Our robust clinical pipeline includes six major clinical stage drug candidates, three of which are based on a proprietary Orascovery oral absorption technology, using our novel, highly-selective P-gp inhibitor in combination with widely-used cytotoxic agents enabling oral administration of currently injectable only drugs. The remaining three are novel proprietary Src Kinase inhibitors that have multiple mechanisms of action.

Over the last three years alone, our research and development platform has enabled us to file three U.S. investigational new drug applications, or INDs. In addition to the current clinical pipeline, our team is working both on new applications of our existing technologies and on innovating new platform technologies. We believe that our Orascovery platform can be applied to other existing drug therapies to achieve better PK, clinical response and tolerability profiles. Additionally, we have applied our research knowledge and experience of human oral absorption functions and have identified late stage novel molecule candidates which could represent additional future platform technologies. Our research scientists have also developed proprietary systems to identify and screen new molecules, including target binding sites, leading to a more efficient and effective innovation process. We believe these systems and platforms will likely lead to additional clinical candidates.

Our Major Product Candidates

Program Drug Candidate Indication Major Territories Owned Pre-Clinical Phase 1 Phase 2 Phase 3
Orascovery
(P-gp + chemo-therapeutic agents)
Oraxol Breast cancer U.S., EU, China, India
Oraxol with ramucirumab* Gastric cancer U.S., EU, China, India
Oratecan Solid tumors U.S., EU, China, India
Oradoxel Solid tumors U.S., EU, China, India
Oratopo Solid tumors U.S., EU, China, India
Src Kinase Inhibition KX-01 Ointment Actinic Keratosis Worldwide, except China
Psoriasis Worldwide, except China
Skin cancers Worldwide, except China
KX-01 Oral Liquid tumors Worldwide, except China
Ovarian cancer Worldwide, except China
KX-02 Oral Glioblastoma Worldwide, except China
Dual Inhibition ATNX-04 (CYP / P-gp) Multiple tumors Worldwide

* Collaboration with Eli Lilly and Company, makers of ramucirumab

Orascovery Platform

We are developing a series of orally administered chemotherapeutic agents using our proprietary P-gp pump inhibitor delivery system. The technology enables the oral administration of multiple anti-cancer agents, which currently are only given by IV due to poor oral absorption. Oral administration of certain cytotoxic chemotherapies can potentially overcome several key challenges associated with IV administration.  We believe that our Orascovery platform overcomes these challenges by allowing more frequent dosing over longer periods of time, which is expected to be better tolerated and allow for higher total dosage and longer time exposure to the chemotherapeutic agent. Further, we believe additional agents like immuno-oncology and targeted therapies can be better optimized when combined with the benefits of oral chemotherapy agents.

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Src Kinase Inhibition

Src Kinase, a tyrosine kinase protein involved in regulating cell growth, is strongly implicated in regulating metastatic potential.  Defects in Src Kinase are implicated in a number of cancers, and inhibiting this protein may limit the growth or proliferation of cancerous cell types. The Src Kinase Inhibition platform refers to novel small molecule compounds that have multiple mechanisms of action, including the inhibition of the activity of Src Kinase and the inhibition of tubulin polymerization during cell division. We believe the combination of these mechanisms of action provide a broader range of anti-cancer activity as compared to either mechanism of action alone. Our key clinical product candidates in this platform are KX-01 ointment for pre-cancerous lesions of the skin and KX-02 for glioblastoma multiforme, or GBM.

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Dual Inhibition

Athenex research and development teams are exploring a CYP and P-gp dual inhibitor technology to generate new product candidates. This class of dual absorption enhancers has shown potential to significantly improve the oral bioavailability of certain other drugs in laboratory tests, and may expand the application of our oral absorption platform to drugs where the CYP barrier to oral absorption is also important. These dual absorption enhancers may lead to better performing next- generation oral medicines in our pipeline of clinical products.

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