Healthy
Conditions
Brief summary
The purpose of this study is to compare the amount of tirzepatide that gets into the blood stream and how long it takes the body to get rid of it, when injected under the skin of the upper arm and thigh compared to the abdomen. The study will be conducted in healthy males and females with different body sizes. The tolerability of tirzepatide will be evaluated and information about any side effects experienced will be collected. For each participant, the study will last about 20 weeks, including screening.
Interventions
DRUGTirzepatide
Tirzepatide administered SC
Sponsors
Eli Lilly and Company
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 70 Years
Healthy volunteers
Yes
Inclusion criteria
* Healthy males or females of nonchildbearing potential as determined by medical history, physical examination, and other screening procedures * Are between the body mass index (BMI) of 18.5 and 45.0 kilograms per meter squared (kg/m²), inclusive, at screening * Are agreeable to receiving study treatment by injections under the skin
Exclusion criteria
* Have known allergies to tirzepatide or related compounds * Have a personal or family history of medullary thyroid carcinoma or have multiple endocrine neoplasia syndrome type 2 * Have a history or presence of pancreatitis (history of chronic pancreatitis or idiopathic acute pancreatitis), elevation in serum amylase or lipase or gastrointestinal (GI) disorder (eg, relevant esophageal reflux or gall bladder disease) or any GI disease which impacts gastric emptying (eg, gastric bypass surgery, pyloric stenosis, with the exception of appendectomy) or could be aggravated by glucagon-like peptide-1 (GLP-1) analogs or dipeptidyl peptidase IV (DPP-IV) inhibitors * Have a prior history of malignant disease(s) in the past 5 years prior to screening * Smoke more than the equivalent of 10 cigarettes per day * Is a known user of drugs of abuse
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve of Tirzepatide From Time Zero to Infinity (AUC[0-∞]) | Predose, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 336, 480 hours post dose | Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve of Tirzepatide From Time Zero to Infinity (AUC\[0-∞\]) was evaluated. |
| PK: Maximum Concentration (Cmax) of Tirzepatide | Predose, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 336, 480 hours post dose | PK: Maximum Concentration (Cmax) of Tirzepatide was evaluated. |
Countries
United States
Participant flow
Pre-assignment details
There was a washout period of at least 35 days between Tirzepatide injections.
Participants by arm
| Arm | Count |
|---|---|
| All Participants Participants received 5mg Tirzepatide by subcutaneous injection administered through either upper arms or abdomen or thigh as per the dosing sequence. | 54 |
| Total | 54 |
Withdrawals & dropouts
| Period | Reason | FG000 | FG001 | FG002 |
|---|---|---|---|---|
| Period 3 | Physician Decision | 0 | 1 | 0 |
Baseline characteristics
| Characteristic | All Participants |
|---|---|
| Age, Continuous | 47.1 years STANDARD_DEVIATION 12.8 |
| Ethnicity (NIH/OMB) Hispanic or Latino | 16 Participants |
| Ethnicity (NIH/OMB) Not Hispanic or Latino | 38 Participants |
| Ethnicity (NIH/OMB) Unknown or Not Reported | 0 Participants |
| Race (NIH/OMB) American Indian or Alaska Native | 0 Participants |
| Race (NIH/OMB) Asian | 0 Participants |
| Race (NIH/OMB) Black or African American | 14 Participants |
| Race (NIH/OMB) More than one race | 0 Participants |
| Race (NIH/OMB) Native Hawaiian or Other Pacific Islander | 0 Participants |
| Race (NIH/OMB) Unknown or Not Reported | 0 Participants |
| Race (NIH/OMB) White | 40 Participants |
| Region of Enrollment United States | 54 Participants |
| Sex: Female, Male Female | 17 Participants |
| Sex: Female, Male Male | 37 Participants |
Adverse events
| Event type | EG000 affected / at risk | EG001 affected / at risk | EG002 affected / at risk |
|---|---|---|---|
| deaths Total, all-cause mortality | 0 / 54 | 0 / 54 | 0 / 53 |
| other Total, other adverse events | 37 / 54 | 31 / 54 | 23 / 53 |
| serious Total, serious adverse events | 0 / 54 | 0 / 54 | 0 / 53 |
Outcome results
Primary
Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve of Tirzepatide From Time Zero to Infinity (AUC[0-∞])
Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve of Tirzepatide From Time Zero to Infinity (AUC\[0-∞\]) was evaluated.
Time frame: Predose, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 336, 480 hours post dose
Population: All randomized participants who received at least one dose of study drug and had evaluable PK samples.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Tirzepatide - Abdomen | Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve of Tirzepatide From Time Zero to Infinity (AUC[0-∞]) | 112000 Hour * nanogram per milliliter (h*ng/mL) | Geometric Coefficient of Variation 24 |
| Tirzepatide - Upper Arm | Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve of Tirzepatide From Time Zero to Infinity (AUC[0-∞]) | 111000 Hour * nanogram per milliliter (h*ng/mL) | Geometric Coefficient of Variation 21 |
| Tirzepatide - Thigh | Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve of Tirzepatide From Time Zero to Infinity (AUC[0-∞]) | 106000 Hour * nanogram per milliliter (h*ng/mL) | Geometric Coefficient of Variation 22 |
90% CI: [0.935, 0.97]Linear mixed effects model
90% CI: [0.972, 1.01]Linear mixed effects model
Primary
PK: Maximum Concentration (Cmax) of Tirzepatide
PK: Maximum Concentration (Cmax) of Tirzepatide was evaluated.
Time frame: Predose, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 336, 480 hours post dose
Population: All randomized participants who received at least one dose of study drug and had evaluable PK samples.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Tirzepatide - Abdomen | PK: Maximum Concentration (Cmax) of Tirzepatide | 603 Nanogram per Millilitre (ng/mL) | Geometric Coefficient of Variation 25 |
| Tirzepatide - Upper Arm | PK: Maximum Concentration (Cmax) of Tirzepatide | 556 Nanogram per Millilitre (ng/mL) | Geometric Coefficient of Variation 23 |
| Tirzepatide - Thigh | PK: Maximum Concentration (Cmax) of Tirzepatide | 520 Nanogram per Millilitre (ng/mL) | Geometric Coefficient of Variation 21 |
90% CI: [0.818, 0.909]Linear mixed effects model
95% CI: [0.874, 0.971]Linear mixed effects model