Delving into the Latest Updates on Lovastatin/Nicotinic Acid with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Advicor, Niacin/lovastatin, Nicostatin

+ [2]

Target

HCAR3 x NIACR1

Mechanism

HCAR3 agonists(HM74 nicotinic acid GPCR agonists), NIACR1 agonists(Hydroxycarboxylic acid receptor 2 agonists)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Primary hypercholesterolemia

Inactive Indication

Intermittent ClaudicationPeripheral Vascular Diseases

Originator Organization

AbbVie, Inc.

Active Organization-

Inactive Organization

KOS Pharmaceuticals, Inc.

Drug Highest PhasePhase 1

First Approval Date-

Regulation-

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Structure

Molecular FormulaC30H41NO7

InChIKeyYVPOVOVZCOOSBQ-AXHZAXLDSA-N

CAS Registry365453-26-5

洛伐他汀烟酸缓释片（受试制剂）进行人体药代动力学试验，观察健康志愿受试者单次、多次给药后的血药浓度经时过程，计算各组分及其主要代谢产物的药动学参数，并与国内外文献资料进行比较，评价洛伐他汀烟酸缓释片在人体内的药代动力学特征，旨在为临床合理用药提供依据

[Translation]

The human pharmacokinetic test of lovastatin niacin sustained-release tablets (test preparation) was conducted to observe the time course of blood drug concentration after single and multiple administrations of healthy volunteers, calculate the pharmacokinetic parameters of each component and its main metabolites, and compare them with domestic and foreign literature data to evaluate the pharmacokinetic characteristics of lovastatin niacin sustained-release tablets in humans, aiming to provide a basis for rational clinical drug use

Start Date09 Nov 2012

Sponsor / Collaborator

Shanxi Kangbao Biological Product Co. Ltd.

NCT00345657 / CompletedPhase 4

Extended-Release Niacin/Lovastatin Versus Usual Care for Treatment of Dyslipidemia in a Primary Care Setting (EXTEND Study)

The purpose of this study is to investigate the benefits of combination niacin ER/lovastatin in patients receiving standard care who are not at LDL goal per ATP III guidelines.

Start Date01 Jul 2003

Sponsor / Collaborator

In His Image

[+1]

100 Clinical Results associated with Lovastatin/Nicotinic Acid

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100 Translational Medicine associated with Lovastatin/Nicotinic Acid

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100 Patents (Medical) associated with Lovastatin/Nicotinic Acid

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18

Literatures (Medical) associated with Lovastatin/Nicotinic Acid

28 Apr 2020·Clinical Chemistry and Laboratory Medicine (CCLM)Q3 · MEDICINE

Method development for quantitative determination of seven statins including four active metabolites by means of high-resolution tandem mass spectrometry applicable for adherence testing and therapeutic drug monitoring

Q3 · MEDICINE

Article

Author: Hemmer, Selina ; Meyer, Markus R. ; Wagmann, Lea ; Caspar, Achim T.

AbstractBackgroundStatins are used to treat and prevent cardiovascular diseases (CVDs) by reducing the total serum cholesterol concentration. Unfortunately, dose-related side effects and sub-optimal response, attributed to non-adherence amongst others, were described. Therefore, a fast and sensitive liquid chromatography-high-resolution tandem mass spectrometry (LC-HRMS/MS) method for adherence testing and therapeutic drug monitoring of all currently marketed statins and their active metabolites in human blood plasma should be developed, validated and tested for applicability.MethodsAtorvastatin, fluvastatin, lovastatin, pitavastatin, pravastatin, rosuvastatin, and simvastatin, as well as ortho- and para-hydroxy-atorvastatin, lovastatin hydroxy acid and simvastatin hydroxy acid were included and several internal standards (IS) tested. Validation was performed according to the guideline of the European Medicines Agency including selectivity, carry-over, accuracy, precision, matrix effects, dilution integrity and analyte stability. Finally, applicability was tested using 14 patient samples submitted for regular toxicological analysis.ResultsDue to an analytical interference of atorvastatin-d5, diazepam-d5 and pentobarbital-d5 were chosen as IS for positive and negative ionization mode, respectively. All statins and metabolites fulfilled the validation acceptance criteria except for fluvastatin, which could not be quantified reliably and reproducibly, most probably due to instability. Analyses of human plasma samples revealed concentrations of statins and metabolites below the reference plasma concentrations in the case of eight patients. However, nothing was known concerning patients’ adherence and time between intake and sampling.ConclusionsAn LC-HRMS/MS method for identification and quantification of atorvastatin, lovastatin, pitavastatin, pravastatin, rosuvastatin, simvastatin and four active metabolites was successfully developed and applicability demonstrated.

01 Jun 2012·Current Neurovascular ResearchQ4 · MEDICINE

Short-term High-Dose Effect of Lovastatin on Thrombolysis by rt-PA in a Human Whole-Blood in vitro Clot Model

Q4 · MEDICINE

Article

Author: Elkind, Mitchell S. V. ; Shaw, George J. ; Kandadai, Madhuvanthi A. ; Lindsell, Christopher J. ; Meunier, Jason

High-dose hydroxymethylglutaryl coenzyme. A reductase inhibitor (statin) administration reduces neuronal injury and improves outcomes in experimental models of acute ischemic stroke, and has been shown to be safe in a phase 1 dose-escalation study using lovastatin at doses higher than currently approved for daily use. Statins also affect the hemostatic system by upregulating t-PA expression and decreasing plasminogen activator inhibitor (PAI-1) expression, platelet adhesion and thrombus formation in animal models. Since a thrombolytic agent, recombinant tissue plasminogen activator (rt-PA), is currently the only FDA-approved therapy for use in ischemic stroke patients, it is important to ascertain whether high statin doses impact the efficacy of rt-PA. The main goal of this study was to evaluate the effect of a high dose of lovastatin and its active form, lovastatin hydroxy acid, on rt-PA thrombolysis in an in vitro model. Percentage clot lysis was measured in the presence and absence of rt-PA in three different treatment groups: lovastatin, lovastatin hydroxy acid, and ethanol. The effect of ethanol on clot lysis was studied since ethanol was used to disperse the highly hydrophobic lovastatin. The decrease in clot width over time was measured using microscopic imaging of an in vitro human whole blood clot model; an approximately 400 μm diameter clot was formed on suture silk, suspended in human fresh frozen plasma (hFFP) and exposed to treatment. In the absence of rt-PA, clot lysis did not show statistically significant differences in the percentage clot lysis between different treatment groups (p=0.103). In the presence of rt-PA, clot lysis was greater than in the absence of rt-PA for all groups, but there were no statistically significant differences between treatment groups (p=0.385). In this in vitro study, high doses of lovastatin neither impaired nor enhanced the lytic efficacy of rt-PA.

01 Apr 2012·Research in pharmaceutical sciences

Simultaneous determination of lovastatin and niacin in tablet by first and third derivative spectrophotometry and H-point standard addition methods.

Article

Author: Kazemipour, M ; Ramezani, H ; Ansari, M ; Moradalizadeh, M

Most cardiovascular diseases need to be treated by more than a simple drug and the use of combination products diminishes noncompliance. Advicor(®) as a combination product of a vitamin and a fat lowering agent has no monograph in official pharmacopeias for its quality control purposes. In this study, first and third derivative signals for NA and LV quantitation at the two pairs of wavelengths, 261 and 273 nm; 245 and 249 nm were monitored with the addition of standard solutions of NA or LV, respectively. The limits of detection were 0.03 and 0.32 mg/L for LV and NA, respectively. The limits of quantitation were 0.09 and 0.78 mg/L for LV and NA, respectively. RSD% for both interday and intraday precision was lower than 2.6 and 2.7% for LV and NA, respectively. Selectivity of the method was assessed for both degradation products produced in stress conditions and common excipients that may present in the pharmaceutical dosage forms. The recommended procedure was successfully applied to real samples.

100 Deals associated with Lovastatin/Nicotinic Acid

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Lovastatin/Nicotinic Acid	C10BA01	-

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Intermittent Claudication	Phase 2	-	KOS Pharmaceuticals, Inc.	01 Jan 2003
Peripheral Vascular Diseases	Phase 2	-	KOS Pharmaceuticals, Inc.	01 Jan 2003
Primary hypercholesterolemia	Phase 1	CN	-	07 May 2014