First-in-Human Study of Orally Administered GS-441524 for COVID-19

First-in-Human Evaluation of the Safety, Tolerability, and Pharmacokinetics of Orally Administered GS-441524 in a Healthy Human Volunteer

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT04859244

Enrollment

Registered

2021-04-26

Start date

2021-01-01

Completion date

2021-08-01

Last updated

2021-08-10

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

COVID-19

Keywords

GS-441524, remdesivir, GS-5734, Copycat Sciences, Gilead Sciences, COVID-19, antiviral

Brief summary

This is a two-part study is to evaluate the multi-day safety, tolerability, and pharmacokinetics (PK) of orally administered GS-441524 in a healthy human volunteer.

Detailed description

Part 1: 750 mg GS-441524 administered once daily (QD) for 7 days. Part 2: 750 mg GS-441524 administered three times daily (TID) for 3 days.

Interventions

DRUGGS-441524

750 mg administered as a solution

Study design

Allocation

NON_RANDOMIZED

Intervention model

CROSSOVER

Primary purpose

TREATMENT

Masking

NONE

Eligibility

Sex/Gender

FEMALE

Age

18 Years to No maximum

Healthy volunteers

Yes

Inclusion criteria

* Willing and able to provide written informed consent * Negative pregnancy test at screening and prior to dosing * Minimum body weight of 50 kg and body mass index (BMI) of 18-32 kg/m2

Exclusion criteria

* Use of other investigational drugs within 28 days of dosing * Positive pregnancy test * Abuse of alcohol or drugs * Other clinically significant medical conditions or laboratory abnormalities

Design outcomes

Primary

Measure	Time frame	Description
Emergence of treatment-related adverse events (AEs)	Day 7	Treatment-related AEs are defined as significant changes to blood chemistry (CBC, CMP) or 6-lead ECG.

Secondary

Measure	Time frame	Description
PK Parameter: AUClast of GS-441524 in Parts 1 and 2.	Intensive PK: Day 1 to Day 7	AUClast is defined as the concentration of drug from time zero to the last observable concentration.
PK Parameter: T1/2 of GS-441524 in Parts 1 and 2.	Intensive PK: Day 1 to Day 7	T/2 is defined as the estimate of the terminal elimination half-life of the drug
PK Parameter: Cmax of GS-441524 in Parts 1 and 2.	Intensive PK: Day 1 to Day 7	Cmax is defined as the maximum observed concentration of drug.
Pharmacokinetic (PK) Parameter: AUC0-24h of GS-441524 in Parts 1 and 2.	Intensive PK: Day 1 to Day 7	AUC0-24h is defined as the concentration of drug over time between time 0 to time 24 hours.
PK Parameter: Clast of GS-441524 in Parts 1 and 2.	Intensive PK: Day 1 to Day 7	Clast is defined as the last observable concentration of drug.
PK Parameter: Tlast of GS-441524 in Parts 1 and 2.	Intensive PK: Day 1 to Day 7	Tlast is defined as the time (observed time point) of Clast.
PK Parameter: AUCtau of GS-441524 in Parts 1 and 2.	Intensive PK: Day 1 to Day 7	AUCtau is defined as concentration of drug over time (the area under the concentration verses time curve over the dosing interval).
PK Parameter: Tmax of GS-441524 in Parts 1 and 2.	Intensive PK: Day 1 to Day 7	Tmax is defined as the time (observed time point) of Cmax.

Countries

United States

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026