Back to resultsBioequivalence of An Oral Mercaptopurine Suspension 100 Mg / 5 Ml Versus Tablet in Healthy Male Subjects Under Fasting Conditions
Primary Purpose
Acute Lymphoblastic Leukemia
Status
Completed
Phase
Phase 1
Locations
South Africa
Study Type
Interventional
Intervention
Mercaptopurine 20mg/ml oral suspension
Mercaptopurine 50mg tablet
Sponsored by
About this trial
This is an interventional treatment trial for Acute Lymphoblastic Leukemia
Eligibility Criteria
Inclusion Criteria:
- Healthy male subjects, 18 years to 50 years inclusive at time of last administration of the IMP.
- Body Mass Index (BMI) between 18.5 and 30 kg/m2.
- Body mass not less than 50 kg.
- Medical history, physical examination, standard 12-lead electrocardiogram (ECG) and laboratory investigations: Findings clinically acceptable or within laboratory reference ranges for the relevant laboratory tests, unless the investigator considers the deviation to be irrelevant for the purpose of the study.
- Non-smokers.
Exclusion Criteria:
- Current alcohol use > 21 units of alcohol per week for males.
- Regular exposure to substances of abuse (other than alcohol) within the past year.
- Use of any medication, prescribed or over-the-counter or herbal remedies, within 2 weeks prior to the first administration of IMP except if this will not affect the outcome of the study in the opinion of the investigator.
- Participation in another study with an experimental drug, where the last administration of the previous IMP was within 8 weeks before the first administration of IMP in this study.
- Treatment within the previous 3 months before the first administration of IMP with any drug with a well-defined potential for adversely affecting a major organ or system.
- A major illness during the 3 months before commencement of the screening period.
- Subjects with a deficient, low or intermediate TPMT enzyme activity by means of phenotyping.
- Subjects who participated in previous azathioprine/mercaptopurine studies within six months will be excluded.
- Relevant history or laboratory or clinical findings indicative of acute or chronic disease, likely to influence study outcome.
- Donation or loss of blood equal to or exceeding 500 mL during the 8 weeks before the first administration of IMP.
- Diagnosis of hypotension or hypertension made during the screening period or current diagnosis of hypertension.
- Resting pulse of > 100 beats per minute or < 45 beats per minute during the screening period, either supine or standing.
- Positive testing for HIV and/or Hepatitis B and/or Hepatitis C.
- Positive urine screen for drugs of abuse.
- Positive urine screen for tobacco use.
- Subjects who plan to procreate within 12 weeks after IMP administration, or not willing to practice reliable forms of contraception during the study and for at least 12 weeks after the last dose of IMP.
- Immunization using a live organism vaccine within 4 weeks prior to the first dosing of IMP.
- Any specific IMP safety concern.
Sites / Locations
- Parexel International, Bloemfontein Early Phase Clinical Unit
Arms of the Study
Arm 1
Arm 2
Arm Type
Experimental
Active Comparator
Arm Label
Arm 1
Arm 2
Arm Description
Mercaptopurine 20mg/ml Oral Suspension
Mercaptopurine 50mg tablets
Outcomes
Primary Outcome Measures
Bioequivalence
At each treatment period, pharmacokinetic blood samples will be collected through the indwelling venous cannula at the following times: pre-dose and post-dose at 0.17, 0.33, 0.5, 0.75, 1.0, 1.33, 1.67, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 6.0, 7.0, 8.0, 10.0 and 12.0 hours.
The primary outcome measures will be
Maximum observed plasma concentration (Cmax).
AUC time zero to time of the last quantifiable concentration (AUC(0-t))
Area under the plasma concentration versus time data pairs, with extrapolation to infinity (AUC(0-∞)).
Secondary Outcome Measures
Full Information
NCT ID
NCT01697020
First Posted
September 20, 2012
Last Updated
November 28, 2013
Sponsor
Nova Laboratories Limited
1. Study Identification
Unique Protocol Identification Number
NCT01697020
Brief Title
Bioequivalence of An Oral Mercaptopurine Suspension 100 Mg / 5 Ml Versus Tablet in Healthy Male Subjects Under Fasting Conditions
Official Title
A SINGLE CENTER, SINGLE-DOSE, OPEN-LABEL, RANDOMIZED, TWO-PERIOD CROSSOVER STUDY TO ASSESS THE BIOEQUIVALENCE OF AN ORAL MERCAPTOPURINE SUSPENSION 100 mg / 5 mL VERSUS AN ORAL MERCAPTOPURINE TABLET 50 mg (PURINETHOL®) IN AT LEAST 62 HEALTHY MALE SUBJECTS UNDER FASTING CONDITIONS
Study Type
Interventional
2. Study Status
Record Verification Date
November 2013
Overall Recruitment Status
Completed
Study Start Date
September 2012 (undefined)
Primary Completion Date
November 2012 (Actual)
Study Completion Date
November 2012 (Actual)
3. Sponsor/Collaborators
Responsible Party, by Official Title
Sponsor
Name of the Sponsor
Nova Laboratories Limited
4. Oversight
Data Monitoring Committee
No
5. Study Description
Brief Summary
The primary objective of this study is to determine whether the test product, mercaptopurine oral 100 mg/5 mL suspension, and the reference product, Purinethol® 50 mg tablets are bioequivalent. For this purpose the PK profile of 6-mercaptopurine (6-MP) will be compared after administration of a single dose of each of the two formulations, under fasting conditions. The secondary objective is to assess the safety and tolerability of the test product, mercaptopurine oral 100 mg/5 mL suspension.
6. Conditions and Keywords
Primary Disease or Condition Being Studied in the Trial, or the Focus of the Study
Acute Lymphoblastic Leukemia
7. Study Design
Primary Purpose
Treatment
Study Phase
Phase 1
Interventional Study Model
Crossover Assignment
Masking
None (Open Label)
Allocation
Randomized
Enrollment
70 (Actual)
8. Arms, Groups, and Interventions
Arm Title
Arm 1
Arm Type
Experimental
Arm Description
Mercaptopurine 20mg/ml Oral Suspension
Arm Title
Arm 2
Arm Type
Active Comparator
Arm Description
Mercaptopurine 50mg tablets
Intervention Type
Drug
Intervention Name(s)
Mercaptopurine 20mg/ml oral suspension
Other Intervention Name(s)
Xaluprine
Intervention Description
50mg
Intervention Type
Drug
Intervention Name(s)
Mercaptopurine 50mg tablet
Other Intervention Name(s)
Purinethol
Intervention Description
50mg
Primary Outcome Measure Information:
Title
Bioequivalence
Description
At each treatment period, pharmacokinetic blood samples will be collected through the indwelling venous cannula at the following times: pre-dose and post-dose at 0.17, 0.33, 0.5, 0.75, 1.0, 1.33, 1.67, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 6.0, 7.0, 8.0, 10.0 and 12.0 hours.
The primary outcome measures will be
Maximum observed plasma concentration (Cmax).
AUC time zero to time of the last quantifiable concentration (AUC(0-t))
Area under the plasma concentration versus time data pairs, with extrapolation to infinity (AUC(0-∞)).
Time Frame
Within 7 days
10. Eligibility
Sex
Male
Minimum Age & Unit of Time
18 Years
Maximum Age & Unit of Time
50 Years
Accepts Healthy Volunteers
Accepts Healthy Volunteers
Eligibility Criteria
Inclusion Criteria:
Healthy male subjects, 18 years to 50 years inclusive at time of last administration of the IMP.
Body Mass Index (BMI) between 18.5 and 30 kg/m2.
Body mass not less than 50 kg.
Medical history, physical examination, standard 12-lead electrocardiogram (ECG) and laboratory investigations: Findings clinically acceptable or within laboratory reference ranges for the relevant laboratory tests, unless the investigator considers the deviation to be irrelevant for the purpose of the study.
Non-smokers.
Exclusion Criteria:
Current alcohol use > 21 units of alcohol per week for males.
Regular exposure to substances of abuse (other than alcohol) within the past year.
Use of any medication, prescribed or over-the-counter or herbal remedies, within 2 weeks prior to the first administration of IMP except if this will not affect the outcome of the study in the opinion of the investigator.
Participation in another study with an experimental drug, where the last administration of the previous IMP was within 8 weeks before the first administration of IMP in this study.
Treatment within the previous 3 months before the first administration of IMP with any drug with a well-defined potential for adversely affecting a major organ or system.
A major illness during the 3 months before commencement of the screening period.
Subjects with a deficient, low or intermediate TPMT enzyme activity by means of phenotyping.
Subjects who participated in previous azathioprine/mercaptopurine studies within six months will be excluded.
Relevant history or laboratory or clinical findings indicative of acute or chronic disease, likely to influence study outcome.
Donation or loss of blood equal to or exceeding 500 mL during the 8 weeks before the first administration of IMP.
Diagnosis of hypotension or hypertension made during the screening period or current diagnosis of hypertension.
Resting pulse of > 100 beats per minute or < 45 beats per minute during the screening period, either supine or standing.
Positive testing for HIV and/or Hepatitis B and/or Hepatitis C.
Positive urine screen for drugs of abuse.
Positive urine screen for tobacco use.
Subjects who plan to procreate within 12 weeks after IMP administration, or not willing to practice reliable forms of contraception during the study and for at least 12 weeks after the last dose of IMP.
Immunization using a live organism vaccine within 4 weeks prior to the first dosing of IMP.
Any specific IMP safety concern.
Facility Information:
Facility Name
Parexel International, Bloemfontein Early Phase Clinical Unit
City
Bloemfontein
Country
South Africa
12. IPD Sharing Statement
Learn more about this trial
Bioequivalence of An Oral Mercaptopurine Suspension 100 Mg / 5 Ml Versus Tablet in Healthy Male Subjects Under Fasting Conditions
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