Last update Sept. 23, 2023

1-[3-(aminomethyl)phenyl]-N-(5-{(R)-(3-cyanophenyl [(cyclopropylmethyl)amino]methyl}-2-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide

Likely Compatibility

Fairly safe. Mild or unlikely adverse effects. Compatible under certain circumstances. Follow-up recommended. Read Commentary.

Berotralstat is a plasma kallikrein inhibitor that limits the production of bradykinin, a potent vasodilator. Used for prophylaxis of angioedema attacks in patients with hereditary angioedema. Oral administration in a daily dose.

As of the last update, we do not find published data on its excretion in breast milk.

Su elevada fijación a proteínas plasmáticas y moderadamente alto peso molecular hacen improbable su paso a leche materna.

Until more published data are known about this drug in relation to breastfeeding, known safer alternatives may be preferable, especially during the neonatal period and in cases of prematurity. (Yeich 2023, Bouillet 2015)

 

 

Alternatives

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.

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Other names

1-[3-(aminomethyl)phenyl]-N-(5-{(R)-(3-cyanophenyl [(cyclopropylmethyl)amino]methyl}-2-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide is Berotralstat in Chemical name.

Is written in other languages:

Group

1-[3-(aminomethyl)phenyl]-N-(5-{(R)-(3-cyanophenyl [(cyclopropylmethyl)amino]methyl}-2-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide belongs to this group or family:

Tradenames

Main tradenames from several countries containing 1-[3-(aminomethyl)phenyl]-N-(5-{(R)-(3-cyanophenyl [(cyclopropylmethyl)amino]methyl}-2-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide in its composition:

Pharmacokinetics

Variable Value Unit
Molecular weight 563 daltons
Protein Binding 99 %
Tmax 2.5 (1 - 8) hours
T½ 93 (39- 152) hours

References

  1. Yeich A, Elhatw A, Ashoor Z, Park K, Craig T. Safety of medications for hereditary angioedema during pregnancy and lactation. Expert Opin Drug Saf. 2023 Jan;22(1):17-24. Consulted on Sept. 22, 2023 Abstract
  2. BioChryst Ph. Berotralstat. Drug Summary. 2022 Full text (in our servers)
  3. Bouillet L, Lehmann A, Gompel A, Boccon-Gibod I, Launay D, Fain O; CREAK.. Traitements des angiœdèmes héréditaires : recommandations du centre de référence national des angiœdèmes (consensus 2014 de Bordeaux). [Hereditary angiœdema treatments: Recommendations from the French national center for angiœdema (Bordeaux consensus 2014)]. Presse Med. 2015 Abstract

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