Last update May 11, 2019

Thioguanine

Compatible

Safe substance and/or breastfeeding is the best option.

An antineoplastic, antimetabolite and immunosuppressant. It interferes with the synthesis of nucleic acid by inhibiting the metabolism of purines, with actions similar to mercaptopurine.
Its active metabolite, 6-Thioguanine (6-TGN) or thioguanylic acid, is a metabolite of mercaptopurine, which in turn is metabolized by azathioprine (Jorquera 2012, Gearry 2005).
It is administered orally every 24 hours in the treatment of leukemia.

Very low or undetectable levels of in 6-TGN have been found in breastmilk (Pavlidis 2014, Kane 2004), and in plasma of infants breastfed by mothers who were taking azathioprine (Zelinkova 2009, Bernard 2007, Gardiner 2006).

Experts and scientific associations consider the use of mercaptopurine or azathioprine (which are metabolized in the same active form, 6-Thioguanine) as low risk during breastfeeding (Noviani 2016, Nguyen 2016, Mottet 2016, van der Woude 2015 and 2010, Huang 2014, Nielsen 2014, Yarur 2013, Meij 2013, Habal 2012, Ye 2012, Selinger 2012, Van Assche 2010, Gisbert 2010, Raj 2010, Christensen 2008, Mottet 2007).

Given the strong evidence that exists regarding the benefits of breastfeeding for the development of babies and the health of mothers, it is advisable to evaluate the risk-benefit of any maternal treatment, including chemotherapy, individually advising each mother who wishes to continue with breastfeeding (Koren 2013).


See below the information of these related products:

  • Azathioprine (Safe substance and/or breastfeeding is the best option.)
  • Maternal Cancer (Unsafe. Moderate/severe adverse effects. Compatible under certain circumstances. Follow-up recommended. Use safer alternative or discontinue breastfeeding from 5 to 7 T ½ . Read Commentary.)
  • Mercaptopurine (Safe substance and/or breastfeeding is the best option.)

Alternatives

We do not have alternatives for Thioguanine since it is relatively safe.

Suggestions made at e-lactancia are done by APILAM team of health professionals, and are based on updated scientific publications. It is not intended to replace the relationship you have with your doctor but to compound it. The pharmaceutical industry contraindicates breastfeeding, mistakenly and without scientific reasons, in most of the drug data sheets.

Jose Maria Paricio, Founder & President of APILAM/e-Lactancia

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Other names

Thioguanine is also known as


Thioguanine in other languages or writings:

Group

Thioguanine belongs to this group or family:

Tradenames

Main tradenames from several countries containing Thioguanine in its composition:

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 30 ( 14 - 46) %
Molecular weight 167 daltons
pKa 10.57 -
T½ 4 (metab: 9) hours
Theoretical Dose 0.0012 mg/Kg/d
Relative Dose 0.17 %

References

  1. Nguyen GC, Seow CH, Maxwell C, Huang V, Leung Y, Jones J, Leontiadis GI, Tse F, Mahadevan U, van der Woude CJ; IBD in Pregnancy Consensus Group. The Toronto Consensus Statements for the Management of Inflammatory Bowel Disease in Pregnancy. Gastroenterology. 2016 Mar;150(3):734-757.e1. Abstract Full text (link to original source) Full text (in our servers)
  2. Noviani M, Wasserman S, Clowse ME. Breastfeeding in mothers with systemic lupus erythematosus. Lupus. 2016 Aug;25(9):973-9. Abstract
  3. Mottet C, Schoepfer AM, Juillerat P, Cosnes J, Froehlich F, Kessler-Brondolo V, Seibold F, Rogler G, Vavricka SR, Michetti P. Experts Opinion on the Practical Use of Azathioprine and 6-Mercaptopurine in Inflammatory Bowel Disease. Inflamm Bowel Dis. 2016 Nov;22(11):2733-2747. Abstract Full text (link to original source) Full text (in our servers)
  4. van der Woude CJ, Ardizzone S, Bengtson MB, Fiorino G, Fraser G, Katsanos K, Kolacek S, Juillerat P, Mulders AG, Pedersen N, Selinger C, Sebastian S, Sturm A, Zelinkova Z, Magro F; European Crohn’s and Colitis Organization. The second European evidenced-based consensus on reproduction and pregnancy in inflammatory bowel disease. J Crohns Colitis. 2015 Feb;9(2):107-24. Review. Abstract Full text (link to original source) Full text (in our servers)
  5. Pavlidis P, Ansari A, Duley J, Oancea I, Florin T. Splitting a therapeutic dose of thioguanine may avoid liver toxicity and be an efficacious treatment for severe inflammatory bowel disease: a 2-center observational cohort study. Inflamm Bowel Dis. 2014 Abstract
  6. Nielsen OH, Maxwell C, Hendel J. IBD medications during pregnancy and lactation. Nat Rev Gastroenterol Hepatol. 2014 Feb;11(2):116-27. Abstract
  7. Huang VW, Habal FM. From conception to delivery: managing the pregnant inflammatory bowel disease patient. World J Gastroenterol. 2014 Abstract Full text (link to original source) Full text (in our servers)
  8. Koren G, Carey N, Gagnon R, Maxwell C, Nulman I, Senikas V; Society of Obstetricians and Gynaecologists of Canada. Cancer chemotherapy and pregnancy. J Obstet Gynaecol Can. 2013 Mar;35(3):263-278. Abstract Full text (link to original source) Full text (in our servers)
  9. Yarur A, Kane SV. Update on pregnancy and breastfeeding in the era of biologics. Dig Liver Dis. 2013 Oct;45(10):787-94. Abstract Full text (link to original source) Full text (in our servers)
  10. de Meij TG, Jharap B, Kneepkens CM, van Bodegraven AA, de Boer NK; Dutch Initiative on Crohn and Colitis.. Long-term follow-up of children exposed intrauterine to maternal thiopurine therapy during pregnancy in females with inflammatory bowel disease. Aliment Pharmacol Ther. 2013 Jul;38(1):38-43. Abstract Full text (link to original source) Full text (in our servers)
  11. Selinger CP, Leong RW, Lal S. Pregnancy related issues in inflammatory bowel disease: evidence base and patients' perspective. World J Gastroenterol. 2012 Abstract Full text (link to original source) Full text (in our servers)
  12. Habal FM, Huang VW. Review article: a decision-making algorithm for the management of pregnancy in the inflammatory bowel disease patient. Aliment Pharmacol Ther. 2012 Abstract Full text (link to original source) Full text (in our servers)
  13. Jorquera A, Solari S, Vollrath V, Guerra I, Chianale J, Cofré C, Kalergis A, Ibáñez P, Bueno S, Alvarez-Lobos M. [Phenotype and genotype of thiopurine methyltransferase in Chilean individuals]. Rev Med Chil. 2012 Abstract
  14. van der Woude CJ, Kolacek S, Dotan I, Oresland T, Vermeire S, Munkholm P, Mahadevan U, Mackillop L, Dignass A; European Crohn's Colitis Organisation (ECCO). European evidenced-based consensus on reproduction in inflammatory bowel disease. J Crohns Colitis. 2010 Abstract Full text (link to original source) Full text (in our servers)
  15. Van Assche G, Dignass A, Reinisch W, van der Woude CJ, Sturm A, De Vos M, Guslandi M, Oldenburg B, Dotan I, Marteau P, Ardizzone A, Baumgart DC, D'Haens G, Gionchetti P, Portela F, Vucelic B, Söderholm J, Escher J, Koletzko S, Kolho KL, Lukas M, Mottet C, et al. The second European evidence-based Consensus on the diagnosis and management of Crohn's disease: Special situations. J Crohns Colitis. 2010 Abstract Full text (in our servers)
  16. Gisbert JP. Safety of immunomodulators and biologics for the treatment of inflammatory bowel disease during pregnancy and breast-feeding. Inflamm Bowel Dis. 2010 May;16(5):881-95. Abstract
  17. Raj LS, Hawthorne AB. Optimising use of thiopurines in inflammatory bowel disease. Frontline Gastroenterol. 2010 Abstract Full text (link to original source) Full text (in our servers)
  18. Zelinkova Z, De Boer IP, Van Dijke MJ, Kuipers EJ, Van Der Woude CJ. Azathioprine treatment during lactation. Aliment Pharmacol Ther. 2009 Jul;30(1):90-1; author reply 91. Abstract Full text (link to original source) Full text (in our servers)
  19. Christensen LA, Dahlerup JF, Nielsen MJ, Fallingborg JF, Schmiegelow K. Azathioprine treatment during lactation. Aliment Pharmacol Ther. 2008 Abstract Full text (link to original source) Full text (in our servers)
  20. Bernard N, Garayt C, Chol F, Vial T, Descotes J. Prospective clinical and biological follow-up of three breastfed babies from azathioprine-treated mothers. Abstracts Submitted for the Congrès commun de la Société de Physiologie et de la Société Française de Pharmacologie et de Thérapeutique (SFPT). Congrès P2T 2007. Toulouse. Abstact 309 Fundam Clin Pharmacol. 2007
  21. Mottet C, Juillerat P, Pittet V, Gonvers JJ, Froehlich F, Vader JP, Michetti P, Felley C. Pregnancy and breastfeeding in patients with Crohn's disease. Digestion. 2007 Abstract
  22. Gardiner SJ, Gearry RB, Roberts RL, Zhang M, Barclay ML, Begg EJ. Exposure to thiopurine drugs through breast milk is low based on metabolite concentrations in mother-infant pairs. Br J Clin Pharmacol. 2006 Abstract Full text (link to original source) Full text (in our servers)
  23. Gearry RB, Barclay ML. Azathioprine and 6-mercaptopurine pharmacogenetics and metabolite monitoring in inflammatory bowel disease. J Gastroenterol Hepatol. 2005 Abstract
  24. Kane SV, Present DH. Metabolites to immunomodulators are not detected in breast milk. Abstracts Submitted for the 69th Annual Scientific Meeting of the American College of Gastroenterology. Abstract 761 Am J Gastroenterol. 2004 Full text (link to original source) Full text (in our servers)

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