Peringatan Keamanan

The oral LD50 is 500 mg/kg in rats.L48471 There are limited clinical experiences of ertugliflozin overdose. It is recommended to initiate supportive measures in the event of drug overdosage. Removal of ertugliflozin by hemodialysis has not been studied.L48466

Ertugliflozin

DB11827

small molecule approved investigational

Deskripsi

Ertugliflozin is a sodium-dependent glucose cotransporter-2 (SGLT2) inhibitor used to treat type II diabetes mellitus. It works to block glucose reabsorption from the glomerulus.A31581

Ertugliflozin was first approved by the FDA in December 2017.A261951, L1132 It was also approved by the European Commission in March 2018.L48621

Struktur Molekul 2D

Berat 436.89
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal elimination half-life of ertugliflozin ranges from 11 to 17 hours.[A31583] The mean elimination half-life in T2DM patients with normal renal function was estimated to be 16.6 hours based on the population pharmacokinetic analysis.[L48466]
Volume Distribusi The volume of distribution following oral administration was 215.3 L.[L1136] The mean steady-state volume of distribution of ertugliflozin following an intravenous dose is 85.5 L.[L48466]
Klirens (Clearance) In one clinical involving healthy males, the apparent total plasma clearance rate after oral administration of ertugliflozin was 178.7 mL/min and the systemic total plasma clearance after intravenous administration was 187.2 ml/min.[L1136] In another study, the mean systemic plasma clearance following an intravenous 100 µg dose was 11.2 L/hr.[L48466]

Absorpsi

After administering single doses of 5 mg and 15 mg ertugliflozin under fasted conditions, the median Tmax was one hour. Plasma Cmax and AUC of ertugliflozin increase dose-proportionally.L48466 Following administration of a 15 mg dose, the Cmax was 268 ng/mL and the AUC was 1193 ng h/mL.L1136 The absolute oral bioavailability of ertugliflozin following administration of a 15 mg dose was approximately 100%,L48466 though it is reported to range from 70% to 90%.A31583 Administration of ertugliflozin with a high-fat and high-calorie meal decreases ertugliflozin Cmax by 29%. It prolongs Tmax by one hour but does not alter AUC compared to the fasted state. The observed effect of food on ertugliflozin pharmacokinetics is not considered clinically relevant, and ertugliflozin may be administered with or without food.L48466

Metabolisme

Ertugliflozin mainly undergoes O-glucuronidation mediated by UGT1A9 and UGT2B7 to form two pharmacologically inactive glucuronides. About 12% of the drug undergoes CYP-mediated oxidative metabolism.L48466 Several metabolites have been found in plasma, feces, and urine. In plasma, the unchanged form of ertugliflozin was found to be the major component of the administered dose.A31583

Rute Eliminasi

Following administration of an oral 14C-ertugliflozin solution to healthy subjects, approximately 40.9% and 50.2% of the drug-related radioactivity was eliminated in feces and urine, respectively. Only 1.5% of the administered dose was excreted as unchanged ertugliflozin in urine and 33.8% as unchanged ertugliflozin in feces, which is likely due to biliary excretion of glucuronide metabolites and subsequent hydrolysis to form the parent compound.L48466

Interaksi Makanan

2 Data
  • 1. Avoid excessive or chronic alcohol consumption. Alcohol abuse may increase the risk of ketoacidosis.
  • 2. Take with or without food. Food does not significantly affect drug pharmacokinetics. Take the drug the morning.

Interaksi Obat

630 Data
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Ertugliflozin.
Ramipril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Ramipril.
Fosinopril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Fosinopril.
Trandolapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Trandolapril.
Moexipril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Moexipril.
Lisinopril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Lisinopril.
Perindopril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Perindopril.
Quinapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Quinapril.
Omapatrilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Omapatrilat.
Rescinnamine The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Rescinnamine.
Spirapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Spirapril.
Temocapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Temocapril.
Enalaprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Enalaprilat.
Imidapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Imidapril.
Zofenopril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Zofenopril.
Delapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Delapril.
Benazeprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Benazeprilat.
Fosinoprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Fosinoprilat.
Ramiprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Ramiprilat.
Trandolaprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Trandolaprilat.
Moexiprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Moexiprilat.
Perindoprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Perindoprilat.
Quinaprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Quinaprilat.
Enalapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Enalapril.
Captopril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Captopril.
Cilazapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Cilazapril.
Cilazaprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Ertugliflozin is combined with Cilazaprilat.
Lipoic acid The risk or severity of hypoglycemia can be increased when Lipoic acid is combined with Ertugliflozin.
Moxifloxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Moxifloxacin.
Enoxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Enoxacin.
Pefloxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Pefloxacin.
Trovafloxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Trovafloxacin.
Nalidixic acid The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Nalidixic acid.
Rosoxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Rosoxacin.
Cinoxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Cinoxacin.
Lomefloxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Lomefloxacin.
Gatifloxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Gatifloxacin.
Norfloxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Norfloxacin.
Gemifloxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Gemifloxacin.
Ofloxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Ofloxacin.
Temafloxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Temafloxacin.
Fleroxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Fleroxacin.
Technetium Tc-99m ciprofloxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Garenoxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Garenoxacin.
Nemonoxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Nemonoxacin.
Flumequine The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Flumequine.
Enrofloxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Enrofloxacin.
Orbifloxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Orbifloxacin.
Sarafloxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Sarafloxacin.
Difloxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Difloxacin.
Pazufloxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Pazufloxacin.
Prulifloxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Prulifloxacin.
Sitafloxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Sitafloxacin.
Oxolinic acid The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Oxolinic acid.
Rufloxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Rufloxacin.
Pipemidic acid The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Pipemidic acid.
Grepafloxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Grepafloxacin.
Ciprofloxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Ciprofloxacin.
Levofloxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Levofloxacin.
Sparfloxacin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Sparfloxacin.
Methyclothiazide The therapeutic efficacy of Ertugliflozin can be decreased when used in combination with Methyclothiazide.
Chlorthalidone The therapeutic efficacy of Ertugliflozin can be decreased when used in combination with Chlorthalidone.
Bendroflumethiazide The therapeutic efficacy of Ertugliflozin can be decreased when used in combination with Bendroflumethiazide.
Metolazone The therapeutic efficacy of Ertugliflozin can be decreased when used in combination with Metolazone.
Benzthiazide The therapeutic efficacy of Ertugliflozin can be decreased when used in combination with Benzthiazide.
Hydroflumethiazide The therapeutic efficacy of Ertugliflozin can be decreased when used in combination with Hydroflumethiazide.
Indapamide The therapeutic efficacy of Ertugliflozin can be decreased when used in combination with Indapamide.
Chlorothiazide The therapeutic efficacy of Ertugliflozin can be decreased when used in combination with Chlorothiazide.
Hydrochlorothiazide The therapeutic efficacy of Ertugliflozin can be decreased when used in combination with Hydrochlorothiazide.
Trichlormethiazide The therapeutic efficacy of Ertugliflozin can be decreased when used in combination with Trichlormethiazide.
Polythiazide The therapeutic efficacy of Ertugliflozin can be decreased when used in combination with Polythiazide.
Quinethazone The therapeutic efficacy of Ertugliflozin can be decreased when used in combination with Quinethazone.
Cyclopenthiazide The therapeutic efficacy of Ertugliflozin can be decreased when used in combination with Cyclopenthiazide.
Epitizide The therapeutic efficacy of Ertugliflozin can be decreased when used in combination with Epitizide.
Amineptine Amineptine may decrease the hypoglycemic activities of Ertugliflozin.
Dimetacrine Dimetacrine may decrease the hypoglycemic activities of Ertugliflozin.
Butriptyline Butriptyline may decrease the hypoglycemic activities of Ertugliflozin.
Dosulepin Dosulepin may decrease the hypoglycemic activities of Ertugliflozin.
Tianeptine Tianeptine may decrease the hypoglycemic activities of Ertugliflozin.
Oxaprotiline Oxaprotiline may decrease the hypoglycemic activities of Ertugliflozin.
Opipramol Opipramol may decrease the hypoglycemic activities of Ertugliflozin.
Amitriptylinoxide Amitriptylinoxide may decrease the hypoglycemic activities of Ertugliflozin.
Dibenzepin Dibenzepin may decrease the hypoglycemic activities of Ertugliflozin.
Quinupramine Quinupramine may decrease the hypoglycemic activities of Ertugliflozin.
Melitracen Melitracen may decrease the hypoglycemic activities of Ertugliflozin.
Lofepramine Lofepramine may decrease the hypoglycemic activities of Ertugliflozin.
Iprindole Iprindole may decrease the hypoglycemic activities of Ertugliflozin.
Imipramine oxide Imipramine oxide may decrease the hypoglycemic activities of Ertugliflozin.
Protriptyline Protriptyline may decrease the hypoglycemic activities of Ertugliflozin.
Imipramine Imipramine may decrease the hypoglycemic activities of Ertugliflozin.
Nortriptyline Nortriptyline may decrease the hypoglycemic activities of Ertugliflozin.
Amoxapine Amoxapine may decrease the hypoglycemic activities of Ertugliflozin.
Trimipramine Trimipramine may decrease the hypoglycemic activities of Ertugliflozin.
Doxepin Doxepin may decrease the hypoglycemic activities of Ertugliflozin.
Desipramine Desipramine may decrease the hypoglycemic activities of Ertugliflozin.
Clomipramine Clomipramine may decrease the hypoglycemic activities of Ertugliflozin.
Amitriptyline Amitriptyline may decrease the hypoglycemic activities of Ertugliflozin.
Leuprolide The therapeutic efficacy of Ertugliflozin can be decreased when used in combination with Leuprolide.
Goserelin The therapeutic efficacy of Ertugliflozin can be decreased when used in combination with Goserelin.
Torasemide The therapeutic efficacy of Ertugliflozin can be decreased when used in combination with Torasemide.

Target Protein

Sodium/glucose cotransporter 2 SLC5A2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 23169609
    Miao Z, Nucci G, Amin N, Sharma R, Mascitti V, Tugnait M, Vaz AD, Callegari E, Kalgutkar AS: Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects. Drug Metab Dispos. 2013 Feb;41(2):445-56. doi: 10.1124/dmd.112.049551. Epub 2012 Nov 20.
  • PMID: 18996802
    Abdul-Ghani MA, DeFronzo RA: Inhibition of renal glucose reabsorption: a novel strategy for achieving glucose control in type 2 diabetes mellitus. Endocr Pract. 2008 Sep;14(6):782-90. doi: 10.4158/EP.14.6.782.
  • PMID: 21690265
    Kalgutkar AS, Tugnait M, Zhu T, Kimoto E, Miao Z, Mascitti V, Yang X, Tan B, Walsky RL, Chupka J, Feng B, Robinson RP: Preclinical species and human disposition of PF-04971729, a selective inhibitor of the sodium-dependent glucose cotransporter 2 and clinical candidate for the treatment of type 2 diabetes mellitus. Drug Metab Dispos. 2011 Sep;39(9):1609-19. doi: 10.1124/dmd.111.040675. Epub 2011 Jun 20.
  • PMID: 29042751
    Cinti F, Moffa S, Impronta F, Cefalo CM, Sun VA, Sorice GP, Mezza T, Giaccari A: Spotlight on ertugliflozin and its potential in the treatment of type 2 diabetes: evidence to date. Drug Des Devel Ther. 2017 Oct 3;11:2905-2919. doi: 10.2147/DDDT.S114932. eCollection 2017.
  • PMID: 29476348
    Markham A: Ertugliflozin: First Global Approval. Drugs. 2018 Mar;78(4):513-519. doi: 10.1007/s40265-018-0878-6.

Contoh Produk & Brand

Produk: 81 • International brands: 0
Produk
  • Segluromet
    Tablet, film coated • - • Oral • EU • Approved
  • Segluromet
    Tablet, film coated • - • Oral • US • Approved
  • Segluromet
    Tablet, film coated • - • Oral • US • Approved
  • Segluromet
    Tablet, film coated • - • Oral • EU • Approved
  • Segluromet
    Tablet, film coated • - • Oral • EU • Approved
  • Segluromet
    Tablet, film coated • - • Oral • EU • Approved
  • Segluromet
    Tablet, film coated • - • Oral • EU • Approved
  • Segluromet
    Tablet • - • Oral • Canada • Approved
Menampilkan 8 dari 81 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul