Last update Nov. 6, 2022

Imatinib Mesilate, Imatinib Mesylate

Low Risk

Possibly safe. Probably compatible. Mild risk possible. Follow up recommended. Read the Comment.

Tyrosine kinase inhibitor that is used for treatment of chronic myeloid leukaemia, acute lymphoblastic leukaemia, myelodysplastic syndromes and some types of cancer. Oral administration once or twice daily.

Its pharmacokinetic data (high percentage of protein binding, wide volume of distribution and moderately high molecular weight) explain the negligible passage into breast milk observed systematically. (Terao 2021, EMA 2018, Chelysheva 2018, Burwick 2017, Gouraud 2013, Kronenberger 2009, Ali 2009, Gambacorti 2007, Russell 2007)

No problems have been observed among breastfed infants from treated mothers. (Terao 2020, Alizadeh 2015, Jiang 2012, Gambacorti 2007)

Its active metabolite has a very long elimination life (40 hours) and the product has a very high bioavailability, so it could theoretically be absorbed by the infant.

The most frequent side effects of the drug are gastroenteritis, pancytopenia, increased liver transaminases, insomnia, weight loss, respiratory infections.

It is known from pharmacokinetics that after 3 elimination half-lives (T½) 87.5% of the drug is eliminated from the body; after 4 T½ it is 94%, after 5 T½, 96.9%, after 6 T½, 98.4% and after 7 T½ it is 99%. From 7 T½ the plasma concentrations of the drug in the body are negligible. In general, a period of at least five half-lives can be considered a safe waiting period before breastfeeding again.(Anderson 2016).

Taking the longest T½ published as a reference (40 hours), these 5 T½ would correspond to 200 hours (8.3 days). Meanwhile, express and discard milk from the breast regularly. This does not allow breastfeeding during treatment and several authors advise against it. (Grunewald 2015, Jiang 2012)

Abrupt weaning can be psychologically traumatic for both the mother and the infant. (Pistilli 2013). 

If used during lactation, it is advisable to monitor growth and appetite and the possible appearance of diarrhea in the infant, as well as monitor hepatic and hematological function periodically.

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 this related product:

  • Maternal Cancer ( Poorly safe. Evaluate carefully. Use safer alternative or interrupt breastfeeding 3 to 7 T ½ (elimination half-lives). Read the Comment.)

Alternatives

We do not have alternatives for Imatinib Mesilate, Imatinib Mesylate.

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

Your contribution is essential for this service to continue to exist. We need the generosity of people like you who believe in the benefits of breastfeeding.

Thank you for helping to protect and promote breastfeeding.

José María Paricio, founder of e-lactancia.

Other names

Imatinib Mesilate, Imatinib Mesylate is also known as


Imatinib Mesilate, Imatinib Mesylate in other languages or writings:

Groups

Imatinib Mesilate, Imatinib Mesylate belongs to these groups or families:

Tradenames

Main tradenames from several countries containing Imatinib Mesilate, Imatinib Mesylate in its composition:

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 98 %
Molecular weight 590 daltons
Protein Binding 95 %
VD 4.2 ± 1.2 l/Kg
pKa 12.69 -
Tmax 2 - 4 hours
18 (metab: 40) hours
M/P ratio 0.5 (metab: 0.9) -
Theoretical Dose 0.2 - 0.4 mg/Kg/d
Relative Dose 1.4 - 4.8 %

References

  1. Novartis. Imatinib. Drug Summay. 2022 Full text (in our servers)
  2. Terao R, Nii M, Asai H, Nohara F, Okamoto T, Nagaya K, Azuma H. Breastfeeding in a patient with chronic myeloid leukemia during tyrosine kinase inhibitor therapy. J Oncol Pharm Pract. 2021 Apr;27(3):756-760. Abstract
  3. EMA. Imatinib. Ficha técnica. 2018 Full text (in our servers)
  4. Chelysheva E, Aleshin S, Polushkina E, Shmakov R, Shokhin I, Chilov G, Turkina A. Breastfeeding in Patients with Chronic Myeloid Leukaemia: Case Series with Measurements of Drug Concentrations in Maternal Milk and Literature Review. Mediterr J Hematol Infect Dis. 2018 May 1;10(1):e2018027. Abstract Full text (link to original source)
  5. Burwick RM, Kuo K, Brewer D, Druker BJ. Maternal, Fetal, and Neonatal Imatinib Levels With Treatment of Chronic Myeloid Leukemia in Pregnancy. Obstet Gynecol. 2017 May;129(5):831-834. Abstract
  6. Anderson PO. Cancer Chemotherapy. Breastfeed Med. 2016 May;11:164-5. Abstract Full text (link to original source) Full text (in our servers)
  7. Alizadeh H, Jaafar H, Kajtár B. Outcome of 3 pregnancies in a patient with chronic myeloid leukemia who received 3 types of tyrosine kinase inhibitors each in different pregnancy: follow-up of the case with a review of published reports. Ann Saudi Med. 2015 Nov-Dec;35(6):468-71. Abstract Full text (link to original source)
  8. Grunewald S, Jank A. New systemic agents in dermatology with respect to fertility, pregnancy, and lactation. J Dtsch Dermatol Ges. 2015 Abstract Full text (link to original source) Full text (in our servers)
  9. 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)
  10. Pistilli B, Bellettini G, Giovannetti E, Codacci-Pisanelli G, Azim HA Jr, Benedetti G, Sarno MA, Peccatori FA. Chemotherapy, targeted agents, antiemetics and growth-factors in human milk: how should we counsel cancer patients about breastfeeding? Cancer Treat Rev. 2013 May;39(3):207-11. Abstract
  11. Gouraud A, Vial T, Ianotto JC, Bages-Jaffuelc K, Di Pillad L, Gremmo-Fegere G, Gagnieu MC. Imatinib concentration in breast milk: A case report. Fundam Clin Pharmacol 2013;27 (Suppl 1):68. Poster Abstract 1-111. Full text (link to original source)
  12. Jiang Q, Jiang B, Chen SS, Jiang H, Qin YZ, Lai YY, Shi HX, Huang XJ. [Pregnancy outcome among patients with chronic myelogenous leukemia treated with tyrosine kinase inhibitors]. Zhonghua Xue Ye Xue Za Zhi. 2012 Abstract
  13. Di Gion P, Kanefendt F, Lindauer A, Scheffler M, Doroshyenko O, Fuhr U, Wolf J, Jaehde U. Clinical pharmacokinetics of tyrosine kinase inhibitors: focus on pyrimidines, pyridines and pyrroles. Clin Pharmacokinet. 2011 Abstract
  14. Ali R, Ozkalemkas F, Kimya Y, Koksal N, Ozkocaman V, Gulten T, Yorulmaz H, Tunali A. Imatinib use during pregnancy and breast feeding: a case report and review of the literature. Arch Gynecol Obstet. 2009 Abstract
  15. Kronenberger R, Schleyer E, Bornhäuser M, Ehninger G, Gattermann N, Blum S. Imatinib in breast milk. Ann Hematol. 2009 Abstract
  16. Russell MA, Carpenter MW, Akhtar MS, Lagattuta TF, Egorin MJ. Imatinib mesylate and metabolite concentrations in maternal blood, umbilical cord blood, placenta and breast milk. J Perinatol. 2007 Abstract
  17. Gambacorti-Passerini CB, Tornaghi L, Marangon E, Franceschino A, Pogliani EM, D'Incalci M, Zucchetti M. Imatinib concentrations in human milk. Blood. 2007 Abstract
  18. Garderet L, Santacruz R, Barbu V, van den Akker J, Carbonne B, Gorin NC. Two successful pregnancies in a chronic myeloid leukemia patient treated with imatinib. Haematologica. 2007 Abstract

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