Novel Biocompatible Poly(Aspartamide) Based Drug Conjugates

Macromolecular prodrugs. XIII. Hydrosoluble conjugates of 17β-estradiol and estradiol-17β-valerate with polyaspartamide polymer.

Two hydrosoluble conjugates of 17β-estradiol (ED) and estradiol-17β-valerate (EV) with polyaspartamide polymer were prepared and characterized. ED and EV were first chemically modified and bound to poly[α,β-(N-2-hydroxyethyl-DL-aspartamide)]-poly[α,β-(N-2-aminoethyl-DL-aspartamide)] (PAHA), a hydrosoluble polyaspartamide-type copolymer bearing both hydroxyl and amino groups. ED was first conver...

Antibody–drug conjugates as novel anti-cancer chemotherapeutics

Over the past couple of decades, antibody-drug conjugates (ADCs) have revolutionized the field of cancer chemotherapy. Unlike conventional treatments that damage healthy tissues upon dose escalation, ADCs utilize monoclonal antibodies (mAbs) to specifically bind tumour-associated target antigens and deliver a highly potent cytotoxic agent. The synergistic combination of mAbs conjugated to small...

Antibody-Drug Conjugates as Novel and Potent Cancer Therapeutics

Conventional chemotherapeutic drugs to treat cancer suffers from the lack of selectivity towards the tumor site and thus causing damage to even healthy tissues. Drug dose escalation to therapeutically active levels is often impossible with chemotherapeutic drugs due to this toxicity. The selectivity of the treatment was improved with the introduction of monoclonal antibody drugs that are direct...

Development of Novel Quaternary Ammonium Linkers for Antibody-Drug Conjugates.

A quaternary ammonium-based drug-linker has been developed to expand the scope of antibody-drug conjugate (ADC) payloads to include tertiary amines, a functional group commonly present in biologically active compounds. The linker strategy was exemplified with a β-glucuronidase-cleavable auristatin E construct. The drug-linker was found to efficiently release free auristatin E (AE) in the presen...

targeted drug delivery to cancer stem cells by hyaluronic acid-based drug conjugates: synthesis and characterization