• Preclinical work on INS-3001 efficacy in renal fibrosis published

    We are glad to share that our latest preclinical work studying the efficacy of INS-3001 in the context of phosphate-induced renal fibrosis has been published in ACS Pharmacology & Translational Science.

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    Inositec Appoints Serial Entrepreneur and Cardiologist Michael H. Davidson to Board of Directors

    Zurich, Switzerland, October 7, 2020 Inositec, a pioneer in the development of life-saving small molecule drugs for calcification disorders such as aortic valve stenosis, announced today that Michael H. Davidson, MD, has been appointed to the Board of Directors. Currently CEO of New Amsterdam Pharma, Dr. Davidson was previously the founding CEO and Chief Scientific Officer of Corvidia Therapeutics, which was recently acquired by Novo-Nordisk. He also co-founded Omthera Pharmaceuticals, which was acquired by Astra Zeneca.

    “We are truly honored to have Michael join our Board of Directors. His expertise in cardiovascular research and development, and in successfully building biotech companies is an enormous asset to Inositec as we move our lead compound INS-3001 forward into clinical studies in aortic valve stenosis,” stated Dr. Mattias Ivarsson, CEO of Inositec.

    “Aortic valve stenosis is a disease with a high unmet medical need and I am therefore excited to work with the Inositec team to move INS-3001 into clinical development as a first-in-class therapy in this space,” said Dr. Davidson. “There is currently no treatment for cardiovascular calcification despite the fact that it has a dramatic impact on normal cardiovascular function leading to high morbidity and mortality in a multitude of diseases. I was fascinated by the potential of Inositec’s novel small molecules to address the issues caused by this excess of calcium deposits.”   

    Dr. Davidson is a leading expert in the field of lipidology research, with a background that encompasses both pharmaceutical and nutritional clinical trials, including extensive research on statins, novel lipid-lowering drugs, and omega-3 fatty acids. He was also named in “The Best Doctors in America” list for the past 15 years. Dr. Davidson also serves as Clinical Professor and Director of the Lipid Clinic at the University of Chicago Pritzker School of Medicine. He also founded the Chicago Center for Clinical Research, which became the largest investigator site in the United States and was acquired by Pharmaceutical Product Development in 1996. He is board-certified in internal medicine, cardiology, and clinical lipidology, and served as President of the National Lipid Association from 2010 to 2011. Dr. Davidson received his BA/MS from Northwestern University and MD from The Ohio State University School of Medicine.

    About Inositec

    Inositec is pioneering the development of life-saving small molecule drugs based on inositol phosphate, a natural facilitator of diverse cellular functions. Using its broadly applicable InosituneÔ technology to adjust the chemical and physical properties of inositol phosphate (IP6) analogs, Inositec is developing a novel class of drugs currently focusing on high-unmet medical needs related to calcification disorders. The lead compound INS-3001 is a cardiovascular calcification inhibitor in development for aortic valve stenosis. Inositec was founded in December 2015 based on the award-winning research of Dr. Mattias Ivarsson, Prof. Jean-Christophe Leroux and Prof. Bastien Castagner at ETH Zurich, Switzerland. Further information can be found at www.inositec.com.

    Contacts:

    Inositec Halsin Partners
    Mattias Ivarsson Mike Sinclair
    CEO and Co-Founder Partner
    +41 44 271 07 55 +44 (0)20 7318 2955
    info@inositec.com msinclair@halsin.com

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    Inositec Granted US Composition of Matter Patent for Cardiovascular Calcification Inhibitor INS-3001

    Zurich, Switzerland, May 4, 2020 Inositec, a pioneer in the development of life-saving small molecule drugs based on the natural compound inositol hexaphosphate (IP6), announced today that the U.S. Patent and Trademark Office (USPTO) has issued a patent covering its platform of inositol phosphate analogs and specifically INS-3001, an inhibitor of pathological soft tissue calcification. Calcification, particularly in arterial walls and cardiac valves, leads to high cardiovascular morbidity and mortality. Inositec is developing INS-3001 for a number of cardiovascular indications caused by calcification, including aortic valve stenosis. U.S. patent number 10,624,909 covers specifically the composition of matter and use of inositol derivatives for conditions related to pathological calcium crystallization.

    “The issuance of this strong composition of matter patent with its broad claims confirms the innovative nature of our therapeutic approach and allows us to bring our drug candidates to those patients who need them most. The first indication for our lead asset INS-3001 is aortic valve stenosis and we look forward to continuing our progress towards clinical studies,” stated Dr. Mattias Ivarsson, CEO of Inositec.

    About INS-3001

    INS-3001 is a calcification inhibitor based on IP6. In preclinical studies, INS-3001 was found to display superior efficacy, and more favorable pharmacokinetic and tolerability profiles than IP6 itself. The scientific foundations supporting the role of INS-3001 in several potential therapeutic indications has been rigorously validated in a variety of preclinical calcification models. INS-3001 was well tolerated in these preclinical studies.

    About Inositec

    Inositec is pioneering the development of life-saving small molecule drugs based on inositol phosphate, a natural facilitator of diverse cellular functions. Using its broadly applicable InosituneÔ technology to adjust the chemical and physical properties of inositol phosphate (IP6) analogs, Inositec is developing a novel class of drugs currently focusing on high-unmet medical needs related to calcification disorders. Inositec was founded in December 2015 based on the award-winning research of Dr. Mattias Ivarsson, Prof. Jean-Christophe Leroux and Prof. Bastien Castagner at ETH Zurich, Switzerland. Further information can be found at www.inositec.com.

    Contacts:

    Inositec Halsin Partners
    Mattias Ivarsson Mike Sinclair
    CEO and Co-Founder Partner
    +41 44 271 07 55 +44 (0)20 7318 2955
    info@inositec.com msinclair@halsin.com
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    Preclinical work on calcium oxalate inhibitors for renal indications published

    We are thrilled to have published data in Advanced Science that further validates the therapeutic potential of IP6 analogs from Inositec’s InosituneTM platform in calcification disorders, here in the context of calcium oxalate crystal-related diseases. Calcium oxalate is the most common component of kidney stones.

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    Inositec’s INS-3001 Significantly Reduces Cardiovascular Calcification in Proof-of-Concept Studies Published in Nature Communications

    Zurich, Switzerland, February 5, 2020 Inositec, a pioneer in the development of life-saving small molecule drugs based on myo-inositol hexaphosphate (IP6), announced today that positive proof-of-concept data on INS-3001, a novel cardiovascular calcification inhibitor, were published in Nature Communications (DOI: 10.1038/s41467-019-14091-4). INS-3001 was found to be a potent and well tolerated inhibitor of pathological soft tissue calcification in preclinical studies. Calcification, particularly in arterial walls and cardiac valves, leads to an increase in cardiac events. Inositec is developing INS-3001 for a number of cardiovascular indications caused by calcification, including aortic valve stenosis.

    This paper describes designing chemical modifications to IP6 to produce more potent inhibitors with improved pharmacokinetic properties that may enable its convenient administration in an ambulatory care setting. IP6 has been previously found to inhibit cardiovascular calcification progression but  has to date been investigated primarily in clinical trials using intravenous infusion during hemodialysis sessions.

     “These peer-reviewed data show that INS-3001 is well tolerated, has excellent  calcification inhibition potency, and a pharmacokinetic profile that could make this a potential treatment option to a wide variety of patients suffering from the deleterious effects of cardiovascular calcification.  We have now rigorously validated the scientific foundations supporting the role of INS-3001 in several potential therapeutic indications, the first of which that Inositec will be targeting is aortic valve stenosis,” stated Dr. Mattias Ivarsson, CEO of Inositec. “We’d like to thank the valuable contributions from our collaborators on all our research to date, particularly in advancing this paper to publication.”

    A small library of IP6 analogs were synthesized and screened for their ability to inhibit calcification and for their resistance towards hydrolysis. The lead candidate, INS-3001, was found to display superior efficacy, as well as more favorable pharmacokinetic and tolerability profiles than IP6. It potently stabilized calciprotein particle growth and consistently demonstrated low micromolar activity in different in vitro models of cardiovascular calcification. INS-3001 also largely abolished the development of cardiovascular calcification in rodent models, while not causing toxicity related to serum calcium chelation. The published data furthermore suggest a mechanism of action independent of the etiology of cardiovascular calcification, whereby INS-3001 disrupts the nucleation and growth of pathological calcification regardless of its underlying cause.

    About Inositec

    Inositec is pioneering the development of life-saving small molecule drugs based on inositol phosphate, a natural facilitator of diverse cellular functions. Using its broadly applicable InosituneTM technology to adjust the chemical and physical properties of inositol phosphate analogs, Inositec is developing a novel class of drugs currently focusing on high-unmet medical needs related to calcification disorders, including aortic valve stenosis. Inositec was founded in December 2015 based on the award-winning research of Dr Mattias Ivarsson, Prof Jean-Christophe Leroux and Prof Bastien Castagner at ETH Zurich, Switzerland. Further information can be found at www.inositec.com.

    Contacts:

    Inositec Halsin Partners
    Mattias Ivarsson Mike Sinclair
    CEO and Co-Founder Partner
    +41 44 271 07 55 +44 (0)20 7318 2955
    info@inositec.com msinclair@halsin.com
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    Discovery work on Clostridium difficile toxin inhibitors published

    The early work on the rational design of Clostridium difficile toxin inhibitors based on inositol hexaphosphate analogs has been published in Cell Chemical Biology.

    Our Clostridium difficile inhibitors are available for partnering and we are happy to discuss further details with interested parties. Please contact info@inositec.com for further information.

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    Inositec’s INS-3001 Significantly Reduces Vascular Calcification Data Presented at Kidney Week 2018 Indicates

    Zurich, Switzerland, 26 October 2018 Inositec, a pioneer in the development of life-saving small molecule drugs based on myo-inositol hexaphosphate (IP6), announced today that INS-3001, a novel vascular calcification inhibitor, demonstrated the ability to significantly inhibit the calcification process in preclinical studies. The build-up of calcium deposits in arterial walls and cardiac valves lead to an increase in cardiac events, particularly in patients with chronic kidney disease. Data was presented in three abstracts at the American Society of Nephrology’s Annual Meeting Kidney Week 2018 (23-28 October).

    “At present, there is no approved treatment for vascular calcification and affected individuals are left at great risk of experiencing cardiovascular events and death. The data we presented at Kidney Week shows that our novel vascular calcification inhibitor, INS-3001, possesses superior potency and pharmacokinetics to the natural IP6 molecule in terms of inhibiting vascular calcification. This suggests that INS-3001 could provide significant patient benefit if confirmed in clinical studies,” stated Dr. Mattias Ivarsson, CEO of Inositec. “We are now conducting our IND-enabling studies, with first-in-human studies scheduled to begin in 2019.”

    Data Presented at Kidney Week

    To develop a new class of inhibitors of vascular calcification, Inositec conducted multi-step syntheses, starting from protected myo-inositol species, involving selective PEGylation, phosphorylation or sulfation to build a library of novel IP6 analogs with improved drug-like properties. IP6 has previously been shown to be a potent inhibitor of calcification. Data presented from in vitro experiments showed that INS-3001 was superior to natural IP6 with regard to efficacy and stability in a serum calcification propensity assay. INS-3001 also had efficacy superior to IP6 in cell culture studies performed on primary human vascular smooth muscle cells treated with either calciprotein particles or calcification medium to induce formation of calcified deposits.

    In rats, INS-3001 administration significantly blunted carotid calcification following vitamin D overdose, reducing the amount of calcium in tissues by a factor of two compared to controls while a numerical decrease was observed at the level of abdominal aorta. INS-3001 also showed a beneficial effect on the renal function of animals in this model.

    The effect of INS-3001 was further evaluated in vitamin D-warfarin induced calcification in rats. In the abdominal aorta, significantly lower total calcium content was measured in the INS-3001 groups compared to the vehicle group following bolus subcutaneous dosing. The von Kossa positivity (area% of stained tissue representing the extent of calcification) of the abdominal aorta was also significantly lower in the INS-3001 groups compared to the vehicle group. The effects on both the total calcium and the von Kossa positivity were dose-dependent, and correlated with mortality. Similar reductions in total calcium content and area% von Kossa positivity were seen in the thoracic aorta, and the femoral and carotid arteries.

    The uremic state appeared to significantly influence the rat plasma pharmacokinetics of INS-3001 after subcutaneous and intravenous administration, suggesting that uremia extended plasma exposure of INS-3001 without increasing peak plasma levels.

    About Inositec

    Inositec is pioneering the development of life-saving small molecule drugs based on inositol phosphate, a natural facilitator of diverse cellular functions. Using its broadly applicable InosituneTM technology to adjust the chemical and physical properties of inositol phosphate analogs, Inositec is developing a novel class of drugs currently focusing on high-unmet medical needs related to calcification disorders. Inositec was founded in December 2015 based on the award-winning research of Dr Mattias Ivarsson, Prof Jean-Christophe Leroux and Prof Bastien Castagner at ETH Zurich, Switzerland. Further information can be found at www.inositec.com.

    Contacts:

    Inositec
    Mattias Ivarsson
    CEO and Co-Founder
    +41 44 271 07 55
    info@inositec.com

    Halsin Partners
    Mike Sinclair
    +44 (0)20 7318 2955
    msinclair@halsin.com

     

    Links to posters:

    Verhulst et al – INS‐3001 efficiently inhibits severe vascular calcifications
    by direct interference with vessel wall calcification

    Schantl et al – Identification and in vitro characterization of a novel inhibitor of vascular calcification

    Maillard et al – Pharmacokinetic and pharmacodynamic evaluation of a new vascular calcification inhibitor (INS-3001) in rats

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    Inositec AG Appoints Dr Frits van Alphen as Chief Medical Officer

    Zurich, Switzerland, 18 January 2018 Inositec, a pioneer in the development of life-saving small molecule drugs based on inositol hexaphosphate (IP6), announced today the appointment of Frits van Alphen, MD, as Chief Medical Officer.

    Dr van Alphen has over 20 years of experience in clinical development and medical affairs, employed in roles of increasing responsibility. He has joined Inositec from Roche, where he headed the operational excellence team. He previously was Chief Medical Officer at Vifor Pharma, Head Medical Affairs Europe at Novartis as well as heading their Clinical Operations team in the Netherlands. Dr van Alphen has hands-on experience running Phase I to Phase IV studies across several therapeutic areas, including cardiovascular and metabolic diseases, and nephrology. As a physician, Dr van Alphen worked several years in anesthesiology and intensive care. Dr van Alphen earned his medical degree at Leiden University, the Netherlands.

    “As CMO at Inositec, I have the golden opportunity to utilize my broad experience and entrepreneurial mind-set to develop new medicines. These innovative products have the potential to significantly advance patient care in vascular and other calcification disorders, all with high unmet medical need,” said Dr van Alphen.

    “Dr van Alphen is a key addition to Inositec’s team as we enter IND/CTA-enabling studies with our lead program in the vascular calcification space and fine-tune our clinical strategy in view of first-in-human studies in 2019,” said CEO Dr Mattias Ivarsson.

    About Inositec

    Inositec is pioneering the development of life-saving small molecule drugs based on inositol phosphate, a natural facilitator of diverse cellular functions. Using its broadly applicable InosituneTM technology to adjust the chemical and physical properties of inositol phosphate analogs, Inositec is developing a novel class of drugs currently focusing on high-unmet medical needs related to calcification disorders. Inositec was founded in December 2015 based on the award-winning research of Dr Mattias Ivarsson, Prof Jean-Christophe Leroux and Prof Bastien Castagner at ETH Zurich, Switzerland. Further information can be found at www.inositec.com.

    Contacts:

    Inositec
    Mattias Ivarsson
    CEO and Co-Founder
    +41 44 271 07 55
    info@inositec.com

    Halsin Partners
    Mike Sinclair
    +44 (0)20 7318 2955
    msinclair@halsin.com

     

     

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    Inositec wins Swiss Technology Award 2017

    We are proud to have won the Swiss Technology Award 2017. More information here (German).

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    Inositec featured in BioCentury

    BioCentury is featuring Inositec in this week’s emerging company profile. Read the article here (requires subscription).

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