On December 7, 2015 CytRx Corporation (NASDAQ: CYTR), a biopharmaceutical research and development company specializing in oncology, reported that it has selected its next drug, designated DK049, for clinical development in 2016 (Press release, CytRx, DEC 7, 2015, View Source [SID:1234508465]).

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DK049 was created using CytRx’s novel LADR (Linker-Activated Drug Release) technology that allows the drug to bind to albumin in the body’s bloodstream and controls its release at the site of the tumor. The LADR technology used with DK049 employs a two-stage linker that utilizes both pH sensitivity and acts enzymatically to allow release of its cytotoxic drug payload which extends the duration of exposure in tumors. Prolonged inhibition of tumor growth has been demonstrated in human tumor xenograft models of pancreatic cancer, non-small cell lung cancer and ovarian cancer at doses that lack apparent toxicity. As an example of the LADR technology’s capability, human ovarian tumor xenograft models received 85% less drug than a known chemotherapy comparator, yet at the end of the study, DK049-treated tumors were an average 13 times smaller than the chemotherapy-treated animals. These data have been submitted for presentation at the American Association of Cancer Research Annual Meeting in April 2016. Additionally, CytRx has applied for patents for both its LADR technology and DK049 itself.

"We believe that our LADR technology is the next advancement in linker-controlled drug release to be used with both antibody-drug conjugates and albumin-binding approaches, " commented Dr. Felix Kratz, Vice President of Drug Discovery at CytRx. "The ability to adjust the structure and composition of our linkers allows CytRx to attach a variety of lethal agents that include modified standard chemotherapies as well as highly potent agents currently used in antibody-drug conjugates."

"In only its first year, our Drug Discovery Group has created a technology that is capable of providing CytRx with a clinical pipeline for years to come," said Steven A. Kriegsman, Chairman and CEO of CytRx Corporation. "Their creation of DK049 was accomplished very rapidly due to the intelligent drug design and experience of Dr. Kratz’s group. We are confident that their progress with the LADR technology will be a key value driver for CytRx in the future."

CytRx’s LADR technology has several advantages over current linkers:

It allows prolonged drug exposure with accumulation at the site of the tumor.
The linker reduces drug release in healthy cells.
The controlled release allows delivery of payloads that are 10-1000 times more potent than standard chemotherapies.
The LADR conjugates can evade traditional drug resistance mechanisms.