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Poster display session

3962 - Phase 1 study of RX-5902, a novel Orally Bioavailable Inhibitor of Phosphorylated P68, which prevents β-catenin Translocation in Advanced Solid Tumorsv

Date

11 Sep 2017

Session

Poster display session

Presenters

Jennifer Diamond

Citation

Annals of Oncology (2017) 28 (suppl_5): v74-v108. 10.1093/annonc/mdx365

Authors

J. Diamond1, G. Eckhardt2, L. Gluck3, M. Gutierrez4, C. Peterson5, R. Pila5, E. Benaim6

Author affiliations

  • 1 Department Of Medicine, University of Colorado Denver School of Medicine, 80045 - Aurora/US
  • 2 Anschutz Cancer Center, University of Colorado Denver School of Medicine, Aurora/US
  • 3 Oncology, Clinical Research Unit ITOR, Greenville/US
  • 4 John Theurer Cancer Center, Hackensack University Medical Center, Hackensack/US
  • 5 Clinical Operations, Rexahn Pharmaceuticals, Inc, 20850 - Rockville/US
  • 6 Oncology, Rexahn Pharmaceuticals, Inc, 20850 - Rockville/US
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Resources

Abstract 3962

Background

RX-5902 is a novel compound that targets phosphorylated p68 RNA helicase (also known as DDX5), a member of the DEAD box family of RNA helicases. Phosphorylated p68 may play a vital role in cell proliferation and tumor/cancer progression through inhibition of β-catenin translocation. We report preliminary results of the Phase 1 study of RX-5902 as a single agent to treat advanced solid tumors.

Methods

The dose finding portion of the Phase 1 study (NCT02003092) was designed to evaluate safety, tolerability and dose limiting toxicities, to identify the maximum tolerated dose and a recommended phase 2 dose and schedule (RP2D). Secondary objectives were pharmacokinetics (PK) and antitumor activity (RECIST v1.1). Eligible subjects (aged ≥ 18 years), with relapsed/refractory solid tumors that had been heavily pretreated, received oral RX-5902 ranging from 25 mg to 350 mg and administered at 1, 3, 5 or 7 times per week for 3 weeks followed by 1 week of rest or for 4 weeks without rest.

Results

As of May 2017, 35 subjects (23 Females, 12 males) were treated with oral RX-5902. The dose limiting toxicities were G4 hyponatremia (n = 1) and G3 fatigue (n = 1) at 300 mg administered daily for 4 weeks. The maximum tolerated dose of 250 mg, will be studied further in the Phase 2a portion. Of the 35 subjects treated, 15 subjects (breast ER+/PR+/Her2-, triple negative breast (n = 2), cervical (n = 2), neuroendocrine (n = 3), paraganglioma, colorectal (N = 3), pancreatic, ovarian, head and neck cancers) experienced stable disease; 2 subjects have received treatment for > 2.5 years. The most common related adverse events were G1/G2 anorexia, G1/G2 nausea, G1/G2 vomiting, G1/G2 diarrhea, G1 weight loss and G1/G2 fatigue. Oral RX-5902 was bioavailable with median Tmax of 2 hours and median elimination half-life of 12 hours.

Conclusions

Data from this study support that RX-5902 is safe and well-tolerated at the doses and schedules tested. The RP2D of 250 mg of RX-5902 administered daily for 5 consecutive days for 4 weeks is being studied further in metastatic triple negative breast cancer in the Phase 2 portion of this study.

Clinical trial identification

NCT02003092

Legal entity responsible for the study

Rexahn Pharmaceuticals, Inc.

Funding

Rexahn Pharmaceuticals, Inc

Disclosure

C. Peterson, R. Pila, E. Benaim: Employee of Rexahn Pharmaceuticals, Inc. All other authors have declared no conflicts of interest.

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