Hepcludex
Hepcludex Uses, Dosage, Side Effects, Food Interaction and all others data.
Hepatitis D is considered the most severe type of viral hepatitis and leads to the rapid development of cirrhosis, severe decompensation of liver function, and an increased risk of mortality. Until recently, there have been extremely limited treatments available for Hepatitis D infection.
Hepcludex, also known as Hepcludex, is a first-in-class entry inhibitor for the treatment of chronic Hepatitis D infection developed by MYR Pharmaceuticals, now part of Gilead. It was first approved for use in the EU on May 28, 2020; bulevirtide has been granted PRIME scheme eligibility and Orphan Drug Designation by the European Medicines Agency. In the USA, bulevirtide has been granted Orphan Drug Designation and Breakthrough Therapy Designation. Due to potentially beneficial synergistic effects in treating chronic Hepatitis D, bulevirtide is also under investigation in clinical trial NCT03852433 (Phase 2b Study of Hepcludex With Peginterferon Alfa-2a) in Patients With CHD. Completion of this clinical trial is anticipated in early 2023.
Hepcludex prevents Hepatitis D entry into cells. It is effective in the reduction of Hepatitis D virus (HDV) RNA levels and improvement of liver inflammation in cases of Hepatitis D infection.
| Trade Name | Hepcludex |
| Generic | Bulevirtide |
| Bulevirtide Other Names | Bulevirtide |
| Type | |
| Protein binding | The plasma protein binding of bulevirtide is >99%, and it is primarily bound to albumin. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Hepcludex is a drug for the treatment of chronic Hepatitis D infection in adults with compensated liver disease.
Hepcludex is indicated for the treatment of chronic Hepatitis D infection in HDV-RNA positive adult patients with compensated liver disease.
Hepcludex is also used to associated treatment for these conditions: Hepatitis D
How Hepcludex works
The sodium taurocholate co-transporting polypeptide (NTCP) serves to transport bile acids in the sodium salt form to the liver from the portal circulation. It is an important component of enterohepatic circulation. The Hepatitis D virus replicates independently within liver cells but requires the hepatitis B surface antigen in order to propagate. Hepatitis B and D viruses enter hepatocytes through the binding of NTCP (sodium/taurocholate cotransporting polypeptide) to the Hepatitis B virus preS1 surface protein domain.
Hepcludex binds and subsequently inactivates the hepatitis B (HBV) and HDV receptors on hepatocytes. Hepcludex blocks the NTCP binding site, subsequently blocking the entry of the viruses into cells. This prevents viral entry and replication, reducing symptoms of Hepatitis D infection.
Toxicity
There are no reports of overdose with bulevirtide. In the case of an overdose, monitor the patient and provide supportive treatment.
Food Interaction
No interactions found.Volume of Distribution
The volume of distribution of bulevirtide is estimated to be lower than total body water. In animals, bulevirtide distributes into the liver, gastrointestinal tract, kidney, and bladder.
Elimination Route
Human pharmacokinetic data for bulevirtide is limited in the literature. In rats, bulevirtide administered by subcutaneous injection is rapidly absorbed with a Cmax of 4 to 6 hours. The estimated bioavailability is 85% in humans, and steady-state concentrations are expected to occur within weeks of initiating treatment. The AUC for bulevirtide after a 2mg subcutaneous dose was found to be approximately 46 ng/ml.h with a Tmax of 0.5 hours.
Half Life
The half-life of bulevirtide ranges between 4 and 7 hours in healthy adults.
Clearance
The clearance after of bulevirtide after subcutaneous administration (CL/F) in healthy volunteers ranged from 7.98 L/h (±2.02) to 62 L/h (±16.7), depending on the dose administered. The clearance of bulevirtide decreases as the dose increases.
Elimination Route
Elimination through target (NTCP) binding is expected to be the main route of elimination for bulevirtide. In healthy volunteers, bulevirtide was not found to be excreted in the urine.
Innovators Monograph
You find simplified version here Hepcludex
