Peringatan Keamanan

In case of a bexagliflozin overdose, the FDA product label recommends contacting the Poison Help line or a medical toxicologist for additional overdosage management recommendations. Usual supportive measures based on the patient’s clinical status should be employed. The removal of bexagliflozin by hemodialysis has not been evaluated.L44758 Carcinogenicity was evaluated in mice and rats, and no drug-related neoplastic findings were reported at up to the highest doses, which corresponded to 156 times (mice) and 68 times (rats) the clinical dose of bexagliflozin (20 mg) based on AUC. In vitro and in vivo studies found that bexagliflozin was not mutagenic or clastogenic. Fertility studies done in male and female rats showed that bexagliflozin had no effects on mating, fertility or early embryonic development at up to 200 mg/kg/day, which corresponded to 280 and 439 times the clinical dose of bexagliflozin in males and females, respectively.L44758

Bexagliflozin

DB12236

small molecule approved investigational

Deskripsi

Bexagliflozin is a highly specific and potent sodium-glucose co-transporter 2 (SGLT2) inhibitor.A256408,A256413,L44758 Similar to other SGLT2 inhibitors, bexagliflozin contains three basic moieties: glucose, two benzene rings and a methylene bridge.A256413 SGLT2 is responsible for 60% to 90% of renal glucose re-uptake, and unlike other isoforms such as SGLT1, SGLT2 is mainly expressed in the kidney.A256408 By inhibiting SGLT2, bexagliflozin reduces renal reabsorption of filtered glucose and increases urinary glucose excretion, which reduces blood glucose levels independently of insulin sensitivity.A256423,L44758 In January 2023, bexagliflozin was approved by the FDA for the treatment of adults with type 2 diabetes. Its use is not recommended in patients with type 1 diabetes since it may increase their risk of diabetic ketoacidosis.L44758

Struktur Molekul 2D

Berat 464.94
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Bexagliflozin has an apparent terminal elimination half-life of approximately 12 hours.[L44758]
Volume Distribusi Bexagliflozin has an apparent volume of distribution of 262 L.[L44758]
Klirens (Clearance) Population pharmacokinetic modeling has shown that the apparent oral clearance of bexagliflozin is 19.1 L/h.[L44758]

Absorpsi

Healthy subjects and adult patients with type 2 diabetes mellitus given bexagliflozin have similar pharmacokinetic profiles. In a fasted state, the mean Cmax and AUC0-? of bexagliflozin were 134 ng/mL and 1,162 ng·h/mL, respectively. Bexagliflozin does not follow a time-dependent pharmacokinetic profile, and after multiple doses, approximately up to 20% is accumulated in plasma. The peak plasma concentration of bexagliflozin is reached between 2 and 4 hours after oral administration. This timing can be delayed if bexagliflozin is taken after a meal or with medications that slow gastric emptying. Between single doses of 3 mg and 90 mg (0.15 to 4.5 times the recommended dose), the plasma Cmax and AUC of bexagliflozin increase in a dose-proportional manner.L44758 Compared to dosing in the fasted state, consuming a standard high-fat, high-caloric meal leads to a 31% and 10% higher Cmax and AUC, respectively. Under these conditions, the median Tmax was increased to 5 hours. The effects of food on bexagliflozin pharmacokinetics are not considered clinically relevant.L44758

Metabolisme

Bexagliflozin is metabolized in the liver mainly by UGT1A9 and, to a lesser extent, CYP3A. In healthy volunteers given an oral 14C-bexagliflozin solution, the 3'-O-glucuronide, a pharmacologically inactive metabolite, constituted 32.2% of the parent compound AUC. The rest of the bexagliflozin metabolites contributed less than 10% of the parent AUC. None of the metabolites are expected to have clinically relevant pharmacological effects.A256418,L44758

Rute Eliminasi

Bexagliflozin is mainly eliminated through feces and urine. In healthy subjects given an oral 14C-bexagliflozin solution, 91.6% of input radioactivity was recovered. Of this amount, 51.1% was recovered in feces, mainly as the parent compound, while 40.5% was recovered in urine, mostly as the 3'-O-glucuronide. The proportions of input radioactivity recovered as bexagliflozin in urine and feces were 1.5% and 28.7%, respectively.L44758

Interaksi Makanan

1 Data
  • 1. Take with or without food. Peak plasma concentrations of bexagliflozin can be delayed if taken after a meal; however, the effects of food on bexagliflozin pharmacokinetics are not considered clinically relevant.

Interaksi Obat

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

Target Protein

Sodium/glucose cotransporter 2 SLC5A2

Referensi & Sumber

Synthesis reference: Gharpure, M., et al. (2018). A process for the preparation of SGLT2 inhibitor and intermediates thereof (WO 2018/207113 A1). World Intellectual Property Organization. https://patentimages.storage.googleapis.com/8a/8f/d2/343c7232594398/WO2018207113A1.pdf
Artikel (PubMed)
  • PMID: 21215314
    Zhang W, Welihinda A, Mechanic J, Ding H, Zhu L, Lu Y, Deng Z, Sheng Z, Lv B, Chen Y, Roberge JY, Seed B, Wang YX: EGT1442, a potent and selective SGLT2 inhibitor, attenuates blood glucose and HbA(1c) levels in db/db mice and prolongs the survival of stroke-prone rats. Pharmacol Res. 2011 Apr;63(4):284-93. doi: 10.1016/j.phrs.2011.01.001. Epub 2011 Jan 5.
  • PMID: 34292100
    Azzam O, Carnagarin R, Lugo-Gavidia LM, Nolde J, Matthews VB, Schlaich MP: Bexagliflozin for type 2 diabetes: an overview of the data. Expert Opin Pharmacother. 2021 Nov;22(16):2095-2103. doi: 10.1080/14656566.2021.1959915. Epub 2021 Jul 29.
  • PMID: 31432741
    Zhang W, Li X, Ding H, Lu Y, Stilwell GE, Halvorsen YD, Welihinda A: Metabolism and disposition of the SGLT2 inhibitor bexagliflozin in rats, monkeys and humans. Xenobiotica. 2020 May;50(5):559-569. doi: 10.1080/00498254.2019.1654634. Epub 2019 Aug 27.
  • PMID: 32665641
    Cowie MR, Fisher M: SGLT2 inhibitors: mechanisms of cardiovascular benefit beyond glycaemic control. Nat Rev Cardiol. 2020 Dec;17(12):761-772. doi: 10.1038/s41569-020-0406-8. Epub 2020 Jul 14.
  • PMID: 31101403
    Allegretti AS, Zhang W, Zhou W, Thurber TK, Rigby SP, Bowman-Stroud C, Trescoli C, Serusclat P, Freeman MW, Halvorsen YC: Safety and Effectiveness of Bexagliflozin in Patients With Type 2 Diabetes Mellitus and Stage 3a/3b CKD. Am J Kidney Dis. 2019 Sep;74(3):328-337. doi: 10.1053/j.ajkd.2019.03.417. Epub 2019 May 14.

Contoh Produk & Brand

Produk: 4 • International brands: 1
Produk
  • Bexagliflozin
    Tablet • 20 mg/1 • Oral • US • Generic • Approved
  • Bexagliflozin
    Tablet • 20 mg/1 • Oral • US • Generic • Approved
  • Brenzavvy
    Tablet • 20 mg/1 • Oral • US • Approved
  • Brenzavvy
    Tablet • 20 mg/1 • Oral • US • Approved
International Brands
  • Brenzavvy — TheracosBio

Sekuens Gen/Protein (FASTA)

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