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A Drug-Drug Interaction Study to Examine the Impact of Itraconazole and Cyclosporine on PF-07081532 Pharmacokinetics in Overweight or Obese Adults
A PHASE 1, OPEN-LABEL, FIXED-SEQUENCE STUDY TO EVALUATE THE EFFECT OF ITRACONAZOLE AND CYCLOSPORINE ON THE SINGLE-DOSE PHARMACOKINETICS OF PF-07081532 IN OVERWEIGHT OR OBESE ADULT PARTICIPANTS
Lead sponsor
Asset
Lotiglipron
Oral · GLP-1 agonist
Listed sites
1
Recruiting sites
—
Enrollment
16
actual
Study population
Obesity / overweight
Key I/E criteria
•BMI ≥25•Healthy volunteers
Primary endpoint
•Area Under the Curve
Footprint
Where this trial recruits
Site locations as reported to ClinicalTrials.gov. Site count is not enrollment count; per-site enrollment is not available from source.
Identifiers
Registered as
Timeline
Milestones
Assets
Investigational agents
Study populations
Who this study enrolls
Eligibility
Who can enroll
Inclusion criteria
1. Otherwise healthy female and male participants must be at least 18 years of age at the time of signing the ICD (healthy is defined as no clinically relevant abnormalities identified by a detailed medical history, physical examination, including blood pressure and pulse rate measurement, standard 12-lead ECG and clinical laboratory tests).
2. BMI: ≥25.0 kg/m2 at Screening.
3. Stable body weight, defined as <5 kg change (per participant report) for 90 days before Screening.
Exclusion criteria
1. Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurological, or allergic disease (including drug allergies, but excluding untreated, asymptomatic, seasonal allergies at the time of dosing).
2. Diagnosis of type 1 or type 2 diabetes mellitus or secondary forms of diabetes at Screening.
3. Any malignancy not considered cured (except basal cell carcinoma and squamous cell carcinoma of the skin)
4. Personal or family history of MTC or MEN2, or study participants with suspected MTC per the investigator's judgment.
5. Acute pancreatitis, a history of repeated episodes of acute pancreatitis, or history of chronic pancreatitis.
6. Symptomatic gallbladder disease.
7. Medical history or characteristics suggestive of genetic or syndromic obesity or obesity induced by other endocrinological disorders (eg, Cushing Syndrome).
8. History of depressive disorder or history of other severe psychiatric disorders (eg, schizophrenia or bipolar disorder) within the last 2 years from screening.
9. Known medical history of active liver disease, including chronic hepatitis B or C, primary biliary cirrhosis, alcoholic liver disease, primary sclerosing cholangitis, autoimmune hepatitis, overlap syndrome, or prior known drug-induced liver injury.
10. History of HIV infection.
11. Any lifetime history of a suicide attempt.
12. Use of prohibited medications
13. Screening supine BP ≥140 mm Hg (systolic) or ≥90 mm Hg (diastolic), following at least 5 minutes of supine rest.
14. Standard 12-lead ECG that demonstrates clinically relevant abnormalities that mayaffect participant safety or interpretation of study result.
15. Participants with clinical laboratory test abnormalities at Screening. -
Endpoints (26)
What's being measured
Protocol endpoints and posted registry outcome measures, grouped into outcome categories. Composite endpoints show their component event types. Standard codes (LOINC, SNOMED CT) are shown where available.
Coverage by outcome category
Weight & body composition
2 endpointsChange From Baseline in Body Weight at the End of Periods 1, 2, and 3
Time frame:Baseline (pre-dose on Day 1), Day 5 of Period 1 (Study Day 5), Day 5 of Period 2 (Study Day 10), and Day 10 of Period 3 (Study Day 20)
change from baseline, improvement
Posted result
| Group | Value (mean), Kilogram (kg) | 95% CI |
|---|---|---|
| Lotiglipron Then Lotiglipron + Cyclosporine Then Lotiglipron + ItraconazoleBaseline | 87.631 | — |
| Day 5 of Period 1 | -1.631 | — |
| Day 5 of Period 2 | -1.956 | — |
| Day 10 of Period 3 | -2.256 | — |
Change From Baseline in Body Weight at the End of Periods 1, 2, and 3
Time frame:Baseline (pre-dose on Day 1), Day 5 of Period 1 (Study Day 5), Day 5 of Period 2 (Study Day 10), and Day 10 of Period 3 (Study Day 20)
Body weight, absolute change (kg)
change from baseline, improvement
Patient-reported / QoL
2 endpointsNumber of Participants With a Score of ≥15 on Patient Health Questionnaire-9 (PHQ-9)
Time frame:Period 1 Day -1 (Study Day -1), Period 3 Day 10 (Study Day 20) or Early Termination visit
threshold achievement, improvement
Posted result
| Group | Value (count_of_participants), Participants | 95% CI |
|---|---|---|
| Lotiglipron Then Lotiglipron + Cyclosporine Then Lotiglipron + Itraconazole | 0 | — |
Number of Participants With a Score of ≥15 on Patient Health Questionnaire-9 (PHQ-9)
Time frame:Period 1 Day -1 (Study Day -1), Period 3 Day 10 (Study Day 20) or Early Termination visit
threshold achievement, improvement
Safety / tolerability / PK
22 endpointsArea Under the Curve From Time Zero to Extrapolated Infinite Time (AUCinf) of Lotiglipron When Administered Alone and With Itraconazole or Cyclosporine
Time frame:Pre-dose of lotiglipron and at 0.5, 1, 2, 4, 6, 8, 10, 12, 14, 24, 36, 48, 72, 96, 120, and 144 (for Period 3 only) hours post dose of lotiglipron on Day 1 of Periods 1 and 2 and on Day 4 of Period 3.
descriptive
Posted result
| Group | Value (geometric_mean), nanogram*hour/milliliter (ng*hr/mL) | 95% CI |
|---|---|---|
| Active Comparator: Period 1: Lotiglipron | 81800 | — |
| Experimental: Period 2: Lotiglipron + Cyclosporine | 162800 | — |
| Experimental: Period 3: Itraconazole+Lotiglipron | 212900 | — |
Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUCinf) of Lotiglipron When Administered Alone and With Itraconazole or Cyclosporine
Time frame:Pre-dose of lotiglipron and at 0.5, 1, 2, 4, 6, 8, 10, 12, 14, 24, 36, 48, 72, 96, 120, and 144 (for Period 3 only) hours post dose of lotiglipron on Day 1 of Periods 1 and 2 and on Day 4 of Period 3.
AUC₀–∞
concentration, descriptive
Number of Participants With Treatment-Emergent Adverse Events (TEAEs)
Time frame:From the first dose up to 35 days after administration of the final dose of study intervention (Period 3 Day 9, Study Day 19), the maximum duration was 54 Days
event count, event
Posted result
| Group | Value (count_of_participants), Participants | 95% CI |
|---|---|---|
| Lotiglipron Then Lotiglipron + Cyclosporine Then Lotiglipron + ItraconazoleAll causality TEAEs | 11 | — |
| Treatment-Related TEAEs | 11 | — |
| All causality Treatment-emergent SAEs | 0 | — |
Number of Participants With Laboratory Abnormalities
Time frame:Baseline (pre-dose on Day 1), Period 2 Day 5 (Study Day 10), and Period 3 Day 10 (Study Day 20)
event count, event
Posted result
| Group | Value (count_of_participants), Participants | 95% CI |
|---|---|---|
| Lotiglipron Then Lotiglipron + Cyclosporine Then Lotiglipron + ItraconazoleHEMATOLOGY- Ery. Mean Corpuscular Volume (fL) < 0.9*LLN | 1 | — |
| HEMATOLOGY-Ery. Mean Corpuscular Hemoglobin (pg/cell) < 0.9*LLN | 1 | — |
| HEMATOLOGY-Eosinophils/Leukocytes (%)> 1.2*ULN | 1 | — |
| CLINICAL CHEMISTRY-Urate (mg/dL)> 1.2*ULN | 1 | — |
| URINALYSIS-URINE Hemoglobin (Scalar)≥ 1 | 1 | — |
Number of Participants Meeting Pre-Specified Criteria of Vital Signs
Time frame:Pre-dose Day 1 in periods 1, 2 and 3 (Study Days 1, 6, and 11, respectively), and prior to discharge on Period 3 Day 10 (Study Day 20)
event count, event
Posted result
| Group | Value (count_of_participants), Participants | 95% CI |
|---|---|---|
| Lotiglipron Then Lotiglipron + Cyclosporine Then Lotiglipron + Itraconazole | 0 | — |
Number of Participants Meeting Pre-Specified Criteria of Electrocardiogram (ECGs)
Time frame:Pre-dose Day 1 in periods 1, 2 and 3 (Study Days 1, 6, and 11, respectively), and prior to discharge on Period 3 Day 10 (Study Day 20)
event count, event
Posted result
| Group | Value (count_of_participants), Participants | 95% CI |
|---|---|---|
| Lotiglipron Then Lotiglipron + Cyclosporine Then Lotiglipron + Itraconazole | 0 | — |
Number of Participants With Suicidal Ideation or Behavior According to Columbia Suicide Severity Rating Scale (C-SSRS)
Time frame:Period 1 Day -1 (Study Day -1), Period 3 Day 10 (Study Day 20) or Early Termination visit
event count, event
Posted result
| Group | Value (count_of_participants), Participants | 95% CI |
|---|---|---|
| Lotiglipron Then Lotiglipron + Cyclosporine Then Lotiglipron + Itraconazole | 0 | — |
Maximum Observed Plasma Concentration (Cmax) of Lotiglipron When Administered Alone and With Itraconazole or Cyclosporine
Time frame:Pre-dose of lotiglipron and at 0.5, 1, 2, 4, 6, 8, 10, 12, 14, 24, 36, 48, 72, 96, 120, and 144 (for Period 3 only) hours post dose of lotiglipron on Day 1 of Periods 1 and 2 and on Day 4 of Period 3.
concentration, descriptive
Posted result
| Group | Value (geometric_mean), nanogram/milliliter (ng/mL) | 95% CI |
|---|---|---|
| Active Comparator: Period 1: Lotiglipron | 4165 | — |
| Experimental: Period 2: Lotiglipron + Cyclosporine | 5207 | — |
| Experimental: Period 3: Itraconazole+Lotiglipron | 5180 | — |
Time to Cmax (Tmax) of Lotiglipron When Administered Alone and With Itraconazole or Cyclosporine
Time frame:Pre-dose of lotiglipron and at 0.5, 1, 2, 4, 6, 8, 10, 12, 14, 24, 36, 48, 72, 96, 120, and 144 (for Period 3 only) hours post dose of lotiglipron on Day 1 of Periods 1 and 2 and on Day 4 of Period 3.
time to event, event
Posted result
| Group | Value (median), hr | 95% CI |
|---|---|---|
| Active Comparator: Period 1: Lotiglipron | 6.00 | 3.98 – 8.00 |
| Experimental: Period 2: Lotiglipron + Cyclosporine | 6.00 | 2.00 – 12.0 |
| Experimental: Period 3: Itraconazole+Lotiglipron | 5.03 | 2.00 – 10.0 |
Apparent Oral Clearance (CL/F) of Lotiglipron When Administered Alone and With Itraconazole or Cyclosporine
Time frame:Pre-dose of lotiglipron and at 0.5, 1, 2, 4, 6, 8, 10, 12, 14, 24, 36, 48, 72, 96, 120, and 144 (for Period 3 only) hours post dose of lotiglipron on Day 1 of Periods 1 and 2 and on Day 4 of Period 3.
concentration, descriptive
Posted result
| Group | Value (geometric_mean), Litre (L)/hr | 95% CI |
|---|---|---|
| Active Comparator: Period 1: Lotiglipron | 0.4890 | — |
| Experimental: Period 2: Lotiglipron + Cyclosporine | 0.2458 | — |
| Experimental: Period 3: Itraconazole+Lotiglipron | 0.1879 | — |
Apparent Oral Volume of Distribution (Vz/F) of Lotiglipron When Administered Alone and With Itraconazole or Cyclosporine
Time frame:Pre-dose of lotiglipron and at 0.5, 1, 2, 4, 6, 8, 10, 12, 14, 24, 36, 48, 72, 96, 120, and 144 (for Period 3 only) hours post dose of lotiglipron on Day 1 of Periods 1 and 2 and on Day 4 of Period 3.
descriptive
Posted result
| Group | Value (geometric_mean), Litre | 95% CI |
|---|---|---|
| Active Comparator: Period 1: Lotiglipron | 15.01 | — |
| Experimental: Period 2: Lotiglipron + Cyclosporine | 8.261 | — |
| Experimental: Period 3: Itraconazole+Lotiglipron | 11.91 | — |
Terminal Half-life (t1/2) of Lotiglipron When Administered Alone and With Itraconazole or Cyclosporine
Time frame:Pre-dose of lotiglipron and at 0.5, 1, 2, 4, 6, 8, 10, 12, 14, 24, 36, 48, 72, 96, 120, and 144 (for Period 3 only) hours post dose of lotiglipron on Day 1 of Periods 1 and 2 and on Day 4 of Period 3.
concentration, descriptive
Posted result
| Group | Value (mean), hr | 95% CI |
|---|---|---|
| Active Comparator: Period 1: Lotiglipron | 21.96 | — |
| Experimental: Period 2: Lotiglipron + Cyclosporine | 24.14 | — |
| Experimental: Period 3: Itraconazole+Lotiglipron | 45.02 | — |
Number of Participants With Treatment-Emergent Adverse Events (TEAEs)
Time frame:From the first dose up to 35 days after administration of the final dose of study intervention (Period 3 Day 9, Study Day 19), the maximum duration was 54 Days
Treatment-emergent AEs (any)
event count, event
Number of Participants With Laboratory Abnormalities
Time frame:Baseline (pre-dose on Day 1), Period 2 Day 5 (Study Day 10), and Period 3 Day 10 (Study Day 20)
threshold achievement, event
Number of Participants Meeting Pre-Specified Criteria of Vital Signs
Time frame:Pre-dose Day 1 in periods 1, 2 and 3 (Study Days 1, 6, and 11, respectively), and prior to discharge on Period 3 Day 10 (Study Day 20)
threshold achievement, event
componentsDiastolic BP, change, Systolic BP, change, Heart rate, change
Number of Participants Meeting Pre-Specified Criteria of Electrocardiogram (ECGs)
Time frame:Pre-dose Day 1 in periods 1, 2 and 3 (Study Days 1, 6, and 11, respectively), and prior to discharge on Period 3 Day 10 (Study Day 20)
threshold achievement, event
Number of Participants With Suicidal Ideation or Behavior According to Columbia Suicide Severity Rating Scale (C-SSRS)
Time frame:Period 1 Day -1 (Study Day -1), Period 3 Day 10 (Study Day 20) or Early Termination visit
threshold achievement, event
Maximum Observed Plasma Concentration (Cmax) of Lotiglipron When Administered Alone and With Itraconazole or Cyclosporine
Time frame:Pre-dose of lotiglipron and at 0.5, 1, 2, 4, 6, 8, 10, 12, 14, 24, 36, 48, 72, 96, 120, and 144 (for Period 3 only) hours post dose of lotiglipron on Day 1 of Periods 1 and 2 and on Day 4 of Period 3.
Cmax
concentration, descriptive
Time to Cmax (Tmax) of Lotiglipron When Administered Alone and With Itraconazole or Cyclosporine
Time frame:Pre-dose of lotiglipron and at 0.5, 1, 2, 4, 6, 8, 10, 12, 14, 24, 36, 48, 72, 96, 120, and 144 (for Period 3 only) hours post dose of lotiglipron on Day 1 of Periods 1 and 2 and on Day 4 of Period 3.
Tmax
descriptive
Apparent Oral Clearance (CL/F) of Lotiglipron When Administered Alone and With Itraconazole or Cyclosporine
Time frame:Pre-dose of lotiglipron and at 0.5, 1, 2, 4, 6, 8, 10, 12, 14, 24, 36, 48, 72, 96, 120, and 144 (for Period 3 only) hours post dose of lotiglipron on Day 1 of Periods 1 and 2 and on Day 4 of Period 3.
descriptive
Apparent Oral Volume of Distribution (Vz/F) of Lotiglipron When Administered Alone and With Itraconazole or Cyclosporine
Time frame:Pre-dose of lotiglipron and at 0.5, 1, 2, 4, 6, 8, 10, 12, 14, 24, 36, 48, 72, 96, 120, and 144 (for Period 3 only) hours post dose of lotiglipron on Day 1 of Periods 1 and 2 and on Day 4 of Period 3.
descriptive
Terminal Half-life (t1/2) of Lotiglipron When Administered Alone and With Itraconazole or Cyclosporine
Time frame:Pre-dose of lotiglipron and at 0.5, 1, 2, 4, 6, 8, 10, 12, 14, 24, 36, 48, 72, 96, 120, and 144 (for Period 3 only) hours post dose of lotiglipron on Day 1 of Periods 1 and 2 and on Day 4 of Period 3.
Half-life
descriptive
Provenance
Sources
Trial facts come from public ClinicalTrials.gov records. Endpoint categories are Delfa's classification of those records, not a ClinicalTrials.gov field. All figures reflect the July 1, 2026 snapshot.