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Small molecule anti-tumor targeted therapies

Targeted therapies represented by kinase inhibitors are one of the important directions for oncology drug development . Unlike traditional cytotoxic drugs, targeted drugs target gene mutations or over expressions specifically associated with tumor cells, and therefore, often kill tumor cells with lower toxicity and wide safety margin. Aiming at unmet clinical needs in Asian such as lung cancer, breast cancer, gastrointestinal cancer and liver cancer, we take differentiated strategies to develop more effective and safer anti-tumor targeted therapies to meet patients’ needs, extend their lifetime and  improve their quality of life.

Our strategy includes:
1) First-in-class drugs for novel targets;
2) Multifunctional small molecule drugs;
3) Differentiated kinase inhibitors targeting non-enzymatic functions;
4) Novel molecules with unique modes of action such as slow-off and conformational selectivity.

(7lgs, EGFR inhibitor binding to EGFR D770_N771insNGP/V948R) (6c2r, AURORA inhibitor binding to AURORA A)


Immuno-oncology (IO) drugs

Recognizing and killing abnormal cells is a natural attribute of the immune system, but cancer cells often evolve the ability to evade the immune system. Immuno-oncology drugs work through enhancing the body's own immune system or lifting the suppression of cancer cells on the immune system to eradicate tumors. The broad sense of immunotherapy includes immune checkpoint inhibitors, immune cell therapy, oncolytic viruses, cancer vaccines, and other immunomodulators. IO drugs represented by PD-1 monoclonal antibody and CART have achieved revolutionary success, showcasing the power of immune therapy. However, the current IO drugs are predominant monoclonal antibodies that can only access limited extra-cellular or surface proteins, and hence suffer from moderate response rates or limited tumor types. The therapeutic potential of IO remains to be unleashed. We aim to develop the next generation of small molecule IO drugs that can act on a variety of targets to modulate immune system and tumor microenvironment.

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