Delving into the Latest Updates on Amlodipine Besylate/Telmisartan with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Amlodipine/telmisartan, Micardis Amlo, Micardis Anlo

+ [11]

Target

AT1R x VDCCs

Action

antagonists, blockers

Mechanism

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

Therapeutic Areas

Cardiovascular Diseases

Active Indication

Essential HypertensionHypertension

Inactive Indication

Heart FailureMyocardial InfarctionRenal Insufficiency+ [3]

Originator Organization

C.H. Boehringer Sohn AG & Co. KG

Active Organization

Boehringer Ingelheim International GmbH

Boehringer Ingelheim GmbHNippon Boehringer Ingelheim Co., Ltd.

+ [2]

Inactive Organization

Boehringer Ingelheim Pharmaceuticals, Inc.

License Organization-

Drug Highest PhaseApproved

First Approval Date

United States (16 Oct 2009),

Heart FailureHypertensionMyocardial Infarction+ [3]

Regulation-

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Structure/Sequence

Molecular FormulaC26H31ClN2O8S

InChIKeyZPBWCRDSRKPIDG-UHFFFAOYSA-N

CAS Registry111470-99-6

View All Structures (2)

主要研究目的：考察单次口服（空腹/餐后）受试制剂替米沙坦氨氯地平片（规格：80mg/5mg，海南赛立克药业有限公司生产，海南赛立克药业有限公司提供）与参比制剂替米沙坦氨氯地平片（Twynsta®，规格：80mg/5mg，Boehringer Ingelheim International GmbH持证，海南赛立克药业有限公司提供）在中国成年健康受试者体内的药代动力学特征，评价空腹与餐后状态下口服两种制剂的生物等效性。次要研究目的：评价受试制剂和参比制剂单次口服（空腹/餐后）在中国成年健康受试者中的安全性。

[Translation]

Main study objectives: To investigate the pharmacokinetic characteristics of the test preparation Telmisartan Amlodipine Tablets (Specifications: 80mg/5mg, produced by Hainan Selike Pharmaceutical Co., Ltd., provided by Hainan Selike Pharmaceutical Co., Ltd.) and the reference preparation Telmisartan Amlodipine Tablets (Twynsta®, Specifications: 80mg/5mg, certified by Boehringer Ingelheim International GmbH, provided by Hainan Selike Pharmaceutical Co., Ltd.) in healthy adult Chinese subjects, and to evaluate the bioequivalence of the two preparations in fasting and fed states. Secondary study objectives: To evaluate the safety of the test preparation and the reference preparation in healthy adult Chinese subjects after a single oral administration (fasting/fed).

Start Date30 Nov 2024

Sponsor / Collaborator

Hainan Selection Pharmaceutical Co. Ltd.

CTR20241859

/ RecruitingNot Applicable

替米沙坦氨氯地平片（80mg/5mg）在中国健康受试者中空腹和餐后给药条件下随机、开放、单剂量、两序列、四周期、完全重复交叉生物等效性试验

[Translation] A randomized, open-label, single-dose, two-sequence, four-period, completely repeated crossover bioequivalence study of telmisartan and amlodipine tablets (80 mg/5 mg) in Chinese healthy subjects under fasting and postprandial administration conditions

主要研究目的：按有关生物等效性试验的规定，选择 Boehringer Ingelheim International GmbH 为持证商，天津掌心医药科技有限公司提供的替米沙坦氨氯地平片（商品名：Twynsta®，规格：80mg/5mg）为参比制剂，对淄博万杰制药有限公司生产并提供的受试制剂替米沙坦氨氯地平片（规格：80mg/5mg）进行空腹和餐后给药条件下的人体生物等效性试验，比较受试制剂中药物的吸收速度和吸收程度与参比制剂的差异是否在可接受的范围内，评价两种制剂在空腹和餐后给药条件下的生物等效性。次要研究目的：观察健康受试者口服受试制剂替米沙坦氨氯地平片（规格：80mg/5mg）和参比制剂替米沙坦氨氯地平片（商品名：Twynsta®，规格：80mg/5mg）的安全性。

[Translation]

Main purpose of study: According to the relevant provisions of bioequivalence test, Boehringer Ingelheim International GmbH was selected as the licensee, and Telmisartan Amlodipine Tablets (trade name: Twynsta®, specification: 80mg/5mg) provided by Tianjin Palm Pharmaceutical Technology Co., Ltd. was selected as the reference preparation. The human bioequivalence test of the test preparation Telmisartan Amlodipine Tablets (specification: 80mg/5mg) produced and provided by Zibo Wanjie Pharmaceutical Co., Ltd. was conducted under fasting and postprandial administration conditions to compare whether the absorption rate and degree of the drug in the test preparation are within the acceptable range with the reference preparation, and to evaluate the bioequivalence of the two preparations under fasting and postprandial administration conditions. Secondary purpose of study: To observe the safety of oral administration of the test preparation Telmisartan Amlodipine Tablets (specification: 80mg/5mg) and the reference preparation Telmisartan Amlodipine Tablets (trade name: Twynsta®, specification: 80mg/5mg) in healthy subjects.

Start Date13 Jun 2024

Sponsor / Collaborator

Shengjia (Binhai) Biomedical Technology Co., Ltd.

CTR20240509

/ CompletedNot Applicable

替米沙坦氨氯地平片人体生物等效性研究（餐后）

[Translation] Bioequivalence study of telmisartan and amlodipine tablets in healthy volunteers (after meal)

按有关生物等效性试验的规定，选择Boehringer Ingelheim International GmbH为持证商的替米沙坦氨氯地平片（商品名：Twynsta®，规格：每片含替米沙坦80mg，氨氯地平5mg）为参比制剂，对长春海悦药业股份有限公司持证的受试制剂替米沙坦氨氯地平片（规格：每片含替米沙坦80mg，氨氯地平5mg）进行餐后给药人体生物等效性试验，比较受试制剂中药物的吸收速度和吸收程度与参比制剂的差异是否在可接受的范围内，评估两种制剂在餐后给药条件下的生物等效性。

[Translation]

In accordance with the relevant provisions of bioequivalence tests, Telmisartan Amlodipine Tablets (trade name: Twynsta®, specification: each tablet contains 80 mg of telmisartan and 5 mg of amlodipine) certified by Boehringer Ingelheim International GmbH were selected as the reference preparation, and the test preparation Telmisartan Amlodipine Tablets (specification: each tablet contains 80 mg of telmisartan and 5 mg of amlodipine) certified by Changchun Haiyue Pharmaceutical Co., Ltd. were subjected to a human bioequivalence study after meal administration. The differences in the absorption rate and extent of the drug in the test preparation and the reference preparation were compared to see whether they were within an acceptable range, and the bioequivalence of the two preparations under the condition of postprandial administration was evaluated.

Start Date10 Jun 2024

Sponsor / Collaborator

Changchun Haiyue Pharmaceutical Co., Ltd

100 Clinical Results associated with Amlodipine Besylate/Telmisartan

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100 Translational Medicine associated with Amlodipine Besylate/Telmisartan

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100 Patents (Medical) associated with Amlodipine Besylate/Telmisartan

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7

Literatures (Medical) associated with Amlodipine Besylate/Telmisartan

01 Feb 2025·Journal of Pharmaceutical Sciences

The impact of volume of dissolution medium for biopredictive dissolution/permeation studies of enabling formulations: A comparison of two brands of telmisartan / amlodipine tablets

Article

Author: Eriksen, Jonas Borregaard ; Bauer-Brandl, Annette ; Milsmann, Johanna ; Brandl, Martin

For compendial dissolution testing of solid dosage forms, media volumes of 500 to 900 mL are used in apparatus I and II to ensure sink conditions. However, these volumes are considerably larger than those in the gastrointestinal tract. Thus, the experiments are not biomimetic and possibly not suitable for biopredictive dissolution testing. The present study investigates the influence of volumes of dissolution media in non-compendial dissolution/permeation settings. Dissolution/permeation studies of two commercial bilayer tablets (Twynsta® and Arrow) containing the active pharmaceutical ingredients telmisartan (40 mg) and amlodipine (10 mg) were evaluated using the MacroFlux tool with various biomimetic media mimicking fasted and fed states as well as biological variability ("biorelevant"). Particularly, the two-stage dissolution process of telmisartan from the tablets is interesting because the compound has a pH-dependent solubility, and 2-stage dissolution leads to supersaturation and precipitation upon pH shift. For telmisartan, lower dissolution volumes significantly induced precipitation, leading to lower permeation, while no precipitation was observed in the larger volume. The permeation of telmisartan was overly sensitive to both pH and micelle concentrations in the biomimetic media. Amlodipine showed complete dissolution under any conditions, which correlates with its known complete absorption in vivo. In conclusion, volumes of dissolution media (and their compositions) are key parameters and play a significant role for designing relevant biomimetic experiments used to predict the bioavailability of supersaturating systems.

01 Oct 2020·The Journal of Clinical HypertensionQ3 · MEDICINE

Efficacy and safety of co‐administered telmisartan/amlodipine and rosuvastatin in subjects with hypertension and dyslipidemia

Q3 · MEDICINE

Article

Author: Lee, Han Cheol ; Hwang, Jinyong ; Lee, Sang Hyun ; Choi, So‐Yeon ; Hyon, Min Su ; Kim, Ju Han ; Lee, Kyounghoon ; Han, Ki Hoon ; Hong, Seung Pyo ; Ahn, Jeong‐Cheon ; Yoo, Byung Su ; Cho, Yoonhwa ; Park, Chang‐Gyu ; Lee, Hana ; Cho, Jin‐Man ; Jin, Xuan ; Kim, Pum‐Joon ; Seo, Jeong‐Sook ; Cho, Eun Joo ; Lee, Jae‐Hwan ; Hong, Soon Jun ; Shin, Jin Ho ; Chae, In‐Ho ; Sung, Jung‐Hoon ; Kim, Hyo‐Soo ; Kim, Moo Hyun ; Sung, Ki Chul ; Kim, Woo‐Shik ; Kim, Hyungseop ; Kwon, Kihwan ; Rhee, Moo‐Yong

AbstractSingle risk factors, such as hypertension and dyslipidemia, can combine to exacerbate the development and severity of cardiovascular disease. Treatment goals may be more effectively achieved if multiple disease factors are targeted with combination treatment. We enrolled 202 patients who were randomly divided into the following three groups: telmisartan/amlodipine 80/5 mg + rosuvastatin 20 mg, telmisartan 80 mg + rosuvastatin 20 mg, and telmisartan/amlodipine 80/5 mg. The primary efficacy variables were changes from baseline in mean sitting systolic blood pressure (MSSBP) between telmisartan/amlodipine 80/5 mg + rosuvastatin 20 mg and telmisartan 80 mg + rosuvastatin 20 mg at 8 weeks, and the percent changes from baseline in low‐density lipoprotein (LDL) cholesterol between telmisartan/amlodipine 80/5 mg + rosuvastatin 20 mg and telmisartan/amlodipine 80/5 mg at 8 weeks. The secondary efficacy variables were changes in MSSBP, mean sitting diastolic blood pressure (MSDBP), LDL cholesterol and other lipid levels at 4 weeks and 8 weeks, as well as observed adverse events during follow‐up. There were no significant differences between the three groups in demographic characteristics and no significant difference among the three groups in terms of baseline characteristics for the validity evaluation variables. The mean overall treatment compliance in the three groups was, respectively, 98.42%, 96.68%, and 98.12%, indicating strong compliance for all patients. The Least‐Square (LS) mean (SE) for changes in MSSBP in the two (telmisartan/amlodipine 80/5 mg + rosuvastatin 20 mg and telmisartan 80 mg + rosuvastatin 20 mg) groups were −19.3 (2.68) mm Hg and −6.69 (2.76) mm Hg. The difference between the two groups was significant (−12.60 (2.77) mm Hg, 95% CI −18.06 to −7.14, P < .0001). The LS Mean for the percent changes from baseline in LDL cholesterol in the two (telmisartan/amlodipine 80/5 mg + rosuvastatin 20 mg and telmisartan/amlodipine 80/5 mg) groups were −52.45 (3.23) % and 2.68 (3.15) %. The difference between the two groups was significant (−55.13 (3.20) %, 95% CI −61.45 to −48.81, P < .0001). There were no adverse events leading to discontinuation or death. Combined administration of telmisartan/amlodipine 80/5 mg and rosuvastatin 20 mg for the treatment of hypertensive patients with dyslipidemia significantly reduces blood pressure and improves lipid control. ClinicalTrials.gov identifier: NCT03067688.

01 Apr 2019·Clinical Therapeutics

Efficacy and Tolerability of Telmisartan/Amlodipine and Rosuvastatin Coadministration in Hypertensive Patients with Hyperlipidemia: A Phase III, Multicenter, Randomized, Double-blind Study

Article

Author: Rha, Seung-Woon ; Rhee, Moo-Yong ; Kim, Seok-Yeon ; Lee, Han-Cheol ; Kim, Tae-Seok ; Ahn, Jeong-Cheon ; Jeon, Dong-Woon ; Park, Sang-Ho ; Kim, Woo-Sik ; Kim, Yong-Jin ; Sung, Ki-Chul ; Yoo, Byung-Su ; Yoon, Young-Won ; Park, Dae-Gyun ; Cha, Dong-Hun ; Oh, Yong-Seog ; Yoo, Ki-Dong ; Kim, Kye-Hoon ; Yoon, Myung-Ho ; Cho, Sang-Kyoon

PURPOSEDyslipidemia and hypertension increase the risk for cardiovascular disease. Combination therapy improves patient compliance. This study was conducted to compare the efficacy and tolerability of the combination therapies telmisartan/amlodipine + rosuvastatin, telmisartan/amlodipine, and telmisartan + rosuvastatin in patients with hypercholesterolemia and hypertension.METHODSIn this Phase III, multicenter, 8-week randomized, double-blind study, participants with hypertension and dyslipidemia (defined as a sitting systolic blood pressure [sitSBP] of ≥140 mm Hg, a low-density lipoprotein-cholesterol [LDL-C] level of ≤250 mg/dL, and a triglyceride level of ≤400 mg/dL) were screened. After a 4-week washout/run-in period involving therapeutic lifestyle changes and telmisartan 80 mg once a day, eligible patients had a sitSBP of ≥140 mm Hg and met the LDL-C level criteria according to the National Cholesterol Education Program Adult Treatment Panel III cardiovascular disease risk category. Patients were randomly assigned to 1 of 3 groups: (1) telmisartan/amlodipine 80/10 mg + rosuvastatin 20 mg (TAR group); (2) telmisartan/amlodipine 80/10 mg (TA group); or (3) telmisartan 80 mg + rosuvastatin 20 mg (TR group). The primary efficacy end points were the percentage changes from baseline in LDL-C in the TAR and TA groups and the mean changes in sitSBP in the TAR and TR groups at week 8 compared to baseline. Continuous variables were compared using the unpaired t test or the Wilcoxon rank sum model, and categorical variables were compared using the χ² or Fisher exact test. Tolerability was assessed based on adverse events found on physical examination including vital sign measurements, laboratory evaluations, and 12-lead ECG.FINDINGSA total of 134 patients were enrolled. The least squares mean percentage changes in LDL-C at 8 weeks after administration of the drug compared to baseline were -51.9% (3.0%) in the TAR group and -3.2% (2.9%) in the TA group (P < 0.001). At 8 weeks after baseline, the least squares mean (SE) changes sitSBP were -28.3 (2.4) mm Hg in the TAR group and -10.7 (2.1) mm Hg in the TR group (P < 0.001). The prevalence rates of treatment-emergent adverse events were 15.0%, 25.0%, and 12.2% in the TAR, TA, and TR groups, respectively; those of adverse drug reactions were 15.0%, 22.7%, and 10.2%. None of the differences in rates were significant among 3 groups.IMPLICATIONSTriple therapy with TAR can be an effective treatment in patients with dyslipidemia and hypertension. The TAR combination has value for hypertensive patients with hyperlipidemia in terms of convenience, tolerability, and efficacy. ClinicalTrials.gov identifier: NCT03566316.

100 Deals associated with Amlodipine Besylate/Telmisartan

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	C09DB04	-

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Essential Hypertension	European Union	Boehringer Ingelheim International GmbH	07 Oct 2010
Essential Hypertension	Iceland	Boehringer Ingelheim International GmbH	07 Oct 2010
Essential Hypertension	Norway	Boehringer Ingelheim International GmbH	07 Oct 2010
Essential Hypertension	Liechtenstein	Boehringer Ingelheim International GmbH	07 Oct 2010
Hypertension	Japan	Nippon Boehringer Ingelheim Co., Ltd.	23 Jul 2010

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Hypertension	Phase 3	United States	Boehringer Ingelheim Pharmaceuticals, Inc.	16 Oct 2009
Resistant hypertension	Phase 3	Belgium	Boehringer Ingelheim GmbH	01 Oct 2007
Resistant hypertension	Phase 3	South Africa	Boehringer Ingelheim GmbH	01 Oct 2007
Resistant hypertension	Phase 3	Denmark	Boehringer Ingelheim GmbH	01 Oct 2007

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03067688 (Pubmed \| J Clin Hypertens (Greenwich))	Phase 3	Dyslipidemias \| Hypertension	202	telmisartan/amlodipine 80/5 mg + rosuvastatin 20 mg	(zwgchjtmeb) = qprwevxhdc kwfcgjnioh (jxtwjybuix ) View more	-	01 Oct 2020
				telmisartan 80 mg + rosuvastatin 20 mg	(zwgchjtmeb) = mbjjhjbnux kwfcgjnioh (jxtwjybuix )
NCT01975246 (CTgov)	Phase 3	Hypertension	309	Placebo+Telmisartan + amlodipine	vnrtfmclud(ybedgqeqpk) = wpyolsbmyt gfnweinigf (uxyeotzput, xoxnpktbzm - yeqibeggyu) View more	-	29 Nov 2016
579 (ESH2012)	Phase 3	-	40	Telmisartan 80 mg/Amlodipine 5 mg	xoflbnzlcr(fehdglsoic) = thnphmitqw jovsgyuriv (kdsvlwlycu, 7.4) View more	Positive	01 Sep 2012
546 (ESH2012)	Not Applicable	Hypertension	51	Telmisartan 160 mg/Amlodipine 5 mg on awakening	jskbltlqkm(qlggzvncuf) = bkpkhznlgl hukpftbhik (wposqwuhzb ) View more	Positive	01 Sep 2012
				Telmisartan 160 mg/Amlodipine 5 mg at bedtime	jskbltlqkm(qlggzvncuf) = bylfinwggw hukpftbhik (wposqwuhzb ) View more
578 (ESH2012)	Not Applicable	-	314	Telmisartan 80 mg/Amlodipine 5 mg	fbhrqwqvaf(stitokaeht) = 1.9% with Telmisartan 80 mg/Amlodipine 5 mg and 2.4% with Amlodipine 5 mg mvqqiqncga (rrtusuupyx )	Positive	01 Sep 2012
				Amlodipine 5 mg
TEAMSTA-10 (ESH2010)	Not Applicable	-	838	Telmisartan 40 mg/Amlodipine 10 mg	ppgvduemeg(oycabeworm) = 1.9% (16/835) of patients discontinued trial treatment because of adverse events fffbypprlc (xyxbhhqygz ) View more	Positive	01 Jun 2010
				Amlodipine 10 mg
TEAMSTA-5 (ESH2010)	Not Applicable	-	976	Telmisartan/amlodipine 40/5 mg	xbwrfwucoz(gduzguujat) = jogkcckwua fzlausgnur (ktjvjnbile )	Positive	01 Jun 2010