Delving into the Latest Updates on Diltiazem Malate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Diltiazem malate (USAN), Tiamate

Target

CACNG1

Action

blockers

Mechanism

CACNG1 blockers(Voltage-dependent calcium channel gamma-1 subunit blockers)

Therapeutic Areas

Nervous System DiseasesCardiovascular DiseasesOther Diseases+ [2]

Active Indication-

Inactive Indication

Angina PectorisAtrial FibrillationBradycardia+ [3]

Originator Organization

Merck & Co., Inc.

Active Organization-

Inactive Organization

Bristol Myers Squibb Co.

Merck Sharp & Dohme Corp.

Merck & Co., Inc.

License Organization-

Drug Highest PhaseWithdrawn

First Approval Date

United States (04 Oct 1996),

Angina PectorisBradycardiaHypertension

Regulation-

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Structure/Sequence

Molecular FormulaC26H32N2O9S

InChIKeyIUSFTUWHKCSCDY-QTKZZPNDSA-N

CAS Registry144604-00-2

View All Structures (2)

This research aimed to identify sources of pharmaceuticals and personal care products (PPCPs) in the Kozlowa Gora catchment, southern Poland, and assess their temporal and spatial variability.PPCP monitoring was conducted from 2020 to 2022.Samples were taken from the Brynica River and other streams.Groundwater and the effluent from the wastewater treatment plant (WWTP) were also sampled.The monitoring screened 109 PPCPs using the LC-MS/MS method.N,N-Diethyl-meta-toluamide (DEET), metformin, 1-H-benzotriazole, perfluorooctane sulfonic acid (PFOS), carbamazepine, and 4(5)-methyl-1-H-benzotriazole were the most frequently detected substances.The highest total PPCP concentrations in surface waters reached 30790 ng/L, with up to 53 compounds detected at one point.Results indicated temporal and spatial variability, with higher concentrations and more PPCPs during winter periods and increased contamination downstream from the WWTP.DEET was the only contaminant consistently found in the shallow aquifer discharged into the Brynica, however groundwater impact on the river ′s water quality is negligible.The study confirmed the WWTP as the primary source of PPCPs, with the number of detected substances in effluent samples amounting to 65 and their total concentrations reaching 148265 ng/L.Addnl. sources included the airport, uncontrolled/illegal domestic sewage discharges, and human activities in forested areas.This study was the first in Poland to implement a PPCP monitoring approach in a drinking water reservoir catchment area using multiple monitoring points and sampling campaigns.The results revealed the constant presence of PPCPs in a moderately urbanised catchment area, highlighting the importance of regular monitoring to understand PPCP migration in the environment.

01 Jun 2025·Journal of Hydrology

A closed municipal landfill as a source of emerging contaminants in adjacent groundwater: pharmaceuticals and personal care products occurrence and environmental risk assessment

Author: Slosarczyk, Kinga ; Dabrowska, Dominika

The aim of this study was to determine the occurrence and perform the environmental risk assessment (ERA) for emerging contaminants, primarily pharmaceuticals and personal care products (PPCPs), in the groundwater near a closed municipal landfill, on the example of a site in Tychy (southern Poland).Groundwater from a shallow aquifer was sampled in two seasons from eight piezometers located upstream, downstream, and on top of the landfill.The anal. covered 128 PPCPs.Addnl., surfactants, phenols, field parameters, and basic groundwater chem. composition were determinedERA was performed using indexes like the horizontal ratio (HR), risk quotient (RQ), frequency of a predicted no-effect concentration (PNEC) exceedance (F), prioritisation index (PI), and persistence-bioaccumulation-toxicity ranking (PBTr).The number of detected PPCPs in the groundwater reached up to 54, with total PPCP concentrations ranging from 492 to 3,230,036 ng/L.The study also revealed the presence of phenols (up to 62 mg/L) and surface active agents, particularly anionic surfactants (up to 77.7 mg/L).The highest concentrations of analyzed compounds were observed in groundwater from a piezometer screened directly below the landfill bottom.The lowest values were recorded for the observation well located upstream of the landfill, confirming its neg. impact and the release of PPCPs into the aquifer.The influence of the landfill was also reflected by low HR values (below 1) and high values of the site-specific risk quotient (above 1).Based on PI results, ibuprofen, bisphenol A, propyphenazone, and sulfamerazine were considered the compounds of highest risk.The same substances were among compounds with the highest PBTr values.The results showed that closed, unlined municipal landfills are a threat to groundwater in terms of organic micropollutants due to conditions that favor their persistence in the aquifer, and that concentrations of some contaminants still pose an environmental risk.

01 Jun 2025·Food Chemistry

High-throughput screening of new psychoactive substances and related compounds in food by UHPLC-Q/Orbitrap

Article

Author: Wu, Wenlin ; Huang, Xia ; Liu, Shiyao ; Chen, Xiaoqi ; Zhou, Yan ; Wan, Yuping ; Xia, Bing ; Guo, Tianrong ; Shi, Peiyu ; Xiao, Quanwei ; Zhang, Min

Currently, there is concern about food products to which new psychoactive substances (NPS) have been added illegally. However, rapid, high-sensitivity, and high-throughput screening methods for such harmful substances have not been reported yet. In this study, a high-throughput non-targeted screening strategy was developed based on UHPLC-Q/Orbitrap. First, optimized pretreatment methods for typical high-risk matrices were established. Second, an accurate, efficient, and scalable high resolution mass spectrometry database containing 206 NPS and related compounds was constructed. The fragmentation pathways of three different types of fentanyl-related compounds were then systematically investigated to enhance compound identification. Additionally, a non-targeted screening strategy was developed using warning ions derived from 24 fentanyl-related compounds, streamlining the identification of NPS. This strategy was applied to 100 food samples with possible illegal additives and demonstrated its effectiveness. In summary, this study provides robust technical support for regulatory authorities in combating the illegal addition of food products.

100 Deals associated with Diltiazem Malate

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External Link

KEGG	Wiki	ATC	Drug Bank
D03830	Diltiazem Malate	C05AE03 C08DB01	DB00343

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Hepatitis C	Phase 1	Canada	Merck Sharp & Dohme Corp.	01 May 2012
Hypertension	Phase 1	United States	Merck & Co., Inc.	04 Oct 1996
Thrombosis	Preclinical	-	Bristol Myers Squibb Co.	01 Jul 2016
Atrial Fibrillation	Preclinical	United States	Bristol Myers Squibb Co.	01 Sep 2010

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT04551963 (CTgov)	Phase 1	B-Cell Lymphoma	26	Fluconazole+Diltiazem+Zanubrutinib (Arm A: Zanubrutinib With or Without Moderate CYP3A)	cnslqpwyum(rjupligtke) = kimbkimfpc kpdmbymuqd (vmoajkjdtp, bafdrgulnk - iboegfydnb) View more	-	27 Nov 2023
				Voriconazole+Clarithromycin+Zanubrutinib (Arm B: Zanubrutinib With or Without Strong CYP3A)	umzsmhbyvr(squobryvda) = ndnlxkkqvz dceuotqhoo (vlfsdewaww, akbjzmwwix - wstreypwft) View more
NCT02807909 (Pubmed \| Cardiol Ther) Manual	Phase 1	-	28	Itraconazole+Diltiazem+Milvexian	(fcqvuovkiu) = ugwjpozqet duxnqlzvjr (utraqccjie ) View more	Positive	31 May 2022
AAIC2021	Not Applicable	Alzheimer Disease	-	Sildenafil	nfoqfbmfee(mphzsqnsdd): HR = 0.35 (95% CI, 0.29 - 0.44), P-Value = < 1 × 10^-8	-	31 Dec 2021
				Diltiazem
ESC2021	Not Applicable	Maintenance	81	Diltiazem	njbmvfldxc(gtmcztfllx): HR = 0.8 (95% CI, 0.4 - 2.2), P-Value = 0.81 View more	-	29 Jun 2021
				No Diltiazem
Pubmed \| Am J Emerg Med	Not Applicable	Atrial Fibrillation	-	IVP Diltiazem	czokehdmjg(clnfxdzcsv) = whcajbuzpn pvyamgkfpp (yatqiaqqye, 22) View more	Positive	01 Sep 2020
				IVP Metoprolol	czokehdmjg(clnfxdzcsv) = eexkvnxcly pvyamgkfpp (yatqiaqqye, 15) View more
NCT03070470 (CTgov)	Phase 1	Long QT Syndrome	60	Ranolazine (Ranolazine)	tzloekfwsn(cwjqrklkez) = hercxpckmc luzgexgawc (lpnueoqyiq, cnjibidajl - qrvgeoaxmi) View more	-	18 Jan 2020
				Verapamil (Verapamil)	tzloekfwsn(cwjqrklkez) = kceojbccai luzgexgawc (lpnueoqyiq, suootjzedb - jbbrtvxsxp) View more
NCT00319982 (Treatment of Preclinical Hypertrophic Cardiomyopathy With Diltiazem, CTgov)	Phase 2/3	Cardiomyopathy, Hypertrophic	39	Diltiazem (I- Diltiazem)	flfqdcloyx(qkbjgudshq) = xpbnlpojae ozjbjsevbp (pogiguoyvz, gaavocthkv - bwwrbkwirf) View more	-	07 Apr 2015
				Placebo (II- Placebo)	flfqdcloyx(qkbjgudshq) = mjdxlsefiv ozjbjsevbp (pogiguoyvz, woouhehyud - hacehfdiic) View more
NCT00319982 (Treatment of Preclinical Hypertrophic Cardiomyopathy With Diltiazem, Pubmed \| JACC Heart Fail)	Phase 2/3	Cardiomyopathy, Hypertrophic	38	Diltiazem 360 mg/day	rafxskczcv(gikzztuysv) = jvwxsbwrpw cuzpcnbcdb (yfjcxtmzsz )	-	01 Feb 2015
				Placebo	rafxskczcv(gikzztuysv) = zorowxgmud cuzpcnbcdb (yfjcxtmzsz )
NCT01914926 (DiME, CTgov)	Phase 4	Atrial Flutter \| Atrial Fibrillation	54	Metoprolol (Metoprolol Study Group)	ayrpwukbbx(otsiwvxoyi) = zqdcyseoyi qhgozxqxsn (osramarnro, mhbacptyob - jkncqfaulo) View more	-	16 Dec 2013
				Diltiazem (Diltiazem Study Group)	ayrpwukbbx(otsiwvxoyi) = tjvknadpmf qhgozxqxsn (osramarnro, fpdclkqpyb - cwvxynzwee) View more
NCT02801305 \| NCT02419534 (Pubmed)	Not Applicable	Fissure in Ano	61	Diltiazem gel (2%)	khhmijpzjw(cuyfqviiwg) = Headache occurred in all of the patients treated with Glyceril trinitrate but none of the patients treated with Diltiazem developed headache vimorsjhxb (agjfqksolr )	Positive	01 Dec 2012
				Glyceril trinitrate ointment (0.2%)