Delving into the Latest Updates on Hydrochlorothiazide/Olmesartan Medoxomil with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Benicar HCT, Olmesartan Medoxomil and Hydrochlorothiazide, Olmesartan medoxomil/hydrochlorothiazide

+ [6]

Target

AT1R x NCC

Action

antagonists, inhibitors

Mechanism

AT1R antagonists(Angiotensin II Receptor Type 1 antagonists), NCC inhibitors(Thiazide-sensitive sodium-chloride cotransporter inhibitors)

Therapeutic Areas

Cardiovascular Diseases

Active Indication

HypertensionEssential Hypertension

Inactive Indication-

Originator Organization

Daiichi Sankyo Europe GmbH

Active Organization

Daiichi Sankyo Europe GmbH

Daiichi Sankyo Co., Ltd.

Cosette Pharmaceuticals, Inc.Startup

Inactive Organization

Daiichi Sankyo, Inc.EMS SA (Brazil)

Drug Highest PhaseApproved

First Approval Date

Germany (30 Mar 2003),

Essential Hypertension

RegulationPriority Review (China)

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Structure/Sequence

Molecular FormulaC36H38ClN9O10S2

InChIKeyCJPRWUSPLWISJM-UHFFFAOYSA-N

CAS Registry760190-74-7

评估受试制剂奥美沙坦酯氢氯噻嗪片（规格：20 mg/12.5 mg）与参比制剂奥美沙坦酯氢氯噻嗪片（复傲坦®）（规格：20 mg/12.5 mg）在健康成年受试者餐后状态下的单中心、开放、随机、单剂量、两周期、两序列、交叉生物等效性研究

[Translation] A single-center, open-label, randomized, single-dose, two-period, two-sequence, crossover bioequivalence study to evaluate the bioequivalence of the test preparation Olmesartan Medoxomil Hydrochlorothiazide Tablets (Specifications: 20 mg/12.5 mg) and the reference preparation Olmesartan Medoxomil Hydrochlorothiazide Tablets (Fuaotan®) (Specifications: 20 mg/12.5 mg) in healthy adult subjects in the fed state

主要试验目的：研究餐后状态下单次口服受试制剂奥美沙坦酯氢氯噻嗪片（规格：20 mg/12.5 mg，宁波美诺华天康药业有限公司生产）与参比制剂奥美沙坦酯氢氯噻嗪片（复傲坦®，规格：20 mg/12.5 mg；第一三共制药（上海）有限公司生产）在健康受试者体内的药代动力学特征，评价餐后状态口服两种制剂的生物等效性。次要试验目的：研究受试制剂奥美沙坦酯氢氯噻嗪片（规格：20 mg/12.5 mg）和参比制剂奥美沙坦酯氢氯噻嗪片（复傲坦®）（规格：20 mg/12.5 mg）在健康受试者中的安全性。

[Translation]

The main purpose of the study is to study the pharmacokinetic characteristics of the test preparation Olmesartan medoxomil hydrochlorothiazide tablets (specification: 20 mg/12.5 mg, produced by Ningbo Menohua Tiankang Pharmaceutical Co., Ltd.) and the reference preparation Olmesartan medoxomil hydrochlorothiazide tablets (Fuaotan®, specification: 20 mg/12.5 mg; produced by Daiichi Sankyo Pharmaceutical (Shanghai) Co., Ltd.) in healthy subjects after a single oral administration in the fed state, and to evaluate the bioequivalence of the two preparations after oral administration in the fed state. Secondary purpose of the study: to study the safety of the test preparation Olmesartan medoxomil hydrochlorothiazide tablets (specification: 20 mg/12.5 mg) and the reference preparation Olmesartan medoxomil hydrochlorothiazide tablets (Fuaotan®) (specification: 20 mg/12.5 mg) in healthy subjects.

Start Date11 Jun 2022

Sponsor / Collaborator

Ningbo Krka Menovo Pharmaceutical Co., Ltd.

CTR20221127

/ CompletedNot Applicable

评估受试制剂奥美沙坦酯氢氯噻嗪片（规格：20 mg/12.5 mg）与参比制剂奥美沙坦酯氢氯噻嗪片（复傲坦®）（规格：20 mg/12.5 mg）在健康成年受试者空腹状态下的单中心、开放、随机、单剂量、两周期、两序列、交叉生物等效性研究

[Translation] A single-center, open-label, randomized, single-dose, two-period, two-sequence, crossover bioequivalence study to evaluate the bioequivalence of the test preparation Olmesartan Medoxomil Hydrochlorothiazide Tablets (Specifications: 20 mg/12.5 mg) and the reference preparation Olmesartan Medoxomil Hydrochlorothiazide Tablets (Fuaotan®) (Specifications: 20 mg/12.5 mg) in healthy adult subjects under fasting state

主要试验目的：研究空腹状态下单次口服受试制剂奥美沙坦酯氢氯噻嗪片（规格：20 mg/12.5 mg，宁波美诺华天康药业有限公司生产）与参比制剂奥美沙坦酯氢氯噻嗪片（复傲坦®，规格：20 mg/12.5 mg；第一三共制药（上海）有限公司生产）在健康受试者体内的药代动力学特征，评价空腹状态口服两种制剂的生物等效性。次要试验目的：研究受试制剂奥美沙坦酯氢氯噻嗪片（规格：20 mg/12.5 mg）和参比制剂奥美沙坦酯氢氯噻嗪片（复傲坦®）（规格：20 mg/12.5 mg）在健康受试者中的安全性。

[Translation]

The main purpose of the study is to study the pharmacokinetic characteristics of the test preparation Olmesartan medoxomil hydrochlorothiazide tablets (specification: 20 mg/12.5 mg, produced by Ningbo Menohua Tiankang Pharmaceutical Co., Ltd.) and the reference preparation Olmesartan medoxomil hydrochlorothiazide tablets (Fuaotan®, specification: 20 mg/12.5 mg; produced by Daiichi Sankyo Pharmaceutical (Shanghai) Co., Ltd.) in healthy subjects after a single oral administration under fasting conditions, and to evaluate the bioequivalence of the two preparations when taken orally under fasting conditions. Secondary purpose of the study is to study the safety of the test preparation Olmesartan medoxomil hydrochlorothiazide tablets (specification: 20 mg/12.5 mg) and the reference preparation Olmesartan medoxomil hydrochlorothiazide tablets (Fuaotan®) (specification: 20 mg/12.5 mg) in healthy subjects.

Start Date07 Jun 2022

Sponsor / Collaborator

Ningbo Krka Menovo Pharmaceutical Co., Ltd.

100 Clinical Results associated with Hydrochlorothiazide/Olmesartan Medoxomil

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100 Translational Medicine associated with Hydrochlorothiazide/Olmesartan Medoxomil

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100 Patents (Medical) associated with Hydrochlorothiazide/Olmesartan Medoxomil

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12

Literatures (Medical) associated with Hydrochlorothiazide/Olmesartan Medoxomil

26 Dec 2014·Current Medicinal ChemistryQ2 · MEDICINE

Should the Incorporation of Structural Alerts be Restricted in Drug Design? An Analysis of Structure-Toxicity Trends with Aniline-Based Drugs

Q2 · MEDICINE

Review

Author: Kalgutkar, A S

Certain idiosyncratic adverse drug reactions (IADRs) can be triggered by electrophilic protein-reactive metabolites that are formed in the process of drug metabolism. While methodologies (e.g., structural alert concept in drug design, glutathione (GSH) trapping, and protein covalent binding) for examining reactive metabolite (RM) formation are available, predicting the IADR potential applying these parameters remains a significant challenge. The present work examines toxicity trends associated with the aniline structural alert in the top 200 prescribed drugs of 2011 and recently approved (2009-2013) small molecule drugs, in relation with 30 aniline-based drugs withdrawn from commercial use or associated with a black box warning for IADRs. The aniline sub-structure was found in several drugs from the toxic, most prescribed, and recently approved category. RMs resulting from the bioactivation of the aniline alert was also noted in the three categories chosen for comparison. A major discriminator between the toxic drugs and the majority of drugs in the most-prescribed list, however, was the daily dose--drugs most frequented associated with IADRs were the ones with higher daily doses (exceeding hundreds of milligrams). A greater tolerance for IADRs was also noted with certain drugs intended to treat rare, unmet medical needs (e.g., cancer). Overall, the analysis suggests that optimization of pharmacologic potency and pharmacokinetics that would lead to a lower daily dose, and therefore, a lower body burden of parent drug/metabolites, should be taken into consideration in drug discovery.

01 Oct 2014·Journal of Analytical Chemistry

Simultaneous determination and validation of some binary mixtures of antihypertensive drugs using ratio derivative spectrophotometric method

Author: Mehmet Gumustas ; Sevinc Kurbanoglu ; Sibel A. Ozkan

Ratio derivative spectrophotometric technique is presented for the rapid, accurate and precise simultaneous determination of olmesartan medoxomil (OLM), hydrochlorothiazide (HCT), and zofenopril (ZOF) as well as HCT binary mixtures in their dosage forms.First derivative of the ratio spectra (DD1) by measurements using different amplitudes was used and calibration graphs were established for 0.5-12 mg/mL HCT and 0.5-20 mg/mL OLM and ZOF.This method depends on first derivative of the ratio spectra by division of the absorption spectrum of the binary mixture by a standard spectrum of one of the components and then calculating the first derivative of the ratio spectrum.The first derivative of the ratio amplitudes at 250.4 and 291.5 nm for OLM, 250.4 and 298.1 nm for ZOF and 231.8, 332.2, 232.3 and 280.4 nm for HCT were selected for the determinationThe proposed methods were successfully applied for determining of both drug combinations (ZOF-HCT and OLM-HCT) in their synthetic mixtures and in pharmaceutical dosage forms.The described procedures are extensively validated, non-destructive and do not require any separation steps.

01 Jul 2013·American Journal of HypertensionQ3 · MEDICINE

Dynamic View on Affordability of Fixed-Dose Combination Antihypertensive Drug Therapy

Q3 · MEDICINE

Article

Author: Junling Wang ; Song Hee Hong ; Jun Tang

BACKGROUNDThe use of fixed-dose combinations (FDCs) has been increasing since the Seventh Report of the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure recommended using ≥2 drugs as the first-line drug therapy for patients with stage 2 hypertension. FDCs simplify the drug therapy regimen and reportedly lower the drug therapy cost compared with the free combination (FC) of 2 single-agent drugs. This study hypothesized that the affordability of FDCs over FCs would change over time depending on the availability of generic single-agent drugs.METHODSThis study used the 2009 Medical Expenditure Panel Survey. Antihypertensive drugs were identified based on the Food and Drug Administration national drug directory. Based on the 2 databases, regression models were run to predict average monthly drug cost as well as out-of-pocket cost for each prescription along with their 95% confidence intervals (CIs).RESULTSOverall, FDCs (n = 26) had average monthly drug costs similar to respective FCs when FCs were not generically available. However, when FCs were generically available, FDCs (n = 11) had average drugs costs much higher than their respective FCs. For example, Lotrel as an FDC had an average monthly drug cost of $115.97 (95% CI = $96.59-$135.36), whereas its counterpart FC had an average monthly drug cost of $21.00 (95% CI = $18.23-$23.79).CONCLUSIONSThe cost advantage of FDCs over FCs was reversed when FCs were generically available. The finding of this study informs patients, health-care providers, and drug plans of the importance of making dynamic decisions on preferred drug therapy options depending on the availability of generic drugs.

100 Deals associated with Hydrochlorothiazide/Olmesartan Medoxomil

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	C09DA08	-

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Hypertension	United States	Cosette Pharmaceuticals, Inc.Startup	05 Jun 2003
Essential Hypertension	Germany	Daiichi Sankyo Europe GmbH	30 Mar 2003

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Essential Hypertension	Phase 1	Bulgaria	Daiichi Sankyo, Inc.	01 Feb 2007
Essential Hypertension	Phase 1	Belgium	Daiichi Sankyo, Inc.	01 Feb 2007
Essential Hypertension	Phase 1	Ukraine	Daiichi Sankyo, Inc.	01 Feb 2007
Essential Hypertension	Phase 1	Spain	Daiichi Sankyo, Inc.	01 Feb 2007
Essential Hypertension	Phase 1	Netherlands	Daiichi Sankyo, Inc.	01 Feb 2007
Essential Hypertension	Phase 1	Poland	Daiichi Sankyo, Inc.	01 Feb 2007
Essential Hypertension	Phase 1	Slovakia	Daiichi Sankyo, Inc.	01 Feb 2007
Essential Hypertension	Phase 1	Czechia	Daiichi Sankyo, Inc.	01 Feb 2007
Essential Hypertension	Phase 1	France	Daiichi Sankyo, Inc.	01 Feb 2007

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00430950 \| EUCTR2006-003876-37-CZ \| NCT00430508 (Pubmed \| Curr Med Res Opin)	Not Applicable	Hypertension, severe	-	Olmesartan 40 mg	vhjxlnecvg(wajxcqinjy) = erdysntyhp qdogacnrlg (jwlkhjbiib )	-	01 Feb 2012
				Olmesartan/hydrochlorothiazide 20/12.5 mg	vhjxlnecvg(wajxcqinjy) = zdtcohwwjy qdogacnrlg (jwlkhjbiib )
PP.5.203 (ESH2010)	Not Applicable	-	-	Olmesartan Medoxomil/Hydrochlorothiazide 40/25mg	ldynzvppvk(gorurjahww) = gfmjkfyohy nnbtprtqoi (rxjhpwakoq ) View more	Positive	01 Jun 2010
				Olmesartan Medoxomil/Hydrochlorothiazide 20/25mg	ldynzvppvk(gorurjahww) = eoeezjwdvi nnbtprtqoi (rxjhpwakoq ) View more
PP.5.205 (ESH2010)	Not Applicable	Hypertension, severe	-	Olmesartan 40 mg	gkvnjzvfec(nvrdgkrapy) = utkqjpqwin kfldbyhlpi (ifjwekddyx ) View more	Positive	01 Jun 2010
				Olmesartan/Hydrochlorothiazide 40/12.5 mg	gkvnjzvfec(nvrdgkrapy) = gonmmzqoug kfldbyhlpi (ifjwekddyx ) View more