Fulvestrant prodrug

Fulvestrant prodrugs with enhanced water solubility address the low bioavailability and administration challenges of fulvestrant, offering improved treatment efficacy and patient comfort.

JP7653092B2Active Publication Date: 2025-03-28KASHIV BIOSCIENCES LLC
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Patent Information

Application Number
JP2023191446
Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
Priority Date
2018-12-18
Filing Date
2023-11-09
Publication Date
2025-03-28
Estimated Expiration
2039-05-24

AI Technical Summary

Technical Problem

Fulvestrant, a treatment for hormone receptor-positive metastatic breast cancer, faces challenges due to its low solubility and bioavailability, leading to poor release profiles and painful injections when administered intramuscularly.

Method used

Development of fulvestrant prodrugs with improved water solubility, achieved by introducing substituents into the phenolic hydroxyl group, which enhances bioavailability and allows for easier administration.

Benefits of technology

The fulvestrant prodrugs exhibit significantly higher water solubility, leading to improved bioavailability and potentially more effective treatment regimens with reduced dosing frequency and improved patient comfort.

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Abstract

To provide pharmaceutical compositions of fulvestrant prodrugs.SOLUTION: The present invention provides pharmaceutical compositions comprising at least one of fulvestrant prodrugs of formula II, enantiomers, diastereomers, racemates, pharmaceutically acceptable salts and solvates thereof, and pharmaceutically acceptable excipients.SELECTED DRAWING: None
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