KAT6 Inhibitor Dosing Regimens Balancing Efficacy and Adverse Events

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Solution Overview

Problem

There is a need for appropriate dosing regimens of the oral agent COMPOUND A, a potent and selective KAT6 inhibitor, to improve clinical efficacy in treating cancers while minimizing adverse events and risks to patients, particularly in cases of primary or acquired resistance to CDK4/6 inhibitors.

Innovation Solution

Dosing regimens for COMPOUND A, administered as a single agent or in combination with CDK4 inhibitors and antiestrogens, are provided, ranging from about 0.1 mg to about 15 mg daily, to enhance therapeutic benefits and patient convenience.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If COMPOUND A is administered at higher doses to improve cancer treatment efficacy, then clinical benefit is enhanced, but adverse events and patient risks increase

Engineering Contradiction:

Improveclinical efficacyVSAvoidadverse events

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by establishing specific dose ranges (0.1-15 mg daily) and administration schedules (once daily, with flexibility for missed doses) to optimize the balance between efficacy and safety. The dosing regimen parameters are carefully controlled to achieve therapeutic benefit while minimizing adverse events.

Inventive Principle:

Principle #35Parameter changes

2Ease of operation

If COMPOUND A is administered as a single agent to simplify treatment, then patient convenience is improved, but treatment efficacy may be reduced compared to combination therapies

Engineering Contradiction:

Improvepatient convenienceVSAvoidtreatment efficacy

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent establishes that COMPOUND A can be effectively administered as a single agent across multiple cancer types and treatment settings, providing universal applicability. The dosing regimen is designed to work independently without requiring combination therapies, simplifying patient management while maintaining efficacy through the compound's broad inhibitory activity against KAT6 enzymes in various cancer contexts.

Inventive Principle:

Principle #6Universality (Multi-functionality)

3Reliability

If dosing frequency is increased to improve tumor control, then treatment efficacy is enhanced, but patient convenience and quality of life deteriorate

Engineering Contradiction:

Improvetumor controlVSAvoidpatient convenience

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent implements periodic action through once-daily dosing schedules that maintain effective drug levels throughout the 24-hour cycle. The dosing is designed to be administered at convenient times (morning or evening) and can be adjusted based on patient needs, providing regular tumor control without burdening patients with frequent dosing requirements.

Inventive Principle:

Principle #19Periodic action

Data Source

PatentUS20260027087A1Dosing regimens comprising a KAT6 inhibitor for the treatment of cancer

Publication Date: 2026.01.29 PFIZER INC

AI summary

The invention relates to dosing regimens for the treatment of cancer comprising administering to a subject in need thereof a daily dose of a lysine acetyltransferase 6 (KAT6) inhibitor as a single agent or in combination with: a) a cyclin-dependent kinase 4 (CDK4) inhibitor; b) an antiestrogen; or c) a CDK4 inhibitor and an antiestrogen.