Delving into the Latest Updates on Carvedilol Phosphate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

COREG MR, Carvedilol, Carvedilol phosphate (USAN)

+ [4]

Target

α-adrenergic receptor x β1-adrenergic receptor

Mechanism

α-adrenergic receptor antagonists(Alpha adrenergic receptor antagonists), β1-adrenergic receptor antagonists(Beta-1 adrenergic receptor antagonists)

Therapeutic Areas

Cardiovascular Diseases

Active Indication

Heart FailureHypertensionVentricular Dysfunction, Left

Inactive Indication

Essential Hypertension

Originator Organization

GSK Plc

Active Organization

Waylis Therapeutics LLC

Inactive Organization

GSK Plc

Drug Highest PhaseApproved

First Approval Date

US (20 Oct 2006),

Heart FailureHypertensionVentricular Dysfunction, Left

Regulation-

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Structure

Molecular FormulaC48H60N4O17P2

InChIKeyLHNYXTULDSJZRB-UHFFFAOYSA-N

CAS Registry610309-89-2

View All Structures (2)

Remote ischemic conditioning has been shown to protect myocardium from ischemia-reperfusion injury during cardiac intervention or cardiac surgery. However, effect of beta-blocker, commonly used cardiovascular medication in patients with cardiac diseases such as hypertension or angina pectoris, on cardioprotective role of remote ischemic conditioning has not been well documented. The purpose of the study is to investigate the effect of beta-blocker on remote ischemic conditioning in healthy volunteers.

Start Date17 May 2017

Sponsor / Collaborator

Seoul National University Hospital

CTR20150261 / Active, not recruiting

硫酸卡维地洛缓释胶囊（规格：72 mg）在中国健康男性受试者中的单次剂量、随机、开放生物等效性研究

[Translation] A single-dose, randomized, open-label bioequivalence study of carvedilol sulfate extended-release capsules (strength: 72 mg) in healthy Chinese male subjects

研究健康男性受试者在空腹状态或进食高脂食物后，单次口服由江苏恒瑞医药股份有限公司生产的硫酸卡维地洛缓释胶囊（规格：72 mg）和葛兰素史克制药有限公司生产的磷酸卡维地洛缓释胶囊的相对生物利用度，评价两制剂间的生物等效性。评价食物对硫酸卡维地洛缓释胶囊（规格：72 mg）人体内生物利用度的影响。

[Translation]

To study the relative bioavailability of carvedilol sulfate extended-release capsules (specification: 72 mg) produced by Jiangsu Hengrui Medicine Co., Ltd. and carvedilol phosphate extended-release capsules produced by GlaxoSmithKline Pharmaceuticals Co., Ltd. in healthy male subjects after a single oral administration in the fasting state or after a high-fat meal, and to evaluate the bioequivalence between the two preparations. To evaluate the effect of food on the bioavailability of carvedilol sulfate extended-release capsules (specification: 72 mg) in humans.

Start Date30 Sep 2014

Sponsor / Collaborator

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

100 Clinical Results associated with Carvedilol Phosphate

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100 Translational Medicine associated with Carvedilol Phosphate

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100 Patents (Medical) associated with Carvedilol Phosphate

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20

Literatures (Medical) associated with Carvedilol Phosphate

01 Oct 2022·Journal of Pharmaceutical and Biomedical Analysis

Functional group-specific multilateral derivatization cum extraction method for simultaneous quantification of genotoxic impurities in carvedilol phosphate drug using GC-MS and their toxicity assessments

Article

Author: Thenmozhi, Kathavarayan ; Elumalai, Sambandan ; Sabarinathan, Subbaramanian ; Ponnusamy, Vinoth Kumar ; Senthilkumar, Sellappan

A simple and facile functional group-specific multilateral derivatization cum extraction method coupled with GC-MS based analytical methodology has been developed for the rapid identification and determination of five potential genotoxic impurities (GTIs), including epichlorohydrin, hydrazine, phenylhydrazine, 3-chloro-1,2-propanediol and 1-(2-chloroethoxy)- 2-methoxybenzene in the carvedilol phosphate (CRV-P) drug active pharmaceutical ingredient (API). A generic synthetic route has been explored to apply the current investigation to the majority of the market available synthetic routes for the carvedilol process. Five significant GTIs were identified, and their toxicity was examined using in-silico model. The pharmacokinetic and pharmacodynamic properties of the impurities were compared with the drug molecule to evince the associated risk of impurities during therapeutic action. Furthermore, a quantitative comparison has been made for each impurity with the drug molecule for their ADMET properties, and the potential nature of the impurities has been thoroughly assessed. The developed method encompasses simple derivatization cum extraction-oriented GC-MS method for the reported GTIs, which was also validated as per current ICH guidelines. The obtained LOD and LOQ for the method were between 0.06 ~ 0.61 µg/g and 0.17 ~ 1.8 µg/g, respectively, and the r² values (0.994 ~ 0.997) show that the method is very sensitive and linear over a wide range (LOQ to 120 % of the target concentration). The percentage recoveries and relative standard deviation obtained were between 85.3 and 109.5 and 0.1-4.7, respectively, showing fit for purpose. Moreover, method precision, intermediate precision, and robustness of the method have also been successfully demonstrated. Thus, this method could be directly engaged as the quality forecasting tool for the marketed drug samples aimed at the estimation of the reported GTIs at trace level.

01 Apr 2019·Carbohydrate PolymersQ1 · CHEMISTRY

Smart karaya-locust bean gum hydrogel particles for the treatment of hypertension: Optimization by factorial design and pre-clinical evaluation

Q1 · CHEMISTRY

Article

Author: Sen, Kalyan Kumar ; Laha, Bibek ; Maiti, Sabyasachi ; Goswami, Rimpa

This investigation was undertaken to unveil the controlled drug delivery and preclinical anti-hypertensive potential of a novel interpenetrating biopolymer-based network of karaya gum and carboxymethyl locust bean gum (CLBG). The Williamson synthesis of CLBG was confirmed after analyzing FTIR spectra, degree of O-carboxymethyl group substitution and viscosity. The hydrogel particles (HPs) were developed using aluminium chloride solution as cross-linker. A full 3² factorial design approach was adopted for the optimization of two responses: drug entrapment efficiency and drug release (%) in simulated gastrointestinal conditions at 10 h. FE-SEM images and EDX spectra supported the formation of spherical HPs and successful entrapment of the drug in the HPs. Depending upon formulation variables, the drug entrapment efficiency of the HPs lied in the range of 84-98%. The HP matrix was chemically compatible for carvedilol phosphate as was suggested by infrared, thermal and x-ray analyses. The swelling kinetics of HPs corroborated well with the pH-dependent in vitro drug discharge characteristics. The drug release from HPs was found to follow anomalous transport mechanism with varying contribution of simple diffusion and polymer relaxation as was elucidated by Peppas-Sahlin model equation. Preclinical data suggested that the optimized HPs had an excellent blood pressure lowering activity in male Swiss albino mice up to 10 h.

01 Jun 2017·American Heart JournalQ2 · MEDICINE

Lisinopril or Coreg CR in reducing cardiotoxicity in women with breast cancer receiving trastuzumab: A rationale and design of a randomized clinical trial

Q2 · MEDICINE

Article

Author: Krischer, Jeffrey ; Guglin, Maya ; Munster, Pamela ; Fink, Angelina

BACKGROUNDTrastuzumab (TZB) is an established therapy for HER2-positive breast cancer. The use of TZB is commonly associated with cardiotoxicity manifesting as asymptomatic decrease in left ventricular ejection fraction (LVEF) or overt heart failure. Several studies demonstrated favorable effects of angiotensin-converting enzyme (ACE) inhibitors and β-blockers (BBs) in the prevention of chemotherapy-induced cardiotoxicity. We hypothesize that patients, randomized to receive an ACE inhibitor or a BB during trastuzumab therapy for breast cancer, will maintain a higher LVEF than patients randomized to placebo.METHODS AND RESULTSWe designed a prospective, multicenter, randomized, phase II placebo-controlled clinical trial to evaluate the effects of an ACE inhibitor (lisinopril) and a BB (carvedilol phosphate-extended release) on cardiotoxicity in patients with breast cancer who are receiving adjuvant or neoadjuvant TZB therapy. The primary objectives include (1) comparison of incidence of cardiotoxicity and (2) comparison of LVEF as a continuous variable in between the arms. Cardiotoxicity was defined as an absolute decrease in LVEF from baseline of ≥10% at follow-up or an absolute decrease of ≥5% in LVEF from baseline for individuals with <50% LVEF at follow-up. The target accrual is 468 participants, representing patients both with and without anthracycline exposure. The enrollment is completed. The trial is co-sponsored by University of South Florida and National Cancer Institute. The LVEF is being evaluated by echocardiography or multigated acquisition scan.CONCLUSIONSIf we can demonstrate that the use of an ACE inhibitor or a BB can reduce the degree of TZB-induced cardiotoxicity, it is hoped that patients will receive complete and uninterrupted TZB therapy for breast cancer without compromising cardiac function.

100 Deals associated with Carvedilol Phosphate

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External Link

KEGG	Wiki	ATC	Drug Bank
D03415	Carvedilol Phosphate	C07AG02	DB01136

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Heart Failure	US	Waylis Therapeutics LLC	20 Oct 2006
Hypertension	US	Waylis Therapeutics LLC	20 Oct 2006
Ventricular Dysfunction, Left	US	Waylis Therapeutics LLC	20 Oct 2006

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Essential Hypertension	Phase 1	US	GSK Plc	01 Oct 2007
Hypertension	Phase 1	US	GSK Plc	05 Jan 2006
Hypertension	Phase 1	PR	GSK Plc	05 Jan 2006
Hypertension	Phase 1	CA	GSK Plc	05 Jan 2006

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01009918 (Lisinopril or Coreg CR in Reducing Side Effects in Women With Breast Cancer Receiving Trastuzumab, CTgov)	Phase 2	Cardiotoxicity \| Breast Cancer	468	lisinopril (Arm I Lisinopril)	wstrsmebrf(xkyfvfeakf) = xtjnwxohyk vtjdfldnpu (uleamhjmlb, tgbttnynjn - maiexbypxd) View more	-	30 Mar 2021
				Coreg CR® (Arm II Coreg CR®)	wstrsmebrf(xkyfvfeakf) = kpqygvewyg vtjdfldnpu (uleamhjmlb, kidzpientd - rxvqdmxcdq) View more
NCT00742508 (CTgov)	Phase 1	Chronic heart failure	41	CRV-IR+carvedilol (CRV) (CRV-IR)	jjdayzjzxc(ykuqmpmtyz) = agitfjzddc vswwzdagtn (rgbmxcovos, jkthyonart - pimieylhpo) View more	-	19 Aug 2010
				carvedilol (SK&F-105517-D)+SK&F-105517-D (SK&F-105517-D)	jjdayzjzxc(ykuqmpmtyz) = ccaunlsmzh vswwzdagtn (rgbmxcovos, vowuyrncfg - zspvekriaf) View more
NCT00273052 (CTgov)	Phase 3	Hypertension	514	Carvedilol Phosphate (Coreg CR)	klhxpvtchs(gvcmnwpgip) = erotsrlhjw xqdgutgjry (nqrsxzvebm, ysgtdfxljw - nojjgqhewy) View more	-	01 Feb 2010
				Toprol XL (Toprol XL)	klhxpvtchs(gvcmnwpgip) = ayomrnqagw xqdgutgjry (nqrsxzvebm, tkzlksnpji - lpphsnqznq) View more