Phase I clinical study in cancer patients with solid tumors anticipated to begin Q4 2013
ROCKVILLE, MD, USA I September 30, 2013 I Rexahn Pharmaceuticals, Inc. (NYSE MKT: RNN), a clinical stage biopharmaceutical company developing potential best-in-class oncology therapies, today announced the on-line publication of preclinical results for RX-3117 in a peer reviewed medical journal, Investigational New Drugs, in an article titled, “Metabolism, mechanism of action and sensitivity profile of fluorocyclopentenylcytosine (RX-3117; TV-1360)”. Investigational New Drugs is an interdisciplinary journal presenting the latest investigations and discussions of critical questions appropriate to the entire field of new anticancer drug development.
Peter D. Suzdak, Ph.D., Rexahn’s Chief Executive Officer, commented, “The broad spectrum of anti-tumor activity against human cancer cell lines, oral bioavailability in cancer patients, and improved preclinical and clinical safety profile suggest that RX-3117 may represent a major advance in the treatment of solid cancer tumors. Rexahn anticipates initiating a Phase I clinical study in cancer patients with solid tumors in the fourth quarter of 2013.”
The published study characterized the broad spectrum of potent anti-tumor effects of RX-3117 against 50 different human cancer cell lines (including colon, lung, renal and pancreas) and its unique mechanism of activation in cancer cells. In addition, RX-3117 was shown to be effective in gemcitabine resistant human cancer cell lines. Although RX-3117 shares some properties with other nucleoside compounds such as gemcitabine, its cytotoxicity profile, metabolism and mechanism of action make it distinct and potentially clinically superior to existing nucleoside compounds.
Prof. Dr. Godefridus J. (Frits) Peters, Head Laboratory Medical Oncology, VU University Medical Center, Amsterdam, The Netherlands, and lead author of the published results, commented, “RX-3117 is an exciting new nucleoside analog with unique properties both regarding its mechanism of action and its pharmacology. Its excellent oral bioavailability fits very well with the current tendency to give anticancer drugs orally. Its mechanism of action gives several leads for future combination therapies with different drugs.”
About RX-3117
RX-3117 is a novel small molecule nucleoside compound that is incorporated into DNA or RNA of cancer cells and inhibits both DNA and RNA synthesis which induces apoptotic cell death of tumor cells. RX-3117 also mediates the down-regulation of DNA methyltransferase 1 (DNMT1), an enzyme responsible for the methylation of cytosine residues on newly synthesized DNA and also a target for anticancer therapies. Preclinical studies have shown RX-3117 to be effective in both inhibiting the growth of various human cancer xenograft models, including colon, lung, renal and pancreas, as well as overcoming chemotherapeutic drug resistance.
RX-3117 has demonstrated a broad spectrum anti-tumor activity against 50 different human cancer cell lines and efficacy in 12 different mouse xenograft models. The efficacy in the mouse xenograft models was superior to that of gemcitabine. In addition, in human cancer cell lines made resistant to the anti-tumor effects of gemcitabine, RX-3117 still retains its full anti-tumor activity.
In August 2012, Rexahn reported the completion of an exploratory Phase I clinical trial of RX-3117 in cancer patients conducted in Europe, to investigate the oral bioavailability, safety and tolerability of the compound. In this study, oral administration of RX-3117 demonstrated an oral bioavailability of 34-58% and a plasma half-life (T1/2) of 14 hours. In addition, RX-3117 was safe and well tolerated in all subjects throughout the dose range tested.
The Investigational New Drug (IND) application for RX-3117 filed in July 2013 has now cleared the 30 day review period by the US Food and Drug Administration (FDA). Rexahn expects to initiate a Phase I clinical trial in cancer patients during the fourth quarter of 2013. Additionally, Rexahn will be exploring potential partnering opportunities with oncology focused pharmaceutical companies.
About Prof. Dr. Godefridus J. (Frits) Peters
Dr. Peters is head of the Laboratory Medical Oncology of the VU University Medical Center in Amsterdam (the Netherlands). The research of Prof. Peters is focused on translation of preclinical pharmacology of anticancer agents to the clinic. Dr. Peters has published more than 500 peer reviewed articles, review chapters and abstracts in high profile scientific journals. Drug classes studied include antifolates, other antimetabolites, platinum analogs, topoisomerase inhibitors, taxanes and more recently anti-signalling protein kinase inhibitors. He is/was a member of 20 editorial boards, was founder and first president of the Purine and Pyrimidine Society, and is chair of the EORTC-Pharmacology and Molecular Mechanisms Group.
About Rexahn Pharmaceuticals, Inc.
Rexahn Pharmaceuticals is a clinical stage biopharmaceutical company dedicated to developing best-in-class therapeutics for the treatment of cancer. Rexahn currently has three clinical stage oncology candidates, Archexin®, RX-3117, and SupinoxinTM (RX-5902) and a robust pipeline of preclinical compounds to treat multiple types of cancer. Rexahn has also developed proprietary drug discovery platform technologies in the areas of Nano-Polymer-Drug Conjugate Systems (NPDCS), nano-medicines, 3D-GOLD, and TIMES. For more information, please visit www.rexahn.com.
SOURCE: Rexahn Pharmaceuticals
Post Views: 103
Phase I clinical study in cancer patients with solid tumors anticipated to begin Q4 2013
ROCKVILLE, MD, USA I September 30, 2013 I Rexahn Pharmaceuticals, Inc. (NYSE MKT: RNN), a clinical stage biopharmaceutical company developing potential best-in-class oncology therapies, today announced the on-line publication of preclinical results for RX-3117 in a peer reviewed medical journal, Investigational New Drugs, in an article titled, “Metabolism, mechanism of action and sensitivity profile of fluorocyclopentenylcytosine (RX-3117; TV-1360)”. Investigational New Drugs is an interdisciplinary journal presenting the latest investigations and discussions of critical questions appropriate to the entire field of new anticancer drug development.
Peter D. Suzdak, Ph.D., Rexahn’s Chief Executive Officer, commented, “The broad spectrum of anti-tumor activity against human cancer cell lines, oral bioavailability in cancer patients, and improved preclinical and clinical safety profile suggest that RX-3117 may represent a major advance in the treatment of solid cancer tumors. Rexahn anticipates initiating a Phase I clinical study in cancer patients with solid tumors in the fourth quarter of 2013.”
The published study characterized the broad spectrum of potent anti-tumor effects of RX-3117 against 50 different human cancer cell lines (including colon, lung, renal and pancreas) and its unique mechanism of activation in cancer cells. In addition, RX-3117 was shown to be effective in gemcitabine resistant human cancer cell lines. Although RX-3117 shares some properties with other nucleoside compounds such as gemcitabine, its cytotoxicity profile, metabolism and mechanism of action make it distinct and potentially clinically superior to existing nucleoside compounds.
Prof. Dr. Godefridus J. (Frits) Peters, Head Laboratory Medical Oncology, VU University Medical Center, Amsterdam, The Netherlands, and lead author of the published results, commented, “RX-3117 is an exciting new nucleoside analog with unique properties both regarding its mechanism of action and its pharmacology. Its excellent oral bioavailability fits very well with the current tendency to give anticancer drugs orally. Its mechanism of action gives several leads for future combination therapies with different drugs.”
About RX-3117
RX-3117 is a novel small molecule nucleoside compound that is incorporated into DNA or RNA of cancer cells and inhibits both DNA and RNA synthesis which induces apoptotic cell death of tumor cells. RX-3117 also mediates the down-regulation of DNA methyltransferase 1 (DNMT1), an enzyme responsible for the methylation of cytosine residues on newly synthesized DNA and also a target for anticancer therapies. Preclinical studies have shown RX-3117 to be effective in both inhibiting the growth of various human cancer xenograft models, including colon, lung, renal and pancreas, as well as overcoming chemotherapeutic drug resistance.
RX-3117 has demonstrated a broad spectrum anti-tumor activity against 50 different human cancer cell lines and efficacy in 12 different mouse xenograft models. The efficacy in the mouse xenograft models was superior to that of gemcitabine. In addition, in human cancer cell lines made resistant to the anti-tumor effects of gemcitabine, RX-3117 still retains its full anti-tumor activity.
In August 2012, Rexahn reported the completion of an exploratory Phase I clinical trial of RX-3117 in cancer patients conducted in Europe, to investigate the oral bioavailability, safety and tolerability of the compound. In this study, oral administration of RX-3117 demonstrated an oral bioavailability of 34-58% and a plasma half-life (T1/2) of 14 hours. In addition, RX-3117 was safe and well tolerated in all subjects throughout the dose range tested.
The Investigational New Drug (IND) application for RX-3117 filed in July 2013 has now cleared the 30 day review period by the US Food and Drug Administration (FDA). Rexahn expects to initiate a Phase I clinical trial in cancer patients during the fourth quarter of 2013. Additionally, Rexahn will be exploring potential partnering opportunities with oncology focused pharmaceutical companies.
About Prof. Dr. Godefridus J. (Frits) Peters
Dr. Peters is head of the Laboratory Medical Oncology of the VU University Medical Center in Amsterdam (the Netherlands). The research of Prof. Peters is focused on translation of preclinical pharmacology of anticancer agents to the clinic. Dr. Peters has published more than 500 peer reviewed articles, review chapters and abstracts in high profile scientific journals. Drug classes studied include antifolates, other antimetabolites, platinum analogs, topoisomerase inhibitors, taxanes and more recently anti-signalling protein kinase inhibitors. He is/was a member of 20 editorial boards, was founder and first president of the Purine and Pyrimidine Society, and is chair of the EORTC-Pharmacology and Molecular Mechanisms Group.
About Rexahn Pharmaceuticals, Inc.
Rexahn Pharmaceuticals is a clinical stage biopharmaceutical company dedicated to developing best-in-class therapeutics for the treatment of cancer. Rexahn currently has three clinical stage oncology candidates, Archexin®, RX-3117, and SupinoxinTM (RX-5902) and a robust pipeline of preclinical compounds to treat multiple types of cancer. Rexahn has also developed proprietary drug discovery platform technologies in the areas of Nano-Polymer-Drug Conjugate Systems (NPDCS), nano-medicines, 3D-GOLD, and TIMES. For more information, please visit www.rexahn.com.
SOURCE: Rexahn Pharmaceuticals
Post Views: 103
