Aprea receives U.S. patent approval for pharmaceutical formulation of lead compound APR-246
STOCKHOLM – June 26, 2015. Aprea AB, a Karolinska Development AB (STO: KDEV) portfolio company, announced today that the United States Patent and Trademark Office has granted a patent covering a new pharmaceutical formulation of APR-246. The patented formulation enables long term storage which is essential for the future commercial use of APR-246.
Aprea’s first-in-class lead candidate drug APR-246 reactivates dysfunctional p53 tumor suppressor protein, which is found in around 50% of all human tumors as a result of mutations in the p53 gene. The mutations result in loss of p53-dependent cell cycle arrest and apoptosis, important growth control mechanisms that protect against tumor growth. In addition, mutations in p53 or its regulators are associated with increased resistance to standard chemotherapy and hence poor prognosis. Aprea is currently conducting a Phase Ib/II clinical trial with APR-246 in patients with ovarian cancer.
The now granted U.S. patent covers a novel formulation of APR-246 having a greatly improved stability and shelf life compared to prior art formulations of APR-246. By this novel formulation, the challenge of long term storage has been addressed, and Aprea has taken a further step towards providing a commercially useful product. In addition, Aprea is also pursuing corresponding patent applications in all major jurisdictions.
Ulf Björklund, CEO of Aprea noted, "We expect this patent to be a substantial addition to Aprea's patent portfolio. This patent together with previously issued patents related to the utilization of APR-246 will further strengthen our intellectual property portfolio”.
The issued U.S. patent No. 9061016 “Aqueous solution comprising 3-quinuclidinones for the treatment hyperproliferative, autoimmune and heart disease” expires in 2031.
For further information, please contact:
Ulf Björklund, CEO, Aprea AB
Phone: +46 (0) 8 508 845 04
TO THE EDITORS
About Aprea AB
Aprea AB is a Swedish biotech company focusing on discovery and development of novel anticancer compounds targeting the tumor suppressor protein p53. The main owner of Aprea is KDev Investments AB, part of Karolinska Development AB (publ). The other main owners are Östersjöstiftelsen, Praktikerinvest and KCIF Co-Investment Fund KB. For more information, please visit www.aprea.com
About APR-246 APR-246 has been developed based on results from researchers at Karolinska Institutet, and has been shown to reactivate non-functional tumor suppressor protein p53 and induce programmed cell death in many human cancer cells. Preclinical studies have confirmed that APR-246 can activate mutated p53 and demonstrated single agent efficacy and very strong synergy with conventional anti-cancer agents in vitro and in vivo. A clinical Phase Ib/II study in hematological malignancies and prostate cancer has been completed, demonstrating a favorable safety profile and both biological and clinical responses. A Phase Ib/II proof-of-concept study in ovarian cancer patients carrying mutant p53 is currently ongoing.
About the Phase Ib/II PiSARRO trial
The Phase Ib/II trial is designed to evaluate the safety, efficacy, pharmacokinetics and pharmacodynamics of APR-246 in combination with carboplatin (AUC 5) and pegylated doxorubicin (30 mg/m2), a second line standard of care chemotherapy for relapsed platinum sensitive high grade serous ovarian cancer. The Phase Ib/II trial is a two-part study that will enroll approximately 180 patients. Part A is an open-label, multiple ascending dose study. The primary objectives of Phase Ib are to evaluate the safety and tolerability of APR-246 in combination with carboplatin and pegylated doxorubicin, and to confirm the dose of APR-246. Pending successful completion of this phase, Aprea expects to initiate Part B of the trial, which will be a randomized, controlled study investigating the safety and antitumor activity of APR-246 administered in combination with carboplatin and pegylated doxorubicin, compared with carboplatin and pegylated doxorubicin alone. Primary end point of Phase II will be Progression Free Survival (PFS). For details on the PiSARRO trial please visit: www.ClinicalTrials.gov.