Compounds and methods for reducing undesired toxicity of chemotherapeutic agents

Inventors

Hausheer, Frederick H. • Kochat, Harry • Huang, Qiuli

Assignees

Lantern Pharma Inc

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Publication Number

US-7829117-B2

Patent

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 disclosure provides toxicity-reducing compounds for chemotherapeutic regimens in which the compound is X—S—S—R1—R2. In the disclosed structure, X is a polystyrene resin of 200–400 mesh size, R1 is —(CH2)2—, and R2 is —SO3− or —P(O)(OH)2, or a pharmaceutically acceptable salt thereof.

The problem addressed is reducing the toxicity of a chemotherapeutic agent during cancer chemotherapy. The disclosed compositions are directed to toxicity reduction associated with chemotherapeutic agents.

The disclosure further describes corresponding pharmaceutical formulations and administration methods for using the X—S—S—R1—R2 compounds to reduce adverse toxicity during cancer chemotherapy. The described examples include heteroconjugated disulfides of mesna and specific disulfide embodiments formed to provide the stated toxicity-reducing effect.

Claims Coverage

The document provides one independent claim with a defined compound structure intended to reduce toxicity of a chemotherapeutic agent, comprising three inventive elements: a polystyrene resin X of specified mesh size, a specified linker R1, and a specified R2 sulfonate or phosphonate group (or a pharmaceutically acceptable salt).

Resin-bound heteroconjugated disulfide structure for toxicity reduction

A compound to reduce the toxicity of a chemotherapeutic agent, wherein the compound is X—S—S—R1—R2.

Polystyrene resin X of 200–400 mesh size as the heteroconjugate anchor

X is a polystyrene resin of 200–400 mesh size.

Specified linker and sulfonate/phosphonate R2 group

R1 is —(CH2)2— and R2 is —SO3− or —P(O)(OH)2; or a pharmaceutically acceptable salt thereof.

Across the single independent claim, the inventive coverage centers on a toxicity-reducing X—S—S—R1—R2 compound for a chemotherapeutic agent, with X limited to polystyrene resin of 200–400 mesh size, R1 fixed to —(CH2)2—, and R2 fixed to a sulfonate or phosphonate group, including pharmaceutically acceptable salts.

Stated Advantages

Reduces the toxicity of a chemotherapeutic agent.

Reduces adverse toxicity during cancer chemotherapy.

Documented Applications

Cancer chemotherapy for toxicity reduction, including reduction of bladder toxicity associated with chemotherapy.

Inflammatory arthritis.

Inflammatory bowel disease.

Septic shock and ARDS.

Radiation exposure.

Toxic industrial chemicals.

Toxic agricultural chemicals.

Toxic military chemicals.

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