RAD1901-2HCl Polymorph Control for Humidity-Stable Cancer Therapy

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Solution Overview

Problem

Existing treatments for metastatic breast cancer using RAD1901 face challenges in maintaining stability and efficacy due to the drug's sensitivity to humidity and conversion to different polymorphic forms, which can affect its therapeutic effectiveness.

Innovation Solution

The development of specific polymorphic forms of RAD1901-2HCl, including anhydrous Forms 1 and 2, and a hydrated Form 3, which exhibit enhanced stability under varying humidity conditions, along with methods to convert and preserve these forms for improved therapeutic efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of stationary object

If RAD1901 is stored under varying humidity conditions, then the drug can be preserved for use, but it converts to different polymorphic forms affecting therapeutic effectiveness

Engineering Contradiction:

Improvestorage stabilityVSAvoidpolymorphic form consistency

Core Design Contradiction:

Duration of action of stationary objectVSStability of the object's composition

Solution Approach 1:

The patent applies parameter changes by controlling storage conditions (temperature, humidity) to prevent polymorphic conversion. Specific storage parameters are established to maintain the drug in its active polymorphic form, thereby resolving the contradiction between storage duration and compositional stability

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent utilizes composite material approaches by formulating RAD1901 with specific excipients and in a particular polymorphic form that enhances stability. The composite formulation resists humidity-induced conversion, allowing long-term storage while maintaining therapeutic effectiveness

Inventive Principle:

Principle #40Composite materials

2Reliability

If polymorphic forms are converted for stability, then storage conditions are improved, but drug delivery consistency may be affected

Engineering Contradiction:

Improvestorage stabilityVSAvoiddrug delivery consistency

Core Design Contradiction:

ReliabilityVSProductivity

Solution Approach 1:

The patent applies preliminary action by pre-converting the drug to a stable polymorphic form before storage and distribution. This preliminary conversion ensures that the drug remains stable during storage while maintaining its therapeutic effectiveness and delivery consistency when administered

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The patent utilizes parameter changes by establishing specific conversion conditions (temperature, humidity, time) that transform the drug into a stable polymorphic form without compromising its bioavailability or therapeutic effect, thus resolving the contradiction between stability and delivery consistency

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS20260028309A1Polymorphic forms of RAD1901-2hcl

Publication Date: 2026.01.29 RADIUS PHARMACEUTICALS INC

AI summary

Various polymorphic forms of RAD1901-2HCl, including three crystalline and amorphous forms, are prepared and characterized. Uses of the various polymorphic forms of RAD1901-2HCl for cancer treatment are also disclosed.