A Randomized, Open-label, Single-dose, Two-way Crossover Clinical Trial to Investigate the Pharmacokinetics and Safety After Oral Administration of CKD-396 and Co-administration of CKD-501 and D759 in Healthy Adults

The purpose of this study is to evaluate the pharmacokinetics and safety of CKD-396.

Start Date24 Feb 2020

Sponsor / Collaborator

Chong Kun Dang Pharmaceutical Corp.

NCT03499704

/ Active, not recruitingPhase 4

A Multicenter, Randomized, Open-label, Two-arm, Phase 4 Study to Evaluate the Effect of Add-on Pioglitazone or Dapagliflozin in Subjects With Type 2 Diabetes Mellitus Inadequately Controlled by Dipeptidyl Peptidase-4 Inhibitor and Metformin Therapy

The purpose of this study is to assess the pioglitazone plus alogliptin plus metformin is non-inferior to dapagliflozin plus alogliptin plus metformin on glycosylated haemoglobin (HbA1c) change from baseline at Week 26.

Start Date11 Feb 2020

Sponsor / Collaborator

Celltrion Pharm Inc.

100 Clinical Results associated with PPARγ x DPP-4

100 Translational Medicine associated with PPARγ x DPP-4

0 Patents (Medical) associated with PPARγ x DPP-4

Literatures (Medical) associated with PPARγ x DPP-4

01 Dec 2025·Journal of Computer-Aided Molecular Design

Computational investigation to identify multi-targeted anti-hyperglycemic potential of substituted 2-Mercaptobenzimidazole derivatives and synthesis of new α-glucosidase inhibitors

Article

Author: Nadeem, Humaira ; Rajput, Tausif Ahmed ; Waseem, Tanya ; Ahmed, Madiha ; Zargaham, Muhammad Kazim ; Amin, Adnan

One of the most widespread diseases recognized all over the world is diabetes, accounting for 1.5 million deaths each year. Recent studies have demonstrated benzimidazole derivatives as potential antidiabetic agents. Hence, the present study is focused on designing new derivatives of 2-mercaptobenzimidazole by C-S cross-coupling reaction and are subjected to computational screening to identify the most promising candidate. Molecular docking and MM-GBSA calculations were performed to ascertain the binding potential with different antidiabetic targets, including α-glucosidase, PPaR-γ, DPP-4, and AMPK. We observed somewhat moderate binding interactions of the synthesized compound against the α-glucosidase. Since binding affinities can be improved using synthetic chemistry approaches, synthesis of analogues (A-18a-c) by designing hybrids at sites such as the acidic functionality of A-18 was done. The analogue A-18a, with p-fluorobenzyl substitution, exhibited enhanced binding affinity (-4.339 Kcal/mol) with the α-glucosidase compared to the parent compound (-3.827 Kcal/mol). The synthesized analogues were also subjected to an in-vitro α-glucosidase inhibitory assay. Among them, A-18a exhibited the most significant inhibitory potential, with an IC₅₀ value of 0.521 ± 0.01 µM as compared to the standard drug Acarbose (IC₅₀ 21.0 ± 0.5 µM). This aligns with the computational study findings, where A-18a exhibited stronger binding interactions within the active site of the enzyme. Hence, a promising analogue of the designed compound was synthesized through a computationally guided approach as an anti-hyperglycaemic agent. Additionally, most of the designed compounds showed significantly greater binding affinity with PPaR-γ as compared to the standard pioglitazone. A-18 was successfully synthesized by S-arylation reaction using CuI in 89% yield and was subjected to MD-simulation against PPaR-γ, which revealed stable binding throughout the 200 ns run. Future studies will focus on exploring the activity of the designed drugs against PPaR-γ through in-vitro and in-vivo assays.

01 May 2025·Human Immunology

Study on the common mechanisms of gastroesophageal reflux disease and interstitial lung disease

Article

Author: You, Liusheng ; Zhang, Wen ; Jiang, Chenglin ; Chen, Changdan ; Cai, Qizhi ; Zhang, Wei ; Zheng, Xiujin

OBJECTIVEInterstitial lung disease (ILD) and gastroesophageal reflux disease (GERD) have complex interactions and can exacerbate severity of each other. This study aimed to screen shared genes between ILD and GERD and explore their common mechanisms and clinical value.METHODSWe obtained microarray datasets of ILD and GERD from public databases. Shared genes were screened by differential expression analysis and Venn analysis. Hub genes were screened from shared genes using the protein-protein interaction (PPI) network analysis. The ssGSEA algorithm was utilized to estimate immune infiltration level of ILD and GERD, and correlation of hub genes with immune cell infiltration was studied. Finally, potential drugs that may act on hub genes were screened using DSigDB.RESULTS52 shared genes were obtained through Venn analysis. PPI network analysis identified 10 hub genes (BMP4, NT5E, PPARG, EPCAM, DPP4, KLF2, MMP1, AGR2, ADAMTS1, GATA6) that may have diagnostic performance (p < 0.05). The results of immune infiltration showed that hub genes were highly linked to multiple immune cell infiltrations (p < 0.05). In addition, we identified 5 potential drugs. Notably, thioridazine may target 5 hub genes (MMP1, AGR2, KLF2, ADAMTS1, and PPARG) simultaneously (p < 0.05) and had the potential to be a novel therapeutic drug.CONCLUSIONIn summary, we have screened out the hub genes with diagnostic value in ILD and GERD, and also revealed the close relationship between the hub genes and the disease immune microenvironment, providing new research directions for the common mechanism and interaction of the two diseases.

01 Apr 2025·Applied Biochemistry and Biotechnology

Multi Targeted Activity of Cocculus hirsutus through Modulation of DPP-IV and PTP-1B Leading to Enhancement of Glucose Uptake and Attenuation of Lipid Accumulation

Article

Author: Lakshmi, B S ; Riitvek, B ; Bhuvaneswari, D

Multi-targeted therapies are gaining attention in the management of multifactorial diseases due to their poly pharmacology, enhanced potency and reduced toxicity. Metabolic disorders like Type 2 diabetes mellitus (T2DM) and obesity necessitate multi-targeted therapy to improve insulin sensitivity, regulate glucose homeostasis and support weight loss. Medicinal plants rich in bioactive compounds exhibit multi-targetted action with minimal side effects. In the current study, Cocculus hirsutus methanol extract (CME) and its hydromethanolic fraction (HMF) were investigated for their multi-target potential. Significant inhibition of Dipeptidyl peptidase IV (DPP-IV), a key enzyme in glucose metabolism was observed due to CME (54%) and HMF (70%) at 10 µg/ml and 1 µg/ml respectively. Protein Tyrosine Phosphatase 1B (PTP-1B), involved in the regulation of insulin signalling, was also inhibited by CME (67%) and HMF (73%) at 10 µg/ml concentration. An increase in glucose uptake was observed due to CME (62% and 65%) and HMF (63% and 68%) in 3T3-L1 adipocytes and L6 myotubes at 100 ng/ml. Further, investigation of HMF showed a decrease in lipid accumulation by 63% at 1 µg/ml in 3T3-L1 cells. Interestingly, HMF improved insulin sensitivity by upregulating GLUT4 expression (p < 0.05) via the PI3K/AKT pathway in both 3T3-L1 adipocytes and L6 myotubes. An inhibition in lipid accumulation was also observed by suppression of Peroxisome proliferator-activated receptor γ (PPARγ) (p < 0.05), a key regulator of adipogenesis in 3T3-L1 adipocytes. Gas chromatography-mass spectrometry analysis of the HMF showed the major component to be 3-methylmannoside (26.52%).

News (Medical) associated with PPARγ x DPP-4

31 Mar 2021

·www.takeda.com

Takeda Completes Sale of Four Diabetes Products in Japan to Teijin Pharma Limited

Osaka, Japan, April 1, 2021 --- Takeda Pharmaceutical Company Limited (TSE:4502/NYSE:TAK) (“Takeda”) today announced that it has completed the asset transfer associated with a portfolio of select non-core products in Japan to Teijin Pharma Limited (“Teijin Pharma”) for JPY 133.0 billion. This asset transfer agreement was announced in February 2021. The portfolio divested to Teijin Pharma was comprised of four non-core type 2 diabetes products (Nesina®, Liovel®, Inisync® and Zafatek®) sold in Japan, which generated total sales of approximately JPY 30.8 billion in FY2019. While the products included in the asset transfer continue to play important roles in meeting patient needs in the country, they were outside of Takeda’s chosen business areas – Gastroenterology (GI), Rare Diseases, Plasma-Derived Therapies, Oncology, and Neuroscience – core to its global long-term growth strategy. The transaction continues Takeda’s strong momentum toward optimizing its portfolio for growth by discovering and delivering life-transforming treatments in its focused key business areas. Takeda and Teijin Pharma have entered into a manufacturing and supply agreement and distribution agreement, under which Takeda will continue to manufacture the products, supply them and provide the distribution channel to Teijin Pharma. Takeda will, for the time being, continue holding the marketing authorizations of the transferred brands, and the timing of the transfer of the marketing authorizations will be determined later. Takeda intends to use the proceeds from the sale to reduce its debt and accelerate deleveraging towards its target of 2x net debt/adjusted EBITDA within FY2021 – FY2023. Takeda has sustained momentum in its divestiture strategy and has exceeded its $10 billion non-core asset divestiture target. Including this transaction, Takeda has announced 12 deals since January 2019, for a total aggregate value of up to approximately $12.9 billion. As the asset transfer was completed on April 1, 2021, this transaction will be reflected in Takeda’s results for the first quarter of the Fiscal Year 2021. Takeda anticipates the sales price to have a positive impact on Reported Profit before income taxes and Net Profit attributable to owners of the Company of approximately JPY 130.0 billion and JPY 90.0 billion, respectively. Since the gain relates to the divestiture of non-core assets, there will be no impact on Core Operating Profit or Core Net Profit. Takeda will announce its Forecast for the Full Year Consolidated Financials for the Fiscal Year 2021 at the Fiscal Year 2020 financial results announcement scheduled in May 2021.

Financial StatementAcquisition

Analysis

Perform a panoramic analysis of this field.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis