Haichang to expand antisense oligonucleotide pipeline leveraging its proprietary QTsomeTM delivery technology for the treatment of cancer in the US and China

Hangzhou, China [Feb. 08, 2020] — Zhejiang Haichang Biotechnology Co., Ltd. (Haichang), a China and U.S. -based pharmaceutical company specialized in liposomal formulations—QTsome™ technology, today announced that it has entered into an Exclusive License Agreement (Agreement) with Rexahn Pharmaceuticals, Inc. (NASDAQ: REXN), a clinical stage biopharmaceutical company developing innovative therapies for the treatment of cancer.

The Agreement includes two compounds RX-0047 and RX-0201, which inhibit the expression of HIF-1α and Akt-1, respectively, and RX-0301, a nanoliposomal formulation of RX-0201. Under the terms of the Agreement, which supersedes the previous collaboration and license agreement between the parties, Haichang licensed intellectual property owned or controlled by Rexahn which will  permit Haichang to, develop and commercialize the licensed compounds. Rexahn is eligible to receive milestones, royalties, and sublicensing revenues from Haichang.

“We are delighted to expand our antisense oligonucleotide pipeline using our proprietary QTsomeTM technology” said Dr. Ben Zhao, Chief Executive Officer of Haichang. “The inclusion of RX-0047 further strengthens our battle against cancer utilizing our advanced delivery technology. HIF-1α is known to be over-expressed in a broad range of human cancers, and our program has the potential to produce a potential first-in-class therapy for malignancies such as liver cancer and non-small cell lung cancer.”

 “We are impressed with Haichang’s QTsome™ technology and its potential to deliver RX-0201 to liver cancer cells to enhance the efficacy of Akt-1 targeting,” said Douglas Swirsky, president and chief executive officer of Rexahn. “They have made significant progress advancing RX-0301 towards the initiation of a Phase 1/2 clinical study in hepatocellular carcinoma and we look forward to Haichang applying its technology and expertise to develop RX-0047.”

About RX-0047

RX-0047 is a potential first-in-class potent inhibitor of HIF-1α protein kinase. HIF-1α is a major protein regulating the mechanisms of cancer cell growth, invasion, angiogenesis, and radiation and drug resistance. HIF-1α is known to be over-expressed in a broad range of human cancers, and is associated with increased mortality, metastasis and resistance to radiation therapy and chemotherapy of cancer cells. RX-0047 directly inhibits HIF-1α by blocking HIF-1α mRNA expression and lowering protein levels.

In 2019, the Nobel Prize in Physiology or Medicine was awarded to William Kaelin, Jr., Sir Peter Ratcliffe, and Gregg Semenza. During the early 1990’s, Gregg Semenza identified, and then in 1995 purified and cloned, a transcription factor that regulates oxygen-dependent responses. He named this factor HIF, for Hypoxia Inducible Factor, and showed that it consists of two components: one a novel and oxygen-sensitive moiety, HIF-1α, and a second, previously identified and constitutively expressed and non-oxygen-regulated protein known as ARNT. Through the combined work of these three laureates it was demonstrated that the response by gene expression to changes in oxygen is directly coupled to oxygen levels in the animal cell, allowing immediate cellular responses to occur to oxygenation through the action of the HIF transcription factor.

About Zhejiang Haichang Biotechnology Co., Ltd 

Zhejiang Haichang Biotechnology Co., Ltd. is a privately-owned specialized biotechnology company headquartered in Hangzhou, China. The company is focused on the development and manufacture of complex intravenous pharmaceutical products including liposome and microsphere products, primarily for cancer treatment.

Haichang’s QTsome™ technology is a patented gene delivery technology that was co-developed with Professor Robert Lee at the Ohio State University. The technology is designed to enhance cellular uptake of large molecules such as oligonucleotides (antisense, siRNA and miRNA) and to target certain organs such as the liver where nanoparticles accumulate.

About Rexahn Pharmaceuticals, Inc.

Rexahn Pharmaceuticals Inc. (NasdaqCM: REXN) is a clinical stage biopharmaceutical company developing innovative therapies to improve patient outcomes in cancers that are difficult to treat. The company’s mission is to improve the lives of cancer patients by developing next-generation cancer therapies that are designed to maximize efficacy while minimizing the toxicity and side effects traditionally associated with cancer treatment. Rexahn’s product candidates work by targeting and neutralizing specific proteins believed to be involved in the complex biological cascade that leads to cancer cell growth. Preclinical studies show that several of Rexahn’s product candidates may be active against multiple types of cancer, including drug resistant cancers and difficult-to-treat cancers and others may augment current FDA-approved cancer treatments. The company has a pipeline of oncology product candidates in clinical and preclinical development including RX-3117, RX-5902, and RX-0301. For more information about the company and its oncology programs, please visit www.rexahn.com.

Reference

  1. Dikmen, Z. G., Gellert, G. C., Dogan, P., Yoon, H., Lee, Y. B., Ahn, C. H., & Shay, J. W. (2008). In vivo and in vitro effects of a HIF-1α inhibitor, RX-0047. Journal of Cellular Biochemistry, 104(3), 985–994. doi: 10.1002/jcb.21681. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3375689/pdf/nihms-381621.pdf
  2. The Nobel Prize in Physiology or Medicine 2019. NobelPrize.org. Nobel Media AB 2020. Sun. 2 Feb 2020. https://www.nobelprize.org/prizes/medicine/2019/summary/
  3. Wang, G.L., Jiang, B.-H., Rue, E.A. & Semenza, G.L. (1995). Hypoxia-inducible factor 1 is a basic-helix-loop-helix-PAS heterodimer regulated by cellular O2 tension.  Proc Natl Acad Sci USA, 92, 5510-5514