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Phase 3 N=69 Randomized Quadruple-blind Treatment

Comparison of the Pharmacokinetics (PK) and Pharmacodynamics (PD) Biosimilarity of Proposed Biosimilar Rapid-Acting Insulin Aspart (I004) and NovoLog After Single-Dose Subcutaneous Administration to Healthy Volunteers

Pharmacokinetics · Pharmacodynamics

Enrolled (actual)
69
Serious AEs
0.0%
Results posted
Mar 2026
Primary outcome: Primary: Maximum Serum Insulin Aspart Concentration, CIAmax — 2961.8; 2827.4 pg/mL

Study Design & Population

Study type
Interventional
Phase
Phase 3
Interventions
I004 (Drug); NovoLog (Drug)
Age
Adult, Older Adult · 18+ yrs
Sex
All
Sponsor
Amphastar Pharmaceuticals, Inc.
Primary completion
Jan 2023

Outcome Measures

OutcomeResultp-value
PRIMARY
Maximum Serum Insulin Aspart Concentration, CIAmax
2961.8; 2827.4
PRIMARY
Area Under the Curve (AUC) of Insulin Aspart Serum Concentration From Time 0 to 12 Hours Post-dose, AUCIA(0-12h)
7215.0; 6976.9
PRIMARY
Maximum Glucose Infusion Rate, Gmax
10.3; 10.3
PRIMARY
Area Under the Curve (AUC) for Glucose Infusion Rate From Time 0 to 12 Hours Post-dose, AUCG(0-12h)
1906.9; 1985.7
SECONDARY
Area Under the Curve (AUC) of Insulin Aspart Serum Concentration From Time 0 to Infinity, AUCIA(0-∞)
7374.9; 7202.7
SECONDARY
Area Under the Curve (AUC) of Insulin Aspart Serum Concentration From Time 0 to 1 Hour Post-dose, AUCIA(0-1h)
1438.9; 1496.6
SECONDARY
Area Under the Curve (AUC) of Insulin Aspart Serum Concentration From Time 0 to 2 Hours Post-dose, AUCIA(0-2h)
3886.9; 3757.0
SECONDARY
Area Under the Curve (AUC) of Insulin Aspart Serum Concentration From Time 0 to 4 Hours Post-dose, AUCIA(0-4h)
6478.7; 6204.1
SECONDARY
Area Under the Curve (AUC) of Insulin Aspart Serum Concentration From 4 to 12 Hours Post-dose, AUCIA(4-12h)
567.2; 619.8
SECONDARY
Time of Maximum Insulin Aspart Serum Concentration, tIAmax
67.5; 55.0
SECONDARY
Apparent Clearance of Insulin Aspart, CL/F
74.2; 76.3
SECONDARY
Apparent Volume of Distribution of Insulin Aspart, Vz/F
96.8; 104.1
SECONDARY
Half-life of Insulin Aspart, t1/2
53.0; 60.8
SECONDARY
Maximum Serum Human Insulin Concentration, CHImax
559.4; 563.8
SECONDARY
Area Under the Curve (AUC) of Human Insulin Serum Concentration From Time 0 to 12 Hours Post-dose, AUCHI(0-12h)
2662.7; 2634.8
SECONDARY
Time of Maximum Human Insulin Serum Concentration, tHImax
80.0; 105.0
SECONDARY
Area Under the Curve (AUC) for Glucose Infusion Rate Due to Insulin Aspart From Time 0 to 12 Hours Post-dose, AUCGA(0-12h)
1308.1; 1364.8
SECONDARY
Maximum Glucose Infusion Rate Due to Insulin Aspart, GAmax
8.1; 8.3
SECONDARY
Area Under the Curve (AUC) for Glucose Infusion Rate (GIR) From Time 0 to the Time of Last Measurable GIR, AUCG(0-last)
1906.9; 1985.7
SECONDARY
Area Under the Curve (AUC) for Glucose Infusion Rate From Time 0 to 1 Hour Post-dose, AUCG(0-1h)
115.8; 123.6
SECONDARY
Area Under the Curve (AUC) for Glucose Infusion Rate From Time 0 to 2 Hours Post-dose, AUCG(0-2h)
481.5; 501.9
SECONDARY
Area Under the Curve (AUC) for Glucose Infusion Rate From Time 0 to 4 Hours Post-dose, AUCG(0-4h)
1268.9; 1305.0
SECONDARY
Area Under the Curve (AUC) for Glucose Infusion Rate From Time 4 to 12 Hours Post-dose, AUCG(4-12h)
555.9; 589.3
SECONDARY
Last Measurable Glucose Infusion Rate, Glast
0.1; 0.0
SECONDARY
Time of Maximum Glucose Infusion Rate, tGmax
160.0; 136.0
SECONDARY
Time of Glucose Infusion Start, tGonset
22.0; 20.0
SECONDARY
Time of Last Measurable Glucose Infusion Rate, tGlast
720.0; 712.0
SECONDARY
Time to Half of Maximum Glucose Infusion Rate (Gmax) Before Gmax Is Reached, tG50%Early
76.7; 71.5
SECONDARY
Time to Half of Maximum Glucose Infusion Rate (Gmax) After Gmax Is Reached, tG50%Late
211.9; 216.2

Summary

This study is a randomized, double-blinded, two-treatment, two-period, two-sequence crossover pivotal Biosimilar study. The purpose of this study is to establish pharmacokinetic (PK) and pharmacodynamics (PD) biosimilarity of proposed biosimilar I004 and the US-approved NovoLog.

Eligibility Criteria

Inclusion Criteria

  • Upon review, agree to participate and sign informed consent.
  • Healthy male and female subjects ≥ 18 to ≤ 65 years of age.
  • Body mass index (BMI) ≥ 18.5 to ≤ 29.9 kg/m2
  • Weight ≥ 50 kg.
  • Fasting plasma glucose of 1 year post-menopausal, surgically sterile, or practicing a clinically acceptable form of birth control and confirmed by negative serum pregnancy test at Screening.

Exclusion Criteria

  • History of diabetes mellitus.
  • Resting blood pressure (BP) > 140/90 mmHg or 450 ms in men, > 470 ms in women at Screening.
  • Liver function test results of AST and/or ALT ≥ 2.5 upper normal limit (ULN)
  • Subject has a history of syncope.
  • History of any major surgery within 6 months.
  • History of any active infection, other than mild viral illness within 30 days prior to dosing.
  • History of blood clots (e.g., deep vein thrombosis or embolism) or a frequent appearance in 1st degree relatives as judged by the Investigator.
  • Known history or positive test of hepatitis B surface antigen (HBsAG), hepatitis C antibody (HCV Ab), or human immunodeficiency virus type 1 (HIV-1) or 2 (HIV-2) antibody.
  • History of alcohol abuse as judged by the Investigator within approximately 1 year. Average weekly alcohol intake > 21 units/week (males) and > 14 units/week (females) or are unwilling to stop alcohol consumption from 24 hours prior to each dosing until discharged from the clinical research unit (CRU). Positive alcohol test at Screening. (One unit of alcohol equals about 250 mL of beer or lager, one glass of wine, or 20 mL of spirits).
  • History of illicit drug abuse, including marijuana, within approximately 1 year or evidence of current use as judged by the Investigator. Positive drug test at Screening.
  • Donation or loss of > 500 mL of blood within 56 days.
  • Chronic use of over-the-counter or prescription medication within 7 or 14 days prior to dosing (apart from vitamin/mineral supplements, occasional paracetamol, or birth control methods [Desogestrel is not allowed]).
  • Unable to comply with the safety monitoring requirements of this clinical study or is considered by the investigator to be an unsuitable candidate for the study.
View full record on ClinicalTrials.gov →

Data sourced from ClinicalTrials.gov (NCT05539872). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication.

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