Peringatan Keamanan

Safety studies have demonstrated an excellent safety profile and a wide safety margin.A39816 In animal studies, the results of the 2.5-12X overdose were observed as soft-formed or mucous feces, occasionally bloody and vomiting.F2061

Grapiprant

DB12836

small molecule investigational vet_approved

Deskripsi

Grapiprant, also known as AT-001 and CJ-023, is a drug from the piprant class. These molecules were derived from acylsulfonamide and are characterized to be a novel series of para-N-acylaminomethylbenzoic acid known to be prostaglandin receptor antagonists.A39838 This type of molecules is currently in development for veterinary patients.A39816 This class of drugs was defined in 2013 by the World Health Organization.L4766

Grapiprant has been approved in March 2016 by the FDA's Center for Veterinary Medicine as a non-cyclooxygenase inhibiting NSAID for veterinary use.A39836

Struktur Molekul 2D

Berat 491.61
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The reported elimination half-life in animal studies (horse) is of 5.86 hours.[A39836]
Volume Distribusi The reported volume of distribution in animal studies (cats) was reported to be 918 ml/kg.[A39837]
Klirens (Clearance) The reported clearance rate in animal studies (cats) was reported to be 173.2 ml/hr.kg.[A39837]

Absorpsi

Studies in animals (horse) have shown the presence of a concentration >0.005 ng/ml in serum 72 hours after initial administration of a dose of 2 mg/kg. It is rapidly absorbed and the reported Cmax in this reports was 31.9 ng/ml in a Tmax of 1.5 hours and AUC of 2000 ng.hr/ml.A39836 In the case of bioavailability, grapiprant presents a mean bioavailability of 39%.A39837 The bioavailability, time for peak concentration and maximal concentration has been reported to be significantly reduced after food.A39842

Metabolisme

In vitro studies with dog microsomes have reported the identification of four metabolites, an N-deamination metabolite which is the major metabolite in urine and feces, two hydroxylated metabolites and one N-oxidation metabolite.F2060

Rute Eliminasi

Following an oral dose, the majority of the dose an within the first 72 hours.F2060 Studies in animals (horse) have shown the presence of a concentration >0.005 ng/ml in urine 96 hours after initial administration of a dose of 2 mg/kg.A39836 From the excreted dose, 55%, 15% and 19% of the administered dose is excreted in bile, urine, and feces respectively.F2060

Interaksi Obat

236 Data
Ranolazine The serum concentration of Grapiprant can be increased when it is combined with Ranolazine.
Lumacaftor The serum concentration of Grapiprant can be decreased when it is combined with Lumacaftor.
Vemurafenib The serum concentration of Grapiprant can be increased when it is combined with Vemurafenib.
Apalutamide The serum concentration of Grapiprant can be decreased when it is combined with Apalutamide.
Pitolisant The serum concentration of Grapiprant can be increased when it is combined with Pitolisant.
Isavuconazole The serum concentration of Grapiprant can be increased when it is combined with Isavuconazole.
Isavuconazonium The serum concentration of Grapiprant can be increased when it is combined with Isavuconazonium.
Fluconazole The serum concentration of Grapiprant can be increased when it is combined with Fluconazole.
Erythromycin The serum concentration of Grapiprant can be increased when it is combined with Erythromycin.
Sildenafil The serum concentration of Grapiprant can be increased when it is combined with Sildenafil.
Reserpine The serum concentration of Grapiprant can be increased when it is combined with Reserpine.
Sorafenib The serum concentration of Grapiprant can be increased when it is combined with Sorafenib.
Loxapine The serum concentration of Grapiprant can be increased when it is combined with Loxapine.
Quinine The serum concentration of Grapiprant can be increased when it is combined with Quinine.
Ritonavir The serum concentration of Grapiprant can be increased when it is combined with Ritonavir.
Toremifene The serum concentration of Grapiprant can be increased when it is combined with Toremifene.
Verapamil The serum concentration of Grapiprant can be increased when it is combined with Verapamil.
Tamoxifen The serum concentration of Grapiprant can be increased when it is combined with Tamoxifen.
Mifepristone The serum concentration of Grapiprant can be increased when it is combined with Mifepristone.
Vardenafil The serum concentration of Grapiprant can be increased when it is combined with Vardenafil.
Tacrolimus The serum concentration of Grapiprant can be increased when it is combined with Tacrolimus.
Conivaptan The serum concentration of Grapiprant can be increased when it is combined with Conivaptan.
Quinidine The serum concentration of Grapiprant can be increased when it is combined with Quinidine.
Zonisamide The serum concentration of Grapiprant can be increased when it is combined with Zonisamide.
Tipranavir The serum concentration of Grapiprant can be increased when it is combined with Tipranavir.
Ketoconazole The serum concentration of Grapiprant can be increased when it is combined with Ketoconazole.
Amiodarone The serum concentration of Grapiprant can be increased when it is combined with Amiodarone.
Carvedilol The serum concentration of Grapiprant can be increased when it is combined with Carvedilol.
Itraconazole The serum concentration of Grapiprant can be increased when it is combined with Itraconazole.
Propafenone The serum concentration of Grapiprant can be increased when it is combined with Propafenone.
Clarithromycin The serum concentration of Grapiprant can be increased when it is combined with Clarithromycin.
Saquinavir The serum concentration of Grapiprant can be increased when it is combined with Saquinavir.
Lapatinib The serum concentration of Grapiprant can be increased when it is combined with Lapatinib.
Paliperidone The serum concentration of Grapiprant can be increased when it is combined with Paliperidone.
Mibefradil The serum concentration of Grapiprant can be increased when it is combined with Mibefradil.
Lopinavir The serum concentration of Grapiprant can be increased when it is combined with Lopinavir.
Biricodar The serum concentration of Grapiprant can be increased when it is combined with Biricodar.
Dronedarone The serum concentration of Grapiprant can be increased when it is combined with Dronedarone.
Nilotinib The serum concentration of Grapiprant can be increased when it is combined with Nilotinib.
Elacridar The serum concentration of Grapiprant can be increased when it is combined with Elacridar.
Flibanserin The serum concentration of Grapiprant can be increased when it is combined with Flibanserin.
Vandetanib The serum concentration of Grapiprant can be increased when it is combined with Vandetanib.
Telaprevir The serum concentration of Grapiprant can be increased when it is combined with Telaprevir.
Zosuquidar The serum concentration of Grapiprant can be increased when it is combined with Zosuquidar.
Tariquidar The serum concentration of Grapiprant can be increased when it is combined with Tariquidar.
Temsirolimus The serum concentration of Grapiprant can be increased when it is combined with Temsirolimus.
Simeprevir The serum concentration of Grapiprant can be increased when it is combined with Simeprevir.
Brefeldin A The serum concentration of Grapiprant can be increased when it is combined with Brefeldin A.
Ticagrelor The serum concentration of Grapiprant can be increased when it is combined with Ticagrelor.
Ivacaftor The serum concentration of Grapiprant can be increased when it is combined with Ivacaftor.
Lomitapide The serum concentration of Grapiprant can be increased when it is combined with Lomitapide.
Crizotinib The serum concentration of Grapiprant can be increased when it is combined with Crizotinib.
Linagliptin The serum concentration of Grapiprant can be increased when it is combined with Linagliptin.
Regorafenib The serum concentration of Grapiprant can be increased when it is combined with Regorafenib.
Ponatinib The serum concentration of Grapiprant can be increased when it is combined with Ponatinib.
Canagliflozin The serum concentration of Grapiprant can be increased when it is combined with Canagliflozin.
Afatinib The serum concentration of Grapiprant can be increased when it is combined with Afatinib.
Ledipasvir The serum concentration of Grapiprant can be increased when it is combined with Ledipasvir.
Vorapaxar The serum concentration of Grapiprant can be increased when it is combined with Vorapaxar.
Suvorexant The serum concentration of Grapiprant can be increased when it is combined with Suvorexant.
Netupitant The serum concentration of Grapiprant can be increased when it is combined with Netupitant.
Cobicistat The serum concentration of Grapiprant can be increased when it is combined with Cobicistat.
Palbociclib The serum concentration of Grapiprant can be increased when it is combined with Palbociclib.
Daclatasvir The serum concentration of Grapiprant can be increased when it is combined with Daclatasvir.
Niguldipine The serum concentration of Grapiprant can be increased when it is combined with Niguldipine.
Rolapitant The serum concentration of Grapiprant can be increased when it is combined with Rolapitant.
Venetoclax The serum concentration of Grapiprant can be increased when it is combined with Venetoclax.
Velpatasvir The serum concentration of Grapiprant can be increased when it is combined with Velpatasvir.
Neratinib The serum concentration of Grapiprant can be increased when it is combined with Neratinib.
Valspodar The serum concentration of Grapiprant can be increased when it is combined with Valspodar.
Dacomitinib The serum concentration of Grapiprant can be increased when it is combined with Dacomitinib.
Glasdegib The serum concentration of Grapiprant can be increased when it is combined with Glasdegib.
Voxilaprevir The serum concentration of Grapiprant can be increased when it is combined with Voxilaprevir.
Sarecycline The serum concentration of Grapiprant can be increased when it is combined with Sarecycline.
Laniquidar The serum concentration of Grapiprant can be increased when it is combined with Laniquidar.
Enasidenib The serum concentration of Grapiprant can be increased when it is combined with Enasidenib.
Pibrentasvir The serum concentration of Grapiprant can be increased when it is combined with Pibrentasvir.
Glecaprevir The serum concentration of Grapiprant can be increased when it is combined with Glecaprevir.
Dexniguldipine The serum concentration of Grapiprant can be increased when it is combined with Dexniguldipine.
ONT-093 The serum concentration of Grapiprant can be increased when it is combined with ONT-093.
Entrectinib The serum concentration of Grapiprant can be increased when it is combined with Entrectinib.
Fedratinib The serum concentration of Grapiprant can be increased when it is combined with Fedratinib.
Istradefylline The serum concentration of Grapiprant can be increased when it is combined with Istradefylline.
Norgestimate The serum concentration of Grapiprant can be increased when it is combined with Norgestimate.
Carfilzomib The serum concentration of Grapiprant can be increased when it is combined with Carfilzomib.
Asunaprevir The serum concentration of Grapiprant can be increased when it is combined with Asunaprevir.
Favipiravir The serum concentration of Grapiprant can be increased when it is combined with Favipiravir.
Methylene blue The serum concentration of Grapiprant can be increased when it is combined with Methylene blue.
Ripretinib The serum concentration of Grapiprant can be increased when it is combined with Ripretinib.
Pralsetinib The serum concentration of Grapiprant can be increased when it is combined with Pralsetinib.
Lonafarnib The serum concentration of Grapiprant can be increased when it is combined with Lonafarnib.
Clofazimine The serum concentration of Grapiprant can be increased when it is combined with Clofazimine.
Arsenic trioxide The serum concentration of Grapiprant can be increased when it is combined with Arsenic trioxide.
Mefloquine The serum concentration of Grapiprant can be increased when it is combined with Mefloquine.
Cethromycin The serum concentration of Grapiprant can be increased when it is combined with Cethromycin.
Ixabepilone The serum concentration of Grapiprant can be increased when it is combined with Ixabepilone.
Voclosporin The serum concentration of Grapiprant can be increased when it is combined with Voclosporin.
Eliglustat The serum concentration of Grapiprant can be increased when it is combined with Eliglustat.
Umbralisib The serum concentration of Grapiprant can be increased when it is combined with Umbralisib.
Diosmin The serum concentration of Grapiprant can be increased when it is combined with Diosmin.

Target Protein

Prostaglandin E2 receptor EP4 subtype PTGER4

Referensi & Sumber

Artikel (PubMed)
  • PMID: 29067176
    Kirkby Shaw K, Rausch-Derra LC, Rhodes L: Grapiprant: an EP4 prostaglandin receptor antagonist and novel therapy for pain and inflammation. Vet Med Sci. 2015 Dec 21;2(1):3-9. doi: 10.1002/vms3.13. eCollection 2016 Feb.
  • PMID: 21752876
    Woodward DF, Jones RL, Narumiya S: International Union of Basic and Clinical Pharmacology. LXXXIII: classification of prostanoid receptors, updating 15 years of progress. Pharmacol Rev. 2011 Sep;63(3):471-538. doi: 10.1124/pr.110.003517. Epub 2011 Jul 13.
  • PMID: 17495127
    Nakao K, Murase A, Ohshiro H, Okumura T, Taniguchi K, Murata Y, Masuda M, Kato T, Okumura Y, Takada J: CJ-023,423, a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties. J Pharmacol Exp Ther. 2007 Aug;322(2):686-94. doi: 10.1124/jpet.107.122010. Epub 2007 May 10.
  • PMID: 27075237
    Rausch-Derra L, Huebner M, Wofford J, Rhodes L: A Prospective, Randomized, Masked, Placebo-Controlled Multisite Clinical Study of Grapiprant, an EP4 Prostaglandin Receptor Antagonist (PRA), in Dogs with Osteoarthritis. J Vet Intern Med. 2016 May;30(3):756-63. doi: 10.1111/jvim.13948. Epub 2016 Apr 13.
  • PMID: 29575649
    Knych HK, Seminoff K, McKemie DS: Detection and pharmacokinetics of grapiprant following oral administration to exercised Thoroughbred horses. Drug Test Anal. 2018 Mar 25. doi: 10.1002/dta.2378.
  • PMID: 28459136
    Lebkowska-Wieruszewska B, De Vito V, Owen H, Poapholatep A, Giorgi M: Pharmacokinetics of grapiprant, a selective EP4 prostaglandin PGE2 receptor antagonist, after 2 mg/kg oral and i.v. administrations in cats. J Vet Pharmacol Ther. 2017 Dec;40(6):e11-e15. doi: 10.1111/jvp.12414. Epub 2017 Apr 29.
  • PMID: 28169162
    Okumura Y, Yamagishi T, Nukui S, Nakao K: Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist. Bioorg Med Chem Lett. 2017 Mar 1;27(5):1186-1192. doi: 10.1016/j.bmcl.2017.01.067. Epub 2017 Jan 25.
  • PMID: 27691904
    Lebkowska-Wieruszewska B, Barsotti G, Lisowski A, Gazzano A, Owen H, Giorgi M: Pharmacokinetics and estimated bioavailability of grapiprant, a novel selective prostaglandin E2 receptor antagonist, after oral administration in fasted and fed dogs. N Z Vet J. 2017 Jan;65(1):19-23. doi: 10.1080/00480169.2016.1241727. Epub 2016 Oct 19.
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