Study in Healthy Volunteers to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of GS-9674 (Cilofexor), and the Effect of Food on GS-9674 Pharmacokinetics and Pharmacodynamics
CompletedPhase 1Results postedLast updated 12 October 2020
What this trial tests
Phase 1 trial testing Cilofexor in Nonalcoholic Steatohepatitis (NASH) in 120 participants. Completed in 14 July 2016.
AUCinf is defined as the concentration of drug extrapolated to infinite time (area under the plasma concentration versus time curve extrapolated to infinite time).
Ctau is defined as the observed drug concentration at the end of the dosing interval.
Group
Value
95% CI
Cohort 1: Cilofexor 10 mg
2.7
± 1.53
Cohort 2: Cilofexor 30 mg
7.9
± 3.97
Cohort 3: Cilofexor 100 mg
36.3
± 15.44
Cohort 4: Cilofexor 300 mg
70.1
± 39.46
Cohort 5: Cilofexor 100 mg
22.6
± 8.44
Cohort 6: Cilofexor 50 mg
107.6
± 84.58
Cohort 7: Cilofexor 15 mg
28.4
± 14.13
Cohort 8: Cilofexor 10 mg
3.0
± 1.54
Percentage of Participants With at Least One Adverse Event (AE)Primary· First dose date up to last dose date (Maximum: 20 days) plus 30 days
An AE is any untoward medical occurrence in a clinical study participant administered a medicinal product, which does not necessarily have a causal relationship with the treatment. An AE can therefore be any unfavorable and/or unintended sign, symptom, or disease temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product.
Group
Value
95% CI
Cohort 1: Cilofexor 10 mg
33.3
Cohort 2: Cilofexor 30 mg
25.0
Cohort 3: Cilofexor 100 mg
33.3
Cohort 4: Cilofexor 300 mg
25.0
Cohort 5: Cilofexor 100 mg
41.7
Cohort 6: Cilofexor 50 mg
27.3
Cohort 7: Cilofexor 15 mg
75.0
Cohort 8: Cilofexor 10 mg
18.2
All Placebo
29.2
Percentage of Participants With Clinically Significant 12-Lead Electrocardiogram (ECG) AbnormalitiesPrimary· First dose date up to last dose date (Maximum: 20 days) plus 30 days
Investigator determined the ECG findings were clinically significant.
Group
Value
95% CI
Cohort 1: Cilofexor 10 mg
0
Cohort 2: Cilofexor 30 mg
0
Cohort 3: Cilofexor 100 mg
0
Cohort 4: Cilofexor 300 mg
0
Cohort 5: Cilofexor 100 mg
0
Cohort 6: Cilofexor 50 mg
0
Cohort 7: Cilofexor 15 mg
0
Cohort 8: Cilofexor 10 mg
0
All Placebo
0
Percentage of Participants With Clinical Laboratory AbnormalitiesPrimary· First dose date up to last dose date (Maximum: 20 days) plus 30 days
Treatment-emergent laboratory (Hematology, Chemistry, and Urinalysis) abnormalities were defined as values that increase at least one toxicity grade from baseline. Laboratory Abnormalities are graded by the investigator as Grade 1, 2, 3, or 4 according to the modified Gilead Sciences, Inc (GSI) Grading Scale. The most severe graded abnormality from all tests was counted for each participant. Data is only reported for those Grades reported in 1 or more participants.
AUC2-12 is defined as the AUC from time 2 to 12 hours. The ratios calculated were normalized to Day -1. Participants received a single placebo tablet at Day -1 for Baseline. The ratio reported for Day 1 is the AUC2-12 Day 1 /AUC2-12 Day-1. The ratio reported for Day 20 is the AUC2-12 Day 20 /AUC2-12 Day-1.
Cmax is defined as the maximum observed concentration of FGF19 in plasma. The ratios calculated were normalized to Day -1. Participants received a single placebo tablet at Day -1 for Baseline. The ratio reported for Day 1 is the Cmax Day 1 /Cmax Day-1. The ratio reported for Day 20 is the Cmax Day 20 /Cmax Day-1.
AUC2-12 is defined as the AUC from time 2 to 12 hours. The ratios calculated were normalized to Day -1. Participants received a single placebo tablet at Day -1 for Baseline. The ratio reported for Day 1 is the AUC2-12 Day 1 /AUC2-12 Day-1. The ratio reported for Day 20 is the AUC2-12 Day 20 /AUC2-12 Day-1.
Day 1/Day -1
Group
Value
95% CI
Cohort 1: Cilofexor 10 mg
0.681
0.431 – 1.077
Cohort 2: Cilofexor 30 mg
0.640
0.516 – 0.794
Cohort 3: Cilofexor 100 mg
0.427
0.340 – 0.537
Cohort 4: Cilofexor 300 mg
0.347
0.278 – 0.433
All Fasted Placebo
1.147
0.921 – 1.429
Cohort 5: Cilofexor 100 mg
0.837
0.629 – 1.114
Cohort 6: Cilofexor 50 mg
0.653
0.581 – 0.735
Cohort 7: Cilofexor 15 mg
0.863
0.747 – 0.997
Cohort 8: Cilofexor 10 mg
1.108
0.828 – 1.483
All Fed Placebo
1.057
0.893 – 1.252
Day 20/Day -1
Group
Value
95% CI
Cohort 1: Cilofexor 10 mg
0.661
0.456 – 0.959
Cohort 2: Cilofexor 30 mg
0.382
0.277 – 0.525
Cohort 3: Cilofexor 100 mg
0.495
0.348 – 0.704
Cohort 4: Cilofexor 300 mg
0.325
0.223 – 0.474
All Fasted Placebo
1.213
0.828 – 1.777
Cohort 5: Cilofexor 100 mg
0.621
0.414 – 0.933
Cohort 6: Cilofexor 50 mg
0.173
0.109 – 0.275
Cohort 7: Cilofexor 15 mg
0.624
0.472 – 0.825
Cohort 8: Cilofexor 10 mg
0.974
0.677 – 1.402
All Fed Placebo
0.843
0.681 – 1.043
Adverse events — posted to ClinicalTrials.gov
Time frame: First dose date up to last dose date (Maximum: 20 days) plus 30 days.
Reporting threshold: 5%.
Adverse-event reports describe events observed during the trial — not all are caused by the drug.
This study will evaluate the safety and tolerability of escalating single- and multiple-oral doses of cilofexor, and characterize the single- and multiple-dose pharmacokinetics (PK) of cilofexor. The study will be conducted in 3 parts (Part A, Part B, and Part C). Participants will receive either cilofexor or cilofexor placebo.
Part A will proceed in 4 prespecified staggered cohorts. Within each cohort, the cumulative, blinded safety data will be evaluated for dose escalation from single-dose (Period 1) to multiple-dose (Period 2). Based on the available safety, pharmacokinetics, and/or pharmacodynamics (PD) data from cohorts in Part A and Part C (if applicable), total daily doses and frequency of dosing will be chosen for the cohorts in Part B. Parts B and C will consist of adaptive cohorts and may be initiated in parallel. Part B cohorts may be initiated in parallel with cohorts in Part A if the total dose under evaluation is at or below a dose already evaluated.
This study is partially blinded (no one is blinded on Day -1).
Publications & conference data
7 peer-reviewed publications reference this trial (live from Europe PMC):
NCT04060147 — Safety and Tolerability of Cilofexor in Participants With Primary Sclerosing Cholangitis (PSC) and Compensated Cirrhosis
· Phase 1
· terminated
NCT03987074 — Safety, Tolerability, and Efficacy of Monotherapy and Combination Regimens in Participants With Nonalcoholic Steatohepat
· Phase 2
· completed
NCT03890120 — Study of Cilofexor in Adults With Primary Sclerosing Cholangitis
· Phase 3
· terminated
NCT02943447 — Study to Evaluate the Safety, Tolerability, and Efficacy of Cilofexor in Adults With Primary Biliary Cholangitis Without
· Phase 2
· terminated
NCT02943460 — Study to Evaluate the Safety, Tolerability, and Efficacy of Cilofexor in Adults With Primary Sclerosing Cholangitis With
· Phase 2
· completed
Other recruiting trials for Nonalcoholic Steatohepatitis (NASH)
Currently open trials in the same condition.
NCT06216041 — To Evaluate the Safety, Tolerability, Pharmacokinetics and Food Effects of IMM-H014 in Healthy Subjects
· Phase 1
· recruiting
NCT05842512 — Study of ADI-PEG 20 Versus Placebo in Subjects With NASH
· Phase 2
· recruiting
NCT05692492 — A Randomized, Double-blind, Placebo-controlled Study of ZSP1601 in Adult Subjects With Nonalcoholic Steatohepatitis (NAS
· Phase 2
· active not recruiting
NCT03572465 — Quantitative Ultrasound Techniques for Diagnosis of Nonalcoholic Steatohepatitis
· recruiting
Other Gilead Sciences trials
Trials by the same sponsor.
NCT07115368 — Study of GS-1219 in Participants With HIV-1
· Phase 1
· terminated
NCT06784973 — Study of Obeldesivir to Treat Children With Respiratory Syncytial Virus (RSV) Infection
· Phase 2
· terminated
NCT06683482 — A Qualitative Study on Advanced Breast Cancer Patients and Their Caregivers in Spain
· completed
NCT06613685 — Study of Oral Weekly GS-1720 and GS-4182 Compared With Biktarvy in People With HIV-1 Who Have Not Been Treated
· Phase 2, PHASE3
· terminated
NCT06585150 — Study of Obeldesivir to Treat Nonhospitalized Adults With Acute Respiratory Syncytial Virus (RSV) Infection
· Phase 2
· terminated
Publications: Europe PMC API search by NCT ID, retrieved 10 June 2026
Drug + disease cross-links: matched in real time against Drug Landscape's normalised drug + company + condition tables
Sponsor: as reported to ClinicalTrials.gov by Gilead Sciences
Last refreshed: 12 October 2020
Drug Landscape aggregates and links these public records for informational use only. Always verify against the primary source before clinical or regulatory decisions. Canonical URL: https://druglandscape.com/trial/NCT02654002.