Baricitinib

Baricitinib
Nomi alternativi
Olumiant
Caratteristiche generali
Formula bruta o molecolareC16H17N7O2S
Numero CAS1187594-09-7
Numero EINECS691-421-4
PubChem44205240
DrugBankDBDB11817
SMILES
CCS(=O)(=O)N1CC(C1)(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3
Dati farmacocinetici
Biodisponibilità79%
Legame proteico50%
MetabolismoCYP3A4 (<10%)
Emivita12,5 h
Escrezione75% urina, 20% feci
Indicazioni di sicurezza

Baricitinib, venduto a marchio Olumiant e altri, è un farmaco per il trattamento dell'artrite reumatoide (RA) in adulti che non rispondono a inibitori TNF.[1] Lavora come gli Inibitori delle JAK (JAK), bloccando i sottotipi JAK1 e JAK2.[2] Il farmaco è approvato in Unione Europea[3] e in USA.[1][4] Effetti collaterali notevoli sono la possibilità di infezioni opportunistiche, batteriche, di miceti, di funghi e virus.[5]

Uso

Nel febbraio 2017 è stato approvato per l'uso contro l'artrite reumatoide moderata e severa, da solo o con metotrexato.[3][6]

Nel 2018 la FDA approva l'uso per artrite reumatoide, moderata o severa, in soggetti che non rispondono agli antagonisti TNF.[1][4][7]

Nel settembre 2021 viene approvata dall'AIFA per il trattamento di COVID-19.

Nel giugno 2022 viene approvata dall'FDA per il trattamento dell'Alopecia areata.[8][9]

Controindicazioni

Controindicato in gravidanza.[6]

Effetti collaterali

Infezioni del tratto respiratorio superiore e ipercolesterolemia nel 10% dei pazienti. Meno comuni infezioni da herpes zoster, herpes simplex, del tratto urinario e gastroenteriti.[6]

COVID-19

Nell'aprile 2020 viene sperimentato dalla Lilly come farmaco contro il COVID-19.[10]

Nel luglio 2021 la FDA rivede l'autorizzazione EUA per l'uso in pazienti COVID-19 ospedalizzati con ventilazione assistita, invasiva e non, o circolazione extracorporea ECMO.[11] Viene rivisto l'uso associato a remdesivir, non più necessario.[11]

Alopecia

Nel giugno 2022, la Food and Drug Administration ha autorizzato il Baricitinib per il trattamento delle formi gravi di Alopecia areata.[8][9] La sua sicurezza ed efficacia è stata verificata mediante due sperimentazioni in fase III (Trial AA-1 and Trial AA-2) nei quali i partecipanti hanno ottenuto una riduzione di almeno 50% della caduta di capelli, misurata con apposita strumentazione, rispetto al gruppo di controllo con placebo, per un periodo di almeno sei mesi.[8]

Note

  1. ^ a b c Drug Trials Snapshots: Olumiant, su U.S. Food and Drug Administration (FDA), 31 maggio 2018. URL consultato il 16 marzo 2020.
  2. ^ Summary of opinion for Olumiant (PDF), su ema.europa.eu, European Medicines Agency (EMA), 15 dicembre 2016. URL consultato il 30 settembre 2021 (archiviato dall'url originale il 15 marzo 2018).
  3. ^ a b Olumiant EPAR, su ema.europa.eu, European Medicines Agency (EMA), 3 dicembre 2019. Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  4. ^ a b Drug Approval Package: Olumiant (baricitinib), su U.S. Food and Drug Administration (FDA), 5 luglio 2018. URL consultato il 16 marzo 2020.
  5. ^ O'Shea JJ, Kontzias A, Yamaoka K, Tanaka Y, Laurence A, Janus kinase inhibitors in autoimmune diseases, in Annals of the Rheumatic Diseases, vol. 72, suppl 2, aprile 2013, pp. ii111-5, DOI:10.1136/annrheumdis-2012-202576, PMC 3616338, PMID 23532440.
  6. ^ a b c Olumiant: EPAR – Product Information (PDF), su ema.europa.eu, European Medicines Agency, 13 febbraio 2017. URL consultato il 30 settembre 2021 (archiviato dall'url originale il 12 luglio 2018).
  7. ^ Olumiant- baricitinib tablet, film coated, su DailyMed, 13 novembre 2019. URL consultato il 16 marzo 2020.
  8. ^ a b c FDA Approves First Systemic Treatment for Alopecia Areata, su U.S. Food and Drug Administration (FDA), 13 giugno 2022. URL consultato il 13 giugno 2022 (archiviato dall'url originale il 14 giugno 2022).
  9. ^ a b FDA Approves Lilly and Incyte's Olumiant (baricitinib) As First and Only Systemic Medicine for Adults with Severe Alopecia Areata, su prnewswire.com, Eli Lilly, 13 giugno 2022. URL consultato il 13 giugno 2022 (archiviato dall'url originale il 14 giugno 2022). Ospitato su PR Newswire.
  10. ^ Eli Lilly to study baricitinib for Covid-19 treatment, in Clinical Trials Arena.
  11. ^ a b Coronavirus (COVID-19) Update: July 30, 2021, su U.S. Food and Drug Administration (FDA), 30 luglio 2021. URL consultato il 30 luglio 2021.

Bibliografia

Altri progetti

Collegamenti esterni

  • Baricitinib, in Drug Information Portal, U.S. National Library of Medicine.

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