Peringatan Keamanan

Multiple doses of 800mg once daily (double the maximum recommended dose) have been administered to healthy volunteers without evidence of overdose symptoms.L39705 In the event of a suspected overdose, administer supportive treatment as clinically indicated.

Sotagliflozin

DB12713

small molecule approved investigational

Deskripsi

Sotagliflozin is a dual inhibitor of SGLT1 and SGLT2, the first of its kind,A244499 which is approved for use in the EU, in combination with insulin, to improve glycemic control in patients with type 1 diabetes mellitus (T1DM) and a BMI ?27 kg/m2.L39705 Its potency in inhibiting SGLT2 is similar to that of other SGLT2 inhibitors, such as canagliflozin and dapagliflozin, but its potency in inhibiting SGLT1 is >10-fold higher than its predecessors.A244499 The added inhibition of intestinal SGLT1 delays glucose absorption in the distal small intestine and colon, thereby reducing post-prandial glucose levels.A244470,A244499

Sotagliflozin was approved by the EMA under the brand name "Zynquista" on April 26, 2019, for the treatment of type 1 diabetes.L39734 A similar approval has also been sought in the US, but the FDA has since published a proposal to refuse the approval because the data submitted did not show that it was safe under the proposed conditions of use.L39739 On March 22, 2022, the marketing authorization of sotagliflozin for the treatment of type 1 diabetes mellitus was withdrawn by the EMA due to commercial reasons.L46616

In May 2023, sotagliflozin was approved by the FDA to reduce the risk of cardiovascular death and heart failure in patients with high risk factors.

Struktur Molekul 2D

Berat 424.94
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 terminal half-life of sotagliflozin ranged from 21 to 35 hours and from 19 to 26 hours for its M19 metabolite.[L39705]
Volume Distribusi Sotagliflozin has a mean apparent volume of distribution of 9392 L.[L39705]
Klirens (Clearance) In healthy volunteers, the mean apparent clearance of sotagliflozin ranged from 261 to 374 L/h.[L39705] The mean apparent clearance estimated in a population of mostly type 1 diabetic patients was 239 L/h.[L39705]

Absorpsi

Following a single dose, the Tmax of sotagliflozin ranged from 1.25 to 3 hours.L39705 Following multiple doses, the Tmax ranged from 2.5 to 4 hours.L39705 The estimated oral bioavailability of sotagliflozin is 71%.L39705

Metabolisme

The major metabolite of sotagliflozin is a 3-O-glucuronide (M19), which comprised ~94% of of the radioactivity in plasma following the oral administration of a radiolabeled dose of sotagliflozin.L39705 The M19 metabolite is effectively inactive, with >275-fold less activity at SGLT1 and SGLT2 compared to the parent drug.L39725 The primary route of metabolism is via glucuronidation by UGT1A9 (and both UGT1A1 and UGT2B7, to a lesser extent) as well as oxidation via CYP3A4.L39705

Rute Eliminasi

Sotagliflozin is primarily eliminated via the renal route, with 57% of administered drug material appearing in the urine and 37% appearing in the feces.L39705

Interaksi Makanan

1 Data
  • 1. Take before a meal. Sotagliflozin should be taken once daily before the first meal of the day.

Interaksi Obat

798 Data
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Sotagliflozin.
Lipoic acid The risk or severity of hypoglycemia can be increased when Lipoic acid is combined with Sotagliflozin.
Moxifloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Moxifloxacin.
Grepafloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Grepafloxacin.
Enoxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Enoxacin.
Pefloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Pefloxacin.
Ciprofloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Ciprofloxacin.
Trovafloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Trovafloxacin.
Nalidixic acid The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Nalidixic acid.
Rosoxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Rosoxacin.
Cinoxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Cinoxacin.
Lomefloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Lomefloxacin.
Gatifloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Gatifloxacin.
Norfloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Norfloxacin.
Levofloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Levofloxacin.
Gemifloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Gemifloxacin.
Ofloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Ofloxacin.
Sparfloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Sparfloxacin.
Temafloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Temafloxacin.
Fleroxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Fleroxacin.
Technetium Tc-99m ciprofloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Garenoxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Garenoxacin.
Nemonoxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Nemonoxacin.
Flumequine The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Flumequine.
Enrofloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Enrofloxacin.
Orbifloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Orbifloxacin.
Sarafloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Sarafloxacin.
Difloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Difloxacin.
Pazufloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Pazufloxacin.
Prulifloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Prulifloxacin.
Delafloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Delafloxacin.
Sitafloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Sitafloxacin.
Oxolinic acid The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Oxolinic acid.
Rufloxacin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Rufloxacin.
Pipemidic acid The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Pipemidic acid.
Methyclothiazide The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Methyclothiazide.
Chlorthalidone The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Chlorthalidone.
Bendroflumethiazide The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Bendroflumethiazide.
Metolazone The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Metolazone.
Benzthiazide The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Benzthiazide.
Hydroflumethiazide The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Hydroflumethiazide.
Indapamide The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Indapamide.
Chlorothiazide The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Chlorothiazide.
Hydrochlorothiazide The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Hydrochlorothiazide.
Trichlormethiazide The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Trichlormethiazide.
Polythiazide The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Polythiazide.
Quinethazone The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Quinethazone.
Cyclopenthiazide The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Cyclopenthiazide.
Epitizide The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Epitizide.
Amitriptyline Amitriptyline may decrease the hypoglycemic activities of Sotagliflozin.
Protriptyline Protriptyline may decrease the hypoglycemic activities of Sotagliflozin.
Imipramine The serum concentration of Imipramine can be increased when it is combined with Sotagliflozin.
Nortriptyline The serum concentration of Nortriptyline can be increased when it is combined with Sotagliflozin.
Amoxapine Amoxapine may decrease the hypoglycemic activities of Sotagliflozin.
Trimipramine The serum concentration of Trimipramine can be increased when it is combined with Sotagliflozin.
Doxepin Doxepin may decrease the hypoglycemic activities of Sotagliflozin.
Desipramine Desipramine may decrease the hypoglycemic activities of Sotagliflozin.
Clomipramine Clomipramine may decrease the hypoglycemic activities of Sotagliflozin.
Amineptine Amineptine may decrease the hypoglycemic activities of Sotagliflozin.
Dimetacrine Dimetacrine may decrease the hypoglycemic activities of Sotagliflozin.
Butriptyline Butriptyline may decrease the hypoglycemic activities of Sotagliflozin.
Dosulepin Dosulepin may decrease the hypoglycemic activities of Sotagliflozin.
Tianeptine Tianeptine may decrease the hypoglycemic activities of Sotagliflozin.
Oxaprotiline Oxaprotiline may decrease the hypoglycemic activities of Sotagliflozin.
Opipramol Opipramol may decrease the hypoglycemic activities of Sotagliflozin.
Amitriptylinoxide Amitriptylinoxide may decrease the hypoglycemic activities of Sotagliflozin.
Dibenzepin Dibenzepin may decrease the hypoglycemic activities of Sotagliflozin.
Quinupramine Quinupramine may decrease the hypoglycemic activities of Sotagliflozin.
Melitracen Melitracen may decrease the hypoglycemic activities of Sotagliflozin.
Lofepramine Lofepramine may decrease the hypoglycemic activities of Sotagliflozin.
Iprindole Iprindole may decrease the hypoglycemic activities of Sotagliflozin.
Imipramine oxide Imipramine oxide may decrease the hypoglycemic activities of Sotagliflozin.
Dapagliflozin Dapagliflozin may increase the hypoglycemic activities of Sotagliflozin.
Canagliflozin Canagliflozin may increase the hypoglycemic activities of Sotagliflozin.
Leuprolide The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Leuprolide.
Goserelin The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Goserelin.
Nelfinavir The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Nelfinavir.
Indinavir The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Indinavir.
Ziprasidone The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Ziprasidone.
Etonogestrel The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Etonogestrel.
Desogestrel The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Desogestrel.
Olanzapine The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Olanzapine.
Megestrol acetate The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Megestrol acetate.
Clozapine The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Clozapine.
Levonorgestrel The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Levonorgestrel.
Progesterone The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Progesterone.
Chlorpromazine The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Chlorpromazine.
Haloperidol The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Haloperidol.
Ritonavir The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Ritonavir.
Piperazine The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Piperazine.
Medroxyprogesterone acetate The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Medroxyprogesterone acetate.
Niacin The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Niacin.
Epinephrine The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Epinephrine.
Norethisterone The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Norethisterone.
Risperidone The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Risperidone.
Pentamidine The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Pentamidine.
Ethynodiol diacetate The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Ethynodiol diacetate.
Pseudoephedrine The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Pseudoephedrine.
Tacrolimus The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Tacrolimus.
Sirolimus The serum concentration of Sirolimus can be increased when it is combined with Sotagliflozin.

Target Protein

Sodium/glucose cotransporter 2 SLC5A2
Sodium/glucose cotransporter 1 SLC5A1

Referensi & Sumber

Synthesis reference: Zhao MM, Zhang H, Iimura S, Bednarz MS, Song Q, Lim N, Yan J, Wu W, Dai K, Gu X, Wang Y: Process Development of Sotagliflozin, a Dual Inhibitor of Sodium–Glucose Cotransporter-1/2 for the Treatment of Diabetes Org Process Res Dev. 2020 Oct 7;24(11):2689-2701.
Artikel (PubMed)
  • PMID: 25690134
    Lapuerta P, Zambrowicz B, Strumph P, Sands A: Development of sotagliflozin, a dual sodium-dependent glucose transporter 1/2 inhibitor. Diab Vasc Dis Res. 2015 Mar;12(2):101-10. doi: 10.1177/1479164114563304.
  • PMID: 30819210
    Cefalo CMA, Cinti F, Moffa S, Impronta F, Sorice GP, Mezza T, Pontecorvi A, Giaccari A: Sotagliflozin, the first dual SGLT inhibitor: current outlook and perspectives. Cardiovasc Diabetol. 2019 Feb 28;18(1):20. doi: 10.1186/s12933-019-0828-y.

Contoh Produk & Brand

Produk: 12 • International brands: 0
Produk
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Menampilkan 8 dari 12 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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