Assessment of the safety, pharmacokinetics and pharmacodynamics of GSK3335065, an inhibitor of kynurenine monooxygenase, in a randomised placebo controlled First Time in Human study in healthy volunteers

2021 ◽  
Author(s):  
Disala Fernando ◽  
Richard Dimelow ◽  
Ciara Gorey ◽  
Xinyi Zhu ◽  
Catherine Muya ◽  
...  
Keyword(s):  
Healthy Volunteers ◽  
Human Study ◽  
Pharmacokinetics And Pharmacodynamics ◽  
First Time

First-Time-in-Human Study With GSK249320, a Myelin-Associated Glycoprotein Inhibitor, in Healthy Volunteers

2012 ◽  
Vol 93 (2) ◽  
pp. 163-169 ◽  
Author(s):  
B Abila ◽  
E Cunningham ◽  
M Simeoni
Keyword(s):  
Healthy Volunteers ◽  
Human Study ◽  
Myelin Associated Glycoprotein ◽  
First Time

Abstract 13324: Single Ascending Dose Pharmacokinetics and Pharmacodynamics of MDCO-216 (ApoA-I Milano/POPC) in Healthy Volunteers

Circulation ◽  
2014 ◽  
Vol 130 (suppl_2) ◽  
Author(s):  
S. Eralp Bellibas ◽  
David Kallend ◽  
Alain Bobillier ◽  
Herman Kempen ◽  
Peter L Wijngaard
Keyword(s):  
Healthy Volunteers ◽  
Ex Vivo ◽  
Plaque Burden ◽  
Maximum Effect ◽  
Response Analysis ◽  
Cholesterol Transport ◽  
Pharmacokinetics And Pharmacodynamics ◽  
Double Blind ◽  
First Time ◽  
Dose Dependent

Introduction: MDCO-216, a complex of dimeric recombinant apolipoprotein A-I Milano (apoA-I M) and a phospholipid (POPC), is currently under development to improve cardiovascular outcomes by reducing plaque burden in patients with atherosclerotic disease. An earlier version of MDCO-216 has been shown to reduce atherosclerotic plaque burden in animal models and in patients with ACS. The purpose of this study was to assess the pharmacokinetics (PK), pharmacodynamics (PD), safety and tolerability of newly manufactured MDCO-216 first time in healthy volunteers. Methods: 24 healthy volunteers received a single dose of MDCO-216 (5, 10, 20, 30 or 40 mg/kg) or placebo (in 2:1 ratio) as a 2 hour IV infusion in a double-blind, randomised design. Serial blood samples were collected for PK and anti-drug Ab (ADA) analysis. An ex-vivo cholesterol efflux assay was used as one of several exploratory PD biomarkers for MDCO-216 activity. Results: No ADA was detected with any dose at any time point. Plasma mean T 1/2 of MDCO-216 ranged from 48 to 61 hours (56 hr. in average) and median T max ranged between 2 to 4 hours. No obvious difference in CL was observed with increases in dose and ranged from 0.62 to 0.98 mL/hr/kg. Exposure parameters increased with dose in a slightly less than dose-proportional manner with a range of 138 to 794 μg/mL for C max and 3391 to 20788 μg.hr/mL for AUC 0-48 . Dose-dependent increases in ABCA1-mediated efflux capacity of up to 4-fold above baseline and smaller increases of SRB1-mediated efflux capacity occurred rapidly after infusion at all doses. The dose-response analysis for ABCA1-mediated efflux best fitted into a sigmoid E max (maximum effect) PD model and predicts an E max of 15.6% which saturates around a 30 mg/kg dose of MDCO-216. Conclusions: This data demonstrate that MDCO-216 can profoundly stimulate the first step of reverse cholesterol transport at clinically achievable doses with a predictable PK/PD profile.

scholarly journals A first-in-human study to investigate the safety, tolerability, pharmacokinetics, and pharmacodynamics of KM-819 (FAS-associated factor 1 inhibitor), a drug for Parkinson’s disease, in healthy volunteers

2019 ◽  
Vol Volume 13 ◽  
pp. 1011-1022 ◽  
Author(s):  
Wonsuk Shin ◽  
Kyoung Soo Lim ◽  
Min-Kyoung Kim ◽  
Hyun Sook Kim ◽  
Jihwa Hong ◽  
...  
Keyword(s):  
Healthy Volunteers ◽  
Human Study ◽  
Pharmacokinetics And Pharmacodynamics ◽  
Associated Factor

scholarly journals Safety, tolerability, pharmacokinetics and pharmacodynamics of a TLR7 agonist prodrug RO6870868 in healthy volunteers

2021 ◽  
Author(s):  
Joseph F. Grippo ◽  
Ilia Folitar ◽  
Sharon Passe ◽  
Qiudi Jiang ◽  
Ignacio Rodriguez ◽  
...  
Keyword(s):  
Healthy Volunteers ◽  
Pharmacokinetics And Pharmacodynamics ◽  
Tlr7 Agonist

scholarly journals ONO‐7684 a novel oral FXIa inhibitor: Safety, tolerability, pharmacokinetics and pharmacodynamics in a first‐in‐human study

2021 ◽  
Author(s):  
Dominic Beale ◽  
Jeremy Dennison ◽  
Malcolm Boyce ◽  
Francesca Mazzo ◽  
Naoki Honda ◽  
...  
Keyword(s):  
Human Study ◽  
Pharmacokinetics And Pharmacodynamics

scholarly journals A first‐in‐human study of KMRC011, a potential treatment for acute radiation syndrome, to explore tolerability, pharmacokinetics, and pharmacodynamics

2021 ◽  
Author(s):  
Eunsol Yang ◽  
Hyejung Choi ◽  
Jin‐Sol Park ◽  
Young‐Woock Noh ◽  
Chi‐Min Choi ◽  
...  
Keyword(s):  
Human Study ◽  
Acute Radiation ◽  
Potential Treatment ◽  
Pharmacokinetics And Pharmacodynamics ◽  
Acute Radiation Syndrome

scholarly journals Phase 1 study to access safety, tolerability, pharmacokinetics, and pharmacodynamics of kynurenine in healthy volunteers

2021 ◽  
Vol 9 (2) ◽  
Author(s):  
Mohammad Al‐Mahdi Al‐Karagholi ◽  
Jakob Møller Hansen ◽  
Dalia Abou‐Kassem ◽  
Anna Koldbro Hansted ◽  
Kumari Ubhayasekera ◽  
...  
Keyword(s):  
Healthy Volunteers ◽  
Phase 1 ◽  
Pharmacokinetics And Pharmacodynamics ◽  
Phase 1 Study
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