Small-Molecule FSHR Modulators for Oral Fertility Treatment

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Solution Overview

Problem

The use of FSH in infertility treatments is limited by its high cost, lack of oral dosing, and need for extensive monitoring, necessitating the development of low molecular weight hormone mimetics that can selectively modulate FSHR for oral administration.

Innovation Solution

Development of non-peptidic small molecule FSH modulators, represented by compounds of Formula (I) and their pharmaceutically acceptable salts, which selectively modulate FSHR with potential for oral administration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If FSH (urine-derived or recombinant) is used for ovulation induction and controlled ovarian hyperstimulation, then effective follicle development and oocyte harvesting can be achieved, but the treatment cost becomes high and requires parenteral administration with extensive monitoring

Engineering Contradiction:

Improveeffectiveness of follicle developmentVSAvoidcost and administration convenience

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The invention changes the molecular weight parameter of FSH from large (28-38 kDa) to small (low molecular weight), transforming it from a peptide/protein structure to a small molecule structure. This parameter change enables oral administration while maintaining FSHR modulatory activity, eliminating the need for parenteral injection and extensive monitoring

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The invention creates small molecule copies or mimetics that replicate the biological activity of native FSH. These small molecule FSH modulators copy the essential function of binding to and modulating FSHR receptors, providing the same therapeutic effect as native FSH but with improved pharmacokinetic properties including oral bioavailability

Inventive Principle:

Principle #26Copying

2Reliability

If FSH (large peptide/protein hormone) is administered, then receptor binding and biological activity are achieved, but oral dosing is not possible requiring parenteral administration

Engineering Contradiction:

Improvereceptor binding activityVSAvoidroute of administration

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The invention fundamentally changes the molecular size and chemical structure parameters of FSH from large peptide/protein to small molecule. This parameter transformation confers oral stability and absorption capability while preserving the essential receptor binding activity through careful design of small molecule structures that maintain key pharmacophoric features

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The invention replaces the mechanical injection administration system with an oral dosing system. By transforming FSH into small molecules with appropriate pharmacokinetic properties, the invention substitutes parenteral administration (injection) with oral administration, dramatically improving ease of operation and patient compliance

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

Data Source

PatentUS20260008783A1Modulators of FSHR and uses thereof

Publication Date: 2026.01.08 GEDEON RICHTER

AI summary

Disclosed herein are novel FSH modulator compounds, formulations thereof, and methods of treating diseases by administration of one or more novel FSH modulator compounds.