Trial · Interventional

CompletedPhase 1Results postedRegistry data

A Study of Tirzepatide (LY3298176) in Healthy Participants

NCTNCT03375463Other id16671Other idI8F-MC-GPGE

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Overview

Status: Completed
Phase: Phase 1
Enrollment: 52 participants (actual)
Sponsor: Eli Lilly and Company · Industry
Design: Randomized · Double masking
Countries: 1 country
United States
Start: 19 Dec 2017
Primary completion: 27 Dec 2018
Completion: 27 Dec 2018
First posted: 18 Dec 2017
Last update posted: 5 Feb 2024
Conditions: Healthy

Timeline

1 trial · 1 completed · 1 with posted results

Completed
Ongoing
Not yet recruiting
Stopped
Estimated dates (est.)
Results posted

201720182019

Ph 1
A Study of Tirzepatide (LY3298176) in Healthy Participants
NCT03375463
19 Dec 2017 to 27 Dec 2018

Registry summary

Text and fields below are the sponsor's entries at ClinicalTrials.gov, shown as posted.

This study has four parts. Each participant will enroll in one part. Part A: The purpose of Part A is to compare study drug tirzepatide solution formulation to a powder formulation mixed with water and given subcutaneously (SC) (just under the skin). Part A will measure how much of the study drug gets into the blood stream and how long it takes the body to get rid of it. Part B: The purpose of Part B is to evaluate the safety and tolerability of tirzepatide intravenous (IV) formulation when administered into a vein. Part C: The purpose of Part C is to evaluate the safety and tolerability of tirzepatide following multiple SC weekly doses of a solution. Part D: The purpose of Part D is to evaluate the safety and tolerability of tirzepatide following single IV bolus dose of lyophilized formulation. This study will last approximately 70 days for each part (Part A, Part B or Part D) and 92 days for Part C. This does not include screening. Screening is required within 28 days prior to the start of the study.

Interventions

TirzepatideDrug
TirzepatideDrug
PlaceboDrug
TirzepatideDrug

Arms6

Experimental
5 mg Tirzepatide SC (Solution)-Part A
Participants received 5 milligrams (mg) of tirzepatide subcutaneous (SC) solution formulation.
Experimental
5 mg Tirzepatide SC (Lyophilized)-Part A
Participants received 5 mg of tirzepatide SC lyophilized formulation.
Experimental
0.5 mg LY3298176 IV-Part B
Participants received Intravenous (IV) infusion of a single 0.5 mg dose of tirzepatide formulation.
Experimental
5 mg/7.5 mg/ 10 mg Tirzepatide SC-Part C
Participants received tirzepatide subcutaneous solution at 5 mg on Days 1 (week 1) and 8 (Week 2), 7.5 mg on Day 15 (Week 3) and 10 mg on Day 22 (Week 4).
Placebo comparator
Placebo SC-Part C
Participants received SC injection of placebo.
Experimental
0.5 mg LY3298176 Bolus IV-Part D
Participants received IV bolus of 0.5 mg tirzepatide lyophilized formulation.

Primary outcomes3

Outcomes the sponsor listed as primary.

Pharmacokinetics (PK) Part A: Area Under the Concentration Versus Time Curve [AUC (0-∞)] of Tirzepatide
Time frame · Part A: Predose, 8, 12, 24, 48, 72, 96, 120, 144, 168, 336, 480, 816-864 hours postdose
Registry description
Pharmacokinetics (PK) Part A: Area under the concentration versus time curve \[AUC (0-∞)\] of tirzepatide.
PK Part A: Maximum Observed Drug Concentration (Cmax) of Tirzepatide
Time frame · Part A: Predose, 8, 12, 24, 48, 72, 96, 120, 144, 168, 336, 480 and 816-864 hours postdose
Registry description
PK Part A: Maximum observed plasma drug concentration (Cmax) of tirzepatide.
PK Part B: Area Under the Concentration Versus Time Curve [AUC (0-∞)] of Tirzepatide
Time frame · Part B: Predose, 0.08 hours (h), 0.16h, 0.5h, 1h, 2h, 4h, 8h, 12h, 24h, 36h, 48h, 72h, 96h, 120h, 144h, 168h, 336h, 816h-864h and >=70 days post dose
Registry description
PK Part B: Area under the concentration versus time curve \[AUC (0-∞)\] of tirzepatide.

Secondary outcomes(3)

PK Part C: Area Under the Concentration Versus Time Curve [AUC (0-τ)] of Tirzepatide
Time frame · Part C: Predose, 8 hours (h) (day (D)1), 24h (D2), 48h (D3),72h (D4), predose (D8), predose (D15), 8h (D15), 24h (D16), 48h (D17), 72h (D18), predose (D22), 8h (D22), 24h (D23), 48h (D24), 72h (D25), D57 and >= D96 postdose
Registry description
PK Part C: Area under the concentration versus time curve during one dosing interval (168 hours) \[AUC (0-τ)\] of tirzepatide.
PK Part C: Maximum Observed Drug Concentration (Cmax) of Tirzepatide
Time frame · Part C: Predose, 8 hours (h) (day (D)1), 24h (D2), 48h (D3),72h (D4), predose (D8), predose (D15), 8h (D15), 24h (D16), 48h (D17), 72h (D18), predose (D22), 8h (D22), 24h (D23), 48h (D24), 72h (D25), D57 and >= D96 postdose
Registry description
PK Part C: Maximum observed plasma drug concentration (Cmax) of tirzepatide.
PK Part D: Area Under the Concentration Versus Time Curve [AUC (0-∞)] of Tirzepatide
Time frame · Part D: Predose, 0.08 hours (h), 0.16h, 0.5h, 1h, 2h, 4h, 8h, 12h, 24h, 36h, 48h, 72h, 96h, 120h, 144h, 168h, 336h, 816-864h and >= 70 days postdose
Registry description
PK Part D: Area under the concentration versus time curve \[AUC (0-∞)\] of tirzepatide.

Posted results

Values are shown as posted at ClinicalTrials.gov, with their units. PepBank has not converted, pooled or compared them.

Primary outcome results

Primary outcomeGeometric mean· Part A: Predose, 8, 12, 24, 48, 72, 96, 120, 144, 168, 336, 480, 816-864 hours postdose

Pharmacokinetics (PK) Part A: Area Under the Concentration Versus Time Curve [AUC (0-∞)] of Tirzepatide

Group	Value (nanogramshours per milliliter(nghr/mL))	Spread
5 mg Tirzepatide SC (Lyophilized)-Part A	113000	19
5 mg Tirzepatide SC (Solution)-Part A	109000	17

Primary outcomeGeometric mean· Part A: Predose, 8, 12, 24, 48, 72, 96, 120, 144, 168, 336, 480 and 816-864 hours postdose

PK Part A: Maximum Observed Drug Concentration (Cmax) of Tirzepatide

Group	Value (nanograms per milliliter (ng/mL))	Spread
5 mg Tirzepatide SC (Lyophilized)-Part A	524	27
5 mg Tirzepatide SC (Solution)-Part A	575	22

Primary outcomeGeometric mean· Part B: Predose, 0.08 hours (h), 0.16h, 0.5h, 1h, 2h, 4h, 8h, 12h, 24h, 36h, 48h, 72h, 96h, 120h, 144h, 168h, 336h, 816h-864h and >=70 days post dose

PK Part B: Area Under the Concentration Versus Time Curve [AUC (0-∞)] of Tirzepatide

Group	Value (ng*hr/mL)	Spread
0.5 mg Tirzepatide IV-Part B	6680	26

Secondary and other outcome results(3)

Secondary outcomeGeometric mean· Part C: Predose, 8 hours (h) (day (D)1), 24h (D2), 48h (D3),72h (D4), predose (D8), predose (D15), 8h (D15), 24h (D16), 48h (D17), 72h (D18), predose (D22), 8h (D22), 24h (D23), 48h (D24), 72h (D25), D57 and >= D96 postdose

PK Part C: Area Under the Concentration Versus Time Curve [AUC (0-τ)] of Tirzepatide

Group	Value (ng*hr/mL)	Spread
5 mg Tirzepatide SC-Part C	68900	19
7.5 mg Tirzepatide SC-Part C	149000	26
10 mg Tirzepatide SC-Part C	not posted	–

PK Part C: Maximum Observed Drug Concentration (Cmax) of Tirzepatide

Group	Value (ng/mL)	Spread
5 mg Tirzepatide SC-Part C	663	23
7.5 mg LY3298176 SC-Part C	1270	24
10 mg Tirzepatide SC-Part C	1900	24

Secondary outcomeGeometric mean· Part D: Predose, 0.08 hours (h), 0.16h, 0.5h, 1h, 2h, 4h, 8h, 12h, 24h, 36h, 48h, 72h, 96h, 120h, 144h, 168h, 336h, 816-864h and >= 70 days postdose

PK Part D: Area Under the Concentration Versus Time Curve [AUC (0-∞)] of Tirzepatide

Group	Value (ng*hr/mL)	Spread
0.5 mg Tirzepatide Bolus IV-Part D	14000	16

Adverse events, as posted

Adverse events as posted: participants affected out of participants at risk, by group
Group	Deaths	Serious events	Other events
5 mg Tirzepatide SC (Lyophilized)-Part AParticipants received 5 mg of tirzepatide SC lyophilized formulation.	0 / 20	0 / 20	9 / 20
5 mg Tirzepatide SC (Solution)-Part AParticipants received 5 mg of tirzepatide SC solution formulation.	0 / 20	0 / 20	5 / 20
0.5 mg Tirzepatide IV-Part BParticipants received IV infusion of a single 0.5 mg dose of tirzepatide solution formulation.	0 / 8	0 / 8	1 / 8
Placebo SC-Part CParticipants received SC injection of placebo.	0 / 4	0 / 4	1 / 4
5 mg Tirzepatide SC, First-Part CParticipants received 5 mg of tirzepatide subcutaneous solution formulation on day 1 (week 1).	0 / 12	0 / 12	4 / 12
5 mg Tirzepatide SC, Second Dose-Part CParticipants received 5 mg of tirzepatide subcutaneous solution formulation on day 8 (Week 2).	0 / 12	0 / 12	2 / 12
7.5 mg LY3298176 SC-Part CParticipants received 7.5 mg of tirzepatide subcutaneous solution formulation on day 15 (week 3).	0 / 12	0 / 12	6 / 12
10 mg Tirzepatide SC-Part CParticipants received 10 mg of tirzepatide subcutaneous solution formulation on day 22 (week 4).	0 / 11	0 / 11	4 / 11
0.5 mg Tirzepatide Bolus IV-Part DParticipants received IV bolus of 0.5 mg tirzepatide lyophilized formulation.	0 / 8	0 / 8	3 / 8

Each cell reads participants affected / participants at risk, as the registry posted them.

Registry data comes from ClinicalTrials.gov. Study results come from studies, not from the registry. How PepBank works

Studies0

Studies that cite this trial.

No study cites this trial.

Eligibility

Who could join, as posted.

Sex: All
Age: from 18 Years up to 70 Years
Healthy volunteers: Accepted

Inclusion and exclusion criteria, as posted

Inclusion Criteria: * Overtly healthy males or females, as determined by medical history and physical examination * Male participants: agree to use an effective method of contraception for the duration of the study and for 3 months following the last dose of investigational product * Female participants: not of childbearing potential due to surgical sterilization (hysterectomy or bilateral oophorectomy or tubal ligation) or menopause. Women with an intact uterus are deemed postmenopausal if they are greater than or equal to (≥)45 years old and have not taken hormones or oral contraceptives within the last year and had cessation of menses for at least 1 year. Or, have had at least 6 months of amenorrhea with follicle-stimulating hormone levels consistent with a postmenopausal state * Have a body mass index of 18.5 to 32.0 kilograms per meter squared (kg/m²) inclusive Exclusion Criteria: * Currently enrolled in a clinical trial involving an investigational product or any other type of medical research judged not to be scientifically or medically compatible with this study * Received treatment with a drug that has not received regulatory approval for any indication within 30 days of screening * Have a history of heart block, or a pulse rate (PR) interval greater than (\>)200 milliseconds (msec), or any abnormality in the 12-lead electrocardiogram (ECG) at screening that, in the opinion of the investigator, increases the risks associated with participating in the study * Have a significant history of or current cardiovascular (myocardial infarction, congestive heart failure, cerebrovascular accident, venous thromboembolism, etc.), respiratory, hepatic, renal, gastrointestinal (GI), endocrine, hematological (including history of thrombocytopenia), or neurological disorders capable of significantly altering the absorption, metabolism, or elimination of drugs, or of constituting a risk when taking the study medication, or interfering with the interpretation of data

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