Transforming suboptimized drugs to prodrugs
with improved safety and efficacy
Our goal is to improve the physicochemical, biopharmaceutical, and/or pharmacokinetic properties of parent drugs to create new medicines with peak performance and clinical utility.
For more than 100 years, prodrug technology has been successfully utilized to develop therapeutics and treat patients; many widely used pharmaceuticals are, in fact, prodrugs.
A prodrug is an inactive precursor of a drug that becomes pharmacologically active in the body by normal metabolic conversion mainly through enzymatic or chemical action. Prodrugs are used when certain active drugs have unattractive ADME (Absorption, Distribution, Metabolism, and Excretion) properties, e.g., poor drug permeability or poor tolerability. A prodrug can improve the safety and efficacy of an approved drug. Prodrugs are formed from reversible linkages to active drugs. Formation of an ester is an example of a prodrug methodology for modification of a functional group of the active drug to improve lipophilicity for passive membrane transport or to increase aqueous solubility. About 10% of drugs approved worldwide can be classified as prodrugs. Notable examples of prodrugs are acetylsalicylic acid (aspirin), levodopa, sofosbuvir, lisdexamfetamine, simvastatin, and omeprazole. A prodrug may be characterized as a new chemical entity (NCE) if the drug contains no active moiety that has been previously approved by the FDA, or a 505(b)(2) if the parent drug has already been approved. Both NCEs and 505(b)(2)s are subject to exclusivity as per FDA guidelines.
Kashiv BioSciences is developing a prodrug of an injectable cancer drug that can be orally active in pill form. The program is in an early development stage.