Difference between revisions of "Mercaptopurine (6-MP)"
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==General information== | ==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)]].<ref name="insert">[http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/009053s032lbl.pdf Mercaptopurine (Purinethol) package insert]</ref><ref>[http:// | + | 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)]].<ref name="insert">[http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/009053s032lbl.pdf Mercaptopurine (Purinethol) package insert]</ref><ref>[[Media:Mercaptopurine.pdf | Mercaptopurine (Purinethol) package insert (locally hosted backup)]]</ref><ref>[http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205919s000lbl.pdf Mercaptopurine (Purixan) package insert]</ref><ref>[[Media:Mercaptopurineliquid.pdf | Mercaptopurine (Purixan) package insert (locally hosted backup)]]</ref> |
<br>Route: PO | <br>Route: PO | ||
<br>Extravasation: n/a | <br>Extravasation: n/a | ||
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==Patient drug information== | ==Patient drug information== | ||
| − | *[http://chemocare.com/ | + | *[http://chemocare.com/chemotherapy/drug-info/Mercaptopurine.aspx Mercaptopurine (Purinethol) patient drug information (Chemocare)]<ref>[http://chemocare.com/chemotherapy/drug-info/Mercaptopurine.aspx Mercaptopurine (Purinethol) patient drug information (Chemocare)]</ref> |
*[http://www.uptodate.com/contents/mercaptopurine-patient-drug-information Mercaptopurine (Purinethol) patient drug information (UpToDate)]<ref>[http://www.uptodate.com/contents/mercaptopurine-patient-drug-information Mercaptopurine (Purinethol) patient drug information (UpToDate)]</ref> | *[http://www.uptodate.com/contents/mercaptopurine-patient-drug-information Mercaptopurine (Purinethol) patient drug information (UpToDate)]<ref>[http://www.uptodate.com/contents/mercaptopurine-patient-drug-information Mercaptopurine (Purinethol) patient drug information (UpToDate)]</ref> | ||
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| + | ==History of changes in FDA indication== | ||
| + | *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] | ||
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| + | ==Also known as== | ||
| + | 6-MP, 6-Mercaptopurine, Purixan (oral suspension formulation). | ||
==References== | ==References== | ||
<references/> | <references/> | ||
| + | |||
| + | [[Category:Drug index]] | ||
| + | [[Category:Chemotherapy]] | ||
[[Category:Antimetabolites]] | [[Category:Antimetabolites]] | ||
[[Category:Purine analogues]] | [[Category:Purine analogues]] | ||
| + | [[Category:Acute lymphocytic leukemia medications]] | ||
| + | [[Category:Acute promyelocytic leukemia medications]] | ||
| + | [[Category:Drugs FDA approved in 2014]] | ||
Revision as of 05:31, 29 April 2014
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
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
Also known as
6-MP, 6-Mercaptopurine, 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)