Newswise — RALEIGH, N.C., November 1, 2011 -- DARA BioSciences, Inc. (NASDAQ: DARA), announces the positive results from a successfully completed Phase 1b clinical study for DB959, its peroxisome proliferator activated receptor (PPAR)-delta/gamma agonist, a non-TZD oral drug in development for the treatment of type 2 diabetes. This study’s main objectives were to determine the safety and pharmacokinetics of multiple ascending oral doses of DB959Na.
Overall, the safety profile of once daily doses of DB959Na for seven sequential days was comparable to placebo, demonstrating that DB959Na is safe and well-tolerated throughout the 40-fold dose-range tested. Results of steady-state pharmacokinetic measurements indicate that the compound is highly likely to meet the target dosing regimen of once-a-day. Changes in the circulating profile of adiponectin, the established biomarker of PPAR agonism, seen in this study suggests that DB959Na will be pharmacologically active in patients with type 2 diabetes within the well tolerated dose range utilized in this study. The study was a randomized, placebo-controlled, double-blind, escalating multiple dose clinical trial that enrolled 32 healthy male and female volunteers at Quintiles’ Phase 1 facility in Overland Park, Kansas. The company plans to present detailed results at an upcoming scientific meeting in the first half of 2012.
As presented earlier, preclinical results in validated models of human disease demonstrated that DB959 lowered glucose to normal levels, raised HDL, raised the HDL:LDL ratio, and lowered triglycerides. These beneficial effects on glucose and lipids were observed without causing the weight gain which has been seen with other PPAR agonists. The positive lipid effects (e.g., cholesterol and triglycerides) are important because approximately 85% of patients with type 2 diabetes also have lipid abnormalities. Also presented previously were the results of the company’s Phase 1a single-ascending-dose study, in which all doses were demonstrated to be safe and well-tolerated. These positive results will allow DB959 to enter Phase 2; DARA has begun planning for a Phase 2a study in patients with type 2 diabetes.
Steve Grossman, MD, Medical Consultant to DARA, said, “The positive safety results over a wide dose range in healthy volunteers and the evidence of pharmacologic activity provides a strong basis for the next phase of development.”
Richard A. Franco, CEO of DARA, said, “DARA is meeting its goals and now has two first-in-class drug candidates in clinical trials. DB959 is entering Phase 2 with a positive track record from both preclinical and now Phase 1 clinical studies, while KRN5500 has recently been granted Fast Track Drug status by the US FDA and has recently had the positive results from its Phase 2a study published in the Journal of Pain and Symptom Management.”
About DB959
DB959 activates certain nuclear receptors (peroxisome proliferator-activated receptors, PPARs) that regulate the genes involved in controlling blood sugar levels and certain lipids (e.g. total cholesterol, HDL-cholesterol, triglycerides). The compound acts as an agonist of PPAR-delta and PPAR-gamma.
About Adiponectin
Adiponectin is a fat tissue-derived plasma protein whose expression is regulated by PPAR-gamma. It may play a modulatory role in multiple metabolic processes; plasma levels of adiponectin correlate with insulin sensitivity and correlate inversely with percent body fat. Improvements in one’s metabolic health, as may be seen with weight loss, can be accompanied by increases in plasma adiponectin. Plasma adiponectin levels can be used as a biomarker or indicator of in vivo PPAR-gamma agonism. Numerous published studies have shown that PPAR-gamma agonists dose-dependently increase plasma adiponectin levels in both non-diabetic and diabetic populations at doses known to improve glucose homeostasis and insulin sensitivity.
About DARA BioSciences, Inc.
DARA is a clinical stage pharmaceutical development company that acquires high quality, promising therapeutic molecules in early stage development (late pre-clinical or Phase 1). Acquired molecules have the potential to fill significant medical needs and represent large commercial opportunities for participation in large and growing markets. DARA expedites development through proof-of-concept in humans (prior to Phase 3) for subsequent partnering, sale or out-licensing to large healthcare and pharmaceutical companies. The effective implementation of this strategy has the potential to greatly enhance return on investment.
Presently, DARA has two (2) lead drug candidates advancing through clinical trials. The first is KRN5500 for the treatment of neuropathic pain in patients with cancer, which has successfully completed a Phase 2a study. The second is DB959 for the treatment of type 2 diabetes and dyslipidemia, which has successfully completed both Phase 1a and 1b studies.
DARA also has three promising pre-clinical drug candidate programs for future development and monetization which include:
DB160 is a lead dipeptidylpeptidase (DPPIV) inhibitor from a family of DPPIV inhibitors. DPPIV is an enzyme that inactivates a key hormone involved in promoting control of blood sugar levels, thus giving people with diabetes better control of their blood sugar levels. Studies have demonstrated that potent DPPIV inhibitors may also be beneficial for stem cell transplantation and cancer targets.
DB900 is a series of compounds which are PPAR- agonists for the treatment of type 2 diabetes and inflammatory diseases. These compounds activate genes involved in the metabolism of sugars and fats, thereby improving the body's ability to regulate blood sugar. As such, they have the potential to raise HDL ‘good’ cholesterol, lower LDL ‘bad’ cholesterol, lower triglycerides, and facilitate weight loss.
DB200 is a series of compounds that inhibit the enzyme carnitine palmitoyltransferase-1 (CPT-1) for the topical treatment of psoriasis. These drug candidates have the potential to inhibit inflammation and the proliferation of skin cells, thus resulting in decreased reddening and flaking of the skin.
Safe Harbor Statement
All statements in this news release that are not historical are forward-looking statements within the meaning of the Securities Exchange Act of 1934, as amended. Such forward-looking statements are subject to factors that could cause actual results to differ materially for DARA from those projected. Those factors include risks and uncertainties relating to DARA's current cash position and its need to raise additional capital in order to be able to continue to fund its operations, risks and uncertainties relating to the potential delisting of DARA's common stock from the NASDAQ Capital Market, risks and uncertainties relating to DARA's ability to develop and bring new products to market as anticipated, the current regulatory environment in which the company develops and sells its products, the market acceptance of those products, dependence on partners, successful performance under collaborative and other commercial agreements, competition, the strength of DARA's intellectual property, the intellectual property of others, and other risk factors identified in the documents DARA has filed, or will file, with the Securities and Exchange Commission ("SEC"). Copies of DARA's filings with the SEC may be obtained from the SEC Internet site at http://www.sec.gov. DARA expressly disclaims any obligation or undertaking to release publicly any updates or revisions to any forward -looking statements contained herein to reflect an y change in DARA's expectations with regard thereto or any change in events, conditions, or circumstances on which any such statements are based. DARA BioSciences and the DARA logo are trademarks of DARA BioSciences, Inc.
The drug discovery and development process is highly uncertain, and we have not developed, and may never develop, a drug candidate that ultimately leads to a commercially viable drug. Our most advanced drug candidates are in the early stages of development, and we do not have any drugs approved for commercial sale. Before a drug product is approved by the FDA for commercial marketing, it is tested for safety and effectiveness in clinical trials that can take up to six years or longer. Promising results in preclinical development or clinical trials may not be predictive of results obtained in later clinical trials. A number of pharmaceutical companies have experienced significant setbacks in advanced clinical trials, even after obtaining promising results in earlier preclinical and clinical trials. At any time, the FDA may place a clinical trial on clinical hold, or temporarily or permanently stop the trial, for a variety of reasons, principally for safety concerns. We or our collaborators may experience numerous unforeseen events during, or as a result of, the clinical development process that could delay or prevent our drug candidates from being successfully commercialized, including: (1) Failure to achieve clinical trial results that indicate a candidate is effective in treating a specified condition or illness in humans; (2) Safety issues, including the presence of harmful side effects; (3) Determination by the FDA that the submitted data do not satisfy the criteria for approval; (4) Lack of commercial viability of the drug; (5) Failure to acquire, on reasonable terms, intellectual property rights necessary for commercialization; and (6) Existence of therapeutics that are more effective.
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