Peringatan Keamanan

There is no specific antidote for rimegepant overdosage and clinical experience is limited.L11971 Treatment should consist of general supportive and symptomatic measures including monitoring of vital signs and general observation. Hemodialysis is unlikely to be of benefit given rimegepant's high serum protein binding.L11971

Rimegepant

DB12457

small molecule approved investigational

Deskripsi

Rimegepant is an oral antagonist of the CGRP receptor developed by Biohaven Pharmaceuticals.L11028 It received FDA approval on February 27, 2020 for the acute treatment migraine headache,L11974 and was subsequently approved by the European Commission in April 2022 for both the treatment and prevention of migraines.L41640 While several parenteral antagonists of CGRP and its receptor have been approved for migraine therapy (e.g. erenumab, fremanezumab, galcanezumab), rimegepant and ubrogepant were the only CGRP antagonists that possessed oral bioavailabilityA189207 until the approval of atogepant in 2021.L38814

The current standard of migraine therapy involves abortive treatment with "triptans", such as sumatriptan, but these medications are contraindicated in patients with pre-existing cerebrovascular and cardiovascular disease due to their vasoconstrictive properties.A189207 Antagonism of the CGRP pathway has become an attractive target for migraine therapy as, unlike the triptans, oral CGRP antagonists have no observed vasoconstrictive properties and are therefore safer for use in patients with contraindications to standard therapy.A189330,A189207

Struktur Molekul 2D

Berat 534.568
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 in healthy subjects is approximately 11 hours.[L11971]
Volume Distribusi At steady state, the volume of distribution is approximately 120 L.[L11971]
Klirens (Clearance) -

Absorpsi

The absolute oral bioavailability of rimegepant is approximately 64%.L11971 Following oral administration of the orally disintegrating tablet, maximum plasma concentrations were achieved at 1.5 hours (Tmax).L11971 When administered with a high-fat meal, Tmax is delayed by 1 hour, Cmax is decreased by 42-53%, and AUC is decreased by 32-38%.L11971 The clinical significance of this difference in pharmacokinetics is unknown.

Metabolisme

Rimegepant is metabolized by CYP3A4 and, to a lesser extent, CYP2C9.L11971 Specific metabolites of rimegepant have not been characterized and no major metabolites have been detected in plasma.L11971 Approximately 77% of an administered dose is eliminated unchanged,L11971 suggesting metabolism is likely to be a minor means of drug elimination.

Rute Eliminasi

Following oral administration of radiolabeled rimegepant in healthy subjects, 78% of the administered radioactivity was recovered in feces and 24% in urine.L11971 Unchanged parent drug was the major component in each, comprising 42% and 51% of the recovered doses, respectively.

Interaksi Makanan

1 Data
  • 1. Take with or without food. Pharmacokinetics may be altered when administered with high-fat meals, but the clinical relevance of these effects is unknown.

Interaksi Obat

457 Data
Venlafaxine Venlafaxine may increase the excretion rate of Rimegepant which could result in a lower serum level and potentially a reduction in efficacy.
Cholesterol Cholesterol may increase the excretion rate of Rimegepant which could result in a lower serum level and potentially a reduction in efficacy.
Metreleptin The metabolism of Rimegepant can be increased when combined with Metreleptin.
Digoxin The serum concentration of Digoxin can be increased when it is combined with Rimegepant.
Vincristine The serum concentration of Vincristine can be increased when it is combined with Rimegepant.
Sirolimus The serum concentration of Sirolimus can be increased when it is combined with Rimegepant.
Digitoxin The serum concentration of Digitoxin can be increased when it is combined with Rimegepant.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Rimegepant.
Bendamustine The serum concentration of Bendamustine can be increased when it is combined with Rimegepant.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Rimegepant.
Binimetinib The serum concentration of Binimetinib can be increased when it is combined with Rimegepant.
Bortezomib The serum concentration of Bortezomib can be increased when it is combined with Rimegepant.
Cabergoline The serum concentration of Cabergoline can be increased when it is combined with Rimegepant.
Gemcitabine The serum concentration of Gemcitabine can be increased when it is combined with Rimegepant.
Imipramine The serum concentration of Imipramine can be increased when it is combined with Rimegepant.
Trimipramine The serum concentration of Trimipramine can be increased when it is combined with Rimegepant.
Axitinib The serum concentration of Axitinib can be increased when it is combined with Rimegepant.
Nortriptyline The serum concentration of Nortriptyline can be increased when it is combined with Rimegepant.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Rimegepant.
Morphine The serum concentration of Rimegepant can be increased when it is combined with Morphine.
Tenofovir disoproxil The serum concentration of Rimegepant can be increased when it is combined with Tenofovir disoproxil.
Bisoprolol The serum concentration of Rimegepant can be increased when it is combined with Bisoprolol.
Mannitol The serum concentration of Rimegepant can be increased when it is combined with Mannitol.
Clomifene The serum concentration of Rimegepant can be increased when it is combined with Clomifene.
Fexofenadine The serum concentration of Rimegepant can be increased when it is combined with Fexofenadine.
Dactinomycin The serum concentration of Dactinomycin can be increased when it is combined with Rimegepant.
Tegaserod The serum concentration of Rimegepant can be increased when it is combined with Tegaserod.
Sitagliptin The serum concentration of Rimegepant can be increased when it is combined with Sitagliptin.
Belinostat The serum concentration of Rimegepant can be increased when it is combined with Belinostat.
Indacaterol The serum concentration of Rimegepant can be increased when it is combined with Indacaterol.
Cobimetinib The serum concentration of Cobimetinib can be increased when it is combined with Rimegepant.
Trastuzumab emtansine The serum concentration of Trastuzumab emtansine can be increased when it is combined with Rimegepant.
Romidepsin The serum concentration of Romidepsin can be increased when it is combined with Rimegepant.
Silodosin The serum concentration of Rimegepant can be increased when it is combined with Silodosin.
Tolvaptan The serum concentration of Tolvaptan can be increased when it is combined with Rimegepant.
Rivaroxaban The serum concentration of Rimegepant can be increased when it is combined with Rivaroxaban.
Ambrisentan The serum concentration of Rimegepant can be increased when it is combined with Ambrisentan.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Rimegepant.
Panobinostat The serum concentration of Panobinostat can be increased when it is combined with Rimegepant.
Apixaban The serum concentration of Rimegepant can be increased when it is combined with Apixaban.
Odanacatib The serum concentration of Rimegepant can be increased when it is combined with Odanacatib.
Pomalidomide The serum concentration of Pomalidomide can be increased when it is combined with Rimegepant.
Dolutegravir The serum concentration of Rimegepant can be increased when it is combined with Dolutegravir.
Sofosbuvir The serum concentration of Rimegepant can be increased when it is combined with Sofosbuvir.
Ceritinib The serum concentration of Ceritinib can be increased when it is combined with Rimegepant.
Edoxaban The serum concentration of Rimegepant can be increased when it is combined with Edoxaban.
Umeclidinium The serum concentration of Rimegepant can be increased when it is combined with Umeclidinium.
Nintedanib The serum concentration of Rimegepant can be increased when it is combined with Nintedanib.
Technetium Tc-99m sestamibi The serum concentration of Rimegepant can be increased when it is combined with Technetium Tc-99m sestamibi.
Ombitasvir The serum concentration of Rimegepant can be increased when it is combined with Ombitasvir.
Selexipag The serum concentration of Rimegepant can be increased when it is combined with Selexipag.
Elbasvir The serum concentration of Rimegepant can be increased when it is combined with Elbasvir.
Grazoprevir The serum concentration of Rimegepant can be increased when it is combined with Grazoprevir.
Vinflunine The serum concentration of Vinflunine can be increased when it is combined with Rimegepant.
Tezacaftor The serum concentration of Rimegepant can be increased when it is combined with Tezacaftor.
Talazoparib The serum concentration of Talazoparib can be increased when it is combined with Rimegepant.
Talinolol The serum concentration of Rimegepant can be increased when it is combined with Talinolol.
Revefenacin The serum concentration of Rimegepant can be increased when it is combined with Revefenacin.
Lemborexant The serum concentration of Rimegepant can be increased when it is combined with Lemborexant.
Duvelisib The serum concentration of Rimegepant can be increased when it is combined with Duvelisib.
Betrixaban The serum concentration of Rimegepant can be increased when it is combined with Betrixaban.
Omadacycline The serum concentration of Rimegepant can be increased when it is combined with Omadacycline.
Lefamulin The serum concentration of Lefamulin can be increased when it is combined with Rimegepant.
Grapiprant The serum concentration of Grapiprant can be increased when it is combined with Rimegepant.
Tazemetostat The serum concentration of Tazemetostat can be increased when it is combined with Rimegepant.
Enfortumab vedotin The serum concentration of Enfortumab vedotin can be increased when it is combined with Rimegepant.
Lusutrombopag The serum concentration of Lusutrombopag can be increased when it is combined with Rimegepant.
Tenofovir The serum concentration of Tenofovir can be increased when it is combined with Rimegepant.
Ubrogepant The serum concentration of Ubrogepant can be increased when it is combined with Rimegepant.
Selumetinib The serum concentration of Rimegepant can be increased when it is combined with Selumetinib.
Dabigatran etexilate The serum concentration of Rimegepant can be increased when it is combined with Dabigatran etexilate.
Idelalisib The serum concentration of Rimegepant can be increased when it is combined with Idelalisib.
Prednisolone phosphate The serum concentration of Prednisolone phosphate can be increased when it is combined with Rimegepant.
Belantamab mafodotin The serum concentration of Belantamab mafodotin can be increased when it is combined with Rimegepant.
Relugolix The serum concentration of Rimegepant can be increased when it is combined with Relugolix.
Lenvatinib The serum concentration of Rimegepant can be increased when it is combined with Lenvatinib.
Trilaciclib The serum concentration of Trilaciclib can be increased when it is combined with Rimegepant.
Colchicine The serum concentration of Rimegepant can be increased when it is combined with Colchicine.
Daptomycin The serum concentration of Rimegepant can be increased when it is combined with Daptomycin.
Loncastuximab tesirine The serum concentration of Loncastuximab tesirine can be increased when it is combined with Rimegepant.
Cenobamate The serum concentration of Rimegepant can be decreased when it is combined with Cenobamate.
Fluvoxamine The metabolism of Rimegepant can be decreased when combined with Fluvoxamine.
Ziprasidone The metabolism of Rimegepant can be decreased when combined with Ziprasidone.
Isradipine The metabolism of Rimegepant can be decreased when combined with Isradipine.
Diltiazem The metabolism of Rimegepant can be decreased when combined with Diltiazem.
Haloperidol The metabolism of Rimegepant can be decreased when combined with Haloperidol.
Ciprofloxacin The metabolism of Rimegepant can be decreased when combined with Ciprofloxacin.
Nicardipine The metabolism of Rimegepant can be decreased when combined with Nicardipine.
Aprepitant The metabolism of Rimegepant can be decreased when combined with Aprepitant.
Isoniazid The metabolism of Rimegepant can be decreased when combined with Isoniazid.
Tioconazole The metabolism of Rimegepant can be decreased when combined with Tioconazole.
Primaquine The metabolism of Rimegepant can be decreased when combined with Primaquine.
Miconazole The metabolism of Rimegepant can be decreased when combined with Miconazole.
Zimelidine The metabolism of Rimegepant can be decreased when combined with Zimelidine.
Milnacipran The metabolism of Rimegepant can be decreased when combined with Milnacipran.
Desvenlafaxine The metabolism of Rimegepant can be decreased when combined with Desvenlafaxine.
Nilvadipine The metabolism of Rimegepant can be decreased when combined with Nilvadipine.
Seproxetine The metabolism of Rimegepant can be decreased when combined with Seproxetine.
Luliconazole The metabolism of Rimegepant can be decreased when combined with Luliconazole.
Indalpine The metabolism of Rimegepant can be decreased when combined with Indalpine.

Target Protein

Calcitonin gene-related peptide type 1 receptor CALCRL

Referensi & Sumber

Synthesis reference: Luo G, Chen L, Conway CM, Kostich W, Macor JE, Dubowchik GM: Asymmetric Synthesis of Heterocyclic Analogues of a CGRP Receptor Antagonist for Treating Migraine. Org Lett. 2015 Dec 18;17(24):5982-5.
Artikel (PubMed)
  • PMID: 31291516
    Lipton RB, Croop R, Stock EG, Stock DA, Morris BA, Frost M, Dubowchik GM, Conway CM, Coric V, Goadsby PJ: Rimegepant, an Oral Calcitonin Gene-Related Peptide Receptor Antagonist, for Migraine. N Engl J Med. 2019 Jul 11;381(2):142-149. doi: 10.1056/NEJMoa1811090.
  • 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: 26650258
    Luo G, Chen L, Conway CM, Kostich W, Macor JE, Dubowchik GM: Asymmetric Synthesis of Heterocyclic Analogues of a CGRP Receptor Antagonist for Treating Migraine. Org Lett. 2015 Dec 18;17(24):5982-5. doi: 10.1021/acs.orglett.5b02921. Epub 2015 Dec 9.

Contoh Produk & Brand

Produk: 6 • International brands: 0
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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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