Characterization of the Angiotensin II Receptor Antagonist TCV-116 in Healthy Volunteers

Hypertension ◽  
1995 ◽  
Vol 25 (1) ◽  
pp. 14-21 ◽  
Author(s):  
Etienne Delacrétaz ◽  
Jürg Nussberger ◽  
Jerôme Biollaz ◽  
Bernard Waeber ◽  
Hans R. Brunner
Keyword(s):  
Angiotensin Ii ◽  
Healthy Volunteers ◽  
Receptor Antagonist ◽  
Angiotensin Ii Receptor ◽  
Angiotensin Ii Receptor Antagonist

scholarly journals The Pharmacological Characterization of FK 739, a New Angiotensin II-Receptor Antagonist

1993 ◽  
Vol 63 (3) ◽  
pp. 335-344 ◽  
Author(s):  
Kaori Hamada ◽  
Yoshimitsu Nakajima ◽  
Hisataka Nirei ◽  
Chie Nakajima ◽  
Akira Nagashima ◽  
...  
Keyword(s):  
Angiotensin Ii ◽  
Receptor Antagonist ◽  
Angiotensin Ii Receptor ◽  
Angiotensin Ii Receptor Antagonist ◽  
Pharmacological Characterization

scholarly journals Pharmacological characterization of KT3-671, a new nonpeptide angiotensin II receptor antagonist.

1993 ◽  
Vol 61 ◽  
pp. 212
Author(s):  
Seiichiro Mochizuki ◽  
Tomoe Sato ◽  
Chika Fukai ◽  
Kenji Hase ◽  
Kazuhiro Kosakai ◽  
...  
Keyword(s):  
Angiotensin Ii ◽  
Receptor Antagonist ◽  
Angiotensin Ii Receptor ◽  
Angiotensin Ii Receptor Antagonist ◽  
Pharmacological Characterization

scholarly journals Pharmacodynamic Effects of an Angiotensin II Receptor-Antagonist in Phase I—Comparison between Healthy Subjects and Patients with Hypertension

2007 ◽  
Vol 2 ◽  
pp. 117727190700200 ◽  
Author(s):  
Georg Wensing ◽  
Klaus Ochmann ◽  
Michael Boettcher ◽  
Anja Schäfer ◽  
Jochen Kuhlmann
Keyword(s):  
Angiotensin Ii ◽  
Phase I ◽  
Healthy Volunteers ◽  
Receptor Antagonist ◽  
Healthy Subjects ◽  
Antihypertensive Agents ◽  
Plasma Renin ◽  
Angiotensin Ii Receptor ◽  
Angiotensin Ii Receptor Antagonist ◽  
Hypertensive Patients

Biomarkers are increasingly used to provide decision making data early in phase I by showing Proof of Mechanism or Proof of Concept (PoM/PoC). For antihypertensive agents, the administration of multiple doses (md) to hypertensive patients is assumed to be necessary for an early go/no-go decision. We compared the effects of an Angiotensin II receptor antagonist (ARA) on Plasma Renin and blood pressure (BP) following an oral single dose (sd) and once daily md for seven days to healthy volunteers and patients with essential hypertension (diastolic BP 95 mmHg to 114 mmHg; systolic BP 130 mmHg to 200 mmHg). Methods: 5–12 healthy male subjects/dose received 10 mg to 300 mg ARA sd and 50 to 300 mg md for 7 days; patients (9–10/dose) received 20 mg–400 mg ARA for 7 days. The studies were designed as randomized, single blind, placebo-controlled, group comparison or crossover dose-escalation studies. Plasma Renin and BP were monitored up to 24 hours after dosing. Results: Plasma Renin showed a high interindividual variability in both healthy volunteers and patients. Healthy subjects showed a dose- and time-related increase in plasma Renin after sd from 40 mg to 300 mg and md of 50 mg to 300 mg (p < 0.05 for doses of 200 mg and 300 mg). In patients, increases in plasma Renin occurred at 8 hours and beyond starting at sd of 100 mg and md of 50 mg (p < 0.05 for the dose of 400 mg). While healthy volunteers showed no relevant decrease in BP, in hypertensive patients a reduction in BP in doses of 100 mg to 400 mg occurred (p < 0.05); effects were more pronounced after md compared to sd. Conclusion: Early PoM for an antihypertensive agent can be shown by use of laboratory biomarkers following sd to healthy subjects. PoC can be achieved after sd in hypertensive patients. Administration of sd to healthy volunteers is sufficient for an early go/no-decision.

In vitropharmacological characterization of UP 269-6, a novel nonpeptide angiotensin II receptor antagonist

1995 ◽  
Vol 9 (2) ◽  
pp. 119-128 ◽  
Author(s):  
F. Caussade ◽  
A. Virone-Oddos ◽  
C. Delchambre ◽  
M. Cazes ◽  
A. Versigny ◽  
...  
Keyword(s):  
Angiotensin Ii ◽  
Receptor Antagonist ◽  
Angiotensin Ii Receptor ◽  
Angiotensin Ii Receptor Antagonist
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