Mercaptopurine

Information about Mercaptopurine

Mercaptopurine (also referred to as 6-mercaptopurine or 6-MP) is a purine analogue that is effective both as an anticancer and an immunosuppressive agent, and is used to treat leukemia and autoimmune diseases as a corticosteroid-sparing agent. 

Liver safety of Mercaptopurine

Mercaptopurine therapy is associated with a high rate of serum aminotransferase elevations which can be accompanied by jaundice.  In addition, mercaptopurine has been linked to instances of clinically apparent acute liver injury and long term therapy to nodular regenerative hyperplasia. 

Mechanism of action of Mercaptopurine

Mercaptopurine (mer kap" toe pure' een) is a purine analogue that acts as an antimetabolite by antagonism of purine metabolism which results in a general inhibition of DNA, RNA and subsequent protein synthesis.  Mercaptopurine also has antiinflammatory and immunosuppressive activity, inhibiting the maturation of T cells and blocking delayed hypersensitivity reactions. 

FDA approval information for Mercaptopurine

Mercaptopurine was introduced into use in the 1950s for the therapy of leukemia and lymphoma and was formally approved for use in the United States in 1953.  It is still used in therapy of acute lymphocytic leukemia and off-label for autoimmune conditions such as Crohn’s disease. 

Dosage and administration for Mercaptopurine

Mercaptopurine is available generically and under the brand name of Purinethol as tablets of 50 mg.  The usual dose is 1 to 3 mg per kilogram or 50 to 150 mg daily, and it is typically given long term. 

Side effects of Mercaptopurine

Common side effects include nausea, abdominal upset, rash, aphthous ulcers and dose related bone marrow suppression.

Antineoplastic Agents
Alkylating Agents - Altretamine, Bendamustine, Busulfan, Carmustine, Chlorambucil, Cyclophosphamide, Dacarbazine, Ifosfamide, Lomustine, Mechlorethamine, Melphalan, Procarbazine, Streptozocin, Temozolomide, Thiotepa, Trabectedin
Platinum Coordination Complexes - Carboplatin, Cisplatin, Oxaliplatin
Antibiotics Cytotoxic - Bleomycin, Dactinomycin, Daunorubicin, Doxorubicin, Epirubicin, Idarubicin, Mitomycin, Mitoxantrone, Plicamycin, Mithramycin, Valrubicin
Antimetabolites Antifolates - Methotrexate, Pemetrexed, Pralatrexate, Trimetrexate
Purine Analogues - Azathioprine, Cladribine, Clofarabine, Fludarabine, Mercaptopurine, Nelarabine, Pentostatin, Thioguanine
Pyrimidine Analogues - Azacitidine, Capecitabine, Cytarabine, Decitabine, Floxuridine, Fluorouracil, Gemcitabine, Trifluridine/Tipracil
Biologic Response Modifiers - Aldesleukin (IL-2), Denileukin Diftitox, Interferon gamma
Histone Deacetylase Inhibitors - Belinostat, Panobinostat, Romidepsin, Vorinostat
Hormonal Agents Antiandrogens - Abiraterone, Bicalutamide, Cyproterone, Enzalutamide, Flutamide, Nilutamide
Antiestrogens (including Aromatase Inhibitors) - Anastrozole, Exemestane, Fulvestrant, Letrozole
Selective Estrogen Receptor Modulators - Raloxifene, Tamoxifen, Toremifene
Gonadotropin Releasing Hormone Analogues - Degarelix, Goserelin, Histrelin, Leuprolide, Triptorelin
Peptide Hormones - Lanreotide, Octreotide, Pasireotide
Monoclonal Antibodies - Alemtuzumab, Atezolizumab, Avelumab, Bevacizumab, Blinatumomab, Brentuximab, Cetuximab, Daratumumab, Dinutuximab, Durvalumab, Elotuzumab, Gemtuzumab, Inotuzumab Ozogamicin, Ipilimumab, Necitumumab, Nivolumab, Ofatumumab, Olaratumab, Panitumumab, Pembrolizumab, Pertuzumab, Ramucirumab, Rituximab, Tositumomab, Trastuzumab
Protein Kinase Inhibitors - Abemaciclib, Acalabrutinib, Afatinib, Alectinib, Axitinib, Bortezomib, Bosutinib, Brigatinib, Cabozantinib, Carfilzomib, Ceritinib, Cobimetinib, Copanlisib, Crizotinib, Dabrafenib, Dasatinib, Enasidenib, Erlotinib, Gefitinib, Ibrutinib, Idelalisib, Imatinib, Ivosidenib, Ixazomib, Lapatinib, Lenvatinib, Neratinib, Nilotinib, Niraparib, Olaparib, Osimertinib, Palbociclib, Pazopanib, Ponatinib, Regorafenib, Ribociclib, Rucaparib, Ruxolitinib, Sonidegib, Sorafenib, Sunitinib, Trametinib, Vandetanib, Vemurafenib, Vismodegib
Taxanes - Cabazitaxel, Docetaxel, Paclitaxel
Topoisomerase Inhibitors - Etoposide, Irinotecan, Teniposide, Topotecan
Tyrosine Kinase Receptor Inhibitors See Protein Kinase Inhibitors
Vinca Alkaloids - Vinblastine, Vincristine, Vinorelbine
Miscellaneous - Asparaginase (Pegaspargase), Bexarotene, Eribulin, Everolimus, Hydroxyurea, Ixabepilone, Lenalidomide, Mitotane, Omacetaxine, Pomalidomide, Temsirolimus, Thalidomide, Venetoclax

 

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