Pipeline: Stenoparib (2X-121)
Stenoparib — A Dual PARP and Tankyrase Inhibitor
Stenoparib is Allarity’s lead program, and is an orally-available, small molecule dual-targeted inhibitor of PARP1/2 and telomerase maintenance enzymes (Tankyrase 1 and 2). At present, tankyrases are attracting significant attention as emerging therapeutic targets for cancer, principally due to their role in the Wnt signaling pathway. Aberrant Wnt/β-catenin signaling has been implicated in the development and progression of multiple cancers, potentially giving stenoparib a unique, dual tumor inhibitory action. Stenoparib was originally developed by Eisai Co. Ltd. and was formerly known under the names E7449 and 2X-121. Allarity has the exclusive, global rights for the development and commercialization of stenoparib.
The Stenoparib DRP® is validated for ovarian cancer. It is currently being evaluated for the treatment of advanced ovarian cancer using the Stenoparib DRP® companion diagnostic to guide patient enrollment and improve therapeutic outcome.
Initial Data from Phase 2 Monotherapy Trial
Following the implementation of a protocol change in 2023 to optimize the drug exposure, taking into account the half-life of stenoparib in patients, DRP® selected patients received stenoparib in a twice daily (BID) dosing regimen (200 mg morning, 400 mg evening). After this change, data has been published in press releases on December 5, 2023, on November 18, 2024, and several other press releases. Please refer to our News section for all Allarity press releases.
Fast Track Designation
The U.S. Food and Drug Administration (FDA) has granted Fast Track designation to stenoparib for the treatment of advanced ovarian cancer. This designation recognizes the potential of stenoparib to address a serious, life-threatening condition with limited treatment options. Fast Track status provides Allarity with enhanced access to FDA feedback during clinical development, eligibility for Accelerated Approval and Priority Review, and the ability to submit data on a rolling basis. These regulatory advantages are intended to accelerate the review process and increase the likelihood of bringing stenoparib to patients sooner. The designation highlights both the significant unmet need in advanced ovarian cancer and the encouraging results from early Phase 2 clinical data.Myelotoxicity
Some approved PARP inhibitors have recently been shown to be associated with less favorable survival outcomes than initially established. Allarity’s Phase 2 trial data for stenoparib to date shows that the drug has much less myelotoxicity than the FDA approved PARP inhibitors. Specifically, in 42 evaluable women in Phase 2 studies with stenoparib, anemia (21%), neutropenia (2%) and thrombocytopenia (0%) was lower than the approved PARP inhibitor niraparib with anemia 51%, neutropenia in 20% and thrombocytopenia oberved in in 52% of 463 patients. Allarity anticipates that this lower myelotoxicity may make stenoparib a better candidate for combination with other drugs.
IDE
The U.S. FDA has approved an Investigational Device Exemption (IDE) for use of the Stenoparib DRP® as a companion diagnostic in the clinical trial.