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

The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details. Identifier: NCT01697020
Recruitment Status : Completed
First Posted : October 2, 2012
Last Update Posted : December 2, 2013
Information provided by (Responsible Party):
Nova Laboratories Limited

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.

Condition or disease Intervention/treatment Phase
Acute Lymphoblastic Leukemia Drug: Mercaptopurine 20mg/ml oral suspension Drug: Mercaptopurine 50mg tablet Phase 1

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Study Type : Interventional  (Clinical Trial)
Actual Enrollment : 70 participants
Allocation: Randomized
Intervention Model: Crossover Assignment
Masking: None (Open Label)
Primary Purpose: Treatment
Study Start Date : September 2012
Actual Primary Completion Date : November 2012
Actual Study Completion Date : November 2012

Resource links provided by the National Library of Medicine

Arm Intervention/treatment
Experimental: Arm 1
Mercaptopurine 20mg/ml Oral Suspension
Drug: Mercaptopurine 20mg/ml oral suspension
Other Name: Xaluprine

Active Comparator: Arm 2
Mercaptopurine 50mg tablets
Drug: Mercaptopurine 50mg tablet
Other Name: Purinethol

Primary Outcome Measures :
  1. Bioequivalence [ Time Frame: Within 7 days ]

    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-∞)).

Information from the National Library of Medicine

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Ages Eligible for Study:   18 Years to 50 Years   (Adult)
Sexes Eligible for Study:   Male
Accepts Healthy Volunteers:   Yes

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.

Information from the National Library of Medicine

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.

Please refer to this study by its identifier (NCT number): NCT01697020

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South Africa
Parexel International, Bloemfontein Early Phase Clinical Unit
Bloemfontein, South Africa
Sponsors and Collaborators
Nova Laboratories Limited

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Responsible Party: Nova Laboratories Limited Identifier: NCT01697020     History of Changes
Other Study ID Numbers: INV298
First Posted: October 2, 2012    Key Record Dates
Last Update Posted: December 2, 2013
Last Verified: November 2013

Additional relevant MeSH terms:
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Precursor Cell Lymphoblastic Leukemia-Lymphoma
Leukemia, Lymphoid
Neoplasms by Histologic Type
Lymphoproliferative Disorders
Lymphatic Diseases
Immunoproliferative Disorders
Immune System Diseases
Molecular Mechanisms of Pharmacological Action
Antimetabolites, Antineoplastic
Antineoplastic Agents
Immunosuppressive Agents
Immunologic Factors
Physiological Effects of Drugs
Nucleic Acid Synthesis Inhibitors
Enzyme Inhibitors