Delving into the Latest Updates on Amlodipine besilate/Valsartan with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Amlodipine (as besylate)/Valsartan, Amlodipine /Valsartan, Amlodipine/Valsartan

+ [16]

Target

AT1R x VDCCs

Mechanism

AT1R antagonists(Angiotensin II Receptor Type 1 antagonists), VDCCs blockers(Voltage-gated calcium channel blockers)

Therapeutic Areas

Cardiovascular Diseases

Active Indication

HypertensionEssential Hypertension

Inactive Indication-

Originator Organization

Novartis Pharma AG

Active Organization

Novartis Europharm Ltd.

Novartis Pharmaceuticals Corp.

Mylan NV

+ [1]

Inactive Organization

Novartis AG

Drug Highest PhaseApproved

First Approval Date

EU (15 Jan 2007),

Essential Hypertension

Regulation-

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Structure

Molecular FormulaC24H29N5O3

InChIKeyACWBQPMHZXGDFX-QFIPXVFZSA-N

CAS Registry137862-53-4

View All Structures (2)

The American College of Cardiology/American Heart Association hypertension guidelines recommend treatment initiation with dual antihypertensive therapy in adults with stage 2 hypertension (corresponding to grade 1 and 2 in the ESH classification) and an average BP >20/10 mm Hg above target. Amlodipine and valsartan are two of the most commonly prescribed medications for the treatment of hypertension (high blood pressure). In Pakistan multiple studies were conducted on Hypertension and use of Single Pill Combination in uncontrolled Hypertension. However, no study was conducted to assess the role of Single Pill Combination (SPC) like Amlodipine and Valsartan in newly diagnosed hypertension and to assess their quality of life by patients' satisfaction with their medication after managing the hypertension with the SPC.

Start Date28 Sep 2024

Sponsor / Collaborator

The Searle Co. Ltd.

CTR20242402 / RecruitingNot Applicable

缬沙坦氨氯地平片（I）在健康人体空腹/餐后状态下的生物等效性试验

[Translation] Bioequivalence study of valsartan and amlodipine tablets (I) in healthy volunteers in fasting and postprandial states

主要研究目的本研究以石家庄市普力制药有限公司持证的缬沙坦氨氯地平片（I）（规格：每片含缬沙坦 80mg、氨氯地平 5mg）为受试制剂，Novartis Pharma SchweizAG 持证的缬沙坦氨氯地平片（I）（商品名：倍博特，规格：每片含缬沙坦80mg、氨氯地平 5mg）为参比制剂，进行空腹/餐后状态下人体生物等效性试验，评价受试制剂和参比制剂在健康受试者体内的生物等效性。次要研究目的观察受试制剂和参比制剂在健康受试者中的安全性。

[Translation]

Main research purpose This study uses the valsartan amlodipine tablets (I) (specification: each tablet contains 80 mg valsartan and 5 mg amlodipine) certified by Shijiazhuang Puli Pharmaceutical Co., Ltd. as the test preparation and the valsartan amlodipine tablets (I) (trade name: Bebot, specification: each tablet contains 80 mg valsartan and 5 mg amlodipine) certified by Novartis Pharma SchweizAG as the reference preparation to conduct a human bioequivalence test under fasting/postprandial conditions to evaluate the bioequivalence of the test preparation and the reference preparation in healthy subjects. Secondary research purpose Observe the safety of the test preparation and the reference preparation in healthy subjects.

Start Date05 Aug 2024

Sponsor / Collaborator

Shijiazhuang Puli Pharmaceutical Co Ltd.

NCT06193044 / Not yet recruitingPhase 1

A Single Dose, Randomized, Open-label, Two-treatment, Four-period, Two-sequence, Replicate Crossover Bioequivalence Study of Generic Amlodipine and Valsartan Tablets 10/160 mg and Reference Product (Exforge® 10/160 mg Tablets)

Comparative randomized, Single dose, Two-treatment, Four-period, Two-sequence, Replicate Crossover Bioequivalence Study to determine the bioequivalence of Amlodipine / valsartan from Amlodipine/Valsartan 10/160 film coated tablets and Exforge10/160 mg film coated tablets (Novartis Pharma, USA).

Start Date07 May 2024

Sponsor / Collaborator

International Bio Research

100 Clinical Results associated with Amlodipine besilate/Valsartan

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100 Translational Medicine associated with Amlodipine besilate/Valsartan

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100 Patents (Medical) associated with Amlodipine besilate/Valsartan

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11

Literatures (Medical) associated with Amlodipine besilate/Valsartan

01 Nov 2022·Archives of biochemistry and biophysics

Sacubitril/valsartan attenuates myocardial ischemia/reperfusion injury via inhibition of the GSK3β/NF-κB pathway in cardiomyocytes

Article

Author: Zhang, Hanwen ; Chen, Mingyue ; He, Hao ; Liu, Meng ; Hu, Qianfan ; Hong, Mei ; Zhang, Lai ; Xiao, Fangping ; Wang, Lei ; Yang, Yaqing ; Jia, Zhiqiang

In ischemia/reperfusion (I/R) injury, both inflammation and apoptosis play a vital role, and the inhibition of excessive inflammation and apoptosis show substantial clinical potential in the treatment of I/R disease. The role of sacubitril/valsartan (SAC/VAL)-a first-in-class angiotensin receptor-neprilysin inhibitor (ARNI)-in inflammation regulation and apoptosis in the context of I/R injury needs to be further explored. In this study, we investigate the short- and long-term effects of SAC/VAL administration in treating adult murine I/R injury both in vivo and in vitro. Our results verified that the application of SAC/VAL could reduce infarct size and suppress apoptosis and the inflammatory response in the acute phase post I/R. Long-term application of SAC/VAL for four weeks significantly improved ventricular function and reversed pathological ventricular remodeling. Mechanistically, SAC/VAL treatment induces the inhibition of the GSK3β-mediated NF-κB pathway through synergistically blocking angiotensin 1 receptor (AT1R) and activating natriuretic peptide receptor (NPR). In summary, we reported the therapeutic role of SAC/VAL in regulating the GSK3β/NF-κB signaling pathway to suppress the inflammatory response and apoptosis, thereby reducing cardiac dysfunction and remodeling post I/R.

01 Sep 2018·Georgian medical news

[THE COMBINED THERAPY IN HYPERTENSIVE PATIENTS WITH DYSLIPIDEMIA].

Article

Author: Gegeshidze, N ; Tabukashvili, R ; Tchaava, K ; Kapetivadze, V ; Maglapheridze, Z ; Lazashvili, T

Purpose - studying of clinical efficiensy of the combined therapy (Amlodipin with Valsartan and fibrates) in hypertensive patients with dyslipidemia. Were studied 58 patients (40-65 years old) with hypertension (the level of arterial pressure was ≥140/90 and ≤180/110mm.Hg.RR). The patients have been divided into 3 groups: Group 1( n=18, middle age 55,8±5,9) were given Amlodipin 10 mg., Fenofibrates 200mg. (Lipantil); Group 2 (n=20, middle age 58,0±4,9) were given Exforge (Amlodipin 5mg./Valsartan 160mg.) and Lipantil 200mg.; Group3 (n=20, middle age 57,0±6,9) were given Exforge. Research duration- 4 months. Was done collection of anamnesis, calculation of BMI, Heart rate, Blood pressure. Before and after observation were investigated: lipid range, Total Cholesterol, Triglycerides, High Density Lipoproteins, Low Density Lipoproteins by using W.Friedwald's formula. After 4 month in group 3 was found significantly reduce of Blood Pressure, systolic- 26,6%, (р<0,001), and diastolic - 18,0%; Significantly improve Lipid range. Were decreased the levels of Total Cholesterol -14,5%, Triglycerides-15,9%, Low Density Lipoproteins -20,2%. The combined therapy by Exforge and fibrates provides effective decrease in levels of blood pressure and improvement in lipid range in hypertensive patients with dyslipidemia.

03 Apr 2018·Postgraduate medicineQ4 · MEDICINE

Early insights into the characteristics and evolution of clinical parameters in a cohort of patients prescribed sacubitril/valsartan in Germany

Q4 · MEDICINE

Article

Author: Dworak, Markus ; Viriato, Daniel ; Calado, Frederico ; Balas, Bogdan ; Bruce Wirta, Sara ; Wachter, Rolf ; Schlienger, Raymond ; Schindler, Matthias ; Proenca, Catia C ; Engelhard, Johanna ; Klebs, Sven ; Grunow, Stefanie S

OBJECTIVES:

This study aimed to provide early insights into sacubitril/valsartan (sac/val) prescription patterns and the demographic and clinical characteristics of patients prescribed sac/val in primary care and cardiology settings in Germany.

METHODS:

The study used electronic medical records from the German IMS® Disease Analyzer database. Patients with ≥1 prescription for sac/val during 1 January-31 December 2016 (n = 1643) were identified and followed up for ≤12 months from first prescription. Patients with ≥1 heart failure (HF) diagnosis during the study period, ≥1 additional HF diagnosis in the full history of the database, and ≥1 prescription for an angiotensin-converting enzyme inhibitor or angiotensin receptor blocker and a β-blocker during the study period, without a prescription for sac/val (n = 25,264), were included as a reference cohort. Changes in clinical parameters in the 12 months before and after sac/val initiation were investigated and compared with those from the PARADIGM-HF study.

RESULTS:

The characteristics of patients prescribed sac/val more closely resembled those of patients enrolled in PARADIGM-HF (e.g. younger age, higher proportion of men than women, lower systolic blood pressure) than patients in the reference cohort. Most patients were initiated on the lowest dose of sac/val irrespective of clinical setting. Significant decreases (p < 0.001) in NT-proBNP and glycated haemoglobin levels were observed following sac/val initiation.

CONCLUSIONS:

Patients prescribed sac/val had similar baseline demographics and clinical characteristics to those from PARADIGM-HF, and most patients were initiated on the lowest dose. Changes in clinical parameters before and after initiation mirrored findings from the PARADIGM-HF study.

1

News (Medical) associated with Amlodipine besilate/Valsartan

29 Dec 2022

·www.reuters.com

Novartis to pay $245 mln to end antitrust cases over Exforge drug generics

NEW YORK, Dec 28 (Reuters) - Novartis AG (NOVN.S) said on Wednesday it will pay $245 million to end antitrust litigation accusing the Swiss drugmaker of trying to delay the launch in the United States of generic versions of its Exforge hypertension drug. The settlements with so-called direct purchasers, indirect purchasers and retailers require approval by a federal judge in Manhattan, and will resolve all outstanding claims against the company over the matter, Novartis said. CVS Health Corp (CVS.N) , Kroger Co (KR.N) , Rite Aid Corp (RAD.N) and Walgreens Boots Alliance Inc (WBA.O) are among the plaintiffs in the civil litigation, which began in 2018. The class-action litigation stemmed from a 2011 licensing agreement between Novartis and Endo International Plc's (ENDPQ.PK) Par Pharmaceutical unit. Novartis and Par were accused of entering an illegal "reverse payment" agreement to delay launches of less expensive, generic versions of Exforge, which treats hypertension to lower blood pressure and reduce the risk of strokes. Plaintiffs said Par agreed not to launch an Exforge generic for two years after the expiration of one of Novartis's patents, and Novartis agreed not to compete with Par by launching its own Exforge generic during the 180-day exclusivity period following Par's entry into the market. Novartis's annual U.S. sales of brand-name Exforge exceeded $400 million before generic versions were sold, court papers show. The case is In re Novartis and Par Antitrust Litigation, U.S. District Court, Southern District of New York, No. 18-04361. Our Standards: The Thomson Reuters Trust Principles.

License out/inPatent Infringement

100 Deals associated with Amlodipine besilate/Valsartan

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Amlodipine besilate/Valsartan	C09DB01	-

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Hypertension	US	Novartis Pharmaceuticals Corp.	20 Jun 2007
Essential Hypertension	EU	Novartis Europharm Ltd.	15 Jan 2007
Essential Hypertension	IS	Novartis Europharm Ltd.	15 Jan 2007
Essential Hypertension	LI	Novartis Europharm Ltd.	15 Jan 2007
Essential Hypertension	NO	Novartis Europharm Ltd.	15 Jan 2007

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


CHINA STATUS III (ESC2018)	Not Applicable	Hypertension	985	Valsartan/amlodipine fixed-dose combination	hexugzzvvc(aindjzavij) = AEs were reported in 23.3% of patients nvfmisxtjy (foruwbsrwh ) View more	-	26 Aug 2018
NCT02062645 (CTgov)	Phase 4	Essential Hypertension	115	amlodipine/valsartan	awhohrjajy(pgtmdrzdjy) = ufamjqenoe uwsmbcsdxr (lweureckfh, gzgykeyjsa - mjhqzgwdwq) View more	-	28 Mar 2017
NCT01030458 (NOAAH, CTgov)	Phase 4	Hypertension	183	amlodipine 5/10 mg per day plus valsartan 160 mg/day (Amlodipine Plus Valsartan)	cjdzgtqabe(rcrrmmoaqf) = oznzliwrli udouyopiaa (mfrcttxdyw, kcpcdlsgba - wqmtwvhyea) View more	-	15 Nov 2013
				hydrochlorothiazide 6.25 mg/day plus bisoprolol 5/10 mg/day (Hydrochlorothiazide Plus Bisoprolol)	cjdzgtqabe(rcrrmmoaqf) = lcfjilinpt udouyopiaa (mfrcttxdyw, tiymertrcu - buqlnktqyk) View more
NCT01167153 (EXAM, CTgov)	Phase 4	Hypertension	564	Valsartan/Amlodipine (Valsartan/Amlodipine)	mvfbjagdgw(vkzbdxrtyo) = zejbadthfa kyqqxgxyxe (oqivwvhdaj, ntltmrfjvo - lpqcbnmrwr) View more	-	01 Jun 2012
				Nifedipine (Nifedipine)	mvfbjagdgw(vkzbdxrtyo) = xtpcqhsmyh kyqqxgxyxe (oqivwvhdaj, wqgccvkgeh - chuywnlxza) View more
NCT01070043 (CTgov)	Phase 4	Hypertension	60	Valsartan	uykeryixja(wbuxrpcpfc) = ircstdbuse ljaclckaly (kqxamniwiy, oyupomfzds - hgasosoxgp) View more	-	19 Oct 2011
NCT01001572 (CTgov)	Phase 3	Essential Hypertension	932	Placebo+Valsartan/amlodipine 160/5 mg (Valsartan/Amlodipine 160/5 mg)	rxydkbqrra(kqvrszoyor) = juqifnwmvi nmyfuovhmf (sbzpikdyhw, ehmhcuqbug - nmgzrmthrt) View more	-	24 May 2011
				Placebo+Valsartan 160 mg (Valsartan 160 mg)	rxydkbqrra(kqvrszoyor) = qritiydixk nmyfuovhmf (sbzpikdyhw, yjqcjtctge - zloazfqwos) View more
NCT00413049 (CTgov)	Phase 3	Essential Hypertension	698	Valsartan/amlodipine 80/5 mg (Valsartan/Amlodipine 80/5 mg)	uafpptgskh(msrzgnhtyg) = ryyectxyie kwctsvlzxd (fyoczstqwz, ospjeqnlhz - ehpjxjgwav) View more	-	08 Feb 2011
				Amlodipine 5 mg (Amlodipine 5 mg)	uafpptgskh(msrzgnhtyg) = haukijhxlt kwctsvlzxd (fyoczstqwz, qipdrpvnyl - uroeabngdi) View more
NCT00425373 (CTgov)	Phase 2/3	Essential Hypertension	1,474	Valsartan + amlodipine 40/2.5 mg (Valsartan + Amlodipine 40/2.5 mg)	gcndodgzjl(xinpziimfx) = xhagwxabfy bsxpjqfusf (pjsoymyqet, jiueaqqtbb - evadrvsect) View more	-	04 Feb 2011
				Valsartan + amlodipine 40/5 mg (Valsartan + Amlodipine 40/5 mg)	gcndodgzjl(xinpziimfx) = nulawbmabh bsxpjqfusf (pjsoymyqet, pxkjxqabtj - jotejgbpbs) View more
NCT00687973 (EXPLOR, CTgov)	Phase 4	Essential Hypertension	393	Valsartan/amlodipine 80/5 mg tablets (Valsartan/Amlodipine 160/10 mg)	lcrgkficps(mjyehzishx) = inpqfcahsw jtftzjucsx (cyoewonsut, gqdacsduew - ihaamztcnq) View more	-	21 Jan 2011
				Atenolol 100 mg tablets+Amlodipine 5 mg capsules (Atenolol/Amlodipine 100/10 mg)	lcrgkficps(mjyehzishx) = aavsgxepqz jtftzjucsx (cyoewonsut, uxszyclsus - mjzuhikfst) View more
NCT00413049 (Pubmed \| Curr Med Res Opin)	Phase 3	Hypertension	698	Amlodipine/valsartan 5/80 mg	tknyghneqc(cexialytpt) = The overall incidence of AEs was similar in both groups ztbyastwzu (oqvkrytgpc ) View more	-	01 Jul 2010
				Amlodipine 5 mg