Heteroconjugated disulfides of 2-mercaptoethane sulfonate sodium
Inventors
Hausheer, Frederick H. • Kochat, Harry • Huang, Qiuli
Assignees
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Publication Number
US-7829538-B2
Publication Date
2010-11-09
Expiration Date
Abstract
Novel compositions and formulations are disclosed that have use as toxicity-reducing agents for various chemotherapeutic agents and as treatment for certain diseases and conditions. The compositions of matter are amino acid and peptide heteroconjugated disulfides of 2-mercaptoethane sulfonate sodium.
Core Innovation
The invention relates to heteroconjugated disulfides of mesna for reducing chemotherapy-related toxicity. The compounds are defined by a structural concept corresponding to Formula I in which the composition includes an X—S—S—R1—R2 arrangement, where X includes a sulfur-containing amino acid or a 2 to 10 aa peptide, and R1 and R2 include lower alkylene and sulfonate or phosphonate features.
In the disclosed embodiments, X—S—S—R1—R2 includes specific X selections such as L-cysteine, DL-homocysteine, glutathione, cysteinyl glycine, and γ-glutamylcysteine to form corresponding mesna disulfides. The disclosure includes pharmaceutical compositions containing compounds of Formula I, including pharmaceutically acceptable salts and prodrugs, and it associates these compositions with reducing the toxicity of chemotherapeutic agents.
The document further describes methods of co-administering an effective dose of the disclosed Formula I compounds to patients receiving chemotherapeutic agents. Example chemotherapeutic agents mentioned include cisplatin, carboplatin, and paclitaxel, and the disclosed formulations include unit dosage forms such as hard gelatin capsules, tablets, suspensions, and an intravenous solution.
Claims Coverage
The provided independent claim contains core structural limitations defining a heteroconjugated mesna disulfide and an option for a pharmaceutically acceptable salt.
Compound defined by X—S—S—R1—R2 with L-cysteine
A compound to reduce the toxicity of a chemotherapeutic agent, where the compound has an X—S—S—R1—R2 structure with X—S being L-Cysteine, R1 being —(CH2)2—, and R2 being —P(O)(OH)2; or a pharmaceutically acceptable salt thereof.
The claim coverage is limited to a specific Formula I-type mesna heteroconjugated disulfide structure with X—S as L-cysteine, including defined R1 and R2 groups, and explicitly permits pharmaceutically acceptable salts.
Stated Advantages
Reduces the toxicity of a chemotherapeutic agent.
Documented Applications
Co-administration to patients receiving chemotherapeutic agents to reduce chemotherapy-related toxicity.
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