Our robust clinical pipeline includes small molecule, biologic and cellular therapies for treatment of cancer. The Athenex team continues to fuel the rapid expansion of this clinical pipeline now comprised of seven total IND’s, five of which were allowed in the US alone within the last five years, and more are planned. Our Orascovery oral absorption technology, using our novel, highly-selective P-gp inhibitor in combination with widely-used cytotoxic agents, enables oral administration of currently injectable-only drugs. We have two Src Kinase/tubulin polymerization inhibitors, KX-01 and KX-02, that are being developed both orally for cancers such as glioblastoma, as well as topically for the pre-cancerous disease actinic keratosis. On the biologics front we have Pegtomarginase, which is an enzyme capable of depleting tumors of a key resource for their growth and survival, the amino acid arginine. Lastly we have our Cellular Immunotherapy platform, TCR-T, which harnesses and enhances the patient’s own immune system to target and eliminate cancer. Taken together, our clinical pipeline balances a range of therapeutic approaches for the treatment of cancer to enable us to improve the lives of cancer patients.

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
Oral Eribulin 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
Cellular Immunotherapy TCR-T Immunotherapy Multiple Tumors Worldwide, except China
Pegylated Modified Human Arginase Pegtomarginase 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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Pegylated Modified Human Arginase

Malignant tumor cells grow and multiply quickly, demanding a significant supply of nutrition and amino acids as building blocks to sustain expansion. Athenex is developing a pegylated, genetically modified, human arginase therapeutic that deprives tumors of an essential amino acid building block of tumors, arginine. It is established that unlike normal healthy cells, several tumor cell types lack the machinery to produce arginine internally, making the tumor‘s growth highly dependent on external sources of arginine. This biological therapeutic is designed to actively deprive the tumor of its source of arginine, depleting growth and survival of the tumor cells, while healthy cells capable of making arginine are unaffected.

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TCR-T Immunotherapy

Athenex is developing next-generation cell based therapies that take advantage of the exquisite specificity of a patient’s own immune system to selectively identify and destroy tumor cells. Athenex’s technology builds upon the incredible natural abilities of the T cell receptor (TCR), adding more potency and selectivity based on actual patient tumor information, to bring to patients two related therapeutic approaches to targeting cancer. In the first, immune T cells isolated from patients are isolated and engineered to express an enhanced TCR before being infused into the patient. In the second approach, engineered high affinity transgenic TCR (HATac) can infused directly into the patient. This HATac is able to “bridge” a patient’s own T cells with tumor targets, effectively re-directing the T cells to selectively attack the tumor targets. Both approaches have the incredible potential for potent and selective treatment of cancer.

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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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