Last update Feb. 11, 2020

3-{(3R,4R)-4-Methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl}-3-oxo-propanenitrile

Incompatible

Very unsafe. Contraindicated. Use of an alternative or cessation of breastfeeding. Read the Commentary.

A selective and reversible inhibitor of Janus kinases 1 and 2.
It is used alone or associated with methotrexate in moderate to severe rheumatoid arthritis, in psoriatic arthritis and ulcerative colitis.
Oral administration twice a day.

Since the last update we have not found published data on its excretion in breastmilk.

Its pharmacokinetic data makes it difficult to accurately predict its possible excretion in breastmilk, because although its high volume of distribution would hinder it, its low molecular weight and low fixation to plasma proteins would facilitate it.

Its frequent side effects are infections that can be serious, anemia and hypertension

Until there is more published data on this drug in relation to breastfeeding, safer known alternatives may be preferable (Mahadevan 2019, Louthrenoo 2017, Götestam 2016), especially during the neonatal period and in cases of prematurity.


See below the information of these related products:

Alternatives

  • Auranofin (Fairly safe. Mild or unlikely adverse effects. Compatible under certain circumstances. Follow-up recommended. Read Commentary.)
  • Aurothiomalate Sodium (Fairly safe. Mild or unlikely adverse effects. Compatible under certain circumstances. Follow-up recommended. Read Commentary.)
  • Certolizumab (Safe substance and/or breastfeeding is the best option.)
  • Hydroxychloroquine Sulfate (Safe substance and/or breastfeeding is the best option.)
  • Infliximab (Safe substance and/or breastfeeding is the best option.)
  • Methotrexate (obstetric and immunosuppressive use) (Fairly safe. Mild or unlikely adverse effects. Compatible under certain circumstances. Follow-up recommended. Read Commentary.)
  • Penicillamine (Safe substance and/or breastfeeding is the best option.)
  • Sulfasalazine (Safe substance and/or breastfeeding is the best option.)

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

3-{(3R,4R)-4-Methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl}-3-oxo-propanenitrile is Tofacitinib in Chemical name.

Is written in other languages:

3-{(3R,4R)-4-Methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl}-3-oxo-propanenitrile is also known as

Group

3-{(3R,4R)-4-Methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl}-3-oxo-propanenitrile belongs to this group or family:

Tradenames

Main tradenames from several countries containing 3-{(3R,4R)-4-Methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl}-3-oxo-propanenitrile in its composition:

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 74 %
Molecular weight 312 daltons
Protein Binding 40 %
VD 1.2 l/Kg
pKa 7.13 - 8.46 -
Tmax 0.5 - 1 hours
3.2 hours

References

  1. Mahadevan U, Robinson C, Bernasko N, Boland B, Chambers C, Dubinsky M, Friedman S, Kane S, Manthey J, Sauberan J, Stone J, Jain R. Inflammatory Bowel Disease in Pregnancy Clinical Care Pathway: A Report From the American Gastroenterological Association IBD Parenthood Project Working Group. Gastroenterology. 2019 Apr;156(5):1508-1524. Abstract Full text (link to original source)
  2. EMA-Pfizer. Tofacitinib (Xeljanz). Drug Summary. 2017 Full text (in our servers)
  3. Louthrenoo W, Kasitanon N, Katchamart W, Aiewruengsurat D, Chevaisrakul P, Chiowchanwisawakit P, Dechanuwong P, Hanvivadhanakul P, Mahakkanukrauh A, Manavathongchai S, Muangchan C, Narongroeknawin P, Phumethum V, Siripaitoon B, Suesuwan A, Suwannaroj S, Uea-Areewongsa P, Ukritchon S, Asavatanabodee P, Koolvisoot A, Nanagara R, Totemchokchyakarn K, et al. 2016 updated Thai Rheumatism Association Recommendations for the use of biologic and targeted synthetic disease-modifying anti-rheumatic drugs in patients with rheumatoid arthritis. Int J Rheum Dis. 2017 Sep;20(9):1166-1184. Abstract
  4. EMA-Pfizer. Tofacitinib (Xeljanz). Ficha técnica. 2017 Full text (in our servers)
  5. Götestam Skorpen C, Hoeltzenbein M, Tincani A, Fischer-Betz R, Elefant E, Chambers C, da Silva J, Nelson-Piercy C, Cetin I, Costedoat-Chalumeau N, Dolhain R, Förger F, Khamashta M, Ruiz-Irastorza G, Zink A, Vencovsky J, Cutolo M, Caeyers N, Zumbühl C, Østensen M. The EULAR points to consider for use of antirheumatic drugs before pregnancy, and during pregnancy and lactation. Ann Rheum Dis. 2016 May;75(5):795-810. Abstract Full text (link to original source) Full text (in our servers)
  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. 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
  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)

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