Selective Androgen Receptor Modulator for Tissue-Selective Therapy
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Solution Overview
Problem
Current treatments for male contraception, androgen deficiency-related conditions, osteoporosis, muscle wasting, and hormone-related disorders lack effective and convenient options, with existing hormonal therapies having drawbacks such as frequent injections and side effects like supraphysiologic peak testosterone levels.
Innovation Solution
A pharmaceutical composition comprising a selective androgen receptor modulator (SARM) compound, represented by the structure of Formula S-(I) or its optical isomer, which acts as a partial agonist or antagonist, providing tissue-selective androgenic and anabolic effects for treating conditions like prostate cancer, osteoporosis, muscle wasting, and hormone-related disorders.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If testosterone esters are administered to treat androgen deficiency conditions, then androgenic effects are achieved, but supraphysiologic peak testosterone levels occur causing side effects
Solution Approach 1:
The invention changes the chemical structure parameters of the androgen compound by developing non-steroidal SARM compounds with modified molecular frameworks. This structural parameter change allows the compound to achieve androgenic effects without producing supraphysiologic peak testosterone levels, thereby resolving the side effect issue while maintaining therapeutic efficacy
Solution Approach 2:
The invention replaces the natural testosterone ester mechanism with an artificial SARM compound mechanism. Instead of using endogenous testosterone esters that cause supraphysiologic peaks, the patent introduces exogenous SARM compounds that bind to androgen receptors through a different molecular mechanism, achieving the desired androgenic effects without the harmful peak levels
2Reliability
If frequent injections are used to maintain therapeutic levels, then effective treatment is achieved, but patient convenience and compliance deteriorate
Solution Approach 1:
The invention implements periodic action through extended-release formulations and long-acting SARM compounds that maintain therapeutic levels over extended periods. This allows treatment to be administered less frequently (e.g., weekly or monthly injections rather than daily), maintaining therapeutic effectiveness while significantly improving patient convenience and compliance
Solution Approach 2:
The invention enables self-service through oral formulations of SARM compounds that can be easily self-administered without requiring medical professional intervention for injection. This self-administerable oral form maintains therapeutic effectiveness while dramatically improving ease of operation and patient autonomy
3Reliability
If steroid hormones are used to treat hormone-related conditions, then physiological effects are achieved, but cross-reactivity with other steroid receptors occurs
Solution Approach 1:
The invention applies local quality by designing SARM compounds with specific molecular features that enable selective binding to the androgen receptor while avoiding other steroid receptors. The compound structure is locally optimized with specific functional groups and spatial arrangements that create high affinity for AR but low affinity for ER, PR, and other steroid receptors, achieving both hormonal activity and receptor selectivity
Data Source
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AI summary
This invention provides a pharmaceutical composition comprising a compound of formula S-(I): or its isomer, pharmaceutically acceptable salt, pharmaceutical product, crystal, N-oxide, hydrate or any combination thereof, for use in treating or preventing breast cancer in a subject.