Tolerability of Increasing Single Oral Doses of Clentiazem in Healthy Volunteers

1992 ◽  
Vol 4 (3) ◽  
pp. 276-282 ◽  
Author(s):  
Jean-Marie Houle ◽  
Pierre Major ◽  
John McCans ◽  
Hélène Landriault ◽  
Marc LeFebvre ◽  
...  
Keyword(s):  
Healthy Volunteers ◽  
Oral Doses

Inhibition of Platelet Aggregation in Man by Indobufen (K 3920)

1981 ◽  
Vol 9 (1) ◽  
pp. 12-17 ◽  
Author(s):  
A Vittoria ◽  
F Laghi Pasini ◽  
G L Messa ◽  
T Di Perri ◽  
G Corvi ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Healthy Volunteers ◽  
Crossover Trial ◽  
Marked Effect ◽  
Threshold Concentration ◽  
Dose Effect ◽  
Inhibition Of Platelet Aggregation ◽  
Oral Doses

A complete crossover trial was undertaken in six healthy volunteers to gain information on dose-effect responses to indobufen by assessing the intensity and duration of the effect of 3 single oral doses of the drug on platelet aggregation induced by threshold concentration of ADP and by 3 added doses of collagen. The results of the study confirm that the activity is dose-related and is reversible since 24 hours after administration it has practically disappeared. The effect of the same dose of indobufen differed significantly according to the amount of collagen added to plasma, whereas increasing doses of indobufen provoked a significantly more marked effect when the amount of inducer employed was the same.

scholarly journals Suction-induced blister fluid penetration of cefdinir in healthy volunteers following ascending oral doses

1995 ◽  
Vol 39 (5) ◽  
pp. 1082-1086 ◽  
Author(s):  
M. Richer ◽  
S. Allard ◽  
L. Manseau ◽  
F. Vallee ◽  
R. Pak ◽  
...  
Keyword(s):  
Healthy Volunteers ◽  
Blister Fluid ◽  
Fluid Penetration ◽  
Oral Doses

scholarly journals Effects of Single Oral Doses of Gemifloxacin (320 Milligrams) versus Trovafloxacin (200 Milligrams) on Fecal Flora in Healthy Volunteers

2001 ◽  
Vol 45 (2) ◽  
pp. 608-611 ◽  
Author(s):  
Gloria Garcia-Calvo ◽  
Ana Molleja ◽  
Maria J. Giménez ◽  
Araceli Parra ◽  
Eva Nieto ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Healthy Volunteers ◽  
Washout Period ◽  
Crossover Trial ◽  
Fecal Flora ◽  
Randomized Crossover Trial ◽  
The Family ◽  
Stool Samples ◽  
Resistant Strains ◽  
Oral Doses

ABSTRACT Gemifloxacin and trovafloxacin were administered to 12 volunteers in a randomized crossover trial with a 2-week washout period. Stool samples were collected predose and 1, 2, and 3 days postdose. Both quinolones reduced the number of organisms of the familyEnterobacteriaceae and aerobic gram-positive organisms. Escherichia coli reduction was greater with gemifloxacin than with trovafloxacin, with postdose isolation of quinolone-resistant strains for which MICs of trovafloxacin were higher than those of gemifloxacin.

PHARMACOKINETICS OF REBOXETINE IN HEALTHY VOLUNTEERS. SINGLE AGAINST REPEATED ORAL DOSES AND LACK OF ENZYMATIC ALTERATIONS

1996 ◽  
Vol 17 (7) ◽  
pp. 623-633 ◽  
Author(s):  
C. PELLIZZONI ◽  
I. POGGESI ◽  
N. P. JØRGENSEN ◽  
D. M. F. EDWARDS ◽  
E. PAUS ◽  
...  
Keyword(s):  
Healthy Volunteers ◽  
Oral Doses

scholarly journals First-in-human study to assess the safety, pharmacokinetics and pharmacodynamics of BMS-986177/JNJ-70033093, a direct, reversible, small molecule Factor XIa inhibitor in healthy volunteers

2020 ◽  
Vol 41 (Supplement_2) ◽  
Author(s):  
V Perera ◽  
Z Wang ◽  
J Luettgen ◽  
J Wang ◽  
D Li ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Healthy Volunteers ◽  
Small Molecule ◽  
Healthy Subjects ◽  
Funding Source ◽  
Private Company ◽  
Factor Xia ◽  
Clinically Significant ◽  
Oral Doses ◽  
The Impact

Abstract Background Inhibition of Factor XIa (FXIa) may provide a novel mechanism for systemic anticoagulation without increasing the risk of clinically significant bleeding in many conditions predisposing to a high risk of thrombotic or bleeding events. BMS-986177/JNJ-70033093 (BMS-177/JNJ-3093) is a small molecule that inhibits FXIa with high affinity and selectivity. Depending on the indication, BMS-177/JNJ-3093 may provide benefit to patients as add-on therapy to current standard of care (SOC) antithrombotic agents or potentially as a replacement for current SOC. Purpose To assess the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of single and multiple oral doses of BMS-177/JNJ-3093 in healthy subjects. Methods This was a 2-part, randomized, double-blind, placebo-controlled, sequential single- (Part A) and multiple- (Part B) ascending dose study to assess the safety, tolerability, PK, and PD of BMS-177/JNJ-3093 in healthy subjects. In Part A (SAD) of the study, 48 subjects were treated in 6 panels (8 subjects per panel). The 200 mg and 500 mg dose panels investigated the impact of a high fat diet on PK. In Part B (MAD), 56 subjects were treated in 7 panels (8 subjects per panel) on a once daily (QD) or twice daily (BID) regimen for a 14-day period. Within each panel in Parts A and B, subjects were randomized to receive either BMS-177/JNJ-3093 or matched placebo (3:1). Results Administration of single ascending doses of BMS-177/JNJ-3093 up to 500 mg and multiple ascending doses of BMS-177/JNJ-3093 up to 200 mg BID or 500 mg QD for 14 days were safe and well tolerated. No subjects had a clinically significant bleeding event. All treatment-emergent adverse events were mild in severity. After single doses of BMS-177/JNJ-3093 ranging from 4 to 500 mg in fasted status, BMS-177/JNJ-3093 plasma concentration reached Cmax at 3 h postdose in all panels, indicating a similar rate of absorption. The terminal half-life ranged from 8.26 to 13.8 h across SAD panels. Over 20 to 200 mg, a dose proportional increase was observed; however, saturable absorption was seen at higher doses of 300 and 500 mg. Food also increased the bioavailability of BMS-177/JNJ-3093. In the MAD portion of the study, based on visual inspection of trough plasma concentration profiles, BMS-177/JNJ-3093 plasma concentration steady state was reached between 1–3 dosing days (ie, Days 2–4) for the QD panels and 6 dosing days (ie, Day 7) for the 200 mg BID panel. Renal excretion was relatively low, ranging from 8–20%. After single oral dose or multiple oral doses, there is a clear trend that aPTT was prolonged and the magnitude of change was related to drug exposure. Conclusion BMS-177/JNJ-3093 was safe and well tolerated in healthy volunteers. The PK and PD profile demonstrates suitable dosing properties for further clinical studies. Currently, two Phase II studies are ongoing. Funding Acknowledgement Type of funding source: Private company. Main funding source(s): This work was sponsored by Bristol-Myers Squibb and Janssen Research & Development, LLC

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