Last update April 1, 2021

{1-(Ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}ethanenitrile

Limited compatibility

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.

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.
Oral administration once a day.
Used experimentally in the treatment of the COVID-19 coronavirus (Favalli 2020).

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 molecular weight and low fixation to plasma proteins would facilitate it.

Its frequent side effects are mild to moderate infections and thrombocytopenia.

Until there is more published data on this drug in relation to breastfeeding, safer known alternatives may be preferable, especially during the neonatal period and in cases of prematurity.

It is known from pharmacokinetics that after 5 elimination half-lives (T½) 96.9 % of the drug is eliminated from the body and from 7 T½ the plasma concentrations of the drug in the body are negligible. In general, a period of five to seven half-lives can be considered a safe waiting period before resuming breastfeeding.
Taking the longest published T½ (12.5 h) as a reference, these 5 - 7 T½ would correspond to 2,5 -3,5 days. Meanwhile, express and discard milk from the breast regularly to maintain production.


See below the information of this related product:

Alternatives

  • Adalimumab (Safe substance and/or breastfeeding is the best option.)
  • 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.)
  • Etanercept (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.)
  • Tocilizumab (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

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Other names

{1-(Ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}ethanenitrile is Baricitinib in Chemical name.

Is written in other languages:

Group

{1-(Ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}ethanenitrile belongs to this group or family:

Tradenames

Main tradenames from several countries containing {1-(Ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}ethanenitrile in its composition:

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 79 %
Molecular weight 371 daltons
Protein Binding 50 %
VD 1.1 l/Kg
pKa 13.89 -
Tmax 1 (0.5 - 3) hours
T½ 12.5 hours

References

  1. Favalli EG, Biggioggero M, Maioli G, Caporali R. Baricitinib for COVID-19: a suitable treatment? Lancet Infect Dis. 2020 Sep;20(9):1012-1013. Consulted on Sept. 10, 2020 Abstract
  2. EMA - Eli Lilly. Baricitinib (Olumiant). Ficha técnica. 2017 Full text (in our servers)
  3. EMA - Eli Lilly. Baricitinib (Olumiant). Drug Summary. 2017 Full text (in our servers)
  4. Anderson PO. Cancer Chemotherapy. Breastfeed Med. 2016 May;11:164-5. Abstract Full text (link to original source) Full text (in our servers)
  5. 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
  6. 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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