Peringatan Keamanan

The most common adverse reactions (>5%) are constipation, nausea and abdominal pain.

Eluxadoline

DB09272

small molecule approved investigational

Deskripsi

Eluxadoline is a mixed mu-opioid receptor agonist, kappa-opioid receptor agonist, and a-delta opioid receptor antagonist indicated for use in diarrhea-predominant irritable bowel syndrome (IBS-D). The mu-, kappa-, and delta-opioid receptors mediate endogenous and exogenous opioid response in the central nervous system and peripherally in the gastrointestinal system. Agonism of peripheral mu-opioid receptors results in reduced colonic motility, while antagonism of central delta-opioid receptors results in improved analgesia, making eluxadoline usable for the symptoms of both pain and diarrhea characteristic of IBS-D.

Marketed under the tradename Viberzi (FDA), eluxadoline is an antimotility agent that decreases bowel contractions, inhibits colonic transit, and reduces ?uid/ion secretion resulting in improved symptoms of abdominal pain and reductions in the Bristol Stool Scale.

Struktur Molekul 2D

Berat 569.662
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 plasma elimination half-life ranged from 3.7 hours to 6 hours.
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

The oral absorption of eluxadoline is poor - estimated to be 1.02%, this could be attributed to poor in vitro GI permeability, and its zwitterionic nature leading to a negatively charged molecule across the GI pH range.

Metabolisme

The metabolism of eluxadoline is currently unclear, however evidence suggests limited glucoronidation forms an acyl glucuronide metabolite that is then excreted into urine.

Rute Eliminasi

82% excreted in feces, <1% excreted in urine.

Interaksi Makanan

2 Data
  • 1. Avoid excessive or chronic alcohol consumption. The risk of pancreatitis is increased with excess/chronic alcohol consumption.
  • 2. Take with food.

Interaksi Obat

829 Data
Alvimopan The risk or severity of adverse effects can be increased when Eluxadoline is combined with Alvimopan.
Desmopressin The risk or severity of hyponatremia can be increased when Eluxadoline is combined with Desmopressin.
Pegvisomant The therapeutic efficacy of Pegvisomant can be decreased when used in combination with Eluxadoline.
Succinylcholine The risk or severity of bradycardia can be increased when Succinylcholine is combined with Eluxadoline.
Aspartame The excretion of Eluxadoline can be decreased when combined with Aspartame.
Pravastatin The excretion of Eluxadoline can be decreased when combined with Pravastatin.
Cefotiam The excretion of Eluxadoline can be decreased when combined with Cefotiam.
Liothyronine The excretion of Eluxadoline can be decreased when combined with Liothyronine.
Lansoprazole The excretion of Eluxadoline can be decreased when combined with Lansoprazole.
Cefalotin The excretion of Eluxadoline can be decreased when combined with Cefalotin.
Tenoxicam The excretion of Eluxadoline can be decreased when combined with Tenoxicam.
Cefotaxime The excretion of Eluxadoline can be decreased when combined with Cefotaxime.
Zidovudine The excretion of Eluxadoline can be decreased when combined with Zidovudine.
Cimetidine The excretion of Eluxadoline can be decreased when combined with Cimetidine.
Guanidine The excretion of Eluxadoline can be decreased when combined with Guanidine.
Piroxicam The excretion of Eluxadoline can be decreased when combined with Piroxicam.
Methotrexate The excretion of Eluxadoline can be decreased when combined with Methotrexate.
Cephalexin The excretion of Eluxadoline can be decreased when combined with Cephalexin.
Enalapril The excretion of Eluxadoline can be decreased when combined with Enalapril.
Oxytetracycline The excretion of Eluxadoline can be decreased when combined with Oxytetracycline.
Leucovorin The excretion of Eluxadoline can be decreased when combined with Leucovorin.
Esomeprazole The excretion of Eluxadoline can be decreased when combined with Esomeprazole.
Tetracycline The excretion of Eluxadoline can be decreased when combined with Tetracycline.
Acyclovir The excretion of Eluxadoline can be decreased when combined with Acyclovir.
Phenylbutazone The excretion of Eluxadoline can be decreased when combined with Phenylbutazone.
Cefaclor The excretion of Eluxadoline can be decreased when combined with Cefaclor.
Dinoprostone The excretion of Eluxadoline can be decreased when combined with Dinoprostone.
Famotidine The excretion of Eluxadoline can be decreased when combined with Famotidine.
Salicylic acid The excretion of Eluxadoline can be decreased when combined with Salicylic acid.
Acetylsalicylic acid The excretion of Eluxadoline can be decreased when combined with Acetylsalicylic acid.
Ganciclovir The excretion of Eluxadoline can be decreased when combined with Ganciclovir.
Ketoprofen The excretion of Eluxadoline can be decreased when combined with Ketoprofen.
Minocycline The excretion of Eluxadoline can be decreased when combined with Minocycline.
Probenecid The excretion of Eluxadoline can be decreased when combined with Probenecid.
Mercaptopurine The excretion of Eluxadoline can be decreased when combined with Mercaptopurine.
Benzylpenicillin The excretion of Eluxadoline can be decreased when combined with Benzylpenicillin.
Melatonin The excretion of Eluxadoline can be decreased when combined with Melatonin.
Cefadroxil The excretion of Eluxadoline can be decreased when combined with Cefadroxil.
Ceftriaxone The excretion of Eluxadoline can be decreased when combined with Ceftriaxone.
Cefamandole The excretion of Eluxadoline can be decreased when combined with Cefamandole.
Cefazolin The excretion of Eluxadoline can be decreased when combined with Cefazolin.
Cefoperazone The excretion of Eluxadoline can be decreased when combined with Cefoperazone.
Ceftizoxime The excretion of Eluxadoline can be decreased when combined with Ceftizoxime.
Cefacetrile The excretion of Eluxadoline can be decreased when combined with Cefacetrile.
Ceftibuten The excretion of Eluxadoline can be decreased when combined with Ceftibuten.
Liotrix The excretion of Eluxadoline can be decreased when combined with Liotrix.
Cilastatin The excretion of Eluxadoline can be decreased when combined with Cilastatin.
Tazobactam The excretion of Eluxadoline can be decreased when combined with Tazobactam.
trans-2-hydroxycinnamic acid The excretion of Eluxadoline can be decreased when combined with trans-2-hydroxycinnamic acid.
Topiroxostat The excretion of Eluxadoline can be decreased when combined with Topiroxostat.
Glutaric Acid The excretion of Eluxadoline can be decreased when combined with Glutaric Acid.
Benzoic acid The excretion of Eluxadoline can be decreased when combined with Benzoic acid.
Caprylic acid The excretion of Eluxadoline can be decreased when combined with Caprylic acid.
Ataluren The excretion of Eluxadoline can be decreased when combined with Ataluren.
Dolutegravir The excretion of Eluxadoline can be decreased when combined with Dolutegravir.
Cefaloridine The excretion of Eluxadoline can be decreased when combined with Cefaloridine.
Cabotegravir The excretion of Eluxadoline can be decreased when combined with Cabotegravir.
Apalutamide The serum concentration of Eluxadoline can be decreased when it is combined with Apalutamide.
Letermovir The serum concentration of Eluxadoline can be increased when it is combined with Letermovir.
Pradigastat The excretion of Eluxadoline can be decreased when combined with Pradigastat.
Ibuprofen The excretion of Eluxadoline can be decreased when combined with Ibuprofen.
Favipiravir The excretion of Eluxadoline can be decreased when combined with Favipiravir.
Tafamidis The excretion of Eluxadoline can be decreased when combined with Tafamidis.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Eluxadoline.
Methylnaltrexone Eluxadoline may increase the opioid antagonism activities of Methylnaltrexone.
Naloxegol Eluxadoline may increase the opioid antagonism activities of Naloxegol.
Mirtazapine Eluxadoline may increase the serotonergic activities of Mirtazapine.
Alosetron Alosetron may increase the constipating activities of Eluxadoline.
Valsartan The serum concentration of Eluxadoline can be increased when it is combined with Valsartan.
Troglitazone The serum concentration of Eluxadoline can be increased when it is combined with Troglitazone.
Erythromycin The serum concentration of Eluxadoline can be increased when it is combined with Erythromycin.
Sildenafil The serum concentration of Eluxadoline can be increased when it is combined with Sildenafil.
Reserpine The serum concentration of Eluxadoline can be increased when it is combined with Reserpine.
Pantoprazole The serum concentration of Eluxadoline can be increased when it is combined with Pantoprazole.
Nelfinavir The serum concentration of Eluxadoline can be increased when it is combined with Nelfinavir.
Indinavir The serum concentration of Eluxadoline can be increased when it is combined with Indinavir.
Diethylstilbestrol The serum concentration of Eluxadoline can be increased when it is combined with Diethylstilbestrol.
Conjugated estrogens The serum concentration of Eluxadoline can be increased when it is combined with Conjugated estrogens.
Indomethacin The serum concentration of Eluxadoline can be increased when it is combined with Indomethacin.
Aminohippuric acid The excretion of Eluxadoline can be decreased when combined with Aminohippuric acid.
Digoxin The serum concentration of Eluxadoline can be increased when it is combined with Digoxin.
Beclomethasone dipropionate The serum concentration of Eluxadoline can be increased when it is combined with Beclomethasone dipropionate.
Progesterone The serum concentration of Eluxadoline can be increased when it is combined with Progesterone.
Rosiglitazone The serum concentration of Eluxadoline can be increased when it is combined with Rosiglitazone.
Cerivastatin The serum concentration of Eluxadoline can be increased when it is combined with Cerivastatin.
Quinine The serum concentration of Eluxadoline can be increased when it is combined with Quinine.
Ritonavir The serum concentration of Eluxadoline can be increased when it is combined with Ritonavir.
Caspofungin The serum concentration of Eluxadoline can be increased when it is combined with Caspofungin.
Vincristine The serum concentration of Eluxadoline can be increased when it is combined with Vincristine.
Vinblastine The serum concentration of Eluxadoline can be increased when it is combined with Vinblastine.
Levocarnitine The serum concentration of Eluxadoline can be increased when it is combined with Levocarnitine.
Diclofenac The serum concentration of Eluxadoline can be increased when it is combined with Diclofenac.
Fluticasone propionate The serum concentration of Eluxadoline can be increased when it is combined with Fluticasone propionate.
Ivermectin The serum concentration of Eluxadoline can be increased when it is combined with Ivermectin.
Simvastatin The serum concentration of Eluxadoline can be increased when it is combined with Simvastatin.
Nystatin The serum concentration of Eluxadoline can be increased when it is combined with Nystatin.
Amprenavir The serum concentration of Eluxadoline can be increased when it is combined with Amprenavir.
Irinotecan The serum concentration of Eluxadoline can be increased when it is combined with Irinotecan.
Roxithromycin The serum concentration of Eluxadoline can be increased when it is combined with Roxithromycin.
Estradiol The serum concentration of Eluxadoline can be increased when it is combined with Estradiol.

Target Protein

Mu-type opioid receptor OPRM1
Delta-type opioid receptor OPRD1
Kappa-type opioid receptor OPRK1

Referensi & Sumber

Synthesis reference: Breslin HJ, Diamond CJ, Kavash RW, Cai C, Dyatkin AB, Miskowski TA, Zhang SP, Wade PR, Hornby PJ, He W: Identification of a dual delta OR antagonist/mu OR agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d). Bioorg Med Chem Lett. 2012 Jul 15;22(14):4869-72. doi: 10.1016/j.bmcl.2012.05.042. Epub 2012 May 24. Pubmed(http://www.ncbi.nlm.nih.gov/pubmed/22695132)
Artikel (PubMed)
  • PMID: 26149369
    Garnock-Jones KP: Eluxadoline: First Global Approval. Drugs. 2015 Jul;75(11):1305-10. doi: 10.1007/s40265-015-0436-4.
  • PMID: 26558923
    Nee J, Zakari M, Lembo AJ: Current and emerging drug options in the treatment of diarrhea predominant irritable bowel syndrome. Expert Opin Pharmacother. 2015 Dec;16(18):2781-92. doi: 10.1517/14656566.2015.1101449. Epub 2015 Nov 11.
  • PMID: 23583433
    Dove LS, Lembo A, Randall CW, Fogel R, Andrae D, Davenport JM, McIntyre G, Almenoff JS, Covington PS: Eluxadoline benefits patients with irritable bowel syndrome with diarrhea in a phase 2 study. Gastroenterology. 2013 Aug;145(2):329-38.e1. doi: 10.1053/j.gastro.2013.04.006. Epub 2013 Apr 9.
  • PMID: 25491493
    Davenport JM, Covington P, Bonifacio L, McIntyre G, Venitz J: Effect of uptake transporters OAT3 and OATP1B1 and efflux transporter MRP2 on the pharmacokinetics of eluxadoline. J Clin Pharmacol. 2015 May;55(5):534-42. doi: 10.1002/jcph.442. Epub 2015 Jan 14.
  • PMID: 25261794
    Fujita W, Gomes I, Dove LS, Prohaska D, McIntyre G, Devi LA: Molecular characterization of eluxadoline as a potential ligand targeting mu-delta opioid receptor heteromers. Biochem Pharmacol. 2014 Dec 1;92(3):448-56. doi: 10.1016/j.bcp.2014.09.015. Epub 2014 Sep 28.

Contoh Produk & Brand

Produk: 10 • International brands: 0
Produk
  • Truberzi
    Tablet, film coated • 75 mg • Oral • EU
  • Truberzi
    Tablet, film coated • 75 mg • Oral • EU
  • Truberzi
    Tablet, film coated • 100 mg • Oral • EU
  • Truberzi
    Tablet, film coated • 100 mg • Oral • EU
  • Truberzi
    Tablet, film coated • 75 mg • Oral • EU
  • Truberzi
    Tablet, film coated • 100 mg • Oral • EU
  • Viberzi
    Tablet, film coated • 75 mg/1 • Oral • US • Approved
  • Viberzi
    Tablet, film coated • 100 mg/1 • Oral • US • Approved
Menampilkan 8 dari 10 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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