Delving into the Latest Updates on Fenoldopam Mesylate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Fenoldopam, Fenoldopam mesylate (USP)

+ [8]

Target

ADRA2 x D1 receptor

Action

agonists

Mechanism

ADRA2 agonists(Adrenergic receptors alpha-2 agonists), D1 receptor agonists(Dopamine D1 receptor agonists)

Therapeutic Areas

Cardiovascular DiseasesUrogenital Diseases

Active Indication-

Inactive Indication

Acute Kidney InjuryEssential HypertensionHeart Diseases+ [4]

Originator Organization

Abbott Laboratories

Active Organization-

Inactive Organization

Yangtze River Pharmaceutical Group Beijing Haiyan Pharmaceutical Co., Ltd.

Abbott Laboratories

Hospira, Inc.

Drug Highest PhaseWithdrawn

First Approval Date

United States (23 Sep 1997),

Hypertension, MalignantHypertension

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC17H20ClNO6S

InChIKeyCVKUMNRCIJMVAR-UHFFFAOYSA-N

CAS Registry67227-57-0

View All Structures (2)

The investigators will conduct a prospective, blinded, randomized, placebo-controlled trial with a sample size of 20 patients in each of the two arms (fenoldopam vs placebo) based upon a difference in serum creatinine by one standard deviation. Fluid and salt intake will be held constant within clinical parameters and carefully measured. Fenoldopam will be started at 0.1 ug/kg/min. If, after 6 hrs there is no decrease in blood pressure, the dose will be increased to 0.2 ug/kg/min. This dose will be continued throughout the remainder of the study. A study of pediatric patients previously provided to the FDA showed no hypotension at a dose of 0.2 ug/kg/min. Fenoldopam will be started 12 hrs before the first dose of indomethacin and discontinued 12 hrs after the 3rd dose of indomethacin. Study samples will include both blood and urine. The primary outcome will be a reduction in renal dysfunction, as determined by creatinine and urine output over the course of treatment. Additional outcomes will include determination of known and novel metabolomic urine markers of renal dysfunction.

Start Date06 Feb 2019

Sponsor / Collaborator

Medical College of Wisconsin

CTR20131661

/ CompletedPhase 1

甲磺酸非诺多泮注射液在高血压患者的人体药代动力学试验

[Translation] Pharmacokinetic study of fenoldopam mesylate injection in patients with hypertension

以高血压患者舒张压降低值来评价药物的线性关系，估算非诺多泮主要药代动力学参数。

[Translation]

The linear relationship of the drug was evaluated by the reduction of diastolic blood pressure in hypertensive patients, and the main pharmacokinetic parameters of fenoldopam were estimated.

Start Date05 Nov 2013

Sponsor / Collaborator

Yangtze River Pharmaceutical Group Beijing Haiyan Pharmaceutical Co., Ltd.

CTR20130438

/ CompletedPhase 2

甲磺酸非诺多泮注射液治疗高血压急症的随机、单盲、阳性药平行对照、多中心临床试验

[Translation] A randomized, single-blind, positive-drug parallel-controlled, multicenter clinical trial of fenoldopam mesylate injection in the treatment of hypertensive emergencies

以注射用硝普钠为对照，评价甲磺酸非诺多泮注射液治疗高血压急症的有效性和安全性。

[Translation]

To evaluate the efficacy and safety of fenoldopam mesylate injection in the treatment of hypertensive emergencies using sodium nitroprusside injection as a control.

Start Date04 Sep 2012

Sponsor / Collaborator

Yangtze River Pharmaceutical Group Beijing Haiyan Pharmaceutical Co., Ltd.

100 Clinical Results associated with Fenoldopam Mesylate

Login to view more data

100 Translational Medicine associated with Fenoldopam Mesylate

Login to view more data

100 Patents (Medical) associated with Fenoldopam Mesylate

Login to view more data

1,026

Literatures (Medical) associated with Fenoldopam Mesylate

01 Feb 2025·Naunyn-Schmiedeberg's Archives of Pharmacology

Contractile effects of stimulation of D1-dopamine receptors in the isolated human atrium

Article

Author: Grundig, P ; Pham, T H ; Rayo Abella, L M ; Dhein, S ; Gergs, U ; Neumann, J ; Hesse, C ; Hofmann, B

AbstractDopamine receptors have been claimed not to directly increase contractility in the human heart. Therefore, we performed contraction experiments in isolated electrically driven human atrial preparations (HAP). For comparison, we performed contraction experiments with left atrial preparations of transgenic mice which harbor a cardiac overexpression of human D1-dopamine receptors (D1-TG). In D1-TG, first we noted that dopamine (10 nM–10 µM cumulatively applied) in the presence of propranolol exerted a concentration- and time-dependent positive inotropic effect in D1-TG. In a similar fashion, dopamine increased force of contraction in the presence of 0.4 µM propranolol in HAP and these effects were amplified by pre-treatment with inhibitor of phosphodiesterase III (1 µM) cilostamide. Moreover, contractile effects of dopamine in the presence of propranolol 0.4 µM in HAP were antagonized by odapipam, haloperidol, or raclopride. Ten micromolars of fenoldopam in the presence of cilostamide increased force of contraction in HAP and this effect was antagonized by SCH 23390. We conclude that stimulation of human D1-dopamine receptors can increase force of contraction in the HAP.

01 Jan 2025·Pediatric Nephrology

Efficacy and safety of fenoldopam for the treatment of hypertensive crises in children with kidney disease: a retrospective study

Article

Author: Vigezzi, Serena ; Vidal, Enrico ; Meneghesso, Davide ; Daverio, Marco ; Tinnirello, Matteo ; Bertazza Partigiani, Nicola ; Brazzale, Alessandra Rosalba

AbstractBackgroundHypertensive crises in children represent critical medical situations characterized by severe hypertension and potential organ damage. Fenoldopam, a dopaminergic medication, offers a viable therapeutic option for managing such clinical scenarios. We aimed to evaluate efficacy and safety of fenoldopam in the management of hypertensive urgencies and emergencies.MethodsThis retrospective analysis focused on pediatric patients affected by acute or chronic kidney disease, aged 1 month–18 years, admitted to the Pediatric Nephrology and the Pediatric Intensive Care Unit at University-Hospital of Padua, Italy, who presented with a hypertensive crisis treated with fenoldopam between March 2010 and December 2022.ResultsThe study included 74 patients with median age 10 years (interquartile range [IQR] 4–15 years) who received 102 fenoldopam infusions. Seventy-two percent were already receiving antihypertensive treatment before admission. In all cases, fenoldopam was associated with a reduction of blood pressure (BP) after 8 h of treatment, but in 87% of patients reduction of the initial mean arterial pressure (MAP) was higher than 25% of calculated drop pressure. MAP normalized in 26% of cases after 24 h and in 35% after 48 h. Occurrence of hypotension was 7%, while hypokalemia was observed in 13% of cases. Patients who presented a MAP reduction not exceeding 25% of calculated drop pressure received a lower median fenoldopam dose (0.2 mcg/kg/min; IQR 0.1–0.2) compared with patients having a MAP reduction > 25% of calculated drop pressure (0.4 mcg/kg/min; IQR 0.2–0.6; p = 0.002).ConclusionsFenoldopam seems effective and safe for the treatment of hypertensive crises in children with kidney disease, at a starting dose of 0.2 mcg/kg/min. Strict BP monitoring is required to identify possible excessive drop pressure in the first hours of infusion.Graphical abstract

01 Dec 2024·Kidney International

Chronic endothelial dopamine receptor stimulation improves endothelial function and hemodynamics in autosomal dominant polycystic kidney disease

Article

Author: Hamzaoui, Mouad ; Joannidès, Robinson ; Dumesnil, Anaïs ; Arndt, Hans-Dieter ; Renet, Sylvanie ; Richard, Vincent ; Lévêque, Emilie ; Audrézet, Marie-Pierre ; Remy-Jouet, Isabelle ; Enzensperger, Christoph ; Brunel, Valéry ; Bellien, Jérémy ; Dumont, Audrey ; Groussard, Déborah ; Bertrand, Dominique ; Iacob, Michèle ; Hanoy, Mélanie ; Chevalier, Laurence ; Le Roy, Frank ; Guerrot, Dominique ; Duflot, Thomas ; Michel-Després, Aurore

Altered polycystin-mediated endothelial flow mechanosensitivity contributes to the development of hypertension and cardiovascular complications in patients with autosomal dominant polycystic kidney disease (ADPKD). Stimulation of endothelial type 5 dopamine receptors (DR5) can acutely compensate for the endothelial consequences of polycystin deficiency, but the chronic impact of this approach must be evaluated in ADPKD. Nineteen patients with ADPKD on standard of care therapy were randomized to receive a 2-month treatment with the DR agonist rotigotine using transdermal patches, nine at 2 mg/24hours and ten at 4 mg/24hours or while ten were untreated. Rotigotine at the dose of 4 mg/24hours significantly increased nitric oxide release (nitrite levels from 10±30 to 46±34 nmol/L) and radial artery endothelium-dependent flow-mediated dilatation (from 16.4±6.3 to 22.5±7.3%) in response to hand skin heating. Systemic hemodynamics were not significantly modified but aplanation tonometry showed that rotigotine at 4 mg/24hours reduced aortic augmentation index and pulse pressure without affecting carotid-to femoral pulse wave velocity. Plasma creatinine and urea, urinary cyclic AMP, which contributes to cyst growth in ADPKD and copeptin, a surrogate marker of vasopressin, were not affected by rotigotine. In mice with a specific deletion of polycystin-1 in endothelial cells, chronic infusion of the peripheral DR5 agonist fenoldopam also improved mesenteric artery flow-mediated dilatation and reduced blood pressure. Thus, our study demonstrates that in patients with ADPKD, chronic administration of rotigotine improves conduit artery endothelial function through the restoration of flow-induced nitric oxide release as well as hemodynamics suggesting that endothelial DR5 activation may represent a promising pharmacological approach to prevent cardiovascular complications of ADPKD.

100 Deals associated with Fenoldopam Mesylate

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
D00613	Fenoldopam Mesylate	C01CA19	DB00800

R&D Status

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Secondary hypertension	Phase 2	China	Yangtze River Pharmaceutical Group Beijing Haiyan Pharmaceutical Co., Ltd.	05 Nov 2013
Acute Kidney Injury	Phase 2	-	Abbott Laboratories	01 May 2002
Heart Diseases	Phase 2	-	Abbott Laboratories	01 May 2002
Kidney Failure, Chronic	Phase 2	-	Abbott Laboratories	01 May 2002
Essential Hypertension	Phase 1	China	Yangtze River Pharmaceutical Group Beijing Haiyan Pharmaceutical Co., Ltd.	18 Aug 2017
Hypertension	Phase 1	United States	Hospira, Inc.	23 Sep 1997

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00122018 \| NCT00621790 \| NCT00557219 \| NCT00747331 \| NCT02620761 \| NCT00286403 \| NCT00467181 \| NCT00982527 \| NCT01073189 \| NCT00743106 \| NCT01690832 (Pubmed \| Cochrane Database Syst Rev)	Not Applicable	Acute Kidney Injury	3,339	Fenoldopam	bsqxfudlpc(uwalmpekze) = It is uncertain whether adverse events (hypotension, myocardial infarction, drug intolerance, cardiac arrhythmias) differed between the treatment groups as the certainty of the evidence was very low. laewhdnqpq (roknzzataj ) View more	Positive	28 Nov 2024
NCT02620761 (Fenaki, CTgov)	Phase 2/3	Ductus Arteriosus, Patent \| Acute Kidney Injury	1	0.9%NS (Control)	swpvfjvnkl(lqvprcizak) = ycmxwfnulx qxmrmxrdej (flprrykcce, wytvjfwbkz - bgyvhvjrww) View more	-	16 Sep 2022
				Fenoldopam (Fenoldopam)	swpvfjvnkl(lqvprcizak) = lqxuqccstb qxmrmxrdej (flprrykcce, hfdnkvxnfk - ufbvtfgahi) View more
NCT00743106 (CTgov)	Not Applicable	Nephrosis	90	Placebo (Placebo)	mznuougprv(eygoknsbem) = qbhgkosnzv jrpdfzrgea (zjggfzgtjl, trdcvefmit - qkpnelfrgv) View more	-	31 Oct 2016
				Fenoldopam (Fenoldopam)	mznuougprv(eygoknsbem) = ugnbxzzdts jrpdfzrgea (zjggfzgtjl, snhjjkhgbh - nwilurnqqk) View more
NCT00621790 (Pubmed \| JAMA)	Phase 3	-	667	Fenoldopam	(xnnclcuuay) = hwpxnffbzx sztnpovjsq (kvlfrhucjb )	-	03 Dec 2014
				Placebo	(xnnclcuuay) = cyvmluezbt sztnpovjsq (kvlfrhucjb )