Application of GSK2606414 and inhibitor for hepatitis B virus replication

By using GSK2606414 as a replication inhibitor of hepatitis B virus, the problem of existing drugs being unable to completely remove cccDNA and drug resistance was solved, and the significant inhibitory effect of hepatitis B virus was achieved, and good safety and clinical application potential were demonstrated.

CN120459107APending Publication Date: 2025-08-12THE FIRST AFFILIATED HOSPITAL OF GUILIN MEDICAL UNIVERSITY
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Patent Information

Application Number
CN202510750519.X
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-06-06
Publication Date
2025-08-12

AI Technical Summary

Technical Problem

Existing drugs for treating hepatitis B cannot completely remove the cccDNA virus database, which can easily lead to recurrence. Long-term medication can easily induce drug resistance mutations and have significant side effects of interferon, and the response rate is limited.

Method used

GSK2606414 is used as a highly selective PERK inhibitor to prepare an inhibitor of hepatitis B virus replication. By reducing the expression of HBsAg and HBeAg, it inhibits the levels of viral DNA and pgRNA and 2.4/2.1kb subunit RNA to prepare clinically acceptable pharmaceutical preparations.

Benefits of technology

It significantly inhibits the replication and expression of hepatitis B virus in vitro and in vivo, provides new treatment options, shows good safety and tolerance, and has the basis for further clinical transformation.

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Abstract

The invention relates to application of GSK2606414 and an inhibitor for hepatitis B virus replication, and relates to the technical field of biological medicines. The GSK2606414 is used for preparing an inhibitor for replication of the hepatitis B virus. The invention discovers and verifies that the GSK2606414 can obviously inhibit the replication and expression of the hepatitis B virus in vitro and in vivo for the first time, and provides an anti-HBV small molecule drug candidate with a practical application prospect; the GSK2606414 shows good safety and tolerance in animal experiments, has no obvious toxic and side effects, and has the basis of further clinical transformation; therefore, the invention provides a brand-new treatment thought for inhibiting the hepatitis B virus, and a new treatment choice can be provided for patients with drug resistance or ineffectiveness of existing antiviral drugs.
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Citation Information

Patent Citations

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    WO2021231788A1