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MethemoglobinemiaPhase 1NCT02478281

Safety, Tolerability, and Pharmacokinetic Study of Methylene Blue Following a 1 mg/kg Intravenous Dose in Healthy Adults

A Phase 1 study testing Methylene Blue in people with Methemoglobinemia and Congenital Methemoglobinemia, run by American Regent, Inc..

Completed

Finished. The study has ended and is not enrolling. Results may be posted on the official record.

Official record
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Trial 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. Read more about this study

Who is it for?
Ages 18 to 60 yearsHealthy volunteers can take part
What is being tested?
Methylene Blue
Type of treatment
Injection or infusion
Could I receive a placebo?
No, everyone receives an active treatment
How many people
12 participants
Where
No sites listed yet
Study dates
Oct 2012to Mar 2013
Phase
Phase 1
Are there results?
Yes, posted in the registrySummary in the doctors' view

Key requirements

Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.

  • Ages 18 to 60 years
  • All sexes
  • Healthy volunteers accepted
  • Adult

Who may be able to join

  • 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;
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  • 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 < 40 mIU/mL, if they are able to provide documentation of FSH levels 40 mIU/mL before initiation of hormone replacement therapy.
  • Males must use condom with spermicide when engaged in sexual activity and must agree to refrain from sperm donation from check-in through 90 days postdose.
  • Willing to answer inclusion and exclusion criteria questionnaire at check-in.
  • Give voluntary written informed consent to participate in the study.
  • Be able to comply with the protocol and the assessments therein.

Who cannot join

  • History or presence of significant cardiovascular, pulmonary, hepatic, renal, hematological, gastrointestinal, endocrine, immunologic, dermatologic, neurological, or psychiatric disease in the opinion of the PI.
  • History or presence of alcoholism within the past 2 years.
  • History or presence of drug abuse within the past 2 years.
  • History or presence of hypersensitivity or idiosyncratic reaction to Methylene Blue.
  • History or presence of Glucose-6-Phosphate Dehydrogenase (G6PD) dehydrogenase deficiency, retinopathy, blood disorder, myasthenia gravis, psoriasis, epilepsy, clinically significant allergies (except for mild forms of hay fever), or any other clinically significant medical condition, which in the opinion of the PI, might interfere with study participation.
  • History or laboratory evidence of renal insufficiency.
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  • Any screening laboratory test with clinically significant abnormalities in the opinion of the PI (including cell blood count, creatinine, or liver function tests).
  • Have used any drug that acts as a serotonin reuptake inhibitor (SRIs) e.g. selective serotonin reuptake inhibitors (SSRIs), tricyclic antidepressants (TCAs), norepinephrine-dopamine reuptake inhibitors (NDRIs), triptans, or ergot alkaloids within 30 days (or 5 half-lives of the compound, whichever is longer) prior to study drug dosing.
  • Female subjects who are pregnant or lactating, or female subjects who are likely to become pregnant during the study.
  • Had positive results for the urine drug/alcohol screen at screening or check-in.
  • Had positive results at screening for HIV, HBsAg, or hepatitis C virus (HCV).
  • Seated blood pressure is less than 90/40 mmHg or greater than 140/90 mmHg at screening.
  • Heart rate is lower than 40 bpm or higher than 99 bpm at screening.
  • QTc interval is >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.

About this study

Official title: A One-Period, Single-Dose, Safety, Tolerability, and Pharmacokinetic Study of Methylene Blue Injection United States Pharmacopeia (USP) Following a 1 mg/kg Intravenous Dose in Healthy Adult Volunteers

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.

Read the detailed description

This is an open-label, single-center, one-arm, safety, tolerability, and PK study in healthy male and female volunteers of Methylene Blue Injection, USP. Following an overnight fast, twelve healthy adult male and female volunteers will receive a single dose of study drug at a dose of 1 mg/kg solution per kg given intravenously over a period of 5 minutes followed by serial venous blood sampling at 0.042, 0.083, 0.167, 0.25, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 16, 36, 48, and 72 hours postdose.

Being tested
Methylene Blue
Medical subject headings
Methemoglobinemia, Congenital Methemoglobinemia

What participants receive

What participants receive. In a randomised study each person is assigned to one group by chance.

  • Methylene BlueDrug

Study groups in NCT02478281
Study groupRoleWhat they receive
Methylene Blue Injection, United States Pharmacopeia (USP)ExperimentalSingle dose of Methylene Blue Injection, USP at a dose of 1 mg/kg solution per kg given intravenously over a period of approximately 5 minutes.
Receives: Drug: Methylene Blue

What is being measured

The primary outcome is the main question the study is designed to answer.

  1. Area Under the Curve (AUC) From Time Zero to the Time of Last Quantifiable Concentration (AUC 0-t)

    The AUC is a measure of systemic drug exposure, which is obtained by collecting a series of blood samples and measuring the concentrations of drug in each sample; AUC 0-t is defined as AUC from time 0 to the last data point

    Measured: pre-dose, 0.042, 0.083, 0.167, 0.25, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 16, 36, 48, and 72 hours post-dose

  2. Area Under the Curve From Time Zero Extrapolated to Infinity (AUC 0-∞)

    The AUC is a measure of systemic drug exposure, which is obtained by collecting a series of blood samples and measuring the concentrations of drug in each sample. AUC 0-∞ is defined as area under the concentration vs. time curve from zero to infinity.

    Measured: pre-dose, 0.042, 0.083, 0.167, 0.25, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 16, 36, 48, and 72 hours post-dose

  3. The Percent of Extrapolated Area Under the Curve (AUC%Extrap)

    The AUC%extrap refers to the fraction of the total AUC that is due to the extrapolated AUC

    Measured: pre-dose, 0.042, 0.083, 0.167, 0.25, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 16, 36, 48, and 72 hours post-dose

  4. Area Under the Curve Ratio (AUCR)

    AUCR refers to the ratio of AUC 0-t to AUC 0-∞.

    Measured: pre-dose, 0.042, 0.083, 0.167, 0.25, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 16, 36, 48, and 72 hours post-dose

  5. Total Body Clearance (CL)

    CL refers to the Dose/AUC 0-∞

    Measured: pre-dose, 0.042, 0.083, 0.167, 0.25, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 16, 36, 48, and 72 hours post-dose

  6. Maximum Measured Plasma Concentration (Cmax)

    Cmax refers to the highest measured drug concentration which is obtained by collecting a series of blood samples and measuring the concentrations of drug in each sample.

    Measured: pre-dose, 0.042, 0.083, 0.167, 0.25, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 16, 36, 48, and 72 hours post-dose

  7. Time to Maximum Plasma Concentration (Tmax)

    Tmax refers to the time it takes for a drug to reach maximum concentration

    Measured: pre-dose, 0.042, 0.083, 0.167, 0.25, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 16, 36, 48, and 72 hours post-dose

  8. Terminal Elimination Half-life (T1/2)

    T1/2 refers to the time taken for concentration of a drug to decrease from its maximum concentration to half of Cmax

    Measured: pre-dose, 0.042, 0.083, 0.167, 0.25, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 16, 36, 48, and 72 hours post-dose

  9. Terminal Elimination Rate Constant (Lambda Z)

    Lambda Z refers to the terminal elimination phase for drug plasma concentration vs. time data

    Measured: pre-dose, 0.042, 0.083, 0.167, 0.25, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 16, 36, 48, and 72 hours post-dose

  10. Volume of Distribution (Vz) Based on Terminal Phase

    Vz refers to the ratio of amount of drug in a body (dose) to concentration of the drug that is measured in blood, plasma, and un-bound in interstitial fluid.

    Measured: pre-dose, 0.042, 0.083, 0.167, 0.25, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 16, 36, 48, and 72 hours post-dose

  11. Mean Residence Time (MRT)

    MRT refers to the average amount of time that a drug molecule spends in the body before being removed

    Measured: pre-dose, 0.042, 0.083, 0.167, 0.25, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 16, 36, 48, and 72 hours post-dose

Timeline

From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.

  1. First posted23 Jun 2015 (estimated)
  2. Study startOct 2012
  3. Primary completionOct 2012
  4. Study completionMar 2013

Resources

More details

For doctors and researchers: how the study is designed, who runs it, and its registry IDs.

Study design
Study type
Interventional
Phase
Phase 1
Primary purpose
Treatment
Allocation
Not applicable
Intervention model
Single group
Masking
None (open label)
Enrolment
12 participants (actual)
IDs, dates and publications
ClinicalTrials.gov ID
NCT02478281
Sponsor's protocol ID
1MBL12002
Status last verified
Jan 2018
First submitted
28 Apr 2015
Last updated
5 Jun 2025
Data monitoring committee
No

Questions about this trial

What is this clinical trial studying?

A Phase 1 study testing Methylene Blue in people with Methemoglobinemia and Congenital Methemoglobinemia, run by American Regent, Inc..

The full registered description is in the About this study section and the official record.

Who may be eligible to take part?

The sponsor lists 13 inclusion and 19 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.

Is this clinical trial currently recruiting?

The record says: finished, as of the sponsor's last update on 5 Jun 2025. Status can change between updates, so confirm with the study contact before making plans.

What are the possible benefits and risks?

They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.

What does this phase mean?

Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.

Not every study follows the same path, and some studies (observational studies, device studies) have no phase.

Are results available for this study?

Yes. Results are posted in the registry (first posted 5 Jun 2025). A summary is in the For doctors view, and the full results are on ClinicalTrials.gov.

How can a doctor refer a patient or contact the research team?

The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.

What does the primary outcome measure?

Area Under the Curve (AUC) From Time Zero to the Time of Last Quantifiable Concentration (AUC 0-t) (time frame: pre-dose, 0.042, 0.083, 0.167, 0.25, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 16, 36, 48, and 72 hours post-dose). The study lists 11 primary outcomes in all. It is what the study was designed to measure, not a finding.

Where can I read the original study information?
Does a listing mean the treatment is approved or proven to work?

No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.

How often is this information updated?

AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 5 Jun 2025.

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