Our robust clinical pipeline includes small molecule, biologic and cellular therapies for the treatment of cancer. The Athenex team continues to fuel the rapid expansion of this clinical pipeline now comprised of nine total IND’s.

Our Orascovery oral absorption technology, using our novel, highly-selective P-gp pump inhibitor, encequidar (formerly known as HM30181A), in combination with widely-used cytotoxic agents, enables oral administration of currently injectable-only drugs. We have two Src Kinase/tubulin polymerization inhibitors, tirbanibulin (formerly known as KX2-391) and KX2-361, 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 PT01 (also known as Pegtomarginase), which is an enzyme capable of depleting tumors of a key resource for their growth and survival, namely the amino acid arginine. Lastly, we have our TCR-T Immunotherapy platform, 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.


Program Drug Candidate Indication Pre-Clinical Phase 1 Phase 2 Phase 3
(P-gp inhibitor [encequidar] + chemoRx agents)
Oral paclitaxel + encequidar (Oraxol) Metastatic breast cancer
Oral paclitaxel + encequidar (Oraxol) w/ dostarlimab* Neoadjuvant breast cancer (I-SPY 2)
Oral paclitaxel + encequidar (Oraxol) w/ pembrolizumab Solid tumors
Oral paclitaxel + encequidar (Oraxol) w/ ramucirumab** Gastric cancer
Oral irinotecan + encequidar (Oratecan) Solid tumors
Oral docetaxel + encequidar (Oradoxel) Solid tumors
Oral topotecan + encequidar (Oratopo) Solid tumors
Oral eribulin + encequidar (Eribulin ORA) Solid tumors
Src Kinase Inhibition Tirbanibulin (KX2-391) ointment Actinic keratosis
Skin cancers
KX2-361 (KX-02) Glioblastoma
TCR-T Immunotherapy TAEST16001 Multiple tumors
Arginine Deprivation Therapy (PT-01) Pegtomarginase Multiple tumors

* Collaboration with Quantum Leap Healthcare Collaborative and GlaxoSmithKline
** Collaboration with Eli Lilly and Company, makers of ramucirumab

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