Oral composition containing an Lp(a) inhibitor compound

An oral composition with Lp(a) inhibitor compounds, histidine, and a bulking agent reduces nitrosamine formation, addressing the need for effective cardiovascular treatment without carcinogenic impurities.

JP2026086465AInactive Publication Date: 2026-05-26ELI LILLY & CO
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Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
ELI LILLY & CO
Filing Date
2026-01-20
Publication Date
2026-05-26
Estimated Expiration
Not applicable · inactive patent

AI Technical Summary

Technical Problem

Current treatments for elevated lipoprotein(a) levels, a risk factor for cardiovascular diseases, lack effective oral drug options and often result in the formation of potentially carcinogenic nitrosamines, necessitating a composition with reduced nitrosamine levels without affecting stability or disintegration time.

Method used

An oral composition containing an Lp(a) inhibitor compound, histidine, and a bulking agent with a small amount of nitrite, which minimizes nitrosamine formation and maintains stability and disintegration properties.

Benefits of technology

The composition effectively reduces nitrosamine levels to less than 50 ppm, ensuring safety while maintaining the stability and disintegration properties of the oral formulation.

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Patent Text Reader

Abstract

The present invention provides an oral composition for the treatment of cardiovascular disease, comprising an Lp(a) inhibitor compound. [Solution] The following crystalline hydrated Lp(a) inhibitor compound JPEG2026086465000035.jpg60160 A crystalline hydrated Lp(a) inhibitor compound is provided, wherein m is a number from about 0.33 to about 10. The compound is preferably mubaraprin hydrate (form A). An oral composition comprising the compound is also provided, wherein the oral composition is preferably histidine.
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