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Last update 13 May 2025

Rosiglitazone Maleate

Last update 13 May 2025

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(RS)-5-{4-[2-(Methyl-2-pyridylamino)ethoxy]benzyl}-2,4-thiazolidinedion, (±)-5-[p-[2-(methyl-2-pyridylamino)ethoxy]benzyl]-2,4-thiazolidinedione, rosiglitazone

+ [28]

Target

PPARγ

Action

agonists

Mechanism

PPARγ agonists(Peroxisome proliferator-activated receptor γ agonists)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Diabetes Mellitus, Type 2

Inactive Indication

Alzheimer DiseaseAtherosclerosisCarotid Artery Diseases+ [16]

Originator Organization

GSK Plc

Active Organization

GSK Plc

Inactive Organization

Smithkline Beecham Plc

Woodward Pharma Services LLC

License Organization-

Drug Highest PhaseApproved

First Approval Date

United States (25 May 1999),

Diabetes Mellitus, Type 2

Regulation-

Structure/Sequence

Molecular FormulaC22H23N3O7S

InChIKeySUFUKZSWUHZXAV-BTJKTKAUSA-N

CAS Registry155141-29-0

157

Clinical Trials associated with Rosiglitazone Maleate

IRCT20090117001556N159

/ SuspendedPhase 2/3IIT

The effect of Rosiglitazone as an adjuvant therapy on the improvement of negative symptoms in patients with chronic schizophrenia: A randomized, double-blind, placebo-controlled trial

Start Date22 Sep 2024

Sponsor / Collaborator-

CTR20210864

/ CompletedNot Applicable

罗格列酮片人体生物等效性研究

[Translation] Study on the bioequivalence of rosiglitazone tablets in healthy volunteers

采用单中心、随机、开放、双周期、自身交叉、单剂量给药设计比较空腹和餐后给药条件下，成都恒瑞制药有限公司生产的罗格列酮片（4 mg）与SB PHARMCO PUERTO RICO INC持证，加拿大GlaxoSmithKline生产的马来酸罗格列酮片（商品名：AVANDIA®，4 mg，以罗格列酮计）在中国健康人群中吸收程度和吸收速度的差异，并评价成都恒瑞制药有限公司生产的罗格列酮片的安全性。

[Translation]

A single-center, randomized, open, two-period, self-crossover, single-dose design was used to compare the differences in absorption extent and rate between rosiglitazone tablets (4 mg) produced by Chengdu Hengrui Pharmaceutical Co., Ltd. and rosiglitazone maleate tablets (trade name: AVANDIA®, 4 mg, calculated as rosiglitazone) licensed by SB PHARMCO PUERTO RICO INC and produced by GlaxoSmithKline, Canada, under fasting and postprandial administration in healthy Chinese people, and to evaluate the safety of rosiglitazone tablets produced by Chengdu Hengrui Pharmaceutical Co., Ltd.

Start Date26 Apr 2021

Sponsor / Collaborator

Chengdu Hengrui Pharmaceutical Co. Ltd.

NCT04114136

/ RecruitingPhase 2IIT

A Phase II Clinical Trial of Anti-PD-1 mAb Therapy Alone or With Metabolic Modulators to Reverse Tumor Hypoxia and Immune Dysfunction in Solid Tumor Malignancies

Patients with histologically or cytologically confirmed advanced melanoma, renal cell carcinoma, NSCLC, HCC (Child Pugh Class A only), MSI-High solid tumors, Urothelial Cancer, GE junction/Gastric Adenocarcinoma, or HNSCC for which current standard of care treatment for their stage of disease would be with Pembrolizumab or Nivolumab monotherapy, who meet eligibility criteria will undergo a biopsy (core or excisional/incisional; FNA not adequate) for baseline tissue. Patients will then be randomized to one of 3 arms: Anti-PD-1 mAb plus Metformin 500mg po BID, Anti-PD-1 mAb alone, Anti-PD-1 mAb plus Rosiglitazone 4mg po qdaily. Five weeks (+/- 7 days) after initiation of therapy a patient will undergo a repeat biopsy (core or excisional/incisional; FNA not adequate) for correlative analysis. The patient will then continue on study therapy for up to 2 years, or until progression of disease or unacceptable toxicity, whichever occurs first. RECIST 1.1 with modifications, to allow for continued therapy until progressive disease is confirmed if the patient is clinically stable, will be used in the trial.

Start Date14 Sep 2020

Sponsor / Collaborator

University of Pittsburgh

100 Clinical Results associated with Rosiglitazone Maleate

100 Translational Medicine associated with Rosiglitazone Maleate

100 Patents (Medical) associated with Rosiglitazone Maleate

7,372

Literatures (Medical) associated with Rosiglitazone Maleate

01 May 2025·EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A new potent and selective peroxisome proliferator-activated receptor alpha partial agonist displays anti-steatotic effects In vitro and behaves as a safe hypolipidemic and hypoglycemic agent in a diabetic mouse model

Article

Author: Lavecchia, Antonio ; Laghezza, Antonio ; Gilardi, Federica ; Leuci, Rosalba ; Falbo, Emanuele ; Loiodice, Fulvio ; Thomas, Aurélien ; Tortorella, Paolo ; Piemontese, Luca ; Biswas, Abanish ; Paoli, Paolo ; Tambe, Suhas ; Ca, Sudeep ; Jayaprakash, Venkatesan ; Pattnaik, Ashok Kumar ; Brunetti, Leonardo ; Singh, Ravi Pratap ; Wackerlig-Damle, Judith

A rational drug design approach led to the synthesis of three pairs of enantiomers derived from the peroxisome proliferator-activated receptor (PPAR) pan agonist AL29-26, identifying (S)-2 as a potent and selective PPARα partial agonist. Molecular docking and molecular dynamics simulations elucidated the binding modes of (S)-2 within the ligand-binding domains of PPARα and PPARγ. In vitro, (S)-2 demonstrated significant anti-steatotic effects, upregulating key PPARα target genes involved in lipid metabolism. In vivo, (S)-2 exhibited hypolipidemic and antihyperglycemic activity in a diabetic mouse model, outperforming fenofibrate in lowering blood glucose and lipid levels, while showing no toxicity in major organs (artery, kidney, liver, pancreas). The therapeutic effects of ((S)-2 were attributed to its PPARα selectivity, reduced activation of PPARγ, and mild protein tyrosine phosphatase 1B (PTP1B) inhibition. These findings highlight (S)-2 as a promising lead compound for the development of safer and more effective treatments for dyslipidemic type 2 diabetes.

07 Apr 2025·MOLECULAR PHARMACEUTICS

Computational Approaches for Predicting Drug Interactions with Human Organic Anion Transporter 4 (OAT4)

Article

Author: Vignaux, Patricia A. ; Harris, Joshua S. ; Lane, Thomas R. ; Martinez-Guerrero, Lucy ; Ekins, Sean ; Urbina, Fabio ; Wright, Stephen H. ; Cherrington, Nathan J.

Human Organic Anion Transporter 4 (OAT4) is predominantly expressed in the kidneys, particularly in the apical membrane of the proximal tubule cells. This transporter is involved in the renal handling of endogenous and exogenous organic anions (OAs), making it an important transporter for drug-drug interactions (DDIs). To better understand OAT4-compound interactions, we generated single concentration (25 μM) in vitro inhibition data for over 1400 small molecules against the uptake of the fluorescent OA 6-carboxyfluorescein (6-CF) in Chinese hamster ovary (CHO) cells. Several drugs exhibiting higher than 50% inhibition in this initial screen were selected to determine IC₅₀ values against three structurally distinct OAT4 substrates: estrone sulfate (ES), ochratoxin A (OTA), and 6-CF. These IC₅₀ values were then compared to the drug plasma concentration as per the 2020 FDA drug-drug interaction (DDI) guidance. Several screened compounds, including some not previously reported, emerged as novel inhibitors of OAT4. These data were also used to build machine learning classification models to predict the activity of potential OAT4 inhibitors. We compared multiple machine learning algorithms and data cleaning techniques to model these screening data and investigated the utility of conformal predictors to predict OAT4 inhibition of a leave-out set. These experimental and computational approaches allowed us to model diverse and unbalanced data to enable predictions for DDIs mediated by this transporter.

01 Apr 2025·Pharmacological Reports

Tacrolimus and diabetic rodent models

Review

Author: Qian, Minyan ; Hu, Nan ; Wang, Liying ; Guan, Mengmeng

Tacrolimus (TAC) is an immunosuppressant widely utilized in organ transplantation. One of its primary adverse effects is glucose metabolism disorder, which significantly increases the risk of diabetes. Investigating the molecular mechanisms underlying TAC-induced diabetes is essential for developing effective prevention and treatment strategies for these adverse effects. In addition, TAC can induce cost-effective, non-obese animal models of diabetes, where the metabolic parameter changes closely resemble those observed during the onset and progression of type 2 diabetes (T2DM), post-transplantation diabetes mellitus (PTDM), and associated complications. This review, based on articles indexed in PubMed up to August 19, 2024, identified 48 studies focusing on TAC-induced diabetic rodent models and 22 studies exploring the effects of TAC on diabetic or obese rodent models. These studies were systematically summarized based on TAC dosage, route of administration, duration of administration, and glucose metabolism indices used for evaluation. Additionally, the impact of TAC dose reduction or discontinuation on glucose metabolism was assessed, along with pharmacological agents that modulate TAC-induced diabetes, including anti-diabetic medications, anti-inflammatory and antioxidant compounds, biologics, and antibiotics. Key signaling pathways implicated in TAC-induced diabetes include CaN/NFAT, PI3K/AKT/mTOR, and TGF-β/Smad, all of which impair islet β-cell function, thereby contributing to diabetes development. This review provides a concise summary of the characteristics of relevant murine models, offering valuable guidance for selecting appropriate and economical animal models for future research.

News (Medical) associated with Rosiglitazone Maleate

18 Mar 2025

·www.globenewswire.com

CAMP4 Appoints Multiple Industry Veterans to its Board of Directors

With decades of experience in pharmaceutical development and extensive genetic medicine expertise, Doug E. Williams, Ph.D., and Murray Stewart, DM FRCP, will provide strategic guidance for CAMP4’s multiple drug development efforts CAMBRIDGE, Mass., March 18, 2025 (GLOBE NEWSWIRE) -- CAMP4 Therapeutics Corporation (“CAMP4”) (Nasdaq: CAMP), a clinical-stage biotechnology company developing a pipeline of regRNA-targeting antisense oligonucleotide (ASO) therapies to upregulate gene expression to restore healthy protein levels, today announced the appointments of Doug E. Williams, Ph.D., and Murray Stewart, DM FRCP, to the Company’s Board of Directors. “We are delighted to welcome Drs. Williams and Stewart to our Board of Directors,” said Josh Mandel-Brehm, Chief Executive Officer of CAMP4. “With their combined expertise spanning critical aspects of R&D and clinical development, we will benefit greatly from their strategic insights as we advance our lead clinical program for urea cycle disorders and our preclinical program for SYNGAP1-related disorders, while continuing to develop additional RNA-targeting medicines designed to upregulate gene expression and meaningfully address diseases where we believe modest increases in protein levels can have a tremendous impact on the lives of patients.” Dr. Williams commented, “CAMP4’s approach is opening exciting possibilities to upregulate gene expression, a long-sought-after and challenging feat in the field of genetic medicine. I look forward to working with the team to unlock the full potential of this approach and ultimately advance novel therapeutics to the clinic.” Dr. Stewart added, “I’m thrilled to join the CAMP4 team and support its mission of advancing programmable RNA therapeutics for genetic diseases where decreased protein expression drives disease pathophysiology. By pioneering new ways to restore gene expression, CAMP4 has the potential to bring life-changing therapies to patients who currently have limited or no disease-modifying treatment options.” With over 30 years in the biopharma industry, Dr. Williams has contributed to the development of several transformative drugs, including LEUKINE®, ENBREL®, ADCETRIS®, TECFIDERA®, APROLIX®, ELOCTATE®, and SPINRAZA®. He was previously President of R&D at Sana Biotechnology and the Founding President & CEO of Codiak BioSciences. Prior to Sana, Dr. Williams served as EVP of R&D at Biogen, and earlier in his career was CEO of ZymoGenetics (acquired by BMS), and held leadership roles at Seattle Genetics, Amgen, and Immunex. Over the course of his career, he has served on the Board of Directors and Advisory Boards of more than two dozen biotech companies. Dr. Stewart currently serves as a Senior Medical Advisor to several biopharma companies, and was most recently the Chief Medical Officer at Rhythm Pharmaceuticals. Prior to this position, he served as Head of R&D at Novelion Therapeutics. Before joining Novelion, he served as corporate Chief Medical Officer at GlaxoSmithKline. With extensive clinical development experience, he has led studies across all stages, from first-in-human trials to large Phase 4 cardiovascular outcome studies. Dr. Stewart has played a key role in the successful registration and launch of multiple therapies, including AVANDIA®, ARIXTRA®, TANZEUM®, and XOLREMDI®. Before transitioning to industry, he served as a Consultant Physician and Head of Clinical Services at the Diabetes Centre in Newcastle upon Tyne, UK, where his research was focused on lipid metabolism and type 2 diabetes. About CAMP4 Therapeutics CAMP4 is developing disease-modifying treatments for a broad range of rare and prevalent genetic diseases where increasing healthy protein levels may offer meaningful therapeutic benefits. Our approach allows for targeted gene upregulation by harnessing a fundamental mechanism of how genes are controlled. To increase gene expression, our therapeutic ASO drug candidates target regRNAs, which act locally on transcription factors and are the master regulators of gene expression. CAMP4’s proprietary RAP Platform™ enables the mapping of regRNAs and generation of therapeutic candidates designed to target the regRNAs associated with genes underlying haploinsufficient and recessive partial loss-of-function disorders, of which there are more than 1,200, in which a modest increase in protein expression may have the potential to be clinically meaningful. Learn more about us at www.CAMP4tx.com and follow us on LinkedIn and X. Forward-Looking Statements This press release contains forward-looking statements which involve risks, uncertainties and contingencies, many of which are beyond the control of the Company, which may cause actual results, performance, or achievements to differ materially from anticipated results, performance, or achievements. All statements other than statements of historical facts contained in this press release are forward-looking statements. In some cases, you can identify forward-looking statements by terms such as “may,” “will,” “should,” “expect,” “plan,” “anticipate,” “could,” “intend,” “target,” “project,” “contemplate,” “believe,” “estimate,” “predict,” “potential” or “continue” or the negative of these terms or other similar expressions, although not all forward-looking statements contain these words. Forward-looking statements include, but are not limited to, statements concerning CAMP4’s plans, objectives, expectations and intentions. The forward-looking statements in this press release speak only as of the date of this press release and are subject to a number of known and unknown risks, uncertainties and assumptions that could cause the Company’s actual results to differ materially from those anticipated in the forward-looking statements, including, but not limited to: the Company’s limited operating history, incurrence of substantial losses since the Company’s inception and anticipation of incurring substantial and increasing losses for the foreseeable future; the Company’s need for substantial additional financing to achieve the Company’s goals; the uncertainty of clinical development, which is lengthy and expensive, and characterized by uncertain outcomes, and risks related to additional costs or delays in completing, or failing to complete, the development and commercialization of the Company’s current product candidates or any future product candidates; delays or difficulties in the enrollment and dosing of patients in clinical trials; the impact of any significant adverse events or undesirable side effects caused by the Company’s product candidates; potential competition, including from large and specialty pharmaceutical and biotechnology companies; the Company’s ability to realize the benefits of the Company’s current or future collaborations or licensing arrangements and ability to successfully consummate future partnerships; the Company’s ability to obtain regulatory approval to commercialize any product candidate in the United States or any other jurisdiction, and the risk that any such approval may be for a more narrow indication than the Company seeks; the Company’s dependence on the services of the Company’s senior management and other clinical and scientific personnel, and the Company’s ability to retain these individuals or recruit additional management or clinical and scientific personnel; the Company’s ability to grow the Company’s organization, and manage the Company’s growth and expansion of the Company’s operations; risks related to the manufacturing of the Company’s product candidates, which is complex, and the risk that the Company’s third-party manufacturers may encounter difficulties in production; the Company’s ability to obtain and maintain sufficient intellectual property protection for the Company’s product candidates or any future product candidates the Company may develop; the Company’s reliance on third parties to conduct the Company’s preclinical studies and clinical trials; the Company’s compliance with the Company’s obligations under the licenses granted to the Company by others, for the rights to develop and commercialize the Company’s product candidates; risks related to the operations of the Company’s suppliers; and other risks and uncertainties described in the section “Risk Factors” in the Company’s Quarterly Report on Form 10-Q for the quarter ended September 30, 2024, as well as other information we file with the Securities and Exchange Commission. The forward-looking statements in this press release are inherently uncertain and are not guarantees of future events. Because forward-looking statements are inherently subject to risks and uncertainties, some of which cannot be predicted or quantified and some of which are beyond the Company’s control, you should not unduly rely on these forward-looking statements. The events and circumstances reflected in the forward-looking statements may not be achieved or occur and actual future results, levels of activity, performance and events and circumstances could differ materially from those projected in the forward-looking statements. Moreover, the Company operates in an evolving environment. New risks and uncertainties may emerge from time to time, and management cannot predict all risks and uncertainties. Investors, potential investors, and others should give careful consideration to these risks and uncertainties. Except as required by applicable law, the Company does not undertake to publicly update or revise any forward-looking statements contained herein, whether as a result of any new information, future events, changed circumstances or otherwise. Contacts Investor Relations:Sandya von der WeidLifeSci Advisorssvonderweid@lifesciadvisors.com Media:Jason Braco, Ph.D.LifeSci Communicationsjbraco@lifescicomms.com

Executive ChangeOligonucleotide

17 Jun 2024

·www.biospace.com

MyMD Pharmaceuticals Appoints Accomplished Biopharmaceutical Leader and Current Board Member, Mitchell Glass, M.D. as President and Chief Medical Officer

Dr. Glass brings a 35-year career in life sciences with multiple drug approvals including Accolate ®, Avandia ® and Coreg® Dr. Glass brings broad expertise in regulatory strategies: 5 NDAs and MAAs, 7 pre-NDA meetings, 12 End of Phase 2 meetings, and more than 80 INDs Company announces President and CMO transition as clinical development advances through mid-stage trials Company also appoints new independent board member, Mr. Stephen Friscia, an experienced investment strategist BALTIMORE--(BUSINESS WIRE)-- MyMD Pharmaceuticals, Inc. (Nasdaq: MYMD) (“MyMD” or the “Company”), a clinical stage biopharmaceutical company committed to developing novel therapies for age-related diseases and autoimmune and inflammatory conditions, today announced the appointment of Mitchell Glass, M.D., a member of the board of directors of the Company, as president and chief medical officer. The Company also announced the appointment of Mr. Stephen Friscia, a veteran investor, to the board of directors. Appointment of Mitchell Glass, M.D. “Through his many years of biopharma leadership, Dr. Glass has established a successful and productive track record of executing successful early- to mid-stage clinical development and regulatory strategies and bringing numerous companies to market entry and commercialization,” said Josh Silverman, chairman of the board of MyMD. “After completing a successful and statistically significant small Phase 2 study of MYMD-1® in sarcopenia/frailty last year, now is the right time for the Company to bring in a highly experienced leader to guide the Company through further mid-stage clinical development. We believe Dr. Glass has the right expertise and ingenuity necessary to drive continued value creation for the benefit of all stakeholders.” "This is an exciting time to join MyMD. MyMD’s initial Phase 2 data provides guidance to perform larger studies of MYMD-1 focused on patient outcomes. Our team looks forward to providing near-term updates on the path forward for our novel TNF-α inhibitor,” said Dr. Glass. Dr. Glass is board certified in internal medicine, pulmonary and critical care medicine, with a focus in inflammatory diseases and immunopathology. His biopharmaceutical career spans 35 years across diverse life sciences industries and fields, from broad-ranging executive positions at top ten pharmaceutical companies, to founding, leading and funding start-ups and early-stage biopharma companies. As a long-term investor in the healthcare sector, Dr. Glass is a founder and principal of Medpro Investors, a New York-based venture capital firm focused on the healthcare sector. He is a long-term consultant and regulatory representative for company and university engagement with the FDA and international regulatory counterparts, and he currently serves on the American Lung Association’s Scientific Advisory Committee. Dr. Glass holds an extensive and successful track record in leading companies through FDA regulatory pathways from early research and development to late-stage trials and market commercialization. His career highlights include 5 new drug applications (NDAs) and marketing authorization applications (MAAs), 7 pre-NDA meetings including international counterparts, 12 End of Phase 2 (EOP2) meetings with FDA, and more than 80 investigational new drug applications (INDs). Appointment of Stephen Friscia “Stephen Friscia is the newest addition to our board of directors, bringing two decades of equity research and portfolio management experience. His broad perspective and knowledge of the healthcare sector will be key assets as we proceed with strategic value creation,” Silverman concluded. Mr. Friscia is the manager and co-founder of Kipps Capital, a family office established in 2016. Previously, Mr. Friscia was a managing director and portfolio manager for multiple institutional investment and asset management firms, with several focused in small and mid-cap value equities, including Iridian Asset Management LLC, MacKay Shields LLC, Bear Stearns Asset Management Inc., John A. Levin & Co., Inc., and Evergreen Investments LLC (Wachovia Corporation). About MyMD Pharmaceuticals, Inc. MyMD Pharmaceuticals, Inc. (Nasdaq: MYMD), a clinical stage pharmaceutical company committed to extending healthy lifespan, is focused on developing two novel therapeutic platforms that treat the causes of disease rather than only addressing the symptoms. MYMD-1 is a drug platform based on a clinical stage small molecule that regulates the immune system to control TNF-α, which drives chronic inflammation, and other pro-inflammatory cell signaling cytokines. MYMD-1 is being developed to treat diseases and disorders marked by acute or chronic inflammation. The Company’s second drug platform, Supera-CBD, is being developed to treat chronic pain, addiction and epilepsy. Supera-CBD is a novel synthetic derivative of cannabidiol (CBD) and is being developed to address and improve upon the rapidly growing CBD market, which includes both FDA approved drugs and CBD products not currently regulated as drugs. For more information, visit . Cautionary Statement Regarding Forward-Looking Statements This press release may contain forward-looking statements. These forward-looking statements involve known and unknown risks, uncertainties and other factors which may cause actual results, performance or achievements to be materially different from any expected future results, performance, or achievements. Forward-looking statements speak only as of the date they are made and none of MyMD nor its affiliates assume any duty to update forward-looking statements. Words such as “anticipate,” “believe,” “could,” “estimate,” “expect,” “may,” “plan,” “will,” “would’’ and other similar expressions are intended to identify these forward-looking statements. Important factors that could cause actual results to differ materially from those indicated by such forward-looking statements include, without limitation: MyMD’s ability to maintain compliance with the Nasdaq Stock Market’s listing standards; the timing of, and MyMD’s ability to, obtain and maintain regulatory approvals for clinical trials of MyMD’s pharmaceutical candidates; the timing and results of MyMD’s planned clinical trials for its pharmaceutical candidates; the amount of funds MyMD requires for its pharmaceutical candidates; increased levels of competition; changes in political, economic or regulatory conditions generally and in the markets in which MyMD operates; MyMD’s ability to retain and attract senior management and other key employees; MyMD’s ability to quickly and effectively respond to new technological developments; and MyMD’s ability to protect its trade secrets or other proprietary rights, operate without infringing upon the proprietary rights of others and prevent others from infringing on MyMD’s proprietary rights. A discussion of these and other factors with respect to MyMD is set forth in the Company’s Annual Report on Form 10-K for the year ended December 31, 2023, filed by MyMD on April 1, 2024, and subsequent reports that MyMD files with the Securities and Exchange Commission. Forward-looking statements speak only as of the date they are made and MyMD disclaims any intention or obligation to revise any forward-looking statements, whether as a result of new information, future events or otherwise.

Phase 2Executive Change

11 Apr 2024

·www.sciencedaily.com

This outdated diabetes drug still has something to offer

Researchers have discovered the biochemical workings of an old-fashioned diabetes drug, and it's helping them develop new, safer alternatives. Thiazolidinediones (TZDs) are a class of drug that can be used to treat type 2 diabetes by reversing insulin resistance, one of the main hallmarks of the disease. While TZDs were extremely popular in the 1990's and early 2000's, they have fallen out of use among physicians in recent decades because they were discovered to cause unwanted side effects, including weight gain and excess fluid accumulation in body tissues. Now, researchers at University of California San Diego School of Medicine are exploring how to isolate the positive effects of these drugs, which could help yield new treatments that don't come with the old side effects. In a new study published in Nature Metabolism, the researchers discovered how one of the most well-known TZD drugs works at the molecular level and were able to replicate its positive effects in mice without giving them the drug itself. "For decades, TZDs have been the only drugs we have that can reverse insulin resistance, but we seldom use them anymore because of their side effects profile," said Jerrold Olefsky, M.D., a professor of medicine and assistant vice chancellor for integrative research at UC San Diego Health Sciences. "Impaired insulin sensitivity is the root cause of type 2 diabetes, so any treatment we can develop to safely restore this would be a major step forward for patients." The main driver of insulin resistance in type 2 diabetes is obesity, which currently affects more than 40 percent of Americans and in 2021 bore an annual medical cost of nearly $173 billion. In addition to causing adipose tissue (fat) to expand, obesity also causes low levels of inflammation. This inflammation causes immune cells, called macrophages, to accumulate in adipose tissue, where they can comprise up to 40 percent of the total number of cells in the tissue. When adipose tissue is inflamed, these macrophages release tiny nanoparticles containing instructions for surrounding cells in the form of microRNAs, small fragments of genetic material that help regulate gene expression. These microRNA-containing capsules, called exosomes, are released into the circulation and can travel through the bloodstream to be absorbed by other tissues, such as the liver and muscles. This can then lead to the varied metabolic changes associated with obesity, including insulin resistance. For the current study, the researchers wanted to understand how TZD drugs, which restore insulin resistance, affect this exosome system. The researchers treated a group of obese mice with rosiglitazone, a type of TZD drug. Those mice became more sensitive to insulin, but they also gained weight and retained excess fluid, known side effects of rosiglitazone. However, by isolating exosomes from the adipose tissue macrophages of the mice who had received the drug and injecting them into another group of obese mice that had not received it, the researchers were able to deliver the positive effects of rosiglitazone without transferring the negative effects. "The exosomes were just as effective in reversing insulin resistance as the drug itself but without the same side effects," said Olefsky. "This indicates that exosomes can ultimately link obesity-related inflammation and insulin resistance to diabetes. It also tells us that we may be able to leverage this system to boost insulin sensitivity." The researchers were also able to identify the specific microRNA within the exosomes that was responsible for the beneficial metabolic effects of rosiglitazone. This molecule, called miR-690, could eventually be leveraged into new therapies for type 2 diabetes. "It's likely not practical to develop exosomes themselves as a treatment because it would be difficult to produce and administer them, but learning what drives the beneficial effects of exosomes at the molecular level makes it possible to develop drugs that can mimic these effects," said Olefsky. "There's also plenty of precedent for using microRNAs themselves as drugs, so that's the possibility we're most excited about exploring for miR-690 going forward."

100 Deals associated with Rosiglitazone Maleate

External Link

KEGG	Wiki	ATC	Drug Bank
D00596	Rosiglitazone Maleate	A10BG02	DB00412

R&D Status

Approved

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	United States	Woodward Pharma Services LLC	25 May 1999

Developing

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Metabolic Syndrome	Phase 3	United States	GSK Plc	01 Sep 2006
Prediabetic State	Phase 3	United States	GSK Plc	01 Sep 2006
Alzheimer Disease	Phase 3	United States	GSK Plc	12 Jul 2006
Alzheimer Disease	Phase 3	Australia	GSK Plc	12 Jul 2006
Alzheimer Disease	Phase 3	Belgium	GSK Plc	12 Jul 2006
Alzheimer Disease	Phase 3	Bulgaria	GSK Plc	12 Jul 2006
Alzheimer Disease	Phase 3	Canada	GSK Plc	12 Jul 2006
Alzheimer Disease	Phase 3	Czechia	GSK Plc	12 Jul 2006
Alzheimer Disease	Phase 3	Finland	GSK Plc	12 Jul 2006
Alzheimer Disease	Phase 3	France	GSK Plc	12 Jul 2006

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ASCO2022	Not Applicable	Diabetes Mellitus, Type 2 \| Metastatic Pancreatic Ductal Adenocarcinoma First line	232	anti-diabetic medications (DM2 patients)	iczooscxlj(fovwdfqsrw) = nhgkzcdamc gwwslyznww (stnzgwlcan )	Positive	02 Jun 2022
				anti-diabetic medications (Non-DM2 patients)	iczooscxlj(fovwdfqsrw) = hfgavwgwyf gwwslyznww (stnzgwlcan )
P-128 (ESMO_GI2021)	Not Applicable	Pancreatic Ductal Adenocarcinoma First line insulin \| glycemic control	124	anti-diabetic medications (Non-DM2)	pshcfpofxz(voaqpyjnwo) = ezgzueucpu qyiknkrhfi (qncyhgeomg )	Positive	03 Jul 2021
				anti-diabetic medications (Insulin-treated DM2)	pshcfpofxz(voaqpyjnwo) = egacgifegb qyiknkrhfi (qncyhgeomg )
NCT00265148 (CTgov)	Phase 2	Alzheimer Disease	80	Placebo (Placebo)	axmcysccge(opnrfjmlfw) = pzhamnwpsg upmgqvgymx (pxumlvpubs, 0.48541) View more	-	18 Nov 2020
				Rosiglitazone (Rosiglitazone)	axmcysccge(opnrfjmlfw) = lkpypyfeci upmgqvgymx (pxumlvpubs, 0.34985) View more
MON-695 (ENDO2020)	Not Applicable	Lipodystrophy, Familial Partial	2	Pioglitazone	xypwxronob(shcenrvhng) = ixuufnfcjl xvyouzhqmj (gekasjwrvt )	Negative	08 May 2020
NCT00348309 (REFLECT-2, CTgov)	Not Applicable	Alzheimer Disease	1,496	placebo+rosiglitazone (Placebo)	liulpetpgf(prdoszfohe) = lxovlbspzc mjhlfouqaq (wxeukgqipi, 0.54) View more	-	28 Nov 2017
				Rosiglitazone (2mg Rosiglitazone Extended Release)	liulpetpgf(prdoszfohe) = ithdkcyoup mjhlfouqaq (wxeukgqipi, 0.42) View more
NCT00490568 (CTgov)	Phase 3	Alzheimer Disease	1,461	AVA102670+RSG XR	yrhjlonman = txrmmtkjch vksrbqydhx (qyxdpwnrxi, yuyjaknded - aqriwahwrh) View more	-	13 Nov 2017
NCT00550420 (CTgov)	Phase 3	Alzheimer Disease	331	RSG	awkchbnsem = oaklqbzvko fjrcbelgfc (ojlxcgngum, qonjfvitev - aconbwtnuj) View more	-	08 Nov 2017
ASTRO2017	Not Applicable	Glioblastoma	-	Metformin	hqdfkitity(sxltvdnrio) = jpgbwibfnj gbtpyngebd (kzwildwfex )	-	01 Oct 2017
NCT00348140 (REFLECT-3, CTgov)	Phase 3	Alzheimer Disease	1,468	placebo+RSG XR (Placebo)	tbdjugwgjg(kvavascbkx) = gbvpwkywat kjjxibvzrc (vnsnnbhwkk, 0.54) View more	-	05 Sep 2017
				RSG XR (RSG XR 2mg)	tbdjugwgjg(kvavascbkx) = xllmmjjuxa kjjxibvzrc (vnsnnbhwkk, 0.53) View more
[PP.02.04] (ESH2017)	Not Applicable	-	-	rosiglitazone (Acrolein)	oyglgpxlfh(xizcwyalyq) = hzalaxthgd ceqwkunain (xunimuoolw ) View more	Positive	01 Sep 2017
				Rosiglitazone	tzwgmbdwhd(wdpmhnwsep) = ldlatahcbh nvrbftlems (gostjdpwhj ) View more

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