LTK Inhibitor Compound for CLIP1-LTK Fusion-Positive Solid Tumors

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Solution Overview

Problem

Current treatments for lung cancer, particularly for tumors driven by the CLIP1-LTK fusion, lack effective small molecule inhibitors, and there is a need for targeted therapeutic options beyond well-known targets like EGFR and ALK.

Innovation Solution

The development of N2-(4-(4-(dimethylamino)piperidin-1-yl)-2-methoxyphenyl)-N4-(2-(isopropylsulfonyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine, which demonstrates significant inhibitory effects on LTK tyrosine kinase and tumor growth in animals with the CLIP1-LTK fusion protein.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional targeted therapies for well-known targets (EGFR, ALK) are used, then treatment effectiveness is improved for those specific targets, but treatment options are limited for tumors without these targets or with rare targets like CLIP1-LTK

Engineering Contradiction:

Improvetreatment effectivenessVSAvoidtreatment coverage

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The compound N2-(4-(4-(dimethylamino) piperidin-1-yl)-2-methoxyphenyl)-N4-(2-(isopropylsulfonyl) phenyl)-7H-pyrrolo[2,3-d] pyrimidine-2,4-diamine is designed to target multiple tyrosine kinases including LTK, ALK, and RET, enabling a single agent to address multiple rare targets that were previously unaddressed by conventional therapies focused on EGFR and ALK alone

Inventive Principle:

Principle #6Universality (Multi-functionality)

2Adaptability or versatility

If small molecule inhibitors are developed for rare targets like CLIP1-LTK, then treatment options for fusion-positive tumors are expanded, but there is a lack of proven effective inhibitors for these rare targets

Engineering Contradiction:

Improvetreatment options for rare targetsVSAvoidefficacy of inhibitors

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

The compound demonstrates nanomolar potency (IC50 values in the low nanomolar range) against LTK, ALK, and RET kinases, representing a significant improvement in binding affinity and selectivity parameters compared to existing inhibitors for these rare targets, thereby providing reliable efficacy where none previously existed

Inventive Principle:

Principle #35Parameter changes

3Measurement precision

If targeted therapy is pursued for CLIP1-LTK fusion-positive tumors, then precise treatment is achieved, but there are few reports on small molecule inhibitors and insufficient research results to confirm the fusion as the next target

Engineering Contradiction:

Improvetarget identification accuracyVSAvoidavailability of inhibitor compounds

Core Design Contradiction:

Measurement precisionVSQuantity of substance

Solution Approach 1:

The compound has been pre-developed and characterized with demonstrated inhibitory activity against LTK, ALK, and RET kinases before clinical validation, providing a ready-to-use therapeutic agent that addresses the shortage of available inhibitors while the precision of CLIP1-LTK as a target is being confirmed in ongoing research

Inventive Principle:

Principle #10Preliminary action

Data Source

PatentUS20260034133A1Use of pharmaceutical compound in the treatment of solid tumors

Publication Date: 2026.02.05 SHOUYAO HOLDINGS (BEIJING) CO LTD

AI summary

This invention is in the field of pharmaceutical technology, and discloses the use of a pharmaceutical compound in the treatment of solid tumors, the compound is N2-(4-(4-(dimethyl amino)piperidin-1-yl)-2-methoxyphenyl)-N4-(2-(isopropylsulfonyl)phenyl)-7H-pyrrolo[2,3-d] pyrimidine-2,4-diamine, which can be used to treat CLIP1-LTK fusion-positive tumors, including non-small cell lung cancer.