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

Action

antagonists

Mechanism

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

Therapeutic Areas

Cardiovascular Diseases

Active Indication-

Inactive Indication

Chronic heart failureEssential HypertensionHeart Failure+ [3]

Originator Organization

GSK Plc

Active Organization-

Inactive Organization

GSK PlcWaylis Therapeutics LLC

Drug Highest PhaseWithdrawn

First Approval Date

United States (20 Oct 2006),

Heart FailureHypertensionVentricular Dysfunction, Left

Regulation-

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Structure/Sequence

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 recruitingNot Applicable

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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4,957

Literatures (Medical) associated with Carvedilol Phosphate

24 Mar 2025·Journal of Biomolecular Structure and Dynamics

Bioprospecting of Meliaceae family phytomolecules for the treatment of monkeypox virus infection: a QSAR modeling and MD simulation approach

Article

Author: AlShehail, Bashayer M. ; Al Kaabi, Nawal A. ; Alissa, Mohammed ; Alotaibi, Nouf ; Alsomali, Ghaneema ; Al-Subaie, Maha F. ; Alqahtani, Ali S. ; Rabaan, Ali A. ; Halwani, Muhammad A. ; Alshehri, Ahmad A. ; Almansour, Zainab H. ; Khamis, Faryal

Recent monkeypox virus (MPXV) infections show the risk of MPXV transmission that persists today and the significance of surveillance and quick response methods to stop the virus's spread. Currently, the monkeypox virus infection is not specifically treated. In this study, QSAR models were designed using known inhibitors of cysteine proteinase from the vaccinia virus, where the Random Forest model and Ridge model had showed the best correlation between predicted and observed EC₅₀. These models were used to screen Maliaceae family phytochemicals against MPXV cysteine proteinase. The compound, IMPHY010637 was detected in top 5 from both the QSAR screening models and showed best docked score (-8.6 kcal/mol) and thus selected for further investigation. Further, the IMPHY010637 showed interaction with the catalytic residue His²⁴¹ of the protein as reported in earlier studies. The ADMET analysis of the compound showed the acceptable drug-like properties of IMPHY010637. However, these properties could be improved after experimental validation of protein-ligand binding. Both docked complex and poses created in 100 ns MD simulation of the protein-ligand complex showed the presence of multiple hydrogen bonds. RMSD and conformation analysis showed stable binding of IMPHY010637 with the cysteine proteinase of MPXV at its active site. Compared to the known inhibitor, IMPHY010637 showed better binding with the protein as observed by the PCA and MM/GBSA analysis. This study concluded IMPHY010637 as a potential inhibitor for the cysteine proteinase of MPXV using computational methods that could be tested in in-vitro experiments.Communicated by Ramaswamy H. Sarma.

01 Mar 2025·Journal of Molecular Biology

DTA-GTOmega: Enhancing Drug-Target Binding Affinity Prediction with Graph Transformers Using OmegaFold Protein Structures

Article

Author: Qiang, Lyu ; Pan, Deng ; Wu, Jian ; Jiang, Yelu ; Quan, Lijun

Understanding drug-protein interactions is crucial for elucidating drug mechanisms and optimizing drug development. However, existing methods have limitations in representing the three-dimensional structure of targets and capturing the complex relationships between drugs and targets. This study proposes a new method, DTA-GTOmega, for predicting drug-target binding affinity. DTA-GTOmega utilizes OmegaFold to predict protein three-dimensional structure and construct target graphs, while processing drug SMILES sequences with RDKit to generate drug graphs. By employing multi-layer graph transformer modules and co-attention modules, this method effectively integrates atomic-level features of drugs and residue-level features of targets, accurately modeling the complex interactions between drugs and targets, thereby significantly improving the accuracy of binding affinity predictions. Our method outperforms existing techniques on benchmark datasets such as KIBA, Davis, and BindingDB_Kd under cold-start setting. Moreover, DTA-GTOmega demonstrates competitive performance in real-world DTI scenarios involving DrugBank data and drug-target interactions related to cardiovascular and nervous system-related diseases, highlighting its robust generalization capabilities. Additionally, the introduced DTI evaluation metrics further validate DTA-GTOmega's potential in handling imbalanced data.

01 Mar 2025·Journal of Molecular Structure

Diastereoisomeric double salts of Carvedilol with (L)- and (D)-mandelic acids.

Author: Carvalho, Paulo S. Jr ; Tenorio, Juan C. ; Alves, Diego C. B.

Crystallizing racemic Carvedilol with (S)- and (R)-mandelic acids leads to diastereomeric double salts.The salts were prepared by evaporative crystallization methods and the phases were characterized by single crystal and powder X-ray diffraction, differential scanning calorimetry, and solubility measurements.The diastereomeric double salts are isostructural; the most prominent structural feature is the enantiomeric ionic pairs assuming corresponding shapes and assembling them into racemic units.In this unit, the cation conformations are stabilized by a water mol. and the anion-anion recognition provides the formation of the racemic chain.The double salts and the true racemic Cvd mandelate salt exhibit no structural similarity.The double salts exhibit thermal stability and higher solubility than the true racemic form.The comprehension of these structures provides an insight into the interaction between Cvd enantiomers and enantiopure anions and contributes to the future resolution of the compound

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

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Chronic heart failure	Phase 1	Japan	GSK Plc	28 Aug 2008
Prehypertension	Phase 1	United States	GSK Plc	01 Nov 2007
Essential Hypertension	Phase 1	United States	GSK Plc	01 Oct 2007
Hypertension	Phase 1	United States	Waylis Therapeutics LLC	20 Oct 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)	mpjjdwzlsh(bfnlfdmphg) = kdyhuabpoz gmxefrvmly (ucoulklbrr, jqdefukqht - vvgdnbjsaz) View more	-	30 Mar 2021
				Coreg CR® (Arm II Coreg CR®)	mpjjdwzlsh(bfnlfdmphg) = qzbliteewy gmxefrvmly (ucoulklbrr, roxciumtem - oysujhcegi) View more
NCT00742508 (CTgov)	Phase 1	Chronic heart failure	41	CRV-IR+carvedilol (CRV) (CRV-IR)	httpknqmhd(bebcvbvwrj) = fvcqsivvac tffcxuswes (gsvsplynpq, suwtrgahoh - lxvxdwhwgt) View more	-	19 Aug 2010
				carvedilol (SK&F-105517-D)+SK&F-105517-D (SK&F-105517-D)	httpknqmhd(bebcvbvwrj) = axflizezxh tffcxuswes (gsvsplynpq, hubchibfor - bmtljjzvgh) View more
NCT00273052 (CTgov)	Phase 3	Hypertension	514	Carvedilol Phosphate (Coreg CR)	pywjomhwln(siwzteleop) = dltnqrhbrv pbvqfrnqoo (kuasjbqmbu, oopchusteq - wooqarytqm) View more	-	01 Feb 2010
				Toprol XL (Toprol XL)	pywjomhwln(siwzteleop) = szrvdlnpng pbvqfrnqoo (kuasjbqmbu, kipkmmcwtf - tdruudjlho) View more