Peringatan Keamanan

Most common adverse reactions occurring in >3% of patients receiving moderately emetogenic chemotherapy and combinations of anthracycline and cyclophosphamide included decreased appetite, neutropenia, dizziness, dyspepsia, urinary tract infection, stomatitis, and anemia. Most common adverse reactions occurring in patients receiving cisplatin-based highly emetogenic chemotherapy included neutropenia, hiccups, and abdominal pain.

Rolapitant

DB09291

small molecule approved investigational

Deskripsi

Rolapitant is a potent, highly selective, long-acting Neurokinin-1 (NK-1) receptor antagonist approved for the prevention of delayed chemotherapy-induced nausea and vomiting (CINV) in adults. Delayed-phase CINV typically occurs >24 hours after chemotherapy treatment and is principally mediated by Neurokinin-1 and its ligand Substance P, which is released in the gut following chemotherapy administration. Neurokinin-1 is also known as Tachykinin Receptor 1 (TACR1), Neurokinin 1 Receptor (NK1R), and Substance P Receptor (SPR).
By blocking Substance P from interacting with NK-1 receptors in the gut and the central nervous system, rolapitant prevents late-phase CINV. Unlike other available NK-1 receptor antagonists, rolapitant is not an inhibitor of Cytochrome P450 enzyme CYP3A4 and has a long elimination half-life, allowing a single dose to prevent both acute and late-phase CINV during the first 120 hours post-chemotherapy.

Struktur Molekul 2D

Berat 500.485
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Mean terminal half life ranged from 169 to 183 hours (~7 days).
Volume Distribusi 460 L
Klirens (Clearance) 0.96 L/hour

Absorpsi

Following administration of rolapitant, plasma concentrations reached peak levels in about 4 hours.

Metabolisme

Rolapitant is metabolized primarily by Cytochrome P450 enzyme 3A4 (CYP3A4) to its major active and circulating metabolite M19 (C4-pyrrolidine-hydroxylated rolapitant).

Rute Eliminasi

Rolapitant was found to be 14.2% renally excreted and 73% fecally excreted. Of the fecally excreted compounds

Interaksi Makanan

2 Data
  • 1. Avoid St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of rolapitant.
  • 2. Take with or without food.

Interaksi Obat

511 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Rolapitant.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Rolapitant.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Rolapitant.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Rolapitant.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Rolapitant.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Rolapitant.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Rolapitant.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Rolapitant.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Rolapitant.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Rolapitant.
Silodosin The excretion of Silodosin can be decreased when combined with Rolapitant.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Rolapitant.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Rolapitant.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Rolapitant.
Brexpiprazole The metabolism of Brexpiprazole can be decreased when combined with Rolapitant.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Rolapitant.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Rolapitant.
Pimozide The metabolism of Pimozide can be decreased when combined with Rolapitant.
Vincristine The excretion of Vincristine can be decreased when combined with Rolapitant.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Rolapitant.
Bexarotene The metabolism of Rolapitant can be increased when combined with Bexarotene.
Bosentan The metabolism of Rolapitant can be increased when combined with Bosentan.
Nafcillin The metabolism of Rolapitant can be increased when combined with Nafcillin.
Efavirenz The metabolism of Rolapitant can be increased when combined with Efavirenz.
Modafinil The metabolism of Rolapitant can be increased when combined with Modafinil.
Etravirine The metabolism of Rolapitant can be increased when combined with Etravirine.
Avasimibe The metabolism of Rolapitant can be increased when combined with Avasimibe.
Dexamethasone The metabolism of Rolapitant can be increased when combined with Dexamethasone.
Echinacea The metabolism of Rolapitant can be increased when combined with Echinacea.
Dexamethasone acetate The metabolism of Rolapitant can be increased when combined with Dexamethasone acetate.
Imipramine The metabolism of Imipramine can be decreased when combined with Rolapitant.
Clonidine The metabolism of Clonidine can be decreased when combined with Rolapitant.
Trimipramine The metabolism of Trimipramine can be decreased when combined with Rolapitant.
Gefitinib The metabolism of Gefitinib can be decreased when combined with Rolapitant.
Tamoxifen The metabolism of Tamoxifen can be decreased when combined with Rolapitant.
Ponatinib The metabolism of Ponatinib can be decreased when combined with Rolapitant.
Revefenacin The metabolism of Revefenacin can be decreased when combined with Rolapitant.
Dacomitinib The metabolism of Dacomitinib can be decreased when combined with Rolapitant.
Rucaparib The metabolism of Rucaparib can be decreased when combined with Rolapitant.
Enasidenib The metabolism of Enasidenib can be decreased when combined with Rolapitant.
Citalopram The metabolism of Citalopram can be decreased when combined with Rolapitant.
Metoprolol The metabolism of Metoprolol can be decreased when combined with Rolapitant.
Acetaminophen The metabolism of Acetaminophen can be decreased when combined with Rolapitant.
Olanzapine The metabolism of Olanzapine can be decreased when combined with Rolapitant.
Progesterone The metabolism of Progesterone can be decreased when combined with Rolapitant.
Quinine The metabolism of Quinine can be decreased when combined with Rolapitant.
Chlorpromazine The metabolism of Chlorpromazine can be decreased when combined with Rolapitant.
Erlotinib The metabolism of Erlotinib can be decreased when combined with Rolapitant.
Propranolol The metabolism of Propranolol can be decreased when combined with Rolapitant.
Chloroquine The metabolism of Chloroquine can be decreased when combined with Rolapitant.
Ondansetron The metabolism of Ondansetron can be decreased when combined with Rolapitant.
Nifedipine The metabolism of Nifedipine can be decreased when combined with Rolapitant.
Domperidone The metabolism of Domperidone can be decreased when combined with Rolapitant.
Acebutolol The metabolism of Acebutolol can be decreased when combined with Rolapitant.
Nadolol The metabolism of Nadolol can be decreased when combined with Rolapitant.
Paliperidone The metabolism of Paliperidone can be decreased when combined with Rolapitant.
Debrisoquine The metabolism of Debrisoquine can be decreased when combined with Rolapitant.
Celiprolol The metabolism of Celiprolol can be decreased when combined with Rolapitant.
Fesoterodine The metabolism of Fesoterodine can be decreased when combined with Rolapitant.
Mirabegron The metabolism of Mirabegron can be decreased when combined with Rolapitant.
Umeclidinium The metabolism of Umeclidinium can be decreased when combined with Rolapitant.
Dasabuvir The metabolism of Dasabuvir can be decreased when combined with Rolapitant.
Asunaprevir The metabolism of Asunaprevir can be decreased when combined with Rolapitant.
Talinolol The metabolism of Talinolol can be decreased when combined with Rolapitant.
Elagolix The metabolism of Elagolix can be decreased when combined with Rolapitant.
Nevirapine The metabolism of Nevirapine can be decreased when combined with Rolapitant.
Fluvoxamine The metabolism of Fluvoxamine can be decreased when combined with Rolapitant.
Diltiazem The metabolism of Diltiazem can be decreased when combined with Rolapitant.
Risperidone The metabolism of Risperidone can be decreased when combined with Rolapitant.
Sertraline The metabolism of Sertraline can be decreased when combined with Rolapitant.
Fusidic acid The metabolism of Fusidic acid can be decreased when combined with Rolapitant.
Netupitant The metabolism of Netupitant can be decreased when combined with Rolapitant.
Amphetamine The metabolism of Amphetamine can be decreased when combined with Rolapitant.
Cevimeline The metabolism of Cevimeline can be decreased when combined with Rolapitant.
Esmolol The metabolism of Esmolol can be decreased when combined with Rolapitant.
Bortezomib The metabolism of Bortezomib can be decreased when combined with Rolapitant.
Betaxolol The metabolism of Betaxolol can be decreased when combined with Rolapitant.
Ticlopidine The metabolism of Ticlopidine can be decreased when combined with Rolapitant.
Benzatropine The metabolism of Benzatropine can be decreased when combined with Rolapitant.
Lidocaine The metabolism of Lidocaine can be decreased when combined with Rolapitant.
Venlafaxine The metabolism of Venlafaxine can be decreased when combined with Rolapitant.
Bupivacaine The metabolism of Bupivacaine can be decreased when combined with Rolapitant.
Codeine The metabolism of Codeine can be decreased when combined with Rolapitant.
Atenolol The metabolism of Atenolol can be decreased when combined with Rolapitant.
Chlorzoxazone The metabolism of Chlorzoxazone can be decreased when combined with Rolapitant.
Mirtazapine The metabolism of Mirtazapine can be decreased when combined with Rolapitant.
Palonosetron The metabolism of Palonosetron can be decreased when combined with Rolapitant.
Mexiletine The metabolism of Mexiletine can be decreased when combined with Rolapitant.
Remoxipride The metabolism of Remoxipride can be decreased when combined with Rolapitant.
Promazine The metabolism of Promazine can be decreased when combined with Rolapitant.
Prochlorperazine The metabolism of Prochlorperazine can be decreased when combined with Rolapitant.
Fluoxetine The metabolism of Fluoxetine can be decreased when combined with Rolapitant.
Duloxetine The metabolism of Duloxetine can be decreased when combined with Rolapitant.
Celecoxib The metabolism of Celecoxib can be decreased when combined with Rolapitant.
Sotalol The metabolism of Sotalol can be decreased when combined with Rolapitant.
Oxycodone The metabolism of Oxycodone can be decreased when combined with Rolapitant.
Dextromethorphan The metabolism of Dextromethorphan can be decreased when combined with Rolapitant.
Mephenytoin The metabolism of Mephenytoin can be decreased when combined with Rolapitant.
Amoxapine The metabolism of Amoxapine can be decreased when combined with Rolapitant.
Cinnarizine The metabolism of Cinnarizine can be decreased when combined with Rolapitant.

Target Protein

Substance-P receptor TACR1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 26467681
    Syed YY: Rolapitant: first global approval. Drugs. 2015 Nov;75(16):1941-5. doi: 10.1007/s40265-015-0485-8.
  • PMID: 22497992
    Duffy RA, Morgan C, Naylor R, Higgins GA, Varty GB, Lachowicz JE, Parker EM: Rolapitant (SCH 619734): a potent, selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets. Pharmacol Biochem Behav. 2012 Jul;102(1):95-100. doi: 10.1016/j.pbb.2012.03.021. Epub 2012 Mar 31.
  • PMID: 21385988
    Gan TJ, Gu J, Singla N, Chung F, Pearman MH, Bergese SD, Habib AS, Candiotti KA, Mo Y, Huyck S, Creed MR, Cantillon M: Rolapitant for the prevention of postoperative nausea and vomiting: a prospective, double-blinded, placebo-controlled randomized trial. Anesth Analg. 2011 Apr;112(4):804-12. doi: 10.1213/ANE.0b013e31820886c3. Epub 2011 Mar 8.

Contoh Produk & Brand

Produk: 4 • International brands: 0
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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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