Peringatan Keamanan

There are no data regarding overdosage with atogepant. Symptoms of atogepant overdose are likely to be consistent with its adverse effect profile and may therefore include significant gastrointestinal effects, such as nausea and constipation, as well as fatigue and somnolence.L38739 A single oral dose of 300mg (5x the maximum recommended dose) did not result in any serious adverse events and did not appear to impact cardiac function.A239089

Atogepant

DB16098

small molecule approved investigational

Deskripsi

Atogepant is an oral antagonist of calcitonin gene-related peptide (CGRP) receptors indicated for the prevention of episodic migraine headaches. It was developed by AbbVie and received FDA approval under the brand name Qulipta in September 2021.L38814 While its approval was predated by two other members of the same drug family, namely ubrogepant and rimegepant, these agents are indicated only for abortive migraine therapy - atogepant is novel in that it is the first and only oral CGRP antagonist approved for preventative use in migraine.L38814 In December 2022, atogepant received Health Canada approval for the prevention of episodic migraine in adults.L44642 It also received approval for preventive treatment of adult migraine by the EMA in August 2023.L48016

In patients requiring preventative migraine therapy, current practice guidelines recommend the use of certain anti-epileptic medications (e.g. valproic acid or topiramate) or beta-blockers (e.g. propranolol), all of which can be associated with significant adverse effects.A239094 The "gepants" family of drugs, including atogepant, are comparatively well-toleratedA189207,L38739 and may provide a desirable treatment option for patients struggling with adverse reactions to other preventative therapies.

Struktur Molekul 2D

Berat 603.525
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of atogepant following oral administration is approximately 11 hours.[L38739]
Volume Distribusi The mean apparent volume of distribution of atogepant is 292 L.[L38739]
Klirens (Clearance) The mean apparent oral clearance of atogepant is approximately 19 L/h.[L38739]

Absorpsi

The time to peak plasma concentration following oral administration is approximately 2-3 hours.L38739 Atogepant displays dose-proportional pharmacokinetics up to approximately 3-fold its recommended maximum dosage, and its pharmacokinetics are not significantly influenced by co-administration with food.L38739

Metabolisme

The metabolism of atogepant is mediated primarily via CYP3A4.L38739 The most prevalent circulating compounds in plasma are atogepant itself and a glucuronide conjugate metabolite (M23),L38739 comprising approximately 75% and 15% of the administered dose, respectively,A239069 with at least 10 other metabolites detected in feces representing <10% of the administered dose.

Rute Eliminasi

The elimination of atogepant occurs primarily via metabolism by CYP3A4.L38739 Following a single oral dose of radiolabeled atogepant to healthy male subjects, 42% of the administered dose was recovered as unchanged parent drug in the feces and 5% as unchanged parent drug in the urine.L38739 In total, approximately 81% of the radioactivity was recovered in the feces, with only 8% recovered in the urine.A239069

Interaksi Makanan

1 Data
  • 1. Take with or without food. Co-administration with food does not affect the pharmacokinetics of atogepant to a clinically significant extent.

Interaksi Obat

220 Data
Nelfinavir The serum concentration of Atogepant can be increased when it is combined with Nelfinavir.
Indinavir The serum concentration of Atogepant can be increased when it is combined with Indinavir.
Terfenadine The serum concentration of Atogepant can be increased when it is combined with Terfenadine.
Ritonavir The serum concentration of Atogepant can be increased when it is combined with Ritonavir.
Voriconazole The serum concentration of Atogepant can be increased when it is combined with Voriconazole.
Efavirenz The serum concentration of Atogepant can be increased when it is combined with Efavirenz.
Ergotamine The serum concentration of Atogepant can be increased when it is combined with Ergotamine.
Amprenavir The serum concentration of Atogepant can be increased when it is combined with Amprenavir.
Delavirdine The serum concentration of Atogepant can be increased when it is combined with Delavirdine.
Methimazole The serum concentration of Atogepant can be increased when it is combined with Methimazole.
Conivaptan The serum concentration of Atogepant can be increased when it is combined with Conivaptan.
Tipranavir The serum concentration of Atogepant can be increased when it is combined with Tipranavir.
Telithromycin The serum concentration of Atogepant can be increased when it is combined with Telithromycin.
Ketoconazole The serum concentration of Atogepant can be increased when it is combined with Ketoconazole.
Atazanavir The serum concentration of Atogepant can be increased when it is combined with Atazanavir.
Amiodarone The serum concentration of Atogepant can be increased when it is combined with Amiodarone.
Econazole The serum concentration of Atogepant can be increased when it is combined with Econazole.
Nefazodone The serum concentration of Atogepant can be increased when it is combined with Nefazodone.
Itraconazole The serum concentration of Atogepant can be increased when it is combined with Itraconazole.
Clarithromycin The serum concentration of Atogepant can be increased when it is combined with Clarithromycin.
Saquinavir The serum concentration of Atogepant can be increased when it is combined with Saquinavir.
Posaconazole The serum concentration of Atogepant can be increased when it is combined with Posaconazole.
Darunavir The serum concentration of Atogepant can be increased when it is combined with Darunavir.
Danazol The serum concentration of Atogepant can be increased when it is combined with Danazol.
Lopinavir The serum concentration of Atogepant can be increased when it is combined with Lopinavir.
Ditiocarb The serum concentration of Atogepant can be increased when it is combined with Ditiocarb.
Nilotinib The serum concentration of Atogepant can be increased when it is combined with Nilotinib.
Telaprevir The serum concentration of Atogepant can be increased when it is combined with Telaprevir.
Lonafarnib The serum concentration of Atogepant can be increased when it is combined with Lonafarnib.
Midostaurin The serum concentration of Atogepant can be increased when it is combined with Midostaurin.
Boceprevir The serum concentration of Atogepant can be increased when it is combined with Boceprevir.
Cobicistat The serum concentration of Atogepant can be increased when it is combined with Cobicistat.
Elvitegravir The serum concentration of Atogepant can be increased when it is combined with Elvitegravir.
Stiripentol The serum concentration of Atogepant can be increased when it is combined with Stiripentol.
Curcumin The serum concentration of Atogepant can be increased when it is combined with Curcumin.
Ribociclib The serum concentration of Atogepant can be increased when it is combined with Ribociclib.
Danoprevir The serum concentration of Atogepant can be increased when it is combined with Danoprevir.
Troleandomycin The serum concentration of Atogepant can be increased when it is combined with Troleandomycin.
Phenytoin The serum concentration of Atogepant can be decreased when it is combined with Phenytoin.
Pentobarbital The serum concentration of Atogepant can be decreased when it is combined with Pentobarbital.
Carbamazepine The serum concentration of Atogepant can be decreased when it is combined with Carbamazepine.
Mitotane The serum concentration of Atogepant can be decreased when it is combined with Mitotane.
Primidone The serum concentration of Atogepant can be decreased when it is combined with Primidone.
Rimexolone The serum concentration of Atogepant can be decreased when it is combined with Rimexolone.
Rifampin The serum concentration of Atogepant can be decreased when it is combined with Rifampicin.
Phenobarbital The serum concentration of Atogepant can be decreased when it is combined with Phenobarbital.
Rifapentine The serum concentration of Atogepant can be decreased when it is combined with Rifapentine.
Dexamethasone The serum concentration of Atogepant can be decreased when it is combined with Dexamethasone.
Fosphenytoin The serum concentration of Atogepant can be decreased when it is combined with Fosphenytoin.
St. John's Wort The serum concentration of Atogepant can be decreased when it is combined with St. John's Wort.
Enzalutamide The serum concentration of Atogepant can be decreased when it is combined with Enzalutamide.
Lumacaftor The serum concentration of Atogepant can be decreased when it is combined with Lumacaftor.
Apalutamide The serum concentration of Atogepant can be decreased when it is combined with Apalutamide.
Bexarotene The serum concentration of Atogepant can be decreased when it is combined with Bexarotene.
Bosentan The serum concentration of Atogepant can be decreased when it is combined with Bosentan.
Nafcillin The serum concentration of Atogepant can be decreased when it is combined with Nafcillin.
Modafinil The serum concentration of Atogepant can be decreased when it is combined with Modafinil.
Etravirine The serum concentration of Atogepant can be decreased when it is combined with Etravirine.
Avasimibe The serum concentration of Atogepant can be decreased when it is combined with Avasimibe.
Echinacea The serum concentration of Atogepant can be decreased when it is combined with Echinacea.
Dexamethasone acetate The serum concentration of Atogepant can be decreased when it is combined with Dexamethasone acetate.
Cyclosporine The serum concentration of Atogepant can be increased when it is combined with Cyclosporine.
Valsartan The serum concentration of Atogepant can be increased when it is combined with Valsartan.
Troglitazone The serum concentration of Atogepant can be increased when it is combined with Troglitazone.
Erythromycin The serum concentration of Atogepant can be increased when it is combined with Erythromycin.
Sildenafil The serum concentration of Atogepant can be increased when it is combined with Sildenafil.
Reserpine The serum concentration of Atogepant can be increased when it is combined with Reserpine.
Pantoprazole The serum concentration of Atogepant can be increased when it is combined with Pantoprazole.
Diethylstilbestrol The serum concentration of Atogepant can be increased when it is combined with Diethylstilbestrol.
Conjugated estrogens The serum concentration of Atogepant can be increased when it is combined with Conjugated estrogens.
Indomethacin The serum concentration of Atogepant can be increased when it is combined with Indomethacin.
Digoxin The serum concentration of Atogepant can be increased when it is combined with Digoxin.
Beclomethasone dipropionate The serum concentration of Atogepant can be increased when it is combined with Beclomethasone dipropionate.
Progesterone The serum concentration of Atogepant can be increased when it is combined with Progesterone.
Rosiglitazone The serum concentration of Atogepant can be increased when it is combined with Rosiglitazone.
Cerivastatin The serum concentration of Atogepant can be increased when it is combined with Cerivastatin.
Quinine The serum concentration of Atogepant can be increased when it is combined with Quinine.
Caspofungin The serum concentration of Atogepant can be increased when it is combined with Caspofungin.
Vincristine The serum concentration of Atogepant can be increased when it is combined with Vincristine.
Vinblastine The serum concentration of Atogepant can be increased when it is combined with Vinblastine.
Levocarnitine The serum concentration of Atogepant can be increased when it is combined with Levocarnitine.
Diclofenac The serum concentration of Atogepant can be increased when it is combined with Diclofenac.
Fluticasone propionate The serum concentration of Atogepant can be increased when it is combined with Fluticasone propionate.
Ivermectin The serum concentration of Atogepant can be increased when it is combined with Ivermectin.
Nicardipine The serum concentration of Atogepant can be increased when it is combined with Nicardipine.
Simvastatin The serum concentration of Atogepant can be increased when it is combined with Simvastatin.
Nystatin The serum concentration of Atogepant can be increased when it is combined with Nystatin.
Estrone The serum concentration of Atogepant can be increased when it is combined with Estrone.
Verapamil The metabolism of Atogepant can be decreased when combined with Verapamil.
Irinotecan The serum concentration of Atogepant can be increased when it is combined with Irinotecan.
Roxithromycin The serum concentration of Atogepant can be increased when it is combined with Roxithromycin.
Estradiol The serum concentration of Atogepant can be increased when it is combined with Estradiol.
Sulfasalazine The serum concentration of Atogepant can be increased when it is combined with Sulfasalazine.
Mifepristone The serum concentration of Atogepant can be increased when it is combined with Mifepristone.
Tacrolimus The serum concentration of Atogepant can be increased when it is combined with Tacrolimus.
Sirolimus The serum concentration of Atogepant can be increased when it is combined with Sirolimus.
Quinidine The serum concentration of Atogepant can be increased when it is combined with Quinidine.
Dipyridamole The serum concentration of Atogepant can be increased when it is combined with Dipyridamole.
Novobiocin The serum concentration of Atogepant can be increased when it is combined with Novobiocin.
Atorvastatin The serum concentration of Atogepant can be increased when it is combined with Atorvastatin.

Target Protein

Calcitonin gene-related peptide type 1 receptor CALCRL

Referensi & Sumber

Artikel (PubMed)
  • PMID: 31081399
    Negro A, Martelletti P: Gepants for the treatment of migraine. Expert Opin Investig Drugs. 2019 Jun;28(6):555-567. doi: 10.1080/13543784.2019.1618830. Epub 2019 May 17.
  • PMID: 30475090
    Martelletti P, Giamberardino MA: Advances in orally administered pharmacotherapy for the treatment of migraine. Expert Opin Pharmacother. 2019 Feb;20(2):209-218. doi: 10.1080/14656566.2018.1549223. Epub 2018 Nov 26.
  • PMID: -
    Rowe J, Chan H, Chandrasekar P, Rojo J, Boinpally R: Mass Balance and Metabolism of Carbon-14 Atogepant in Healthy Male Participants. Neurology. 2021 April 13;96(15):Supplement 1425.
  • PMID: 33942560
    Boinpally R, McNamee B, Yao L, Butler M, McGeeney D, Borbridge L, Periclou A: A Single Supratherapeutic Dose of Atogepant Does Not Affect Cardiac Repolarization in Healthy Adults: Results From a Randomized, Single-Dose, Phase 1 Crossover Trial. Clin Pharmacol Drug Dev. 2021 Sep;10(9):1099-1107. doi: 10.1002/cpdd.940. Epub 2021 May 4.
  • PMID: 30600979
    Ha H, Gonzalez A: Migraine Headache Prophylaxis. Am Fam Physician. 2019 Jan 1;99(1):17-24.

Contoh Produk & Brand

Produk: 10 • International brands: 1
Produk
  • Aquipta
    Tablet • 10 mg • Oral • EU • Approved
  • Aquipta
    Tablet • 10 mg • Oral • EU • Approved
  • Aquipta
    Tablet • 60 mg • Oral • EU • Approved
  • Aquipta
    Tablet • 60 mg • Oral • EU • Approved
  • Qulipta
    Tablet • 10 mg • Oral • Canada • Approved
  • Qulipta
    Tablet • 30 mg • Oral • Canada • Approved
  • Qulipta
    Tablet • 60 mg • Oral • Canada • Approved
  • Qulipta
    Tablet • 10 mg/1 • Oral • US • Approved
Menampilkan 8 dari 10 produk.
International Brands
  • Qulipta — AbbVie

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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