Fused Ring ADC Conjugates for Potent Tumor-Targeted Drug Delivery

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Solution Overview

Problem

Current ADC drugs face challenges such as low potency of murine antibodies, narrow therapeutic windows, and issues with drug loading rates, limiting their effectiveness in treating various cancers.

Innovation Solution

A novel fused ring compound conjugate is developed, comprising a targeting moiety (Tp), a chemical bond or linker (L), and a group (G) with specific structural components to enhance the delivery and release of cytotoxic drugs to tumor cells, improving pharmacodynamic activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If murine antibodies are used in first-generation ADC drugs, then the ADC structure can be formed to deliver cytotoxic drugs to tumor cells, but the cytotoxicity is not potent enough and the therapeutic effect is limited

Engineering Contradiction:

Improvetherapeutic effectivenessVSAvoidcytotoxicity potency

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent changes the key parameter of antibody type from murine to humanized or human antibodies, which improves the therapeutic effectiveness by reducing immunogenicity and increasing potency while maintaining the ADC structure and mechanism

Inventive Principle:

Principle #35Parameter changes

2Adaptability or versatility

If the drug loading rate is increased to improve cytotoxicity, then the potency increases, but the therapeutic window becomes narrower

Engineering Contradiction:

Improvecytotoxicity potencyVSAvoidtherapeutic window

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

The patent applies local quality by designing a targeted delivery system where the cytotoxic drug is selectively delivered to tumor cells expressing specific antigens, allowing high drug concentration at the target site (improving potency) while maintaining lower systemic exposure (preserving therapeutic window)

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The patent uses a specific linker as an intermediary to connect the antibody to the cytotoxic drug, enabling controlled drug release at the target site through lysosomal degradation, which maintains high local potency while protecting systemic circulation

Inventive Principle:

Principle #24Intermediary (Mediator)

3Adaptability or versatility

If the antibody is designed to target low-expressed antigens to expand applicability, then the versatility increases, but the delivery efficiency and cytotoxicity decrease

Engineering Contradiction:

Improvetarget antigen diversityVSAvoiddelivery efficiency

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

The patent changes the parameter of antibody type to humanized or human antibodies with higher affinity and specificity, which improves delivery efficiency by enhancing binding strength to target antigens, enabling effective targeting even of low-expressed antigens

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS20260001891A1Fused ring compound, conjugate thereof and use thereof

Publication Date: 2026.01.01 CHENGDU CONMED BIOSCI CO LTD

AI summary

The present disclosure relates to a fused ring compound, a conjugate thereof and the use thereof. The compound and the conjugate of the present disclosure have good activity of inhibiting tumor cells, stability, and in vivo drug efficacy in animals.