News Feed Item

Arisaph Pharmaceuticals Reports Positive Results From Two Safety Clinical Trials For Its Niacin Analog (ARI-3037MO)

BOSTON, Nov. 7, 2012 /PRNewswire/ --

  • ARI-3037MO was well tolerated in single and repeat ascending dose trials in healthy volunteers
  • ARI-3037MO did not provoke flushing or any other treatment-related adverse effects in 58 healthy male and female volunteers
  • ARI-3037MO was well absorbed orally and plasma levels demonstrated good dose proportionality
  • ARI-3037MO showed encouraging lipid changes in both clinical trials in healthy subjects

Arisaph Pharmaceuticals, Inc. announced today during an oral presentation at the American Heart Association (AHA) meeting in Los Angeles, CA that its niacin analog, ARI-3037MO, was extremely well tolerated in a single-ascending dose (SAD) and a multiple-ascending dose (MAD) trial in healthy male and female volunteers.  The results showed that ARI-3037MO did not provoke flushing or any other adverse skin changes, nor did it cause increases in liver enzymes or blood glucose at doses up to 6 grams per day. In both clinical trials, ARI-3037MO also demonstrated encouraging lipid effects. Based on these promising results, ARI-3037MO potentially represents a transformational, new niacin-like option for treatment of patients with dyslipidemia, especially in the setting of metabolic syndrome, a disorder that afflicts as many as 70 million Americans1

(Logo: http://photos.prnewswire.com/prnh/20110321/NE69091LOGO )

"The absence of flushing and other niacin induced adverse events highlights a differentiated safety profile for our novel niacin analog," said Christopher P. Kiritsy, Co-Founder, President and Chief Executive Officer of Arisaph Pharmaceuticals. "Moreover, the evidence of lipid changes in such short duration trials in healthy volunteers shows that our preclinical efficacy data are translating and breeds optimism for the development of our best-in-class niacin analog."   

In two placebo controlled, safety and pharmacokinetic trials (SAD and MAD), 58 healthy male and female volunteers were given either single escalating doses of ARI-3037MO (up to 6 grams per day) or repeat escalating doses of ARI-3037MO (up to 3.5 grams per day) for 14 days. In both trials, ARI-3037MO was given once daily without a titration scheme. The results showed that ARI-3037MO was extremely well tolerated with no treatment-related adverse events.  Specifically, treatment with ARI-3037MO did not show any evidence of flushing or adverse skin changes, such as itching or rash, using a validated visual-analog scale. Additionally, no deleterious changes in liver enzymes or blood glucose were observed with ARI-3037MO, even when given at high doses in a repeat-dose setting. 

The pharmacokinetics of ARI-3037MO revealed that the drug was well absorbed orally and showed good dose proportionality. In both clinical trials, ARI-3037MO produced encouraging lipid signals. For example, a single dose of 6 grams of ARI-3037MO produced a 15% increase in HDL and attenuated the postprandial increase in serum triglycerides (TGs). In the MAD trial, the 2g and 3.5g doses of ARI-3037MO decreased LDL-cholesterol (LDL-C) from baseline and improved post-prandial triglycerides by more than 30% compared with placebo. Such lipid trends are encouraging considering that the trials were short-duration, safety and pharmacokinetic studies in healthy volunteers and would not be expected to show pharmacodynamic effects.

"Niacin's efficacy across a broad range of lipid risk factors has long been recognized but flushing and increases in blood glucose have limited its use, particularly in high risk metabolic syndrome patients," commented Dr. Ernst Schaefer, Professor of Medicine, Tufts University School of Medicine. "The results from these two safety trials show that ARI-3037MO is devoid of such dose-limiting side effects, resulting in a significantly improved safety and tolerability profile compared with other niacin-based therapies."

In preclinical studies presented at the AHA in 2011, ARI-3037MO showed robust changes in lipids, including LDL-C, HDL-C and triglycerides. For example, once-daily treatments of ARI-3037MO lowered LDL-C in excess of 50% and lowered TGs by more than 70% compared with placebo in high-fat-fed hamster models. Additionally, non-clinical toxicology studies conducted in dogs and rats with ARI-3037MO showed that high exposure multiples could be achieved without serious adverse events, even at doses greater than 1000 mg per kilogram. The favorable preclinical safety and efficacy data reveal that ARI-3037MO has an extremely wide therapeutic index, indicating that ARI-3037MO will not be dose limited by adverse events. Consequently, it is expected that patients will be able to achieve improved efficacy observed with higher doses of niacin.  

About Niacin Analog Program:
The natural B vitamin niacin is a well-known lipid lowering agent, which has been used to treat mixed lipid disorders for over 50 years.  Niacin is a first-line drug for the treatment of hyperlipidemia, and it is used in combination with statins to further reduce LDL cholesterol and triglycerides or to increase HDL cholesterol in patients with depressed HDL cholesterol levels.  Niacin can produce changes in HDL cholesterol up to 35%, lower LDL cholesterol up to 25% and lower triglycerides up to 50%.  Despite niacin's broad lipid altering profile, the use of niacin-based therapies is diminished because of unpleasant side effects, particularly flushing.  Flushing, representative of tingling and/or redness of the skin, is the principal side effect of niacin, and in some patients it can be extremely uncomfortable.  Arisaph has developed a novel class of structural analogs of niacin that are expected to demonstrate a dramatically improved safety and tolerability profile while retaining the beneficial lipid effects associated with niacin.

About Arisaph
Arisaph Pharmaceuticals Inc, a drug discovery, biopharmaceutical company located in Boston, Massachusetts, was founded by Dr. William Bachovchin (Professor of Biochemistry, Tufts University School of Medicine), Christopher Kiritsy (Former EVP Corporate Development and CFO, Kos Pharmaceuticals, Inc.) and Michael Jaharis (Founder, Chairman Emeritus, Kos Pharmaceuticals, Inc.) to develop differentiated therapies for cardiometabolic diseases and cancer. Arisaph has developed a rich pipeline of products at various stages of development, including a niacin analog (ARI-3037MO), in phase 2 clinical development, and a small molecule immune modulator for the treatment of cancer. The Company's vision is to create a fully integrated pharmaceutical company, leveraging its drug discovery expertise to develop transformational, patent protected, medicines that offer distinct safety, efficacy and/or tolerability benefits compared with existing therapies for large markets, whose needs are not being fully met by current therapeutics.  

Certain statements in this press release, including statements regarding the Company's research and development effort, the Company's expectation to initiate or complete human clinical studies, the Company's ability to finance its development programs into human clinical testing, and the Company's ability to successfully capitalize on the early stage research are subject to risks and uncertainties. These risks and uncertainties include risks and uncertainties related to:  our ability to discover and develop new compounds and products using a novel approach to drug discovery; the early stage of all of our discovery and development efforts; our ability to complete preclinical and clinical development of our products; our ability to obtain and maintain regulatory approvals for our products; competition from other technologies and technologies similar to ours; obtaining, maintaining and protecting intellectual property utilized by our products; changes in legislation and regulations affecting our products and potential product candidates; our need to obtain additional funding to support our business activities; our dependence on collaborators and other third parties for development, manufacture, marketing, sales and distribution of products; the ability of our licensees to achieve developmental, regulatory and other milestones and to commercialize their products; the effect of conditions in the pharmaceutical industry and the economy in general, as well as certain other risks and uncertainties.


1. NHANES  Data, National Health Statistics Report, May 2009


Arisaph Pharmaceuticals, Inc.

Christopher Kiritsy

President and CEO

(617) 986-4500

SOURCE Arisaph Pharmaceuticals, Inc.

More Stories By PR Newswire

Copyright © 2007 PR Newswire. All rights reserved. Republication or redistribution of PRNewswire content is expressly prohibited without the prior written consent of PRNewswire. PRNewswire shall not be liable for any errors or delays in the content, or for any actions taken in reliance thereon.

Latest Stories
Without lifecycle traceability and visibility across the tool chain, stakeholders from Planning-to-Ops have limited insight and answers to who, what, when, why and how across the DevOps lifecycle. This impacts the ability to deliver high quality software at the needed velocity to drive positive business outcomes. In his session at @DevOpsSummit 19th Cloud Expo, Eric Robertson, General Manager at CollabNet, will show how customers are able to achieve a level of transparency that enables everyon...
In past @ThingsExpo presentations, Joseph di Paolantonio has explored how various Internet of Things (IoT) and data management and analytics (DMA) solution spaces will come together as sensor analytics ecosystems. This year, in his session at @ThingsExpo, Joseph di Paolantonio from DataArchon, will be adding the numerous Transportation areas, from autonomous vehicles to “Uber for containers.” While IoT data in any one area of Transportation will have a huge impact in that area, combining sensor...
@DevOpsSummit has been named the ‘Top DevOps Influencer' by iTrend. iTrend processes millions of conversations, tweets, interactions, news articles, press releases, blog posts - and extract meaning form them and analyzes mobile and desktop software platforms used to communicate, various metadata (such as geo location), and automation tools. In overall placement, @DevOpsSummit ranked as the number one ‘DevOps Influencer' followed by @CloudExpo at third, and @MicroservicesE at 24th.
“Media Sponsor” of SYS-CON's 19th International Cloud Expo, which will take place on November 1–3, 2016, at the Santa Clara Convention Center in Santa Clara, CA. CloudBerry Backup is a leading cross-platform cloud backup and disaster recovery solution integrated with major public cloud services, such as Amazon Web Services, Microsoft Azure and Google Cloud Platform.
In the next forty months – just over three years – businesses will undergo extraordinary changes. The exponential growth of digitization and machine learning will see a step function change in how businesses create value, satisfy customers, and outperform their competition. In the next forty months companies will take the actions that will see them get to the next level of the game called Capitalism. Or they won’t – game over. The winners of today and tomorrow think differently, follow different...
The Internet of Things (IoT), in all its myriad manifestations, has great potential. Much of that potential comes from the evolving data management and analytic (DMA) technologies and processes that allow us to gain insight from all of the IoT data that can be generated and gathered. This potential may never be met as those data sets are tied to specific industry verticals and single markets, with no clear way to use IoT data and sensor analytics to fulfill the hype being given the IoT today.
Ask someone to architect an Internet of Things (IoT) solution and you are guaranteed to see a reference to the cloud. This would lead you to believe that IoT requires the cloud to exist. However, there are many IoT use cases where the cloud is not feasible or desirable. In his session at @ThingsExpo, Dave McCarthy, Director of Products at Bsquare Corporation, will discuss the strategies that exist to extend intelligence directly to IoT devices and sensors, freeing them from the constraints of ...
So you think you are a DevOps warrior, huh? Put your money (not really, it’s free) where your metrics are and prove it by taking The Ultimate DevOps Geek Quiz Challenge, sponsored by DevOps Summit. Battle through the set of tough questions created by industry thought leaders to earn your bragging rights and win some cool prizes.
The Internet of Things will challenge the status quo of how IT and development organizations operate. Or will it? Certainly the fog layer of IoT requires special insights about data ontology, security and transactional integrity. But the developmental challenges are the same: People, Process and Platform and how we integrate our thinking to solve complicated problems. In his session at 19th Cloud Expo, Craig Sproule, CEO of Metavine, will demonstrate how to move beyond today's coding paradigm ...
Fifty billion connected devices and still no winning protocols standards. HTTP, WebSockets, MQTT, and CoAP seem to be leading in the IoT protocol race at the moment but many more protocols are getting introduced on a regular basis. Each protocol has its pros and cons depending on the nature of the communications. Does there really need to be only one protocol to rule them all? Of course not. In his session at @ThingsExpo, Chris Matthieu, co-founder and CTO of Octoblu, walk you through how Oct...
SYS-CON Events announced today that SoftNet Solutions will exhibit at the 19th International Cloud Expo, which will take place on November 1–3, 2016, at the Santa Clara Convention Center in Santa Clara, CA. SoftNet Solutions specializes in Enterprise Solutions for Hadoop and Big Data. It offers customers the most open, robust, and value-conscious portfolio of solutions, services, and tools for the shortest route to success with Big Data. The unique differentiator is the ability to architect and ...
A completely new computing platform is on the horizon. They’re called Microservers by some, ARM Servers by others, and sometimes even ARM-based Servers. No matter what you call them, Microservers will have a huge impact on the data center and on server computing in general. Although few people are familiar with Microservers today, their impact will be felt very soon. This is a new category of computing platform that is available today and is predicted to have triple-digit growth rates for some ...
Everyone knows that truly innovative companies learn as they go along, pushing boundaries in response to market changes and demands. What's more of a mystery is how to balance innovation on a fresh platform built from scratch with the legacy tech stack, product suite and customers that continue to serve as the business' foundation. In his General Session at 19th Cloud Expo, Michael Chambliss, Head of Engineering at ReadyTalk, will discuss why and how ReadyTalk diverted from healthy revenue an...
Without lifecycle traceability and visibility across the tool chain, stakeholders from Planning-to-Ops have limited insight and answers to who, what, when, why and how across the DevOps lifecycle. This impacts the ability to deliver high quality software at the needed velocity to drive positive business outcomes. In his general session at @DevOpsSummit at 19th Cloud Expo, Eric Robertson, General Manager at CollabNet, will discuss how customers are able to achieve a level of transparency that e...
SYS-CON Events announced today that Cemware will exhibit at the 19th International Cloud Expo, which will take place on November 1–3, 2016, at the Santa Clara Convention Center in Santa Clara, CA. Use MATLAB functions by just visiting website mathfreeon.com. MATLAB compatible, freely usable, online platform services. As of October 2016, 80,000 users from 180 countries are enjoying our platform service.