An Open Label 52-week Study to Evaluate the Safety and Efficacy of Tegaserod Given Orally for the Treatment of Opioid-induced Constipation (OIC) in Patients With Chronic Non-cancer Pain

This study will evaluate the safety and efficacy of Tegaserod in opioid-induced constipation in patients with non-cancer pain.
Patients who enter this study PRIOR to the core study (CHTF919N2201) interim analysis receive the treatment as follows:
Patients will be randomly assigned to receive open label tegaserod 6 mg b.i.d. or tegaserod 12 mg o.d. using an allocation ratio of 1:1.
Patients who enter this study AFTER the core study interim analysis receive the treatment as follows:
Patients will be assigned to receive the selected tegaserod dose regimen (as determined by the core study interim analysis) in an open label fashion.

Start Date01 Feb 2007

Sponsor / Collaborator

Novartis AG

NCT00390975 / TerminatedPhase 4

An Open-label Pilot Trial to Assess the Effect of Tegaserod on Improvement of Gastric Emptying in Patients With Diabetic Gastroparesis and Upper Gastrointestinal Symptoms

This study will assess gastric emptying in patients with symptoms of diabetic gastroparesis treated with tegaserod over 2 weeks.

Start Date01 Jan 2007

Sponsor / Collaborator

Novartis AG

NCT00399659 / TerminatedPhase 3

A 52-week Extension to Study CHTF919N2201 to Evaluate the Safety and Efficacy of Tegaserod (6 mg b.i.d. and 12 mg o.d.) Given Orally for the Treatment of Opioid-induced Constipation (OIC) in Patients With Chronic Non-cancer Pain

This study will evaluate the safety and efficacy of Tegaserod in opioid-induced constipation (OIC) in patients with non-cancer pain.
Patients who enter this study PRIOR to the core study (CHTF919N2201) interim analysis (IA) receive the treatment as follows:
Patients on tegaserod 6 mg twice daily (b.i.d.) or 12 mg once daily (o.d.) in the core study will remain on the same dose in the extension (double-blind).
Patients on placebo during the core study will receive tegaserod 12 mg o.d. (open-label)
Patients who enter this study AFTER the core study interim analysis will receive the selected tegaserod dose regimen (open-label) determined by the core study IA.

Start Date01 Nov 2006

Sponsor / Collaborator

Novartis AG

100 Clinical Results associated with Tegaserod maleate

100 Translational Medicine associated with Tegaserod maleate

100 Patents (Medical) associated with Tegaserod maleate

464

Literatures (Medical) associated with Tegaserod maleate

10 Oct 2024·JOURNAL OF MEDICINAL CHEMISTRY

Discovery and Development of Highly Potent and Orally Bioavailable Nonpeptidic α_vβ₆ Integrin Inhibitors

Article

Author: Macdonald, Simon J. F. ; Copley, Royston C. B. ; Barrett, Tim N. ; Pritchard, John M. ; Slack, Robert J. ; Crawford, Matthew H. J. ; Hancock, Ashley P. ; Lippa, Rhys A. ; Thorp, Lee R. ; Barrett, John ; Procopiou, Panayiotis A. ; Sollis, Steven L. ; Hatley, Richard J. D. ; Rowedder, James E.

A series of 3-aryl((S)-3-fluoropyrrolidin-1-yl)butanoic acids were developed as potent orally bioavailable α_vβ₆ integrin inhibitors. Starting from a zwitterionic peptidomimetic series optimized for inhaled administration, the balancing of potency and passive permeability to achieve suitable oral agents through modification and exploration of aryl substituents and pK_a of the central cyclic amine is described. (S)-4-((S)-3-Fluoro-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)-3-(3-(2-methoxyethoxy)phenyl)butanoic acid was found to have highly desirable oral pharmacokinetic profiles in rat, dog, and minipig, with low to moderate clearance (26%, 7%, and 18% liver blood flow, respectively), moderate volumes of distribution (3.6, 1.4, and 0.9 L/kg, respectively), high to complete oral bioavailabilities, high α_vβ₆ integrin potency of pIC50 of 8.0, and high solubility in physiological media (>2 mg/mL). Equating to the estimated human dose range of 10-75 mg b.i.d. to achieve 90% α_vβ₆ target engagement at C_min, it was selected for further investigation as a potential therapeutic agent for the treatment of idiopathic pulmonary fibrosis.

23 May 2024·EXPERT OPINION ON PHARMACOTHERAPY

Current and future pharmacotherapies for the management of constipation-predominant irritable bowel syndrome

Review

Author: Jacenik, Damian ; Fichna, Jakub ; Biniszewska, Olga ; Tarasiuk, Aleksandra

INTRODUCTION:

Irritable bowel syndrome (IBS) is a common gastrointestinal disorder affecting 9-23% of the world's population, with a higher prevalence among women. IBS is a complex disorder influenced by psychosocial, physiological, and genetic factors, exacerbated by stress.

AREAS COVERED:

Research confirms that the most common subtype of IBS is IBS-C. Therefore, new therapies are being developed to speed up bowel movement and reduce constipation, with drugs such as linaclotide, plecanatide, lubiprostone, or tegaserod available to reduce IBS-C symptoms. In addition, patients' condition is improved by foods rich in fiber and low in FODMAP and the use of biotics.

EXPERT OPINION:

The topic is of great importance due to the growing number of patients suffering from IBS-C and its significant impact on quality of life. Current clinical trials of new therapeutic options are not too successful, and it seems that one of the plausible treatment options could be the multi-drug cocktail with some, or perhaps even all its ingredients emerging from drug re-purposing. Another important path that needs to be explored further in IBS-C patients is the adjustment of dietary habits and/or introduction of dietary or nutritional intervention.

01 Oct 2023·Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie

Corrigendum to “Tegaserod maleate exhibits antileukemic activity by targeting TRPM8” [Biomed. Pharmacother. 154 (2022) 113566]

Author: Yang, Wanwen ; Li, Luyao ; Zhou, Xuan ; Zhao, Chenbo ; Li, Yuhua ; Qiu, Zeyou ; Zhang, Keqin ; Chen, Zhuanzhuan ; Bai, Xiaochun ; Xie, Xiaoling ; Qiu, Yingqi ; Zhang, Wuju ; Lu, Yao ; Wang, Hao ; Lai, Eryong ; Hu, Yuxing

News (Medical) associated with Tegaserod maleate

26 Sep 2023

·www.biopharmadive.com

Intercept, after biotech rollercoaster ride, agrees to buyout by Alfasigma

Liver drug developer Intercept Pharmaceuticals has agreed to be acquired by Italian company Alfasigma for about $800 million, the companies announced Tuesday, ending one of biotechnologys most noteworthy stories of investor exuberance and clinical disappointment in the last decade.Alfasigma will pay Intercept investors $19 per share in cash, an 82% premium from Intercepts closing price on Monday. Alfasigma will fund the transaction with cash on hand and corporate credit facilities, and expects to close the deal by the end of 2023.With the acquisition, Alfasigma will gain Ocaliva, a drug that treats the rare autoimmune disorder primary biliary cholangitis, or PBC, which had sales of $152 million in the first six months of the year. The company recorded losses of $38 million over the same period.Alfasigma executives said the transaction will help it develop its U.S. presence. Intercept represents a compelling fit with Alfasigmas core business areas of gastroenterology and hepatology, and we believe that the transaction represents a transformational opportunity for both companies, said Alfasigma CEO Francesco Balestrieri in a statement.A closely held company controlled by the family of its founder, Alfasigma markets drugs like Zelnorm and rifaximin for irritable bowel syndrome and sulodexide for post-thrombotic syndrome. It also provides contract manufacturing services, as well as nutritional supplements. Its factory in Shreveport, Louisiana,manufactures nutritional supplements for the U.S. market.While Ocalivafirst gained approval for PBC, the drugs potential in the liver disease NASH drove investor enthusiasm in Intercept. NASH, or non-alcoholic steatohepatitis, is a disease connected with obesity, and its believed to be growing widely in prevalence.In 2014, a National Institutes of Health Phase 2 study of Ocaliva in people with NASH was stopped early because it had met its primary goal improvement in disease activity score at an interim analysis. Shares in the company nearly quadrupled in value and took the companys valuation to more than $7 billion, sparking an investor rush to find other companies working on NASH drugs.The path to regulators was not straightforward, however. Intercept reported positive Phase 3 data in 2019, but the FDA asked for longer-term data,rejectingIntercepts first NASH application.The FDA turned back a second application earlier this year, as Ocalivas only modest benefit was balanced against signs of liver damage experienced by some trial participants given the drug. Following that rejection, Intercept canceled all work in NASH, claiming it wasnt economically feasible to collect the data asked for by the FDA, and laid off staff.Meanwhile, competition in Intercepts established market of PBC may be emerging, as CymaBays seladelpar and Genfits elafibranor near key milestones.Raymond James analyst Steven Seedhouse described the transaction as a great return for Intercept investors.Given our bullish view of seladelpar and its ability to take market share in PBC beginning as early as late 2024, it isnt clear to us if [Ocaliva] will even generate that much net profit in the next ~10 years, Seedhouse wrote in a note to clients. '

Clinical ResultAcquisitionPhase 2Drug ApprovalPhase 3

08 Mar 2023

·www.biospace.com

Pliant Therapeutics Announces Appointments of Darren Cline and Thomas McCourt to Board of Directors

SOUTH SAN FRANCISCO, Calif., March 08, 2023 (GLOBE NEWSWIRE) -- Pliant Therapeutics, Inc. (Nasdaq: PLRX), a clinical stage biotechnology company focused on discovering and developing novel therapeutics for the treatment of fibrosis, today announced the appointments of Darren Cline and Thomas McCourt to its Board of Directors. "I am pleased to welcome Darren and Thomas whose extensive commercial and operational expertise will be crucial as we progress toward late-stage clinical development,” said Bernard Coulie, M.D., Ph.D., President and Chief Executive Officer of Pliant Therapeutics. “I am confident that their insights and experience will prove invaluable as we execute on our strategy to bring potentially transformative therapeutics to patients.” Mr. Cline is a seasoned pharmaceutical industry executive with over 30 years of strategic and operational experience in building commercial organizations. Mr. Cline currently serves as Chief Executive Officer and President of Epygenix Therapeutics, a clinical stage company developing therapies for rare epilepsies. Prior to this, Mr. Cline served as the U.S. Chief Commercial Officer of GW Pharmaceuticals (acquired by Jazz Pharmaceuticals), where he was responsible for commercial and medical affairs activities associated with Epidiolex®. Prior to joining GW Pharmaceuticals, Mr. Cline held the role of Executive Vice President, Commercial at Seagen where he managed operations with the commercial launch of Adcetris®. Prior to joining Seagen, Mr. Cline held key commercial leadership roles at Intermune, Alexion and Amgen. Mr. Cline currently serves on the board of directors of Pyxis Oncology. Mr. Cline received his B.S. in Business Marketing from San Diego State University and an MBA from Pepperdine University. Mr. McCourt is an accomplished biopharmaceutical executive with over 30 years of experience building commercial strategies and capabilities across multiple companies. Mr. McCourt currently serves as Chief Executive Officer of Ironwood Pharmaceuticals, a role he has held since June 2021. Since joining Ironwood in 2009, Mr. McCourt has served as Senior Vice President of Marketing and Sales, Chief Commercial Officer, and President, leading the commercial launch of LINZESS®, now a blockbuster product. Prior to joining Ironwood, Mr. McCourt led the U.S. brand team for Prolia® at Amgen and held several senior commercial roles within Novartis AG, including leading the launch and growth of ZELNORM™. In addition, Mr. McCourt was a founding team member at Astra Merck Inc., where he led the development of the medical affairs and science liaison group, and then served as brand manager for PRILOSEC® and NEXIUM®. Mr. McCourt also served as an independent director and chair of the nominating and corporate governance committee at Acceleron Pharma before their acquisition. In 2022, he received the ASGE President’s Award in recognition of his pivotal contribution to the field of gastrointestinal endoscopy and treatment. Mr. McCourt received his B.S. degree in Pharmacy and Pharmacology from the University of Wisconsin at Madison. Forward-Looking Statements Statements contained in this press release regarding matters that are not historical facts are "forward-looking statements" within the meaning of the Private Securities Litigation Reform Act of 1995. Words such as "may," "will," "expect," "anticipate," "estimate," "intend," and similar expressions (as well as other words or expressions referencing future events, conditions, or circumstances) are intended to identify forward-looking statements. These statements include those regarding development of our product candidates and corporate strategy. Because such statements deal with future events and are based on our current expectations, they are subject to various risks and uncertainties and actual results, performance or achievements of Pliant Therapeutics could differ materially from those described in or implied by the statements in this press release. These forward-looking statements are subject to risks and uncertainties, including those related to the development and commercialization of our product candidates, including any delays in our ongoing or planned preclinical or clinical trials, the impact of the ongoing COVID-19 pandemic on our business, operations, clinical supply and plans, our reliance on third parties for critical aspects of our development operations, the risks inherent in the drug development process, the risks regarding the accuracy of our estimates of expenses and timing of development, our capital requirements and the need for additional financing, and our ability to obtain and maintain intellectual property protection for our product candidates. These and additional risks are discussed in the sections titled "Risk Factors" and "Management's Discussion and Analysis of Financial Condition and Results of Operations" in our Annual Report on Form 10-K filed for the year ended December 31, 2021 which we filed with the SEC on March 1, 2022, as updated by our Quarterly Report on Form 10-Q for the quarter ended September 30, 2022, which we filed with the SEC on November 8, 2022, each available on the SEC's website at Unless otherwise noted, Pliant is providing this information as of the date of this news release and does not undertake any obligation to update any forward-looking statements contained in this document as a result of new information, future events or otherwise. About Pliant Therapeutics, Inc. Pliant Therapeutics is a clinical stage biopharmaceutical company focused on discovering and developing novel therapies for the treatment of fibrosis. Pliant's lead product candidate, bexotegrast (PLN-74809), is an oral small molecule dual selective inhibitor of αvß6 and αvß1 integrins that is in development in the lead indications for the treatment of idiopathic pulmonary fibrosis, or IPF, and primary sclerosing cholangitis, or PSC. Bexotegrast has received Fast Track Designation and Orphan Drug Designation from the U.S. Food and Drug Administration (FDA) in IPF and PSC and Orphan Drug Designation from the European Medicines Agency in IPF and PSC. Pliant is currently conducting Phase 2a trials of bexotegrast in the lead indications of IPF and PSC. Pliant has also developed PLN-1474, a small molecule, selective inhibitor of αvß1 for the treatment of nonalcoholic steatohepatitis, or NASH with liver fibrosis. Pliant is initiating a Phase 1 study for its third clinical program, PLN-101095, a small molecule, dual-selective inhibitor of αvß8 and αvß1 integrins, that is being developed for the treatment of solid tumors. In addition to clinical stage programs, Pliant currently has a preclinical program targeting muscular dystrophies. For additional information about Pliant Therapeutics, visit and follow us on Twitter, LinkedIn, Facebook and YouTube. Investor and Media Contact: Christopher Keenan Vice President, Investor Relations and Corporate Communications Pliant Therapeutics, Inc. IR@Pliantrx.com

Orphan DrugPhase 2Phase 1Fast TrackExecutive Change

06 Sep 2022

·www.globenewswire.com

Landos Biopharma Announces Appointment of Fabio Cataldi, MD, as Chief Medical Officer

Dr. Cataldi Brings Over Two Decades of Clinical Research and Drug Development Experience in Gastroenterology and ImmunologyNEW YORK, Sept. 06, 2022 (GLOBE NEWSWIRE) -- Landos Biopharma, Inc. (NASDAQ: LABP), a clinical-stage biopharmaceutical company developing novel, oral medicines for patients with autoimmune diseases, today announced the appointment of Fabio Cataldi, MD, as the Company’s Chief Medical Officer, effective September 5, 2022. “We are thrilled to welcome Fabio to Landos, and look forward to benefitting from his extensive clinical and drug development experience as we finalize our portfolio review and execute a focused plan to pursue what we believe are the Company’s most promising molecules and target indications,” said Greg Oakes, President and Chief Executive Officer of Landos. “Fabio’s clinical and research expertise in gastroenterology and immunology, particularly in ulcerative colitis (UC), will be integral as we look to advance NX-13 following our recent announcement of positive top-line results from our Phase 1b trial in UC patients.” Dr. Cataldi joins Landos with more than twenty years of successful experience in the development and commercialization of innovative therapies. He brings deep clinical, medical and scientific knowledge and expertise in immunology and gastroenterology, having served in senior research and development roles at Arena Pharmaceuticals, AbbVie, Shire, Pfizer, Biogen and Novartis. Most recently, Dr. Cataldi served as Arena’s Vice President and Therapeutic Area Head Gastroenterology, where he helped lead the development of etrasimod, until its sale to Pfizer for nearly $7 billion. “Fabio’s appointment as Chief Medical Officer is an important step as we look to continue selectively growing our leadership team with the talent and expertise that we need to successfully advance our pipeline. We are in the final stages of reviewing our clinical development plans, and are planning to provide a comprehensive update later this year,” continued Mr. Oakes. “I am excited to join Landos at such a pivotal time for the Company,” said Dr. Cataldi. “Having spent the majority of my career focused on immunology and gastroenterology drug development, I am looking forward to leveraging my background and experience as I work with Greg and the leadership team to build on Landos’ strong clinical foundation and deliver on its mission of addressing the therapeutic gap for patients with autoimmune diseases.” About Fabio Cataldi, MDDr. Cataldi has over twenty years of diverse and extensive experience in medicine and drug development in the United States and Italy. He most recently served as Vice President and Therapeutic Area Head of Gastroenterology at Arena Pharmaceuticals, where he led the development of etrasimod in inflammatory bowel disease (IBD) and other gastrointestinal (GI) indications and expanded the immunology portfolio. Prior to joining Arena Pharmaceuticals, Dr. Cataldi served as Team Lead of Gastroenterology and Immunology in Global Pharmaceutical Research and Development at AbbVie. Previously, Dr. Cataldi worked at Shire as Vice President of Clinical Development in Internal Medicine/Gastroenterology, where he led the expansion of the IBD portfolio with the out licensing of the anti-MAdCAM antibody from Pfizer. Before Shire, Dr. Cataldi served as Pfizer’s Senior Director of Gastroenterology Biotherapeutics Clinical Programs in Worldwide R&D, where he led the expansion of the Immunology and GI portfolio with assets targeting multiple diseases beyond IBD, including rheumatoid arthritis, systemic lupus erythematosus and dermatology conditions. Earlier in his career, Dr. Cataldi held roles at: Biogen Idec, where he oversaw the approval and launch of Tysabri in Crohn’s Disease; Novartis, where he supported the launch of Zelnorm for treatment of irritable bowel syndrome with constipation; Solvay Pharmaceuticals, where he helped with the New Drug Admission process with the U.S. Food and Drug Administration for Creon; and Beth Israel Deaconess Medical Center in Boston, MA. Dr. Cataldi holds an MD from the Second University of Naples (SUN) in Medicine and Surgery. About Landos BiopharmaLandos Biopharma is a clinical-stage biopharmaceutical company focused on the discovery and development of oral therapeutics for patients with autoimmune diseases. We believe we were the first to identify and target LANCL2, NLRX1 and PLXDC2, which are immunometabolic pathways or targets. We have identified seven novel immunometabolic pathways or targets based on predictions of immunometabolic function using a proprietary advanced artificial intelligence-based integrated computational and experimental precision medicine platform. Our near-term focus is on our clinical-stage programs including omilancor for the treatment of UC, NX-13 for the treatment of UC, and LABP-104 for the potential treatment of systemic lupus erythematosus and rheumatoid arthritis. For more information, please visit www.landosbiopharma.com. Cautionary Note on Forward-Looking Statements Statements in this press release about future expectations, plans and prospects for Landos Biopharma, Inc. (the “Company”), including statements about the Company’s strategy, clinical development and regulatory plans for its product candidates, including NX-13, and other statements containing the words “anticipate”, “plan”, “expect”, “may”, “will”, “could”, “believe”, “look forward”, “potential”, the negatives thereof, variations thereon and similar expressions, or any discussions of strategy constitute forward-looking statements. Actual results may differ materially from those indicated by such forward-looking statements as a result of various important factors, including: the uncertainties inherent in the initiation and enrollment of future clinical trials, expectations of expanding ongoing clinical trials, availability and timing of data from ongoing clinical trials, expectations for regulatory approvals, other matters that could affect the availability or commercial potential of the Company’s product candidates and other similar risks. Risks regarding the Company’s business are described in detail in the Company’s filings with the Securities and Exchange Commission (“SEC”), including in its Annual Reports on Form 10-K and Quarterly Reports on Form 10-Q, which are available on the SEC’s website at www.sec.gov. Additional information will be made available in other filings that the Company makes from time to time with the SEC. Such risks may be amplified by the impacts of the COVID-19 pandemic. In addition, the forward-looking statements included in this press release represent the Company’s views only as of the date hereof. The Company anticipates that subsequent events and developments will cause the Company’s views to change. However, while the Company may elect to update these forward-looking statements at some point in the future, the Company specifically disclaims any obligation to do so, except as may be required by law. These forward-looking statements should not be relied upon as representing the Company’s views as of any date subsequent to the date hereof. Contacts Tanner Kaufman / Kara SperryJoele Frank, Wilkinson Brimmer Katcher212-355-4449

Antibody

100 Deals associated with Tegaserod maleate

External Link

KEGG	Wiki	ATC	Drug Bank
D02730	Tegaserod maleate	A06AX06	DB01079

R&D Status

Approved

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
Irritable bowel syndrome with constipation	US	Alfasigma USA, Inc.	24 Jul 2002

Developing

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Irritable Bowel Syndrome	NDA/BLA	EU	Novartis Europharm Ltd.	-
Chronic Pain	Phase 3	US	Novartis AG	01 Nov 2006
Opioid-Induced Constipation	Phase 3	US	Novartis AG	01 Nov 2006
Heartburn	Phase 3	US	Novartis AG	01 Apr 2005
Constipation	Phase 3	US	Novartis Pharmaceuticals Corp.	01 Nov 2004
Chronic constipation	Phase 3	-	Novartis AG	01 Mar 2004
Dyspepsia	Phase 3	US	Novartis AG	01 Jan 2004
Gastroesophageal Reflux	Phase 3	US	Novartis AG	01 Jun 2003
Diabetic Gastroparesis	Phase 2	CH	Novartis AG	01 May 2004
Esophagitis, Peptic	Phase 2	US	Novartis AG	01 Jan 2004

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


DDW2024	Not Applicable	Dyspepsia	-	Tegaserod 6mg bid	spmrxesplj(tslknsrgrn) = gozraelbnr jwkifekssy (lkexhabjsc )	-	19 May 2024
				Domperidone 10mg tid	spmrxesplj(tslknsrgrn) = bqjimtdlcy jwkifekssy (lkexhabjsc )

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