US Patent Issued for Compound that Delivers Taxotere Chemotherapy Directly into Tumors

US Patent Issued for Compound that Delivers Taxotere Chemotherapy Directly into Tumors

A U.S. patent has been issued for Rexahn Pharmaceuticals‘ RX-21101, a drug that allows the targeted delivery of the chemotherapy agent Taxotere (docetaxel) directly into tumor cells. This may improve the safety and effectiveness of Taxotere in a number of cancers, including prostate cancer.

“We are pleased to expand our intellectual property covering our unique and innovative targeting technologies in preclinical development. RX-21101 is the first proof of concept candidate from our Nano-Polymer-Drug Conjugate Systems (NPDCS),” Rexahn CEO Peter D. Suzdak, PhD, said in a news release.

“Our nanotechnology drug conjugate candidates address the large and immediate market for widely used chemotherapies, and they are a complement to our portfolio of proprietary compounds currently in clinical development,” he said.

In recent decades, researchers have been trying to come up with ways of increasing the specificity of chemotherapy agents, decreasing the lasting side effects that are often associated with such therapies.

Taxotere is a chemotherapy agent that is approved to treat breast, lung, prostate, and stomach cancer, as well as and head and neck cancers. But similar to other chemotherapy agents, it is designed to kill cells that divide quickly, affecting not only cancer cells but other healthy cells that are highly proliferative.

RX-21101, which was selected for preclinical development by the National Cancer Institute’s (NCI) Nanotechnology Characterization Laboratory in 2015, may be a possible treatment approach to decrease the side effects and improve the effectiveness of Taxotere.

The drug is a nano-polymer conjugate that links Taxotere to a molecule that targets tumor cells specifically. Once inside the cells, the compound is designed to be metabolized to free the chemotherapy agent.

This approach is believed to maximize the level of Taxotere in the tumor and minimize the levels of freely circulating Taxotere in the body, which may boost its anti-tumor activity and reduce the number and severity of adverse events. Preclinical studies suggest that RX-21101 may be more effective and better tolerated than Taxotere.

Rexahn has issued other patents covering nano-polymer conjugate systems, including the carboxypropyl-methacrylamide (CPMA) nano-polymer-drug conjugate platform. This platform may offer advantages over other existing conjugate systems, including high water solubility, higher bioavailability, and the possibility to bind several compounds to their chemical backbone.