Peringatan Keamanan

There is no experience regarding human overdosage with abrocitinib.L39769 In clinical trials, there were no specific toxicities observed when abrocitinib was administered in single oral doses of 800 mg and 400 mg daily for 28 days. An overdose should be responded with symptomatic and supportive treatment, as there is no specific antidote for overdose with abrocitinib.L39774

Abrocitinib

DB14973

small molecule approved investigational

Deskripsi

Abrocitinib is an oral small-molecule inhibitor of Janus kinase 1 (JAK1). Janus kinases are intracellular enzymes involved in transduction pathways that regulate hematopoiesis and immune cell function.L39774 The Janus kinase (JAK)–signal transducer and activator of transcription (STAT) signalling pathway plays a central role in the pathogenesis of a variety of autoimmune and inflammatory diseases, including atopic dermatitis, a chronic inflammatory skin disease with complex pathogenesis. Atopic dermatitis is characterized by epidermal hyperplasia, skin barrier dysfunction, and the aberrant activation of immune cells. Patients with moderate-to-severe atopic dermatitis report reduced quality of life and often face limited treatment options. JAK inhibitors recently attracted more attention as potential treatments for inflammatory disorders, as JAK inhibition is associated with rapid and sustained anti-inflammatory efects.A244549

Abrocitinib was approved by the European Commission on December 10, 2021, for the treatment of moderate-to-severe atopic dermatitis (AD) in adults who are candidates for systemic therapy.L39784 On January 14, 2022, the FDA approved abrocitinib for the treatment of refractory, moderate-to-severe AD in adults whose disease is not adequately controlled with other systemic drug products, including biologics, or when the use of those therapies is inadvisable.L39779 Health Canada also approved the use of abrocitinib in pediatric patients 12 years and older.L42395

Struktur Molekul 2D

Berat 323.42
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean elimination half-lives of abrocitinib and its two active metabolites, M1 and M2, range from three to five hours.[L39769]
Volume Distribusi After intravenous administration, the volume of distribution of abrocitinib was approximately 100 L.[L39769]
Klirens (Clearance) There is no information available.

Absorpsi

Abrocitinib is absorbed with over 91% extent of oral absorption and absolute oral bioavailability of approximately 60%. The peak plasma concentrations of abrocitinib are reached within one hour. Steady-state plasma concentrations of abrocitinib are achieved within 48 hours after once-daily administration. Both Cmax and AUC of abrocitinib increased dose proportionally up to 200 mg.L39769 A high-fat meal, high-calorie meal increased AUC by 26% and Cmax by 29%, and prolongs Tmax by two hours; however, there are ultimately no clinically relevant effect on abrocitinib exposures.L39769

Metabolisme

Abrocitinib undergoes CYP-mediated oxidative metabolism. CYP2C19 is the predominant enzyme, accounting for about 53% of drug metabolism. CYP2C9 is responsible for 30% of drug metabolism. About 11% and 6% of the drug is metabolized by CYP3A4 and CYP2B6, respectively. In a human radiolabeled study, the parent drug was the most prevalent circulating species. Polar mono-hydroxylated metabolites of abrocitinib - M1 (3-hydroxypropyl; PF-06471658), M2 (2-hydroxypropyl; PF-07055087), and M4 (pyrrolidinone pyrimidine; PF-07054874) - were also identified in the systemic circulation.L39769,L39774 M2 has a chiral center, thus has an enantiomer M3 (PF-07055090).A244544 At steady state, M2 and M4 are major metabolites and M1 is a minor metabolite.L39774 M2 has a pharmacological activity comparable to abrocitinib while M1 is less pharmacologically active than abrocitinib. M3 and M4 are inactive metabolites. The pharmacologic activity of abrocitinib is attributable to the unbound exposures of the parent molecule (~60%) as well as M1 (~10%) and M2 (~30%) in the systemic circulation. The sum of unbound exposures of abrocitinib, M1 and M2, each expressed in molar units and adjusted for relative potencies, is referred to as the abrocitinib active moiety.L39774

Rute Eliminasi

Abrocitinib is eliminated primarily by metabolic clearance mechanisms, with less than 1% of the dose being excreted in urine as an unchanged parent drug. The metabolites of abrocitinib are excreted predominantly in urine.L39769 Pharmacokinetics data up to and including a single oral dose of 800 mg in healthy adult volunteers indicate that more than 90% of the administered dose is expected to be eliminated within 48 hours.L39774

Interaksi Makanan

1 Data
  • 1. Take at the same time every day. Administer with or without food, as it has no clinically relevant effect on abrocitinib exposures.

Interaksi Obat

561 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Abrocitinib.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Abrocitinib.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Abrocitinib.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Abrocitinib.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Abrocitinib.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Abrocitinib.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Abrocitinib.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Abrocitinib.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Abrocitinib.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Abrocitinib.
Silodosin The excretion of Silodosin can be decreased when combined with Abrocitinib.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Abrocitinib.
Dabrafenib The metabolism of Abrocitinib can be increased when combined with Dabrafenib.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Abrocitinib.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Abrocitinib.
Luliconazole The serum concentration of Abrocitinib can be increased when it is combined with Luliconazole.
Vincristine The serum concentration of Vincristine can be increased when it is combined with Abrocitinib.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Abrocitinib.
Lumacaftor The serum concentration of Abrocitinib can be decreased when it is combined with Lumacaftor.
Fluvoxamine The metabolism of Abrocitinib can be decreased when combined with Fluvoxamine.
Ticlopidine The risk or severity of bleeding and thrombocytopenia can be increased when Ticlopidine is combined with Abrocitinib.
Chloramphenicol The metabolism of Abrocitinib can be decreased when combined with Chloramphenicol.
Lansoprazole The metabolism of Abrocitinib can be decreased when combined with Lansoprazole.
Imipramine The metabolism of Abrocitinib can be decreased when combined with Imipramine.
Fluoxetine The metabolism of Abrocitinib can be decreased when combined with Fluoxetine.
Zafirlukast The metabolism of Abrocitinib can be decreased when combined with Zafirlukast.
Delavirdine The metabolism of Abrocitinib can be decreased when combined with Delavirdine.
Isoniazid The metabolism of Abrocitinib can be decreased when combined with Isoniazid.
Miconazole The metabolism of Abrocitinib can be decreased when combined with Miconazole.
Gemfibrozil The metabolism of Abrocitinib can be decreased when combined with Gemfibrozil.
Clomipramine The metabolism of Abrocitinib can be decreased when combined with Clomipramine.
Stiripentol The metabolism of Abrocitinib can be decreased when combined with Stiripentol.
Efavirenz The metabolism of Abrocitinib can be decreased when combined with Efavirenz.
Sertraline The metabolism of Abrocitinib can be decreased when combined with Sertraline.
Armodafinil The metabolism of Abrocitinib can be decreased when combined with Armodafinil.
Eslicarbazepine acetate The metabolism of Abrocitinib can be decreased when combined with Eslicarbazepine acetate.
Troglitazone The metabolism of Abrocitinib can be decreased when combined with Troglitazone.
Valproic acid The metabolism of Abrocitinib can be decreased when combined with Valproic acid.
Nabilone The metabolism of Abrocitinib can be decreased when combined with Nabilone.
Imatinib The metabolism of Abrocitinib can be decreased when combined with Imatinib.
Mifepristone The metabolism of Abrocitinib can be decreased when combined with Mifepristone.
Quinidine The serum concentration of Quinidine can be increased when it is combined with Abrocitinib.
Felbamate The metabolism of Abrocitinib can be decreased when combined with Felbamate.
Amiodarone The metabolism of Abrocitinib can be decreased when combined with Amiodarone.
Sulfinpyrazone The risk or severity of bleeding and thrombocytopenia can be increased when Sulfinpyrazone is combined with Abrocitinib.
Iproniazid The metabolism of Abrocitinib can be decreased when combined with Iproniazid.
Medical Cannabis The metabolism of Abrocitinib can be decreased when combined with Medical Cannabis.
Fluconazole The metabolism of Abrocitinib can be decreased when combined with Fluconazole.
Floxuridine The metabolism of Abrocitinib can be decreased when combined with Floxuridine.
Nicardipine The metabolism of Abrocitinib can be decreased when combined with Nicardipine.
Capecitabine The serum concentration of Abrocitinib can be increased when it is combined with Capecitabine.
Sulfaphenazole The metabolism of Abrocitinib can be decreased when combined with Sulfaphenazole.
Betrixaban The serum concentration of Betrixaban can be increased when it is combined with Abrocitinib.
Apalutamide The metabolism of Abrocitinib can be increased when combined with Apalutamide.
Daptomycin The serum concentration of Daptomycin can be increased when it is combined with Abrocitinib.
Cyclosporine The serum concentration of Cyclosporine can be increased when it is combined with Abrocitinib.
Pravastatin The serum concentration of Pravastatin can be increased when it is combined with Abrocitinib.
Bortezomib The serum concentration of Bortezomib can be increased when it is combined with Abrocitinib.
Sildenafil The serum concentration of Sildenafil can be increased when it is combined with Abrocitinib.
Morphine The serum concentration of Morphine can be increased when it is combined with Abrocitinib.
Tenofovir disoproxil The serum concentration of Tenofovir disoproxil can be increased when it is combined with Abrocitinib.
Clobazam The serum concentration of Clobazam can be increased when it is combined with Abrocitinib.
Mefloquine The serum concentration of Mefloquine can be increased when it is combined with Abrocitinib.
Digoxin The serum concentration of Digoxin can be increased when it is combined with Abrocitinib.
Gemcitabine The serum concentration of Gemcitabine can be increased when it is combined with Abrocitinib.
Quinine The serum concentration of Quinine can be increased when it is combined with Abrocitinib.
Toremifene The serum concentration of Toremifene can be increased when it is combined with Abrocitinib.
Vinblastine The serum concentration of Vinblastine can be increased when it is combined with Abrocitinib.
Bisoprolol The serum concentration of Bisoprolol can be increased when it is combined with Abrocitinib.
Simvastatin The serum concentration of Simvastatin can be increased when it is combined with Abrocitinib.
Mannitol The serum concentration of Mannitol can be increased when it is combined with Abrocitinib.
Etoposide The serum concentration of Etoposide can be increased when it is combined with Abrocitinib.
Loperamide The excretion of Loperamide can be decreased when combined with Abrocitinib.
Vardenafil The serum concentration of Vardenafil can be increased when it is combined with Abrocitinib.
Sirolimus The serum concentration of Sirolimus can be increased when it is combined with Abrocitinib.
Clomifene The serum concentration of Clomifene can be increased when it is combined with Abrocitinib.
Tipranavir The serum concentration of Tipranavir can be increased when it is combined with Abrocitinib.
Fexofenadine The serum concentration of Fexofenadine can be increased when it is combined with Abrocitinib.
Dactinomycin The serum concentration of Dactinomycin can be increased when it is combined with Abrocitinib.
Tegaserod The serum concentration of Tegaserod can be increased when it is combined with Abrocitinib.
Saquinavir The serum concentration of Saquinavir can be increased when it is combined with Abrocitinib.
Dasatinib The serum concentration of Dasatinib can be increased when it is combined with Abrocitinib.
Sitagliptin The serum concentration of Sitagliptin can be increased when it is combined with Abrocitinib.
Posaconazole The serum concentration of Posaconazole can be increased when it is combined with Abrocitinib.
Darunavir The serum concentration of Darunavir can be increased when it is combined with Abrocitinib.
Paliperidone The serum concentration of Paliperidone can be increased when it is combined with Abrocitinib.
Mibefradil The serum concentration of Mibefradil can be increased when it is combined with Abrocitinib.
Digitoxin The serum concentration of Digitoxin can be increased when it is combined with Abrocitinib.
Belinostat The serum concentration of Belinostat can be increased when it is combined with Abrocitinib.
Indacaterol The serum concentration of Indacaterol can be increased when it is combined with Abrocitinib.
Cobimetinib The serum concentration of Cobimetinib can be increased when it is combined with Abrocitinib.
Telaprevir The serum concentration of Telaprevir can be increased when it is combined with Abrocitinib.
Trastuzumab emtansine The serum concentration of Trastuzumab emtansine can be increased when it is combined with Abrocitinib.
Romidepsin The serum concentration of Romidepsin can be increased when it is combined with Abrocitinib.
Tolvaptan The serum concentration of Tolvaptan can be increased when it is combined with Abrocitinib.
Rivaroxaban The serum concentration of Rivaroxaban can be increased when it is combined with Abrocitinib.
Avanafil The serum concentration of Avanafil can be increased when it is combined with Abrocitinib.
Temsirolimus The serum concentration of Temsirolimus can be increased when it is combined with Abrocitinib.
Simeprevir The serum concentration of Simeprevir can be increased when it is combined with Abrocitinib.
Ambrisentan The serum concentration of Ambrisentan can be increased when it is combined with Abrocitinib.

Target Protein

Tyrosine-protein kinase JAK1 JAK1
Tyrosine-protein kinase JAK2 JAK2
Tyrosine-protein kinase JAK3 JAK3
Non-receptor tyrosine-protein kinase TYK2 TYK2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 34601943
    Tripathy S, Wentzel D, Wan XK, Kavetska O: Validation of enantioseparation and quantitation of an active metabolite of abrocitinib in human plasma. Bioanalysis. 2021 Oct;13(19):1477-1486. doi: 10.4155/bio-2021-0128. Epub 2021 Oct 4.
  • PMID: 30536048
    He H, Guttman-Yassky E: JAK Inhibitors for Atopic Dermatitis: An Update. Am J Clin Dermatol. 2019 Apr;20(2):181-192. doi: 10.1007/s40257-018-0413-2.
  • PMID: 27473820
    Roskoski R Jr: Janus kinase (JAK) inhibitors in the treatment of inflammatory and neoplastic diseases. Pharmacol Res. 2016 Sep;111:784-803. doi: 10.1016/j.phrs.2016.07.038. Epub 2016 Jul 26.
  • PMID: 32969750
    Crowley EL, Nezamololama N, Papp K, Gooderham MJ: Abrocitinib for the treatment of atopic dermatitis. Expert Rev Clin Immunol. 2020 Oct;16(10):955-962. doi: 10.1080/1744666X.2021.1828068. Epub 2020 Oct 8.

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