First-Time-in-Human Study and Prediction of Early Bactericidal Activity for GSK3036656, a Potent Leucyl-tRNA Synthetase Inhibitor for Tuberculosis Treatment-Reference-Cited by-同舟云学术

First-Time-in-Human Study and Prediction of Early Bactericidal Activity for GSK3036656, a Potent Leucyl-tRNA Synthetase Inhibitor for Tuberculosis Treatment

Published:2019-08 Issue:8 Volume:63 Page:
ISSN:0066-4804
Container-title:Antimicrobial Agents and Chemotherapy
language:en
Short-container-title:Antimicrob Agents Chemother

Author:

Tenero David¹,Derimanov Geo²,Carlton Alex³,Tonkyn John⁴,Davies Matt⁵,Cozens Simon⁶,Gresham Stephanie⁷,Gaudion Alison⁸,Puri Adeep⁸,Muliaditan Morris⁹,Rullas-Trincado Joaquin¹⁰,Mendoza-Losana Alfonso¹⁰,Skingsley Andrew¹¹,Barros-Aguirre David¹⁰^ORCID

Affiliation:

1. GlaxoSmithKline Clinical Pharmacology Modeling and Simulation, Collegeville, Pennsylvania, USA

2. GlaxoSmithKline Clinical Pharmacology and Experimental Medicine, Collegeville, Pennsylvania, USA

3. GlaxoSmithKline Biostatistics, Stockley Park, London, United Kingdom

4. GlaxoSmithKline Global Sciences and Delivery, Stevenage, Hertfordshire, United Kingdom

5. GlaxoSmithKline Safety and Medical Governance, Stockley Park, London, United Kingdom

6. GlaxoSmithKline, Translation Project Specialist Team, Ware, Hertfordshire, United Kingdom

7. GlaxoSmithKline, Mechanistic Safety and Disposition, Ware, Hertfordshire, United Kingdom

8. Hammersmith Medicines Research, London, United Kingdom

9. GlaxoSmithKline DMPK Modelling, Stevenage, Hertfordshire, United Kingdom

10. GlaxoSmithKline Global Health, TBDPU, Tres Cantos, Madrid, Spain

11. GlaxoSmithKline Global Health Clinical Drug Development, Stockley Park, London, United Kingdom

Abstract

This first-time-in-human (FTIH) study evaluated the safety, tolerability, pharmacokinetics, and food effect of single and repeat oral doses of GSK3036656, a leucyl-tRNA synthetase inhibitor. In part A, GSK3036656 single doses of 5 mg (fed and fasted), 15 mg, and 25 mg and placebo were administered. In part B, repeat doses of 5 and 15 mg and placebo were administered for 14 days once daily.

Funder

GlaxoSmithKline

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Link

https://journals.asm.org/doi/pdf/10.1128/AAC.00240-19

Reference29 articles.

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