Phase 1
N=12
Safety, Tolerability, and Pharmacokinetic Study of Methylene Blue Following a 1 mg/kg Intravenous Dose in Healthy Adults
Methemoglobinemia · Congenital Methemoglobinemia
Bottom Line
View on ClinicalTrials.gov: NCT02478281 ↗Enrolled (actual)
12
Serious AEs
0.0%
Results posted
Jun 2025
Primary outcome: Primary: Area Under the Curve (AUC) From Time Zero to the Time of Last Quantifiable Concentration (AUC 0-t) — 2600.09 ng*hr/mL
Study Design & Population
- Study type
- Interventional
- Phase
- Phase 1
- Interventions
- Methylene Blue (Drug)
- Age
- Adult · 18+ yrs
- Sex
- All
- Sponsor
- American Regent, Inc.
- Primary completion
- Oct 2012
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Area Under the Curve (AUC) From Time Zero to the Time of Last Quantifiable Concentration (AUC 0-t) |
2600.09 | — |
| PRIMARY Area Under the Curve From Time Zero Extrapolated to Infinity (AUC 0-∞) |
2967.09 | — |
| PRIMARY The Percent of Extrapolated Area Under the Curve (AUC%Extrap) |
11.72 | — |
| PRIMARY Area Under the Curve Ratio (AUCR) |
87.63 | — |
| PRIMARY Total Body Clearance (CL) |
19.02 | — |
| PRIMARY Maximum Measured Plasma Concentration (Cmax) |
457.34 | — |
| PRIMARY Time to Maximum Plasma Concentration (Tmax) |
0.217 | — |
| PRIMARY Terminal Elimination Half-life (T1/2) |
15.908 | — |
| PRIMARY Terminal Elimination Rate Constant (Lambda Z) |
0.04357 | — |
| PRIMARY Volume of Distribution (Vz) Based on Terminal Phase |
436.557 | — |
| PRIMARY Mean Residence Time (MRT) |
17.677 | — |
Summary
A Phase 1 trial to assess the single-dose safety, tolerability, and pharmacokinetic (PK) of Methylene Blue Injection, USP 1 mg/kg in healthy adult volunteers.
Eligibility Criteria
Inclusion Criteria
- Healthy adult male or female volunteers, 18-60 years of age, inclusive.
- Weigh at least 52 kg for males and 45 kg for females and within the normal range according to accepted normal values of the Body Mass Index (BMI) chart 18.5-29.9 kg/m² inclusive.
- Medically healthy with no clinically significant laboratory profiles, vital signs, or ECG's; as deemed by the PI.
- For females of childbearing potential: either be sexually inactive (abstinent) for 14 days prior to the first dose and throughout the study or be using acceptable birth control methods. Female subjects who claim to be sexually inactive, but become sexually active during the course of the study must agree to use a barrier method (e.g. condom, diaphragm)with spermicide from the time of the start of sexual activity through at least 30 days following dosing. In addition, female subjects of childbearing potential will be advised to remain sexually inactive or to keep the same birth control method for at least 30 days following dosing.
- Females of non-childbearing potential must have undergone one of the following sterilization procedures at least 6 months prior to Day 1:
- Hysteroscopic tubal ligation (with a copy of the confirmation test) and be using a barrier method (condom or diaphragm) and spermicide throughout the study;
- Bilateral tubal ligation and be using a barrier method (condom or diaphragm) and spermicide throughout the study;
- Hysterectomy;
- Bilateral oophorectomy or be postmenopausal with amenorrhea for at least 1 year prior to Day 1 and follicle stimulating hormone (FSH) serum levels ≥ 40 milli-International Units per mL (mIU/mL). Females on hormone replacement therapy may be deemed eligible for participation in the study even if their FSH levels 430 msec (males) or >450 msec (females) or deemed clinically abnormal by the PI or use of any drug or agent suspected of causing QT prolongation or torsade de pointes within 14 days (or 5 half- lives of the compound, whichever is longer) prior to study drug dosing.
- Have been on a special diet (for whatever reason) within the 28 days prior to study drug dosing, and throughout the study.
- Have made a donation of blood or had significant blood loss within 56 days prior to study drug dosing.
- Have made a plasma donation within 7 days prior to study drug dosing.
- Have received Methylene Blue within 72 hours prior to study drug dosing.
- Have participated in another clinical trial within 30 days (or 5 half-lives of the compound, whichever is longer) prior to study drug dosing.
Data sourced from ClinicalTrials.gov (NCT02478281). 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.