18 GMT 2023
Code System Code Type Description
WIKIPEDIA
MYRCLUDEX B
Created by admin on Sat Dec 16 12:34:18 GMT 2023 , Edited by admin on Sat Dec 16 12:34:18 GMT 2023
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.
CAS
406461-66-3
Created by admin on Sat Dec 16 12:34:18 GMT 2023 , Edited by admin on Sat Dec 16 12:34:18 GMT 2023
PRIMARY
DRUG BANK
DB14853
Created by admin on Sat Dec 16 12:34:18 GMT 2023 , Edited by admin on Sat Dec 16 12:34:18 GMT 2023
PRIMARY
FDA UNII
JA8K50N04H
Created by admin on Sat Dec 16 12:34:18 GMT 2023 , Edited by admin on Sat Dec 16 12:34:18 GMT 2023
PRIMARY
ACTIVE MOIETY
MYRCLUDEX B
NIH
NCATS
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