Breadcrumb
Novel Payloads for Antibody Drug Conjugates
Benefit
- Unique mechanism of action that results in antiproliferative and antiadhesive activity.
- Capability to overcome drug resistance in cancer treatment.
- Broad spectrum of anticancer activity, particularly against drug-resistance cancers, brain cancer, and triple-negative breast cancer.
- Potential applications include ADCs, bispecific antibody-drug conjugates, small-molecule drug conjugates, peptide-drug conjugates, and aptamer-drug conjugates.
Technology Description
Payload development presents significant challenges in the ADC field. Presently, only three types of compounds are used as payloads in FDA approved ADCs and their mechanisms of action are limited to microtubule inhibition, DNA alkylation, or topoisomerase inhibition. There is a pressing need for the development of additional ADC payloads with novel mechanisms of action.
Inspired by anticancer marine natural product superstolide A, Dr. Zhendong Jin at the University of Iowa is developing a novel class of compounds that can be used as ADC payloads and offer advantages over existing payloads. The new compounds have antiproliferative and antiadhesive effects on cancer cells, conferring the ability to penetrate solid tumors. They also can reverse drug resistance and are particularly active against cancers that lack effective drug therapy, such as brain cancer and triple-negative breast cancer. The compounds have IC50 values in the single-digit nM to sub-nM range, are metabolically stable and water-soluble, and contain a suitable handler for conjugation to antibodies via an ADC linker.
UIRF Case No. 2024-062
Stage of Development
This technology is in the preclinical stage. In vitro studies have been repeated in multiple cell lines, and continued preclinical research is underway. Our compounds are ready to be licensed for commercial applications.
IP Status: Patent Pending
Lead Researcher(s)
- Zhendong Jin, College of Pharmacy