Bioequivalence of An Oral Mercaptopurine Suspension 100 Mg / 5 Ml Versus Tablet in Healthy Male Subjects Under Fasting Conditions

This study has been completed.
Sponsor:
Information provided by (Responsible Party):
Nova Laboratories Limited
ClinicalTrials.gov Identifier:
NCT01697020
First received: September 20, 2012
Last updated: November 28, 2013
Last verified: November 2013

September 20, 2012
November 28, 2013
September 2012
November 2012   (final data collection date for primary outcome measure)
Bioequivalence [ Time Frame: Within 7 days ] [ Designated as safety issue: No ]

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-∞)).
Same as current
Complete list of historical versions of study NCT01697020 on ClinicalTrials.gov Archive Site
Not Provided
Not Provided
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Bioequivalence of An Oral Mercaptopurine Suspension 100 Mg / 5 Ml Versus Tablet in Healthy Male Subjects Under Fasting Conditions
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

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.

Not Provided
Interventional
Phase 1
Allocation: Randomized
Endpoint Classification: Bio-equivalence Study
Intervention Model: Crossover Assignment
Masking: Open Label
Primary Purpose: Treatment
Acute Lymphoblastic Leukemia
  • Drug: Mercaptopurine 20mg/ml oral suspension
    50mg
    Other Name: Xaluprine
  • Drug: Mercaptopurine 50mg tablet
    50mg
    Other Name: Purinethol
  • Experimental: Arm 1
    Mercaptopurine 20mg/ml Oral Suspension
    Intervention: Drug: Mercaptopurine 20mg/ml oral suspension
  • Active Comparator: Arm 2
    Mercaptopurine 50mg tablets
    Intervention: Drug: Mercaptopurine 50mg tablet
Not Provided

*   Includes publications given by the data provider as well as publications identified by ClinicalTrials.gov Identifier (NCT Number) in Medline.
 
Completed
70
November 2012
November 2012   (final data collection date for primary outcome measure)

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.
Male
18 Years to 50 Years
Yes
Contact information is only displayed when the study is recruiting subjects
South Africa
 
NCT01697020
INV298
No
Nova Laboratories Limited
Nova Laboratories Limited
Not Provided
Not Provided
Nova Laboratories Limited
November 2013

ICMJE     Data element required by the International Committee of Medical Journal Editors and the World Health Organization ICTRP