R&D Strategy Overview
Addressing brain metastasis and drug resistance for small molecule target therapies with our unique discovery platform

Our research team has the excellent expertise in drug discovery including computational structure-based design, target binding kinetics, oncology research and CNS compound optimization.


Majority of cancer patients die off metastasis, including brain metastasis. Under stress microenvironment, such as hypoxia, lack of nutrients and drug applications, cancer cells tend to adopt stemness states, which express high levels of active transporters such as ABCB1, ABCC1 and ABCG2 proteins. These cancer stem cells (also called cancer initiating cells) can migrate via blood or lymphatic vessels to different organs such as the liver, the bone, the lung and the brain.



Picture Resource: https://pubs.rsc.org/en/content/articlehtml/2016/cs/c6cs00076b


A brain tumor occurs when abnormal cells form within the brain. Cancerous tumors can be divided into primary tumors, such as glioma, that start within the brain, and secondary tumors known as brain metastasis (BM) tumors that have spread from somewhere else, such as lung, breast or skin. The blood–brain barrier (BBB) is a highly selective permeability barrier that separates the circulating blood from the brain extracellular fluid (CSF) in the central nervous system (CNS).  BBB limits almost most known cancer drugs, biologics or small molecules, to reach therapeutic concentration in the brain.


Our approach is to address the above-mentioned issues by designing and optimizing drug candidates that devoid of ABC active transporter activity and high cell and brain penetration, that can better alleviate drug resistance. We are also exploring various combination therapeutics for inhibiting tumor growth and cancer metastasis synergistically. In addition, we are looking for combination with immune therapy with our small molecule targeted therapies.

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