Capsid Inhibitor and Nucleoside Combination for HBV Genotype Coverage

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Solution Overview

Problem

Current treatments for hepatitis B virus (HBV) infection, while available, lack effectiveness and diversity in addressing various genotypes and drug-resistant strains, necessitating new therapeutic agents that target the synthesis and degradation of nucleocapsids.

Innovation Solution

A pharmaceutical combination comprising a capsid protein inhibitor of formula I, or its pharmaceutically acceptable salt, in conjunction with entecavir or tenofovir, or their respective prodrugs and salts, administered in various dosages and formulations to treat HBV infection.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If nucleoside (nucleotide) drugs such as entecavir and tenofovir are used to inhibit HBV DNA replication, then viral replication is suppressed, but treatment effectiveness is limited against various genotypes and drug-resistant strains

Engineering Contradiction:

Improvetreatment effectivenessVSAvoidcoverage of genotypes and drug-resistant strains

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent combines a capsid protein inhibitor (compound of formula I) with a nucleoside reverse transcriptase inhibitor (entecavir or tenofovir) to create a pharmaceutical combination. This merging of two different mechanisms of action addresses both wild-type HBV and drug-resistant strains more effectively than either agent alone, resolving the contradiction between treatment reliability and adaptability to various genotypes and resistant strains

Inventive Principle:

Principle #5Merging (Combining)

2Adaptability or versatility

If new therapeutic agents targeting nucleocapsid synthesis and degradation are developed, then adaptability to various genotypes and drug-resistant strains is improved, but treatment complexity increases

Engineering Contradiction:

Improvecoverage of genotypes and drug-resistant strainsVSAvoidtreatment regimen complexity

Core Design Contradiction:

Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent merges a capsid protein inhibitor with a nucleoside reverse transcriptase inhibitor into a single pharmaceutical combination product. This combination approach provides broad-spectrum coverage against different HBV genotypes and drug-resistant strains while maintaining manageable treatment complexity through fixed-dose combination therapy

Inventive Principle:

Principle #5Merging (Combining)

Solution Approach 2:

The pharmaceutical combination is designed to be universally effective across multiple HBV genotypes and drug-resistant strains. The capsid protein inhibitor component provides multi-functional activity that enhances the universal applicability of the treatment regimen, addressing various viral variants with a single therapeutic approach

Inventive Principle:

Principle #6Universality (Multi-functionality)

Data Source

PatentUS20230404976A1Pharmaceutical combination containing capsid protein inhibitor and nucleoside analog

Publication Date: 2023.12.21 CHIA TAI TIANQING PHARMA GRP CO LTD

AI summary

A pharmaceutical combination containing a capsid protein inhibitor and a nucleoside analog, selected from entecavir or a pharmaceutically acceptable salt thereof or a solvate thereof, or tenofovir or a pharmaceutically acceptable salt or pharmaceutically acceptable prodrug thereof, as well as a use of said pharmaceutical combination in treating a hepatitis B virus infection. The pharmaceutical combination has a good hepatitis B virus infection-fighting effect.