Overview：First-in-Class Anti-Tubulin for the Treatment of Primary and Metastatic Brain Tumors
LBS-002 is a first-in-class anti-tubulin therapy targeting primary glioblastomas and metastatic brain tumors resulting from breast and lung cancers. LBS-002 displays the same drug-like properties as CNS-active drugs, and is the first anti-tubulin agent to be able to cross the blood-brain barrier (BBB). Pre-clinical data shows that LBS-002 is highly efficacious in aggressive, chemo-resistant brain cancers (including EGFR-mutant glioblastomas in vivo), and exhibits a better therapeutic window than clinically used tubulin inhibitors.
Glioblastomas & Metastatic Brain Tumors
Approximately 50% of primary brain tumors are glioblastomas , which are among the most lethal and least successfully treated solid tumors. The current standard of care includes surgical removal of the tumor, followed by radiation and chemotherapy. Unfortunately, glioblastomas are highly invasive, forming finger-like projections throughout the brain, which makes complete tumor removal nearly impossible. Glioblastomas are also made of multiple cell types, which vary in their response to radiation and chemotherapy. Even with standard treatment, median survival only ranges between 1-3 years.Metastatic brain tumors are caused by cancers that originate in another part of the body, and have spread into the brain. 50% of all brain tumors are metastatic, making them much more common than primary brain tumors. The majority of metastatic brain tumors originate from lung and breast cancers. Recurrance of metastatic brain tumors is common, requiring multiple rounds of treatment, and low median survival rates.
How it Works (Mechanism of Action)：Disrupting Tubulin Formation to Prevent Tumor Growth
Cancer cells are known for their accelerated rate of growth and proliferation. During this process, a cancer cell grows, duplicates its DNA and then divides, resulting in two cancer cells. During cell division, cell structures called microtubules form to segregate the cell’s chromosomal DNA.
Drugs that interrupt the formation of microtubules, known as microtubule-targeting agents (MTA), are highly effective anti-cancer therapies because they target the machinery that enables cancer cells to divide. Unfortunately, the most successful chemotherapy drugs on the market, including MTAs like paclitaxel and vinblastine, are ineffective in treating brain cancers because they’re unable to cross the blood-brain-barrier (BBB). The BBB is a layer of cells that protects the brain from pathogens. Unfortunately, it also makes it extremely difficult for brain cancer therapies to reach their targets.
LBS-002 is the first small molecule microtubule targeting agent with the ability to cross the blood-brain barrier. Once inside the brain, LBS-002 disrupts the division of cancer cells by preventing the polymerization of tubulin, the proteins that form microtubules.