Difference between revisions of "Mercaptopurine (6-MP)"
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*9/11/1953: [http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm?fuseaction=Search.Label_ApprovalHistory#labelinfo Initial FDA approval] | *9/11/1953: [http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm?fuseaction=Search.Label_ApprovalHistory#labelinfo Initial FDA approval] | ||
*4/28/2014: [http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm?fuseaction=Search.Label_ApprovalHistory#apphist Purixan (mercaptopurine oral suspension formulation) FDA approved] | *4/28/2014: [http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm?fuseaction=Search.Label_ApprovalHistory#apphist Purixan (mercaptopurine oral suspension formulation) FDA approved] | ||
+ | *As of most recent package insert: indicated for maintenance therapy of [[:Category:Acute lymphoblastic leukemias|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). | ||
==Also known as== | ==Also known as== |
Revision as of 23:01, 11 January 2020
General information
Class/mechanism: Purine analog of adenine and hypoxanthine, antimetabolite that interferes with DNA synthesis. Mercaptopurine competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is converted to thioinosinic acid (TIMP). TIMP inhibits reactions that typically involve inosinic acid (IMP), such as its conversion to xanthylic acid (XMP) and adenylic acid (AMP) via adenylosuccinate (SAMP). TIMP is also converted to 6-methylthioinosinate (MTIMP); TIMP and MTIMP have been observed to inhibit glutamine-5-phosphoribosylpyrophosphate amidotransferase, which is an early enzyme in the de novo pathway of purine ribonucleotide synthesis. Mercaptopurine is structurally and functionally similar to Thioguanine (Tabloid).[1][2][3][4]
Route: PO
Extravasation: n/a
For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]
Diseases for which it is used
- Acute promyelocytic leukemia
- B-cell acute lymphoblastic leukemia
- CNS leukemia
- Langerhans cell histiocytosis
- T-cell acute lymphoblastic leukemia
Patient drug information
- Mercaptopurine (Purinethol) patient drug information (Chemocare)[5]
- Mercaptopurine (Purinethol) patient drug information (UpToDate)[6]
History of changes in FDA indication
- 9/11/1953: Initial FDA approval
- 4/28/2014: Purixan (mercaptopurine oral suspension formulation) FDA approved
- As of most recent package insert: 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).
Also known as
- Generic names: 6-MP, 6-Mercaptopurine
- Brand names: Purinethol, Purixan (oral suspension formulation)
References
- ↑ 1.0 1.1 Mercaptopurine (Purinethol) package insert
- ↑ Mercaptopurine (Purinethol) package insert (locally hosted backup)
- ↑ Mercaptopurine (Purixan) package insert
- ↑ Mercaptopurine (Purixan) package insert (locally hosted backup)
- ↑ Mercaptopurine (Purinethol) patient drug information (Chemocare)
- ↑ Mercaptopurine (Purinethol) patient drug information (UpToDate)
- Drugs
- Oral medications
- Antimetabolites
- Purine analogues
- Immunosuppressants
- Acute promyelocytic leukemia medications
- B-cell acute lymphoblastic leukemia medications
- CNS leukemia medications
- Langerhans cell histiocytosis medications
- T-cell acute lymphoblastic leukemia medications
- FDA approved in 1953
- FDA approved in 2014
- WHO Essential Cancer Medicine