Clinical Evaluation of the Tolerability and Pharmacokinetics of Azilsartan, a Potent Angiotensin Receptor Blocker, in Healthy Chinese Subjects.

08:00 EDT 25th September 2019 | BioPortfolio

Summary of "Clinical Evaluation of the Tolerability and Pharmacokinetics of Azilsartan, a Potent Angiotensin Receptor Blocker, in Healthy Chinese Subjects."

Azilsartan (AZL), the active metabolite of azilsartan medoxomil, is the newest angiotensin receptor blocker that has been approved for the treatment of hypertension in 2012 in Japan. The present study aimed to evaluate the safety and pharmacokinetic properties of AZL in healthy Chinese subjects. We performed 2 phase 1 studies to investigate the pharmacokinetics and safety of AZL in healthy Chinese adults after a single dose (20 mg or 40 mg) or multiple doses of AZL (40 mg/d for 7 days; Study I) and after a single 40-mg dose under the fasted and fed conditions (Study II). Noncompartmental analysis and nonlinear mixed-effects modeling were used to analyze the pharmacokinetic properties of AZL. Twenty-seven healthy volunteers (14 men and 13 women) aged 20-32 years were enrolled and completed the study. During single dosing of AZL, the pharmacokinetics of AZL exhibited a linear profile between dosage and area under the concentration-time curve. There is no AZL accumulation after multiple doses. Food had no effect on the pharmacokinetic characteristics of AZL. AZL concentrations were best fit with a 2-compartment model, and the typical value of clearance was 1.63 L/h. Body weight had an impact on both the apparent clearance and peripheral volume of distribution. The pharmacokinetic parameters were consistent with previous studies in non-Chinese subjects. Model-based simulations indicated that a 45-kg subject would have approximately double the AZL exposure of a 90-kg subject. Whether the exposure difference has clinical significance needs to be confirmed in further studies among patients.


Journal Details

This article was published in the following journal.

Name: Clinical pharmacology in drug development
ISSN: 2160-7648


DeepDyve research library

PubMed Articles [30251 Associated PubMed Articles listed on BioPortfolio]

Safety, tolerability and pharmacokinetics and pharmacodynamics of HL2351, a novel hybrid Fc-fused IL-1 receptor antagonist, in healthy subjects: a first-in-human study.

We performed a first-in-human study with HL2351, a novel hybrid Fc-fused IL-1 receptor antagonist, to evaluate its tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) after a single subcuta...

Neuroprotective potential of azilsartan against cerebral ischemic injury: Possible involvement of mitochondrial mechanisms.

Mitochondrial dysfunction is a major player in initiating the cellular cascades which lead to neuronal damage post cerebral ischemia. Angiotensin II Type 1 (AT1) receptor blockers are one of the most ...

Comparison of pharmacokinetics, safety and tolerability of secukinumab administered subcutaneously using different delivery systems in healthy volunteers and in psoriasis patients.

The aim of the study was to compare the pharmacokinetics, safety and tolerability of secukinumab with different devices for subcutaneous (s.c.) administration of 2 mL.

First-in-human clinical trial to assess safety, tolerability and pharmacokinetics of P218, a novel candidate for malaria chemoprotection.

This first-in-human clinical trial of P218, a novel dihydrofolate reductase inhibitor antimalarial candidate, assessed safety, tolerability, pharmacokinetics and food effect in healthy subjects.

Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Anti-CD38 Cytolytic Antibody TAK-079 in Healthy Subjects.

This investigation characterised tolerability, pharmacokinetics, and pharmacodynamics of the anti-CD38 antibody TAK-079.

Clinical Trials [15293 Associated Clinical Trials listed on BioPortfolio]

Pharmacokinetics Study of Azilsartan Tablets in Chinese Healthy Volunteers

The main objective is to study the pharmacokinetics of Azilsartan Tablets in human and providing evidence for clinical study and clinical application of this product.

Safety and Efficacy of Azilsartan Medoxomil in Subjects With Mild to Moderate Hypertension

The purpose of this study is to evaluate the safety, efficacy, and tolerability of azilsartan medoxomil, once daily (QD), in individuals with hypertension.

Safety, Tolerability and Efficacy of LMB763 in Patients With Diabetic Nephropathy

LMB763 addresses fibrosis, oxidative stress, inflammation and cell death, and therefore has the potential to improve the management of diabetic kidney disease when added to the standard of...

Efficacy and Safety of Azilsartan in Subjects With Essential Hypertension

The purpose of this study is to determine the safety and efficacy of azilsartan, once daily (QD), in subjects with essential hypertension.

Bioequivalence Study of Azilsartan Tablets in Chinese Healthy Volunteers

The purpose of this study was to determine the bioequivalence of two azilsartan formulations after administration of single doses to healthy subjects under fasted and fed conditions. These...

Medical and Biotech [MESH] Definitions

An octapeptide that is a potent but labile vasoconstrictor. It is produced from angiotensin I after the removal of two amino acids at the C-terminal by ANGIOTENSIN CONVERTING ENZYME. The amino acid in position 5 varies in different species. To block VASOCONSTRICTION and HYPERTENSION effect of angiotensin II, patients are often treated with ACE INHIBITORS or with ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKERS.

An angiotensin receptor subtype that is expressed at high levels in fetal tissues. Many effects of the angiotensin type 2 receptor such as VASODILATION and sodium loss are the opposite of that of the ANGIOTENSIN TYPE 1 RECEPTOR.

A decapeptide that is cleaved from precursor angiotensinogen by RENIN. Angiotensin I has limited biological activity. It is converted to angiotensin II, a potent vasoconstrictor, after the removal of two amino acids at the C-terminal by ANGIOTENSIN CONVERTING ENZYME.

Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.

A potent and specific inhibitor of PEPTIDYL-DIPEPTIDASE A. It blocks the conversion of ANGIOTENSIN I to ANGIOTENSIN II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the RENIN-ANGIOTENSIN SYSTEM and inhibits pressure responses to exogenous angiotensin.

Quick Search

DeepDyve research library

Relevant Topics

Pulmonary Hypertension
Pulmonary arterial hypertension (PAH) is a chronic, life-threatening disorder characterized by abnormally high blood pressure in the arteries between the heart and lungs of affected individuals. Symptoms can range from mild breathles...

Women's Health
Women's Health - key topics include breast cancer, pregnancy, menopause, stroke Follow and track Women's Health News on BioPortfolio: Women's Health News RSS Women'...

Food is any substance consumed to provide nutritional support for the body. It is usually of plant or animal origin, and contains essential nutrients, such as carbohydrates, fats, proteins, vitamins, or minerals. The substance is ingested by an organism ...

Searches Linking to this Article