Mercaptopurine, known chemically as 1,7-dihydro-6 H -purine-6-thione monohydrate, is an analogue of the purine bases adenine and hypoxanthine.
Mercaptopurine tablets are indicated for maintenance therapy of acute lymphatic (lymphocytic, lymphoblastic) leukemia as part of a combination regimen. The response to this agent depends upon the particular subclassification of acute lymphatic leukemia and the age of the patient (pediatric or adult).
Mercaptopurine tablets are not effective for prophylaxis or treatment of central nervous system leukemia.
Mercaptopurine tablets are not effective in acute myelogenous leukemia, chronic lymphatic leukemia, the lymphomas (including Hodgkins Disease), or solid tumors.
Published Studies Related to Mercaptopurine
Randomized trial to compare LSA2L2-type maintenance therapy to daily 6-mercaptopurine and weekly methotrexate with vincristine and dexamethasone pulse for children with acute lymphoblastic leukemia. [2010.08]
CONCLUSIONS: There were no differences in the EFS between the different maintenance therapies in each risk group; however, grade IV liver toxicity occurred more often in the patients receiving 6-MP/MTX with VCR and DEX therapy than in patients receiving LSA2L2. (c) 2010 Wiley-Liss, Inc.
Azathioprine or 6-mercaptopurine for induction of remission in Crohn's disease. [2010.06.16]
CONCLUSIONS: Azathioprine and 6-mercaptopurine are effective therapy for inducing remission in active Crohn's disease. Adverse events were more common among patients on active therapy.
Benefits of the intermittent use of 6-mercaptopurine and methotrexate in maintenance treatment for low-risk acute lymphoblastic leukemia in children: randomized trial from the Brazilian Childhood Cooperative Group--protocol ALL-99. [2010.04.10]
PURPOSE To describe event-free survival (EFS) and toxicities in children with low-risk acute lymphoblastic leukemia (ALL) assigned to receive either continuous 6-mercaptopurine (6-MP) and weekly methotrexate (MTX) or intermittent 6-MP with intermediate-dose MTX, as maintenance treatment... Boys treated with the intermittent schedule had significantly better EFS.
Oral 6-mercaptopurine versus oral 6-thioguanine and veno-occlusive disease in children with standard-risk acute lymphoblastic leukemia: report of the Children's Oncology Group CCG-1952 clinical trial. [2010.04.08]
The Children's Cancer Group 1952 (CCG-1952) clinical trial studied the substitution of oral 6-thioguanine (TG) for 6-mercaptopurine (MP) and triple intrathecal therapy (ITT) for intrathecal methotrexate (IT-MTX) in the treatment of standard-risk acute lymphoblastic leukemia...
Azathioprine or 6-mercaptopurine for induction of remission in Crohn's disease. [2009.10.07]
CONCLUSIONS: Azathioprine and 6-mercaptopurine are effective therapy for inducing remission in active Crohn's disease. The OR of response increases after > 17 weeks of therapy, suggesting that there is a minimum length of time for a trial of azathioprine or 6-mercaptopurine therapy. Adverse events were more common among patients on active therapy.
Clinical Trials Related to Mercaptopurine
Study on Two Different Formulations of 6-mercaptopurine. Tablet Versus Oral Liquid [Recruiting]
Acute lymphoblastic leukemia (ALL) accounts for 30 % of all childhood malignancies. The
patients undergo four phases of treatment, finishing with a late maintenance phase in which
6-mercaptopurine and Methotrexate are essential components. Insufficient treatment intensity
in this phase is associated with increased risk of relapse. Excessive variation in the
bioavailability of 6-mercaptopurine has been observed which can cause both risks of
undertreatment/relapse as well as overtreatment with severe side effects.
In the attempt to achieve individualized 6-mercaptopurine dosing different approaches have
been pursued. Nonetheless variation in bioavailability remains a problem.
Earlier, oral tablets of 50 mg (Purinethol) were the only administration form of
6-mercaptopurine and it was primarily designed for adult patients. Challenges with accurate
dosing and getting the children to swallow the tablets have been a widespread problem,
forcing the caregivers to divide or crush the tablets as well as having to administer
different dosages over 2-3 days. Due to these problems, an oral liquid formulation of
6-mercaptopurine (Xaluprine) has been developed. However this oral liquid has only been
tested on healthy adult volunteers, and not on the target group, childhood patients. This
project will assess the bioavailability and plasma kinetics of oral liquid and tablet
formulation of 6-mercaptopurine in children with acute lymphoblastic leukemia.
The investigators hypothesize to observe comparable plasma kinetics, in children with acute
lymphoblastic leukemia when treated with 6-mercaptopurine in the form of a tablet and oral
liquid formulation, as previously observed in healthy adults.
Pilot Comparative Bioavailability Study of 6Mercaptopurine (Delayed Release vs. Purinethol) in Crohns Disease Patients [Completed]
The study is being conducted to evaluate the pharmacokinetic parameters (Cmax, Tmax and AUC)
of the new delayed release, lowered dose, 40 mg 6MP test formulation as compared to standard
6MP (100 mg Purinethol) in 12 patients with Crohn's Disease.
The study is being undertaken to prove that the new test formulation is indeed
delayed-release and targeted to the ileum, and that the levels of 6MP in the blood following
local absorption are lower than that seen following standard Purinethol dosing. This should
result in lower, safer mercaptopurine dosing, allowing for uninterrupted treatment with
fewer side effects.
Comparative Pharmacokinetics of a Compounded 6-mercaptopurine Liquid Formulation Preparation and Tablets [Recruiting]
The purpose of this study is to compare the pharmacokinetics of a routinely used compounded
liquid formulation of 6-mercaptopurine (6-MP) with commercially available tablets in
patients who are receiving treatment with 6-MP as part of their clinical treatment for acute
lymphoblastic leukemia (ALL).
Multicenter Clinical Efficacy and Safety Study of Delayed Release 6MP in Crohn's Disease [Terminated]
The study is designed to evaluate the clinical efficacy and safety of daily treatment for 12
weeks of oral administration of a delayed release, locally delivered 6MP (mercaptopurine)
drug (80 mg), as compared to standard Purinethol (at a dose of 1-1. 5 mg/kg/body weight), in
alleviating the clinical, immunological and mucosal signs and symptoms of moderately active
Assessing Compliance With Mercaptopurine Treatment in Younger Patients With Acute Lymphoblastic Leukemia in First Remission [Recruiting]
This randomized phase III trial studies compliance to a mercaptopurine treatment
intervention compared to standard of care in younger patients with acute lymphoblastic
leukemia in remission. Assessing ways to help patients who have acute lymphoblastic leukemia
to take their medications as prescribed may help them in taking their medications more
consistently and may improve treatment outcomes.
Reports of Suspected Mercaptopurine Side Effects
Acute Myeloid Leukaemia (26),
OFF Label USE (24),
Maternal Exposure During Pregnancy (15),
Hepatosplenic T-Cell Lymphoma (15), more >>
PATIENT REVIEWS / RATINGS / COMMENTS
Based on a total of 1 ratings/reviews, Mercaptopurine has an overall score of 8. The effectiveness score is 8 and the side effect score is 8. The scores are on ten point scale: 10 - best, 1 - worst.
Mercaptopurine review by 37 year old female patient
|Overall rating:|| || |
|Effectiveness:|| || Considerably Effective|
|Side effects:|| || Mild Side Effects|
|Condition / reason:|| || Crohn's disease|
|Dosage & duration:|| || 100 mg taken 1 time every evening for the period of three years +|
|Other conditions:|| || High cholesterol, depression|
|Other drugs taken:|| || Niaspan, Wellbutrin|
|Benefits:|| || I was prescribed the drug Mercaptopurine after two previous treatment drugs had begun to prove less effective than before. The doctor started on a higher course of the medicine, but the dose is currently 100mg (2 pills) every evening. There was a significant reduction in Crohn's disease symptoms, particularly general intestinal cramping. This was particularly helpful for cramping that tended to occur as I was relaxing to go to sleep. |
|Side effects:|| || Though the Crohn's disease in itself makes me tired, and I feel that the addition of the Mercaptopurine has added to my general fatigue. The fatigue abated somewhat as the dose was lowered (the doctor started at a more aggressive dose). I also seem to catch every bug that is going around. By suppressing my immune system I believe the Mercaptopurine makes it easier for seasonal illnesses to set up shop.|
|Comments:|| || I was diagnosed with Crohn's disease about eight years ago. The doctor started with a series of Remicade and a prescription of Prednisone. This combination made it possible for me to eat again - hurray! As for maintenance drugs, I have been on several, including Asacol and Pentasa. There were probably others, but those are the two that I definitely remember. It seemed as though my body would react well to a drug, but then the drug eventually lost that initial effectiveness. I have been on Mercaptopurine for 3-4 years now, and am getting ready to ask to move to a new drug. Mercaptopurine seems to be continuing to do a good job as a drug, but I'd like to find one that may be less deleterious to my liver.|
Page last updated: 2010-10-05