Conjugated suramin amino compounds for medical conditions

Abstract

Provided is a modification of pharmacokinetics of suramin by use of amino compounds in modification of lipophilicity and protein binding characteristics for tackling the physico-chemical properties of suramin that gives it poor distribution in the body; formulating the resulting product in a form that leads to targeting body fluids like the lymphatic system when administered in a specific way; and determining the route of administration that maximizes targeting with a view to reducing the dosage so as to limit toxicity, hence increase tolerance by patient.

Description

technical field [0001] The present invention relates generally to improving the pharmacokinetics of suramin, and in particular to the use of amino compounds to improve lipophilicity and protein binding characteristics. Background technique [0002] Suramin was introduced in 1920 for the treatment of trypanosomiasis. The original formulation, which is the standard still used today, is in the form of the sodium salt which is prepared aseptically and dissolved in water just before injection. [0003] Over time, suramin has been tested in various conditions including cancer, HIV AIDS, immunomodulatory disorders. However, in all of these trials, suramin was not developed to clinical use because of various difficulties associated with its pharmacokinetics and toxicity. [0004] It is therefore an object of the present invention to form conjugates and derivatives of suramin having features which suitably reduce or eliminate these difficulties when formulated and administered. ...

AI Technical Summary

Problems solved by technology

All of this is compounded by high toxicity limiting long-term administration and poor distribution leading to limited availability of activity to specific sites

The poor profile results in the need to use high doses, which in turn increases toxicity

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