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

Action

agonists

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-

Login to view timeline

Structure/Sequence

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

Login to view more data

100 Translational Medicine associated with Lovastatin/Nicotinic Acid

Login to view more data

100 Patents (Medical) associated with Lovastatin/Nicotinic Acid

Login to view more data

18

Literatures (Medical) associated with Lovastatin/Nicotinic Acid

01 Apr 2015·Future Medicinal ChemistryQ4 · MEDICINE

Repurposing Pharma Assets: An Accelerated Mechanism for Strengthening the Schistosomiasis Drug Development Pipeline

Q4 · MEDICINE

Article

Author: Graef, Katy M ; Ramamoorthi, Roopa ; Dent, Jennifer

Schistosomiasis, one of 17 diseases deemed to be neglected by the World Health Organization, has received little attention from the biopharmaceutical industry. Due to this, only a handful of drugs have been developed to treat schistosomiasis, with only one, praziquantel, used in most endemic regions. Growing concern over resistance coupled with praziquantel's incomplete efficacy across all stages of the Schistosoma platyhelminth life cycle highlights the urgent need for new drugs. The WIPO Re:Search consortium is a platform whereupon biopharmaceutical company compounds are being repurposed to efficiently and cost-effectively develop new drugs for neglected diseases such as schistosomiasis. This article summarizes recent clinical-stage efforts to identify new antischistosomals and highlights biopharmaceutical company compounds with potential for repurposing to treat schistosomiasis.

01 Nov 2013·International Journal of Clinical PracticeQ4 · MEDICINE

The effect of pioglitazone and extended-release niacin on HDL-cholesterol in diabetes patients in a real-world setting

Q4 · MEDICINE

Article

Author: Yarlagadda, K. V. S. N. ; Vaughan, A. G. ; Gleason, S. ; Johnson, J. F. ; Bhargava, A.

OBJECTIVEThis retrospective study was designed to assess the effects of the combination of pioglitazone and extended-release niacin on the lipid panel, particularly HDL-cholesterol, when used in patients with type 2 diabetes in an endocrinology specialty practice.METHODSThe electronic medical records of 434 adult patients with type 2 diabetes receiving extended-release niacin and pioglitazone were screened for review. Patients with type 2 diabetes and hyperlipidemia were included for review if they received the combination of pioglitazone at doses ≥ 15 mg/day and extended-release niacin (Niaspan) at doses ≥ 1000 mg/day for ≥6 months. Statistical analysis used paired t-tests with p < 0.05 as statistically significant. Both ANOVA and the Tukey-Kramer test for multiple comparisons (α = 0.05) were also used.RESULTSA total of 47 patients, 83% were men with average age of 58, met all eligibility criteria for the study. Compared with baseline, a statistically significant increase in HDL-C (+ 25.13%, p < 0.0001) was observed at the conclusion of combination therapy. The HDL-C levels progressively increased with duration of combination treatment, and were not correlated with concomitant statin use. Significant decreases in total cholesterol and triglycerides were detected, and HbA1c decreased 0.84% during combination therapy for all therapies combined.CONCLUSIONThe combination of pioglitazone and extended-release niacin in patients with type 2 diabetes and hyperlipidemia, used in commonly prescribed doses for at least 6 months, resulted in statistically significant improvements in HDL-C, total cholesterol, and triglycerides, and did not result in deteriorations in glycemic control.

14 May 2012·Chromatography Research International

Pharmacokinetics of Single-Dose and Multi-Dose of Lovastatin/Niacin ER Tablet in Healthy Volunteers

Author: Yang, Jing ; Lu, Chen-tao ; Jia, Yan-yan ; Wen, Ai-dong ; Ding, Li-kun ; Ying, Song ; Zhu, Yan-rong

An extended-release (ER) niacin and lovastatin fixed-dose combination has been developed for the treatment of primary hypercholesterolemia and mixed dyslipidemia. The purpose of the present study was to examine the drug interaction between niacin and lovastatin after multi-dose oral administration of lovastatin/niacin ER combination in healthy Chinese volunteers. A single-center, randomized, open-label, 5-period crossover study was conducted in thirty healthy volunteers aged 18 to 45 years with a washout period of 8 days. Subjects were randomized to receive multiple doses of treatment A (1 500 mg niacin ER tablet), B (1 20 mg lovastatin tablet), C (1 20 mg lovastatin and 500 mg niacin-ER tablet), D (2 10 mg lovastatin and 350 mg niacin-ER tablets) or E (2 10 mg lovastatin and 500 mg niacin-ER tablets) in 1 of 5 sequences (ABCDE, BCDEA, CDEAB, DEABC, EABCD) per period. Lovastatin, niacin and its metabolites (nicotinuric acid and nicotinamide) were determined in plasma by LC/MS method. Pharmacokinetic parameters were calculated, and least square mean ratios and 90% confidence intervals for Cmax⁡ and AUC (0–24) were determined for lovastatin/niacin ER versus niacin ER or lovastatin. It revealed that the formulation had no potential drug interaction in healthy Chinese volunteers when the dosage was increased from 500 mg to 1000 mg.

100 Deals associated with Lovastatin/Nicotinic Acid

Login to view more data

External Link

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

R&D Status

10 top R&D records.

Login

to view more data

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