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. We also have our TCR-T Immunotherapy platform, which harnesses and enhances the patient’s own immune system to target and eliminate cancer. Lastly, 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.

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.

ProgramDrug CandidateIndicationPre-ClinicalPhase 1Phase 2Phase 3Stage
Orascovery
(P-gp inhibitor [encequidar] + chemoRx agents)
Oral paclitaxel + encequidar (Oraxol)Metastatic breast cancer
Phase 3
Orascovery
(P-gp inhibitor [encequidar] + chemoRx agents)
Oral paclitaxel + encequidar (Oraxol)Angiosarcoma
Phase 2
Orascovery
(P-gp inhibitor [encequidar] + chemoRx agents)
Oral paclitaxel + encequidar (Oraxol) w/ dostarlimab*Neoadjuvant breast cancer (I-SPY 2)
Phase 2
Orascovery
(P-gp inhibitor [encequidar] + chemoRx agents)
Oral paclitaxel + encequidar (Oraxol) w/ ramucirumab**Gastric cancer
Phase 1
Orascovery
(P-gp inhibitor [encequidar] + chemoRx agents)
Oral paclitaxel + encequidar (Oraxol) w/ pembrolizumabSolid tumors
Phase 1
Orascovery
(P-gp inhibitor [encequidar] + chemoRx agents)
Oral irinotecan + encequidar (Oratecan)Solid tumors
Phase 1
Orascovery
(P-gp inhibitor [encequidar] + chemoRx agents)
Oral docetaxel + encequidar (Oradoxel)Solid tumors
Phase 1
Orascovery
(P-gp inhibitor [encequidar] + chemoRx agents)
Oral topotecan + encequidar (Oratopo)Solid tumors
Phase 1
Orascovery
(P-gp inhibitor [encequidar] + chemoRx agents)
Oral eribulin + encequidar (Eribulin ORA)Solid tumors
Phase 1
Src Kinase InhibitionTirbanibulin (KX2-391) ointmentActinic keratosis
Phase 3
Src Kinase InhibitionTirbanibulin (KX2-391) ointmentPsoriasis
Phase 1
Src Kinase InhibitionTirbanibulin (KX2-391) ointmentSkin cancers
Pre-clinical
Src Kinase InhibitionKX2-361 (KX-02)Glioblastoma
Phase 1
TCR-T ImmunotherapyTCRT-ESO-A2Multiple tumors
Phase 1
Arginine Deprivation Therapy(PT-01) PegtomarginaseMultiple tumors
Pre-clinical
* Collaboration with Quantum Leap Healthcare Collaborative and GlaxoSmithKline
** Collaboration with Eli Lilly and Company, makers of ramucirumab

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