To assess the pharmacokinetic characteristics of valsartan and S-amlodipine after single oral administration of Exforge tab. 10/160mg, a combination formulation of valsartan and amlodipine as reference drug and Lodivixx tab. 5/160mg, a combination formulation of valsartan and S-amlodipine as test drug in healthy male adults

Start Date01 Dec 2013

Sponsor / Collaborator

Hanlim Pharm Co., Ltd.

NCT01819779

/ CompletedPhase 1

Clinical Trial to Assess the Pharmacokinetic Characteristics of Lodivixx Tab. 5/160mg in Healthy Male Subjects

Start Date01 Mar 2013

Sponsor / Collaborator

Hanlim Pharm Co., Ltd.

NCT01652339

/ CompletedPhase 1

Clinical Trial to Assess the Pharmacokinetic Characteristics of Lodivixx Tab. 5/160mg in Healthy Male Subjects

To assess the pharmacokinetic characteristics of Lodivixx tab.5/160mg in healthy male subjects
PK parameter evaluation
Safety profile evaluation

Start Date01 Jul 2012

Sponsor / Collaborator

Hanlim Pharm Co., Ltd.

100 Clinical Results associated with Amlodipine Nicotinate

100 Translational Medicine associated with Amlodipine Nicotinate

100 Patents (Medical) associated with Amlodipine Nicotinate

6,432

Literatures (Medical) associated with Amlodipine Nicotinate

04 May 2025·Autophagy

Lysosomal damage due to cholesterol accumulation triggers immunogenic cell death

Article

Author: Djavaheri-Mergny, Mojgan ; Paillet, Juliette ; Maiuri, Maria Chiara ; Kroemer, Guido ; Alvarez-Valadez, Karla ; Guittat, Lionel ; Sauvat, Allan ; de Brevern, Alexandre G ; Forveille, Sabrina ; Kepp, Oliver ; Lambertucci, Flavia ; Stoll, Gautier ; Muller, Alexandra ; Ferret, Lucille ; Pol, Jonathan G ; Diharce, Julien ; Leduc, Marion ; Wodrich, Harald ; Motiño, Omar

Cholesterol serves as a vital lipid that regulates numerous physiological processes. Nonetheless, its role in regulating cell death processes remains incompletely understood. In this study, we investigated the role of cholesterol trafficking in immunogenic cell death. Through cell-based drug screening, we identified two antidepressants, sertraline and indatraline, as potent inducers of the nuclear translocation of TFEB (transcription factor EB). Activation of TFEB was mediated through the autophagy-independent lipidation of MAP1LC3/LC3 (microtubule associated protein 1 light chain 3). Both compounds promoted cholesterol accumulation within lysosomes, resulting in lysosomal membrane permeabilization, disruption of autophagy and cell death that could be reversed by cholesterol depletion. Molecular docking analysis indicated that sertraline and indatraline have the potential to inhibit cholesterol binding to the lysosomal cholesterol transporters, NPC1 (NPC intracellular cholesterol transporter 1) and NPC2. This inhibitory effect might be further enhanced by the upregulation of NPC1 and NPC2 expression by TFEB. Both antidepressants also upregulated PLA2G15 (phospholipase A2 group XV), an enzyme that elevates lysosomal cholesterol. In cancer cells, sertraline and indatraline elicited immunogenic cell death, converting dying cells into prophylactic vaccines that were able to confer protection against tumor growth in mice. In a therapeutic setting, a single dose of each compound was sufficient to significantly reduce the outgrowth of established tumors in a T-cell-dependent manner. These results identify sertraline and indatraline as immunostimulatory agents for cancer treatment. More generally, this research shed light on novel therapeutic avenues harnessing lysosomal cholesterol transport to regulate immunogenic cell death.Abbreviation: ATG5: autophagy related 5; ATG13: autophagy related 13; DKO: double knockout; ICD: immunogenic cell death; KO: knockout; LAMP1: lysosomal associated membrane protein 1; LAMP2: lysosomal associated membrane protein 2; LGALS3: galectin 3; LDL: low-density lipoprotein; LMP: lysosomal membrane permeabilization; MAP1LC3/LC3: microtubule associated protein 1 light chain 3; MTX: mitoxantrone; NPC1: NPC intracellular cholesterol transporter 1; NPC2: NPC intracellular cholesterol transporter 2; TFE3: transcription factor E3; TFEB: transcription factor EB; ULK1: unc-51 like autophagy activating kinase 1.

01 Apr 2025·Marine Pollution Bulletin

Passive sampling of contaminants of emerging concern in a Caribbean urban estuary of Puerto Rico

Article

Author: Mansilla-Rivera, Imar ; Rodríguez-Sierra, Carlos J ; Bauzá-Ortega, Jorge F

Contaminants of emerging concern (CECs) have not been extensively studied in Caribbean estuaries, particularly in Puerto Rico. Polar organic chemical integrative samplers were deployed in surface waters at five sampling sites in the San Juan Bay Estuary to investigate the occurrence and distribution of 137 CECs, resulting in the detection of 64 chemicals (51 pharmaceuticals and personal care products "PPCPs", 12 hormones plus sucralose) at least in one sampling site, and with 35 chemicals obtaining a 100 % detection frequency. Wastewater intrusion was implicated in the presence of CECs based on the detection of sucralose and other wastewater tracers. Condado Lagoon was the most polluted site impacted by untreated wastewater, showing the highest levels of 30 of the 64 detected CECs, and the largest proportion of detected CECs, particularly PPCPs. Levels of estrone and 17β-estradiol represent a high potential risk for adverse effects on aquatic organisms in this Caribbean urban estuary.

01 Apr 2025·Journal of Molecular Structure

Synthesis and characterization of amlodipine-conjugated Gd3+-Citric acid PEG dendrimers for enhanced cardiac MRI contrast

Author: Ardestani, Mehdi Shafiee ; Khademian, Aynaz ; Mirzaei, Mehdi ; Hamedani, Morteza Pirali ; Ghoreishi, Seyedeh Masoumeh ; Ebrahimi, Seyed Esmaeil Sadat

The incorporation of nanotechnol. in medicine has led to the development of advanced imaging agents, particularly at the nanoscale.Magnetic Resonance Imaging (MRI) stands out in medical imaging due to its non-invasive nature and superior soft tissue contrast.However, the low sensitivity of current MRI contrast agents necessitates the development of improved alternatives.Gadolinium-based contrast agents (GBCAs) enhance diagnostic capabilities but pose toxicity risks, particularly in patients with severe chronic kidney diseases.This study aims to design and synthesize a novel gadolinium-loaded, citric acid-based polyethylene glycol (PEG) dendrimer (dendrimer-G₂) conjugated with amlodipine for enhanced cardiac MR imaging.The final product was characterized using LC-Mass, TEM, and EDX.Cytotoxicity was assessed using the MTT assay on HEK-293 cells.The MR imaging potential and biodistribution were evaluated in vivo, with mice receiving injections of the Gd³⁺-dendrimer-amlodipine complex followed by MRI and plasma mass spectrometry anal.Our result showed that the Gd³⁺-dendrimer-amlodipine complex demonstrated no cytotoxic effects across all tested concentrationsThe complex exhibited superior in vitro relaxivity (r₁) compared to Magnevist, indicating enhanced contrast properties.In vivo studies showed significant cardiac uptake and efficient excretion through renal and hepatobiliary systems, confirming its potential for targeted cardiac imaging.In conclusion, the synthesized Gd³⁺-dendrimer-amlodipine complex demonstrates promising biocompatibility, favorable contrast properties, and efficient excretion patterns in preliminary studies.Further in vivo investigations are warranted to confirm its efficacy and safety profile as a novel MR contrast agent.

100 Deals associated with Amlodipine Nicotinate

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