This is an open-label, single-centre, non-randomized study to investigate the pharmacokinetics of GSK3191607, administered as a single intravenous (IV) dose in healthy male subjects.
Six subjects will be administered an IV microdose of radio-labeled [14C]-GSK3191607. The study will provide an early readout on human pharmacokinetic parameters. The results of this study will be used to estimate the potential duration of anti-parasite effect in humans, define predicted clinical oral doses, and hence inform about the compound's potential safety margin.
Each subject will participate in the study for up to 8 weeks, and will have a screening visit, one treatment period, eight outpatient visits, and a follow-up visit.

Start Date18 Apr 2016

Sponsor / Collaborator

GSK Plc

[+1]

NL-OMON34612 / CompletedNot Applicable

SINGLE-CENTER, SINGLE DOSE ORAL EXCRETION BALANCE STUDY OF RO5200628 IN HEALTHY MALE VOLUNTEERS - [14C]-RO5200628 ADME study

Start Date01 Sep 2010

Sponsor / Collaborator

Hoffmann-La Roche Ltd.

100 Clinical Results associated with GSK-3191607

100 Translational Medicine associated with GSK-3191607

100 Patents (Medical) associated with GSK-3191607

Literatures (Medical) associated with GSK-3191607

01 Mar 2018·British journal of clinical pharmacologyQ2 · MEDICINE

A human microdose study of the antimalarial drug GSK3191607 in healthy volunteers

Q2 · MEDICINE

Article

Author: Fernandez, Esther ; Rolfe, Katie ; Wong, Deborah ; Rami, Harshad ; Koh, Gavin ; Young, Graeme ; Derimanov, Geo ; Pereira, Adrian ; Barnett, Rodger ; Ferrer, Santiago ; Okour, Malek ; Haselden, John ; Gresham, Stephanie ; Hossain, Mohammad ; Gamo, Francisco‐Javier

Aims:

GSK3191607, a novel inhibitor of the Plasmodium falciparum ATP4 (PfATP4) pathway, is being considered for development in humans. However, a key problem encountered during the preclinical evaluation of the compound was its inconsistent pharmacokinetic (PK) profile across preclinical species (mouse, rat and dog), which prevented reliable prediction of PK parameters in humans and precluded a well‐founded assessment of the potential for clinical development of the compound. Therefore, an open‐label microdose (100 μg, six subjects) first time in humans study was conducted to assess the human PK of GSK3191607 following intravenous administration of [14C]‐GSK3191607.

Methods:

A human microdose study was conducted to investigate the clinical PK of GSK3191607 and enable a Go/No Go decision on further progression of the compound. The PK disposition parameters estimated from the microdose study, combined with preclinical in vitro and in vivo pharmacodynamic parameters, were all used to estimate the potential efficacy of various oral dosing regimens in humans.

Results:

The PK profile, based on the microdose data, demonstrated a half‐life (~17 h) similar to other antimalarial compounds currently in clinical development. However, combining the microdose data with the pharmacodynamic data provided results that do not support further clinical development of the compound for a single dose cure.

Conclusions:

The information generated by this study provides a basis for predicting the expected oral PK profiles of GSK3191607 in man and supports decisions on the future clinical development of the compound.

100 Deals associated with GSK-3191607

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Malaria, Falciparum	Phase 1	GB	GSK Plc	18 Apr 2016

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