Lin BioScience said today it has exclusively licensed a microtubule-targeting agent to treat brain cancers from the University of Sydney.

The agent, LBS-002, is a blood–brain barrier permeable, small-molecule drug designed to disrupt the division of cancer cells by preventing the formation of microtubules.

While several current drugs used to target tubulin polymerization have been already shown to effectively treat breast and ovarian cancers and non-Hodgkin’s Lymphoma, those treatments are large molecules that cannot cross the protective blood–brain barrier, making them ineffective in treating brain cancer.

Lin BioScience reasons that LBS-0002 can fight epidermal growth factor receptor (EGFR) mutation cancers on which most forms of chemotherapy fail.

“LBS-002's ability to cross the blood–brain barrier enables it to overcome the permeability limitations experienced by traditional treatments, making it a promising therapeutic candidate,” Lin BioScience founder and CEO Tom Lin, M.D., Ph.D., MBA, said in a statement.

Lin BioScience has gained exclusive global rights to the development and commercialization of LBS-002-related intellectual property developed at University of Sydney by Lenka Munoz, Ph.D., and Michael Kassiou, Ph.D.

“Our research has passed the discovery stage and now our goal is to progress into clinical testing,” Drs. Munoz and Kassiou stated.

While the value of the licensing deal was not disclosed today, the University of Sydney said on March 14 that Lin BioScience had awarded Drs. Munoz and Kassiou a 12-month research funding grant of A$1.2 million (approximately $930,000) in December.

That announcement noted that the researchers had tested the potential of their small-molecule tubulin inhibitor by using experimental models of the most common and fatal primary brain tumor.

“We treated patient-derived glioblastoma cells with the molecule and found that it effectively killed cells. These results are extremely important as there are currently no effective drugs with blood–brain barrier permeability to treat glioblastoma,” Dr. Munoz said.

LBS-002 is one of four pipeline candidates of Lin BioScience. Its lead candidate LBS-008 is an oral dry age-related macular degeneration candidate being developed with Columbia University and the NIH.

LBS-008 is expected to enter Phase I trials this year, as is the company’s most advanced cancer candidate LBS-007, a CDC7 inhibitor being developed in collaboration with Columbia University, Memorial Sloan Kettering Cancer Center, and Johns Hopkins University. LBS-007 has shown activity against chemotherapy-resistant cell lines and other cancer cell lines, including leukemia and solid tumors.

LBS-003, the company’s fourth pipeline candidate, is a novel omega-3 fatty acid-derived anti-cancer small molecule designed to disrupt cellular metabolism and subsequently induce apoptosis in cancer cells. LBS-002 is a discovery-phase candidate being developed with University of Sydney and University of Technology Sydney.

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