The novel P-gp inhibitor HM30181A forms the cornerstone of our Orascovery platform, and enables the administration of oral dosing formats of paclitaxel (Oraxol), irinotecan (Oratecan), and docetaxel (Oradoxel), each of which is currently under clinical development. HM30181A is a novel compound with inhibitory activity specific to P-gp. It does not interfere significantly with the activity of other related transporters, and does not significantly inhibit cytochrome 3A4, an enzyme that is important in the metabolism of commonly used drugs. The feature that distinguishes HM30181A from other small molecule P-gp inhibitors is its minimal oral absorption. This feature localizes P-gp inhibitory activity in the gastrointestinal tract, limiting the potential for interaction at additional systemic sites where P-gp is expressed. Inhibition of gastrointestinal P-gp significantly improves the absorption of chemotherapy agents to achieve systemic exposure profiles which enhance the efficacy and may reduce toxicity of these established chemotherapeutic agents. Based on its pharmacological profile and low systemic absorption, HM30181A is not expected to cause drug-to-drug interactions other than enhancement of oral absorption of medications which are P-gp substrates.

Oral administration can overcome key limitations and challenges around IV administration of certain cytotoxic chemotherapies, such as dosing, tolerability and efficacy, and we believe the Orascovery approach will establish a new paradigm in the use of oral anti-cancer drugs for cancer treatments in at least three ways. First, with the use of HM30181A, clinicians may be able to consistently deliver oral doses of certain chemotherapeutic drugs over a greater number of cycles and duration of time. Second, we believe active drug exposure of chemotherapeutic agents in the patient over time is a critical element in determining efficacy and we have achieved substantially greater tolerability with administration of HM30181A as compared to the current IV standards of care. Third, in light of better tolerability of standard chemotherapies delivered orally, combination with immuno-oncology and targeted anti-cancer treatments can be potentially optimized to achieve greater therapeutic benefit compared to current combination treatment paradigms.

Oraxol: An Oral Formulation of Paclitaxel

Oraxol is an oral formulation of Paclitaxel. Today only intravenous versions of Paclitaxel are available on the market to treat breast, lung, ovarian and pancreatic cancer. We have demonstrated through numerous clinical studies that Paclitaxel is systemically absorbed by the patient through the application of our oral delivery system, offering patients a chance to achieve better clinical outcomes.

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Oratecan: An Oral Formulation of Irinotecan

Oratecan is an oral formulation of Irinotecan. While current Irinotecan products on the market are delivered intravenously to treat colorectal cancer, our clinical data suggest that Irinotecan can be absorbed orally through the application of our Orascovery delivery system, providing therapeutic exposure levels while limiting some of the induced toxicity of IV irinotecan.

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Oradoxel: An Oral Formulation of Docetaxel

Oradoxel is an oral formulation of Docetaxel. Currently only intravenous Docetaxel is available and is US FDA approved for use in head and neck, gastric, breast, prostate and non-small cell lung cancers. Athenex’s US FDA IND application for Oradoxel was allowed in 2016 and this oral formulation is in Phase I clinical trials.

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Oratopo: An Oral Formulation of Topotecan

Oratopo is an oral formulation of Topotecan. Currently intravenous Topotecan is available and is US FDA approved for use in ovarian, cervical and small cell lung cancers. Oral Topotecan is available and is US FDA approved for use only in small cell lung cancer. Athenex’s US FDA IND application for Oratopo was allowed in 2017 and this oral formulation is now progressing towards Phase I clinical trials.

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Eribulin ORA: An Oral Formulation of Eribulin

Eribulin ORA is an oral formulation of eribulin. Intravenous eribulin is widely approved for use in metastatic breast cancer and metastatic liposarcoma. Athenex’s U.S. FDA IND application for Eribulin ORA was allowed in 2018 and a Phase I clinical trial is planned for early 2019.

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