Delving into the Latest Updates on Hydrochlorothiazide/Telmisartan with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

TELMISARTAN/HYDROCHLOROTHIAZIDE, Telmisartan and Hydrochlorothiazide, Telmisartan/Hydrochlorothiazide

+ [14]

Target

AT1R x NCC

Mechanism

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

Therapeutic Areas

Cardiovascular Diseases

Active Indication

Essential HypertensionHypertension

Inactive Indication-

Originator Organization

C.H. Boehringer Sohn AG & Co. KG

Active Organization

KRKA ddBoehringer Ingelheim International GmbH

Daiichi Sankyo Co., Ltd.

+ [5]

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

US (17 Nov 2000),

Hypertension

RegulationPriority Review (CN)

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Structure/Sequence

Molecular FormulaC40H38ClN7O6S2

InChIKeyOZCVMXDGSSXWFT-UHFFFAOYSA-N

CAS Registry485391-74-0

南京黄龙生物科技有限公司研制的替米沙坦氢氯噻嗪片（80mg/12.5mg）与Boehringer Ingelheim International GmbH上市的替米沙坦氢氯噻嗪片（美嘉素®，80mg/12.5mg）在中国健康受试者中进行的随机、开放、单剂量、2序列、4周期、交叉、空腹及餐后状态下的生物等效性研究

[Translation] A randomized, open-label, single-dose, 2-sequence, 4-period, crossover, fasting and fed bioequivalence study of telmisartan hydrochlorothiazide tablets (80 mg/12.5 mg) developed by Nanjing Huanglong Biotechnology Co., Ltd. and telmisartan hydrochlorothiazide tablets (Mekasu®, 80 mg/12.5 mg) marketed by Boehringer Ingelheim International GmbH in healthy Chinese subjects

以南京黄龙生物科技有限公司研制的替米沙坦氢氯噻嗪片（规格：80mg/12.5mg）为受试制剂，以Boehringer Ingelheim International GmbH公司上市的替米沙坦氢氯噻嗪片（美嘉素 ®，规格：80mg/12.5mg）为参比制剂，考察两制剂在空腹及餐后状态下单次给药的药代动力学参数及相对生物利用度，评价两制剂是否具有生物等效性；同时评价两种制剂在健康人体中的安全性和耐受性。

[Translation]

Telmisartan hydrochlorothiazide tablets (specification: 80mg/12.5mg) developed by Nanjing Huanglong Biotechnology Co., Ltd. were used as the test preparation, and Telmisartan hydrochlorothiazide tablets (Mekasu ®, specification: 80mg/12.5mg) marketed by Boehringer Ingelheim International GmbH were used as the reference preparation. The pharmacokinetic parameters and relative bioavailability of the two preparations after single administration in the fasting and postprandial states were investigated to evaluate whether the two preparations were bioequivalent; at the same time, the safety and tolerability of the two preparations in healthy humans were evaluated.

Start Date15 Aug 2024

Sponsor / Collaborator

Nanjing Huanglong Biotechnology Co. Ltd.

CTR20242468

/ CompletedNot Applicable

替米沙坦氢氯噻嗪片（40 mg/12.5 mg）在健康受试者中空腹/餐后生物等效性试验

[Translation] Fasting/fed bioequivalence study of telmisartan hydrochlorothiazide tablets (40 mg/12.5 mg) in healthy subjects

主要目的：在健康男性与女性受试者中于空腹/餐后条件下，评价受试制剂替米沙坦氢氯噻嗪片（规格：40 mg/12.5 mg，生产商：浙江华海药业股份有限公司）和Boehringer Ingelheim为持证商的参比制剂替米沙坦氢氯噻嗪片（MICARDIS HCT，规格：40 mg/12.5 mg）的生物等效性。次要目的：观察受试制剂替米沙坦氢氯噻嗪片与参比制剂替米沙坦氢氯噻嗪片（MICARDIS HCT）在健康受试者中的安全性。

[Translation]

Primary objective: To evaluate the bioequivalence of the test preparation Telmisartan Hydrochlorothiazide Tablets (Specifications: 40 mg/12.5 mg, Manufacturer: Zhejiang Huahai Pharmaceutical Co., Ltd.) and the reference preparation Telmisartan Hydrochlorothiazide Tablets (MICARDIS HCT, Specifications: 40 mg/12.5 mg) of which Boehringer Ingelheim is the licensee in healthy male and female subjects under fasting/postprandial conditions. Secondary objective: To observe the safety of the test preparation Telmisartan Hydrochlorothiazide Tablets and the reference preparation Telmisartan Hydrochlorothiazide Tablets (MICARDIS HCT) in healthy subjects.

Start Date06 Aug 2024

Sponsor / Collaborator

Zhejiang Huahai Pharmaceutical Co., Ltd.

CTIS2023-504812-13-00

/ RecruitingNot ApplicableIIT

Effects of single-pill combination of telmisartan/amlodipine and telmisartan/amlodipine/hydrochlorothiazide on 24-hour blood pressure (BP) reduction, 24-h BP variability and office BP control in patients with arterial hypertension – SATELLITE - KCT02/2023-SATELLITE

Start Date06 May 2024

Sponsor / Collaborator

KRKA TOVARNA ZDRAVIL DD NOVO MESTO

100 Clinical Results associated with Hydrochlorothiazide/Telmisartan

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100 Translational Medicine associated with Hydrochlorothiazide/Telmisartan

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100 Patents (Medical) associated with Hydrochlorothiazide/Telmisartan

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4

Literatures (Medical) associated with Hydrochlorothiazide/Telmisartan

01 Sep 2012·Journal of the Renin-Angiotensin-Aldosterone SystemQ4 · MEDICINE

Efficacy and safety of a single-pill fixed-dose combination of high-dose telmisartan/hydrochlorothiazide in patients with uncontrolled hypertension

Q4 · MEDICINE

ArticleOA

Author: Shirotani, Tetsuro ; Shimizu, Tomohiko ; Miura, Shin-ichiro ; Shiga, Yuhei ; Inoue, Asao ; Morii, Joji ; Saku, Keijiro ; Matsunaga, Eiyu ; Norimatsu, Kenji ; Arimura, Tadaaki ; Mitsutake, Ryoko ; Uehara, Yoshinari ; Nagata, Itsuki ; Fujisawa, Kazuaki ; Kuwano, Takashi

Objective: Many patients still have high blood pressure (BP) after treatment with high-dose angiotensin II type 1 receptor blockers (ARBs) or Preminent® (medium-dose of losartan (50 mg/day)/hydrochlorothiazide (HCTZ) (12.5 mg/day)). Therefore, we analyzed whether Micombi®BP (high-dose telmisartan (80 mg/day)/HCTZ (12.5 mg/day)) could provide better results with regard to efficacy and safety for patients with uncontrolled hypertension. Methods: In total, 44 hypertensive patients (22 males, age 71±14 years) who showed uncontrolled BP despite the use of high-dose ARBs or Preminent® were enrolled in this study. We used a changeover design in which the patients were switched from high-dose ARBs or Preminent® to Micombi®BP. We analyzed BP, heart rate (HR), and biochemical parameters before and after treatment for 3 months. Results: Systolic BP and diastolic BP significantly decreased (125±15/69±11 mmHg) and 85% of the patients achieved their target BP at 3 months after changeover. Patients who switched from ARBs and those who switched from Preminent® showed similar BP-lowering effects. In addition, the reductions in BP after 3 months in patients with or without chronic kidney disease and in those with or without metabolic syndrome (MetS) were also similar. There were no significant changes in HR during the study period. Although blood levels of potassium, hemoglobin A1c and uric acid (UA) significantly increased after 3 months for all of the patients, none of the patients showed serious adverse effects. Conclusion: High-dose telmisartan/HCTZ therapy was associated with a significant reduction in BP and helped patients achieve their target BP.

01 Jan 2008·DrugsQ1 · MEDICINE

A Review of its Use as Fixed-Dose Combinations in Essential Hypertension

Q1 · MEDICINE

Review

Author: Plosker, Greg L. ; White, William B.

Fixed-dose combinations of telmisartan and hydrochlorothiazide (HCTZ) [Micardis Plus, Micardis HCT, PritorPlus] are available in many countries for the treatment of patients with essential hypertension. Combining the angiotensin II receptor antagonist (angiotensin II receptor blocker [ARB]) telmisartan with the thiazide diuretic HCTZ provides antihypertensive therapy with complementary mechanisms of action. In the US and EU, telmisartan/HCTZ is approved for patients whose hypertension is not adequately controlled with telmisartan monotherapy; US labelling for the fixed-dose combination also includes inadequate control of blood pressure (BP) with HCTZ monotherapy.The antihypertensive efficacy of once-daily telmisartan/HCTZ has been demonstrated in several large, randomized trials in patients with stages 1 and 2 hypertension. The addition of HCTZ to telmisartan achieved significant reductions in BP in nonresponders to telmisartan monotherapy, and the antihypertensive efficacy of telmisartan/HCTZ was similar to or significantly greater than that of various comparator agents. Moreover, in studies that used ambulatory BP monitoring, telmisartan/HCTZ provided consistent 24-hour BP reductions throughout morning, daytime and night-time periods. The BP-lowering efficacy over the entire 24-hour dose administration interval is consistent with the pharmacokinetic profile of telmisartan, which has the longest elimination half-life among currently available ARBs and a unique chemical structure. Adverse events with telmisartan/HCTZ in clinical trials were typically mild and transient, and no unexpected events occurred that had not been previously reported with either telmisartan or HCTZ. Extensive tolerability data are available for telmisartan, in particular from the ONTARGET study, the largest clinical outcomes trial with an ARB. As such, fixed-dose combinations of telmisartan/HCTZ provide an effective, rational and generally well tolerated treatment option for the management of patients with hypertension.

01 Sep 2003·Revue medicale de Liege

[Kinzalkomb, a fixed telmisartan-hydrochlorothiazide combination for the treatment of hypertension].

Review

Author: Kulbertus, H

Kinzalkomb marketed in Belgium by Bayer is a fixed combination of telmisartan 80 mg and hydrochlorothiazide 125 mg for the treatment of hypertension. New guidelines for the treatment of hypertension were recently released both in Europe and the United States (see article by J.M. Krzesinski in this issue). They offer the choice of using a fixed biotherapy even as first line treatment. Hydrochlorothiazide at low dose is a frequent component of such biotherapies: it is efficacious and secure. Telmisartan is a highly selective blocker of angiotensin II AT1 receptors ("sartans"); it is at least as effective as the classical antihypertensive agents; thanks to its half-life, the longest of all sartans', it provides adequate antihypertensive coverage throughout the whole 24-hour postdose interval and particularly over the last 6 hours of the dosage interval. Its tolerability profile is equivalent to placebo. The combination telmisartan-hydrochlorothiazide is more effective than each agent alone at lowering blood pressure; furthermore telmisartan possesses a potassium-sparing effect that when the two drugs are coadministered attenuates the kaliuretic effect of hydrochlorothiazide. Various large trials are currently under way (ONTARGET, TRANSCEND, PROFESS, PROTECTION, DETAIL). These studies which together involve some 50,000 patients will hopefully help to further specify the role of telmisartan in condition which require an intervention on the renin-angiotensin system.

100 Deals associated with Hydrochlorothiazide/Telmisartan

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	C09DA07	-

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Essential Hypertension	EU	Bayer AG	19 Apr 2002
Essential Hypertension	IS	Bayer AG	19 Apr 2002
Essential Hypertension	LI	Boehringer Ingelheim International GmbH	19 Apr 2002
Essential Hypertension	LI	Bayer AG	19 Apr 2002
Essential Hypertension	EU	Boehringer Ingelheim International GmbH	19 Apr 2002
Essential Hypertension	IS	Boehringer Ingelheim International GmbH	19 Apr 2002
Essential Hypertension	NO	Boehringer Ingelheim International GmbH	19 Apr 2002
Essential Hypertension	NO	Bayer AG	19 Apr 2002
Hypertension	US	Boehringer Ingelheim GmbH	17 Nov 2000

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Essential Hypertension	Phase 3	JP	Boehringer Ingelheim GmbH	01 Jan 2005
Hypertension	Phase 3	-	Boehringer Ingelheim GmbH	01 Feb 1999

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01911780 (CTgov)	Phase 3	Hypertension	132	amlodipine+telmisartan + HCTZ (Telmisartan + HCTZ + Amlodipine)	vbslvxnozm(pbuxsrygaa) = hhcmaoivjc cadxahhajw (xgcsxrefop, uupzfccljh - jizulfqspa) View more	-	28 Mar 2016
				placebo+telmisartan + HCTZ (Telmisartan + HCTZ + Placebo)	vbslvxnozm(pbuxsrygaa) = lijgxaobfz cadxahhajw (xgcsxrefop, gxdpadjnmk - typwnolehg) View more
PP.5.215 (ESH2010)	Not Applicable	Metabolic Syndrome \| Hypertension	60	Telmisartan 80mg/Hydrochlorothiazide 12.5mg	(kvbiefjruc) = lyzqzvfygu uxucnennkz (kaahoyxpan ) View more	Positive	01 Jun 2010
				Telmisartan 40mg	(kvbiefjruc) = juaizlnqep uxucnennkz (kaahoyxpan ) View more
NCT00267943 (Pubmed \| Expert Opin Pharmacother)	Phase 3	-	639	Telmisartan 80 mg/hydrochlorothiazide 25 mg fixed-dose combination	ntidosdbku(szjauamnwv) = occurred in 29 (4.5%) patients dqeaopunwp (ivwuvhpyeo )	-	01 Feb 2009