New US Patent Protects Key Element of First-in-Class Prodrug Candidate for Triple Negative Breast Cancer

Tumor-targeting and tumor-penetrating peptide enables EnduRx Pharmaceuticals novel prodrug for triple-negative breast cancer

On June 2, 2020 the US Patent and Trademark Office issued US Patent 10,669,311: Targeted Delivery Systems and Methods of Use Therefor to the Sanford Burnham Prebys Medical Discovery Institute of San Diego. The allowed claims relate to a molecule that incorporates a short amino acid sequence AKRGARSTA, also known as LinTT1, that selectively homes to solid tumors. The patent is exclusively licensed to EnduRx Pharmaceuticals, a business unit of OBDURO Biotechnologies.

Under an aggregate $1.75MM grant from the DoD CDMRP Breast Cancer program, OBDURO business unit EnduRx is collaborating with Dr. Naoto Ueno’s breast cancer team at The University of Texas MD Anderson Cancer Center, Houston to develop a novel therapeutic for triple-negative breast cancer and advance it to the point of pre-IND meeting. The prodrug candidate utilizes the LinTT1 tumor-targeting peptide.

“Triple negative breast cancer represents about 20% of breast cancers, but the proportion of African American women diagnosed is significantly higher,” said OBDURO/EnduRx Chief Medical Officer Stephan Morris MD who is Principal Investigator on the grant. “Receptors that enable treatment with drugs like Herceptin® (trastuzumab) are not present in this tumor type. Standard of care utilizes chemotherapy and surgery, with pathological complete response achieved in only 30-40% of cases. The non-responding patients progress, often with metastases to the brain and bones,” Morris said.

An antibody-drug conjugate topoisomerase inhibitor, Trodelvy® (sacituzumab govitecan-hziy), was recently approved for treatment of metastatic triple negative breast cancer, and immunotherapies Tecentriq® (atezolizumab) and Keytruda® (pembrolizumab) have each received approval or are reporting encouraging results in clinical trials.

“Even with these encouraging developments, there remains a large unmet need for effective therapies against this type of breast cancer,” Morris pointed out.

“A proprietary advanced nanoparticle delivery system that is simpler to manufacture than biologics, our first-in-class prodrug candidate targets a protein that is over-expressed on the surface of tumor cells and tumor-associated cells,” said OBDURO/EnduRx Chief Science Officer Sonke Svenson PhD. “The prodrug is rapidly distributed intra-tumorally, enabling cell internalization of an agent that induces apoptosis. Multivalent binding of the prodrug greatly improves effectiveness of delivery and is expected to increase the therapeutic window,” Svenson said.

“In mouse models of breast cancer, a prototype showed tumor volume reduction of over 90%, and some cures. The prodrug mechanism of action is orthogonal to existing drugs and offers clinicians a new tool to address drug resistance. The active agent is unable to internalize into cells of healthy tissues, so fewer adverse off-target effects are expected,” Morris explained.

“Following achievement of in-vitro milestones later this year, we intend to initiate a pipeline expansion,” said David Loynd, CEO of OBDURO/EnduRx. “We plan to utilize elements of our drug delivery system to demonstrate improved intra-tumoral distribution of selected approved chemotherapy agents, potentially extending or reviving patent protection for the pharmaceutical companies that choose to partner.”

About the Congressionally Directed Medical Research Programs:
For more information about CDMRP go to The views expressed in this article are those of the author and may not reflect the official policy or position of the Department of the Army, Department of Defense, or the U.S. Government.

For further information:

David Loynd
President & CEO EnduRx Pharmaceuticals Inc.
(855) 358-2878
Cell (520) 349-2455

Posted in AZBio News.