Difference between revisions of "Thioguanine (Tabloid)"
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==General information== | ==General information== | ||
| − | Class/mechanism: Purine (guanine) analog, antimetabolite that interferes with DNA synthesis. Thioguanine competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is converted to 6-thioguanylic acid (TGMP). TGMP interferes with several processes involving the synthesis of guanine nucleotides. It exerts pseudo-feedback inhibition of glutamine-5-phosphoribosylpyrophosphate amidotransferase, an early enzyme in the de novo pathway for purine ribonucleotide synthesis. TGMP is a competitive inhibitor of inosinic acid (IMP) dehydrogenase, interfering with the conversion of IMP to xanthylic acid (XMP). Thioguanylic acid is converted to thioguanosine diphosphate (TGDP) and thioguanosine triphosphate (TGTP), and they are eventually incorporated into RNA and DNA, which may cause additional cytotoxicity. Thioguanine is structurally and functionally similar to [[Mercaptopurine ( | + | Class/mechanism: Purine (guanine) analog, antimetabolite that interferes with DNA synthesis. Thioguanine competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is converted to 6-thioguanylic acid (TGMP). TGMP interferes with several processes involving the synthesis of guanine nucleotides. It exerts pseudo-feedback inhibition of glutamine-5-phosphoribosylpyrophosphate amidotransferase, an early enzyme in the de novo pathway for purine ribonucleotide synthesis. TGMP is a competitive inhibitor of inosinic acid (IMP) dehydrogenase, interfering with the conversion of IMP to xanthylic acid (XMP). Thioguanylic acid is converted to thioguanosine diphosphate (TGDP) and thioguanosine triphosphate (TGTP), and they are eventually incorporated into RNA and DNA, which may cause additional cytotoxicity. Thioguanine is structurally and functionally similar to [[Mercaptopurine (6-MP)]].<ref name="insert">[http://us.gsk.com/products/assets/us_tabloid.pdf Thioguanine (Tabloid) package insert]</ref><ref>[https://hemonc.org/docs/packageinsert/thioguanine.pdf Thioguanine (Tabloid) package insert (locally hosted backup)]</ref> |
<br>Route: PO | <br>Route: PO | ||
<br>Extravasation: n/a | <br>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. | + | 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 [http://www.thomsonhc.com/home/dispatch Micromedex], [http://online.lexi.com/ Lexicomp], [http://www.utdol.com/online/content/search.do UpToDate (courtesy of Lexicomp)], or the prescribing information.<ref name="insert"></ref> |
==Diseases for which it is used== | ==Diseases for which it is used== | ||
| − | |||
*[[Acute promyelocytic leukemia]] | *[[Acute promyelocytic leukemia]] | ||
| + | *[[B-cell acute lymphoblastic leukemia]] | ||
| + | *[[Waldenström macroglobulinemia]] | ||
| + | |||
| + | ==Diseases for which it was used== | ||
| + | *[[Acute myeloid leukemia - historical|Acute myeloid leukemia]] | ||
==Patient drug information== | ==Patient drug information== | ||
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==History of changes in FDA indication== | ==History of changes in FDA indication== | ||
| − | * | + | * 1966-01-18: Initial approval |
| + | ==History of changes in EMA indication== | ||
| + | *1966-01-18: EURD | ||
| + | ==Also known as== | ||
| + | *'''Generic names:''' 6-TG, 6-thioguanine, 2-Amino-6-Mercaptopurine, tioguanine | ||
| + | *'''Brand name:''' Lanvis, Tabloid, Thioxlant | ||
==References== | ==References== | ||
<references/> | <references/> | ||
| − | [[Category: | + | [[Category:Drugs]] |
| − | + | [[Category:Oral medications]] | |
| − | [[Category:Oral | ||
[[Category:Antimetabolites]] | [[Category:Antimetabolites]] | ||
| − | [[Category:Purine | + | [[Category:Purine analogs]] |
| − | |||
[[Category:Acute promyelocytic leukemia medications]] | [[Category:Acute promyelocytic leukemia medications]] | ||
| + | [[Category:B-cell acute lymphoblastic leukemia medications]] | ||
| + | [[Category:Waldenström macroglobulinemia medications]] | ||
| + | |||
| + | [[Category:Acute myeloid leukemia medications (historic)]] | ||
| − | [[Category: | + | [[Category:FDA approved in 1966]] |
| + | [[Category:EMA approved in 1966]] | ||
| + | [[Category:WHO Essential Cancer Medicine]] | ||
Revision as of 19:32, 23 June 2024
General information
Class/mechanism: Purine (guanine) analog, antimetabolite that interferes with DNA synthesis. Thioguanine competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is converted to 6-thioguanylic acid (TGMP). TGMP interferes with several processes involving the synthesis of guanine nucleotides. It exerts pseudo-feedback inhibition of glutamine-5-phosphoribosylpyrophosphate amidotransferase, an early enzyme in the de novo pathway for purine ribonucleotide synthesis. TGMP is a competitive inhibitor of inosinic acid (IMP) dehydrogenase, interfering with the conversion of IMP to xanthylic acid (XMP). Thioguanylic acid is converted to thioguanosine diphosphate (TGDP) and thioguanosine triphosphate (TGTP), and they are eventually incorporated into RNA and DNA, which may cause additional cytotoxicity. Thioguanine is structurally and functionally similar to Mercaptopurine (6-MP).[1][2]
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
Diseases for which it was used
Patient drug information
- Thioguanine (Tabloid) patient drug information (Chemocare)[3]
- Thioguanine (Tabloid) patient drug information (UpToDate)[4]
History of changes in FDA indication
- 1966-01-18: Initial approval
History of changes in EMA indication
- 1966-01-18: EURD
Also known as
- Generic names: 6-TG, 6-thioguanine, 2-Amino-6-Mercaptopurine, tioguanine
- Brand name: Lanvis, Tabloid, Thioxlant