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CompletedNCT03667547Updated Oct 2, 2019Results posted

Safety, Tolerability, and Pharmacokinetics of Raltegravir (MK-0518) in Healthy Japanese Male Participants (MK-0518-851)

A Phase 4 interventional study of Raltegravir in Human Immunodeficiency Virus (HIV) Infection, sponsored by Merck Sharp & Dohme LLC. Completed at 1 site in Japan. Open to male participants aged 20 Years to 45 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2019-10-02.

Sponsored by Merck Sharp & Dohme LLC (part of Merck & Co., Inc) · Phase 4, Interventional, and Treatment

Phase
Phase 4
Study type
Interventional
Enrollment
12
Allocation
Not applicable
Ages
20 Years to 45 Years
Sex
Male
01

Study summary

This study is designed to evaluate safety, tolerability, and pharmacokinetics of a single 1200-mg dose of raltegravir (MK-0518, ISENTRESS®) in healthy Japanese male participants.

02

Conditions studied

  • Human Immunodeficiency Virus (HIV) Infection
03

In context

Acquired Immunodeficiency Syndrome

2,099 studies on the registry are indexed under Acquired Immunodeficiency Syndrome; 273 are open to participants now.

This study's enrollment of 12 is below the median of 104 across 1,590 interventional studies indexed under Acquired Immunodeficiency Syndrome.

Browse Acquired Immunodeficiency Syndrome studies →

Lead sponsor

Merck Sharp & Dohme LLC is the lead sponsor of 2,160 studies on the registry; 134 are open to participants now.

Of its 497 completed or terminated interventional studies of FDA-regulated products, 369 (74%) have results posted.

Browse Merck Sharp & Dohme LLC studies →All Merck & Co., Inc studies →

Counted across the registry records on this site, refreshed daily.

04

Who can participate

Ages eligible
20 Years to 45 Years
Sexes eligible
Male
Accepts healthy volunteers
Yes

Go through the criteria one by one — yes, no or not sure — and take the list to your doctor or the study team. Kept in this browser only.

Inclusion criteria

  • Japanese male in good health
  • Body mass index (BMI) between 18.5 and 32.0 kg/m\^2
  • Nonsmoker and has not used nicotine-containing products for over 3 months at the time of screening test.

Exclusion criteria

Exclusion Criteria:

  • History of clinically significant endocrine, gastrointestinal, cardiovascular, hematological, hepatic, immunological, renal, respiratory, genitourinary, or neurological (including cerebrovascular stroke and epilepsy) abnormalities or diseases
  • Significant emotional problem at the time of screening test or suspected to occur during the conduct of the study, or has a history of clinically significant psychiatric disorder within the last 5 years
  • History of malignancy
  • History of clinically significant allergies to multiple antigens or severe allergies (e.g., food, drug, and latex [natural rubber] allergies), or has had an anaphylactic reaction or significant intolerability (e.g., systemic allergic reaction) to prescription or non-prescription drugs or food
  • Positive for hepatitis B virus surface antigen, hepatitis C virus antibodies, syphilis, or HIV antigen or antibody on the screening test
  • Had surgery or donated or lost blood within 4 weeks prior to the screening test
  • Participated in another study (clinical trial) within 4 months prior to the screening test
  • Consumes greater than 3 glasses of alcoholic beverages (definition of 1 glass: 354 mL for beer, 118 mL for wine, 29.5 mL for distilled spirits) per day
  • Consumes greater than 6 servings (definition of 1 serving: equivalent to 120 mg of caffeine) of coffee, tea, cola, energy drinks, or other caffeinated beverages per day
  • Regular user of cannabis, any illicit drugs, or has a history of drug or alcohol abuse within 2 years at the time of the screening test. Participants must have a negative predose urine drug screen
  • Unable to consent to refrain from the consumption of citrus beverages and foods (e.g., grapefruits) beginning 2 weeks prior to administration of the study drug until the end of post-study examination, and the consumption of all fruit beverages and foods for 24 hours predose and after dosing
  • Is or has an immediate family member (e.g., spouse, parent/legal guardian, sibling, or child) who is study site or Sponsor staff directly involved with this study.
05

Study design

Phase
Phase 4
Primary purpose
Treatment
Allocation
Not applicable
Intervention model
Single group
Masking
None (open label)
Enrollment
12 participants (actual)

Study arms

  • Experimental
    Raltegravir

    Participants will receive a single oral dose of raltegravir 1200 mg (600 mg tablet X 2) in a fasted state on Day 0 and will be followed up to 2 weeks

    Drug: Raltegravir

Interventions

  • DrugRaltegravir

    Raltegravir 600 mg tablet

    Also known as: MK-0518, ISENTRESS®

06

What researchers measure

Primary outcomes

  1. Number of Participants With an Adverse Event (AE)

    An AE is any untoward medical occurrence in a participant, temporally associated with the use of a study drug, whether or not considered related to the study drug. The number of participants with an AE was reported.

    Time frame: Up to Day 14 after dosing

  2. Number of Participants Discontinued From the Study Due to an AE

    An AE is any untoward medical occurrence in a participant, temporally associated with the use of a study drug, whether or not considered related to the study drug. The number of participants discontinued from the study due to an AE was reported.

    Time frame: Up to Day 14 after dosing

  3. Number of Participants With a Serious Adverse Event (SAE)

    A SAE is an AE that results in death, is life-threatening, requires or prolongs an existing hospitalization, results in significant disability or incapacity, is a congenital anomaly or birth defect, is another medically important event, is a new cancer, or is an overdose. The number of participants with an SAE was reported.

    Time frame: Up to Day 14 after dosing

  4. Number of Participants With a Drug-related AE

    The number of participants with a drug-related AE was reported. Causality was be determined by the investigator.

    Time frame: Up to Day 14 after dosing

Secondary outcomes

  1. Area Under the Concentration-Time Curve Up to Infinity (AUC0-∞) of Plasma Raltegravir

    Blood samples were collected from pre-dose up to 48 hours post-dose in order to measure the concentration of plasma raltegravir. Values below the lower limit of quantitation were replaced with 0. Area under the concentration-time curve from time zero extrapolated to infinity (AUC0-∞) of plasma raltegravir was calculated based on natural log-transformed values.

    Time frame: Predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, and 48 hours after dosing

  2. Maximum Plasma Concentration (Cmax) of Raltegravir

    Blood samples were collected from pre-dose up to 48 hours post-dose in order to measure the concentration of plasma raltegravir. Values below the lower limit of quantitation were replaced with 0. Maximum plasma concentration (Cmax) of raltegravir was calculated based on natural log-transformed values.

    Time frame: Predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, and 48 hours after dosing

  3. Plasma Concentration of Raltegravir at 24 Hours After Dosing (C24)

    Blood samples were collected at 24 hours post-dose in order to measure the concentration of plasma raltegravir. Values below the lower limit of quantitation were replaced with 0. The plasma concentration of raltegravir at 24 hours after dosing (C24) was calculated based on natural log-transformed values.

    Time frame: 24 hours after dosing

  4. Time of Maximum Plasma Concentration (Tmax) of Raltegravir

    Blood samples were collected from pre-dose up to 48 hours post-dose in order to measure the concentration of plasma raltegravir. Values below the lower limit of quantitation were replaced with 0. The time at which Cmax of plasma raltegravir is achieved (Tmax) was reported.

    Time frame: Predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, and 48 hours after dosing

  5. Apparent Plasma Half-life (t1/2) of Raltegravir

    Blood samples were collected from pre-dose up to 48 hours post-dose in order to measure the concentration of plasma raltegravir. Values below the lower limit of quantitation were replaced with 0. The apparent plasma half-life (t1/2) of raltegravir was reported.

    Time frame: Predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, and 48 hours after dosing

  6. Apparent Total Plasma Clearance (CL/F) of Raltegravir

    Blood samples were collected from pre-dose up to 48 hours post-dose in order to measure the concentration of plasma raltegravir. Values below the lower limit of quantitation were replaced with 0. The apparent total plasma clearance of raltegravir after oral dosing (CL/F) was reported.

    Time frame: Predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, and 48 hours after dosing

  7. Apparent Volume of Distribution (Vz/F) of Raltegravir

    Blood samples were collected from pre-dose up to 48 hours post-dose in order to measure the concentration of plasma raltegravir. Values below the lower limit of quantitation were replaced with 0. The apparent volume of distribution of raltegravir during the terminal phase (Vz/F) was reported.

    Time frame: Predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, and 48 hours after dosing

07

Results

Posted Oct 2, 2019

Participant flow

Participant flow — Overall Study
MilestoneRaltegravir
Started12
Completed12
Not completed0

Outcome measures

PrimaryNumber of Participants With an Adverse Event (AE)

An AE is any untoward medical occurrence in a participant, temporally associated with the use of a study drug, whether or not considered related to the study drug. The number of participants with an AE was reported.

Time frame:
Up to Day 14 after dosing
Reported as:
Count of participants · Participants
Number of Participants With an Adverse Event (AE)
ParticipantsRaltegravir
Number of Participants With an Adverse Event (AE)0
PrimaryNumber of Participants Discontinued From the Study Due to an AE

An AE is any untoward medical occurrence in a participant, temporally associated with the use of a study drug, whether or not considered related to the study drug. The number of participants discontinued from the study due to an AE was reported.

Time frame:
Up to Day 14 after dosing
Reported as:
Count of participants · Participants
Number of Participants Discontinued From the Study Due to an AE
ParticipantsRaltegravir
Number of Participants Discontinued From the Study Due to an AE0
PrimaryNumber of Participants With a Serious Adverse Event (SAE)

A SAE is an AE that results in death, is life-threatening, requires or prolongs an existing hospitalization, results in significant disability or incapacity, is a congenital anomaly or birth defect, is another medically important event, is a new cancer, or is an overdose. The number of participants with an SAE was reported.

Time frame:
Up to Day 14 after dosing
Reported as:
Count of participants · Participants
Number of Participants With a Serious Adverse Event (SAE)
ParticipantsRaltegravir
Number of Participants With a Serious Adverse Event (SAE)0
PrimaryNumber of Participants With a Drug-related AE

The number of participants with a drug-related AE was reported. Causality was be determined by the investigator.

Time frame:
Up to Day 14 after dosing
Reported as:
Count of participants · Participants
Number of Participants With a Drug-related AE
ParticipantsRaltegravir
Number of Participants With a Drug-related AE0
SecondaryArea Under the Concentration-Time Curve Up to Infinity (AUC0-∞) of Plasma Raltegravir

Blood samples were collected from pre-dose up to 48 hours post-dose in order to measure the concentration of plasma raltegravir. Values below the lower limit of quantitation were replaced with 0. Area under the concentration-time curve from time zero extrapolated to infinity (AUC0-∞) of plasma raltegravir was calculated based on natural log-transformed values.

Time frame:
Predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, and 48 hours after dosing
Reported as:
Geometric mean · (μM•hr)
Area Under the Concentration-Time Curve Up to Infinity (AUC0-∞) of Plasma Raltegravir
(μM•hr)Raltegravir
Area Under the Concentration-Time Curve Up to Infinity (AUC0-∞) of Plasma Raltegravir62.8 (41.8 to 94.4)
SecondaryMaximum Plasma Concentration (Cmax) of Raltegravir

Blood samples were collected from pre-dose up to 48 hours post-dose in order to measure the concentration of plasma raltegravir. Values below the lower limit of quantitation were replaced with 0. Maximum plasma concentration (Cmax) of raltegravir was calculated based on natural log-transformed values.

Time frame:
Predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, and 48 hours after dosing
Reported as:
Geometric mean · nM
Maximum Plasma Concentration (Cmax) of Raltegravir
nMRaltegravir
Maximum Plasma Concentration (Cmax) of Raltegravir20163 (12211 to 33291)
SecondaryPlasma Concentration of Raltegravir at 24 Hours After Dosing (C24)

Blood samples were collected at 24 hours post-dose in order to measure the concentration of plasma raltegravir. Values below the lower limit of quantitation were replaced with 0. The plasma concentration of raltegravir at 24 hours after dosing (C24) was calculated based on natural log-transformed values.

Time frame:
24 hours after dosing
Reported as:
Geometric mean · nM
Plasma Concentration of Raltegravir at 24 Hours After Dosing (C24)
nMRaltegravir
Plasma Concentration of Raltegravir at 24 Hours After Dosing (C24)74.5 (53.9 to 103)
SecondaryTime of Maximum Plasma Concentration (Tmax) of Raltegravir

Blood samples were collected from pre-dose up to 48 hours post-dose in order to measure the concentration of plasma raltegravir. Values below the lower limit of quantitation were replaced with 0. The time at which Cmax of plasma raltegravir is achieved (Tmax) was reported.

Time frame:
Predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, and 48 hours after dosing
Reported as:
Median · Hours
Time of Maximum Plasma Concentration (Tmax) of Raltegravir
HoursRaltegravir
Time of Maximum Plasma Concentration (Tmax) of Raltegravir1.75 (0.5 to 4.0)
SecondaryApparent Plasma Half-life (t1/2) of Raltegravir

Blood samples were collected from pre-dose up to 48 hours post-dose in order to measure the concentration of plasma raltegravir. Values below the lower limit of quantitation were replaced with 0. The apparent plasma half-life (t1/2) of raltegravir was reported.

Time frame:
Predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, and 48 hours after dosing
Reported as:
Geometric mean · Hours
Apparent Plasma Half-life (t1/2) of Raltegravir
HoursRaltegravir
Apparent Plasma Half-life (t1/2) of Raltegravir7.50 ± 34.6
SecondaryApparent Total Plasma Clearance (CL/F) of Raltegravir

Blood samples were collected from pre-dose up to 48 hours post-dose in order to measure the concentration of plasma raltegravir. Values below the lower limit of quantitation were replaced with 0. The apparent total plasma clearance of raltegravir after oral dosing (CL/F) was reported.

Time frame:
Predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, and 48 hours after dosing
Reported as:
Geometric mean · L/hr
Apparent Total Plasma Clearance (CL/F) of Raltegravir
L/hrRaltegravir
Apparent Total Plasma Clearance (CL/F) of Raltegravir39.6 ± 71.3
SecondaryApparent Volume of Distribution (Vz/F) of Raltegravir

Blood samples were collected from pre-dose up to 48 hours post-dose in order to measure the concentration of plasma raltegravir. Values below the lower limit of quantitation were replaced with 0. The apparent volume of distribution of raltegravir during the terminal phase (Vz/F) was reported.

Time frame:
Predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, and 48 hours after dosing
Reported as:
Geometric mean · Liters
Apparent Volume of Distribution (Vz/F) of Raltegravir
LitersRaltegravir
Apparent Volume of Distribution (Vz/F) of Raltegravir429 ± 81.1

Adverse events

Collected over Up to 14 days after treatment with study drug. Non-serious events are listed at a 0% frequency threshold.

Adverse event summary by group
GroupDeathsSeriousOther
Raltegravir0/12 (0%)0/12 (0%)0/12 (0%)

Baseline characteristics

Age, Continuous
Age, Continuous(Years)Raltegravir
Mean28.17 ± 4.86
Sex: Female, Male
Sex: Female, Male(Participants)Raltegravir
Female0
Male12
Ethnicity (NIH/OMB)
Ethnicity (NIH/OMB)(Participants)Raltegravir
Hispanic or Latino0
Not Hispanic or Latino12
Unknown or Not Reported0
Race (NIH/OMB)
Race (NIH/OMB)(Participants)Raltegravir
American Indian or Alaska Native0
Asian12
Native Hawaiian or Other Pacific Islander0
Black or African American0
White0
More than one race0
Unknown or Not Reported0
08

Study locations

1 site
  • Medical Corporation Houeikai Sekino Clinical Pharmacology Clinic ( Site 0001)
    Tokyo, 171-0014, Japan
09

References and documents

Study documents

  • Protocol and statistical analysis plan · Jul 10, 2018

Documents are hosted by the registry — open the source record to download them.

Individual participant data

Plan to share: Yes — http://engagezone.msd.com/doc/ProcedureAccessClinicalTrialData.pdf

Data sharing details ↗ · engagezone.msd.com

10

Timeline

Tracking since Sep 25, 2026
ElapsedEstimatedEstimated, not yet reachedSimilar studies: half by the dot; the band is the middle halfHalf of similar studies reached it by the dot; the band is the middle half, from a quarter to three quarters

Ran from Sep 2018 to primary completion in Oct 2018, 0 months.

Results were first posted in Oct 2019, 11 months after primary completion.

Of 55 phase 4 interventional studies under Acquired Immunodeficiency Syndrome, half reached primary completion within 29 months of starting (the median), counting those still running; a quarter within 22 and three quarters within 58. This study's 0 months is below that.

How these figures are worked out, and which studies are left out of them.

Registered
Sep 10, 2018
First posted
Sep 12, 2018
StartActual
Sep 27, 2018
Primary completionActual
Oct 23, 2018
CompletionActual
Oct 23, 2018
Results first posted
Oct 2, 2019
Last update
Oct 2, 2019
What these dates mean
Start.
When the first participant enrolled; while estimated, when the study expects to open to recruitment.
Primary completion.
When the last participant was examined or treated to collect data for the study's main question, its primary outcome. A study that stopped early gives the date its data collection stopped.
Completion.
When the last participant's last visit took place, for every outcome, secondary ones and side effects included: the end of the study. Often later than primary completion, sometimes the same day.
Actual and Est.
Actual means the registry says the date has happened. Est. (estimated) is a date the sponsor plans or expects. It can still move, and the sponsor is expected to change it to actual once it has passed.
No changes since tracking began. The registry record was last updated on Oct 2, 2019, before this site started recording changes on Sep 25, 2026. Its history is on ClinicalTrials.gov ↗
11

Registry details

Key details

Study ID
NCT03667547
Lead sponsor
Merck Sharp & Dohme LLC
Responsible party
Sponsor
First posted
Sep 12, 2018
Start date
Sep 27, 2018
Primary completion
Oct 23, 2018
Completion
Oct 23, 2018
Results posted
Oct 2, 2019
Last update
Oct 2, 2019

Study contacts

Medical Director
study director · Merck Sharp & Dohme LLC

Oversight

Data monitoring committee
No
FDA-regulated drug
No
FDA-regulated device
No
View the source record on ClinicalTrials.gov ↗

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