Peringatan Keamanan

Adverse reactions reported in ?5% of patients treated with saxagliptin and more commonly than in patients treated with placebo are: upper respiratory tract infection, urinary tract infection, and headache.

Saxagliptin

DB06335

small molecule approved

Deskripsi

Saxagliptin (rINN) is an orally active hypoglycemic (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. FDA approved on July 31, 2009.

Struktur Molekul 2D

Berat 315.41
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Saxagliptin = 2.5 hours; 5-hydroxy saxagliptin = 3.1 hours;
Volume Distribusi 151 L
Klirens (Clearance) Renal clearance, single 50 mg dose = 14 L/h

Absorpsi

Following a 5 mg single oral dose of saxagliptin to healthy subjects, the mean plasma AUC values for saxagliptin and its active metabolite were 78 ng•h/mL and 214 ng•h/mL, respectively. The corresponding plasma Cmax values were 24 ng/mL and 47 ng/mL, respectively. Saxagliptin did not accumulate following repeated doses. The median time to maximum concentration (Tmax) following the 5 mg once daily dose was 2 hours for saxagliptin and 4 hours for its active metabolite. Bioavailability, 2.5 - 50 mg dose = 67%

Metabolisme

The metabolism of saxagliptin is primarily mediated by cytochrome P450 3A4/5 (CYP3A4/5). 50% of the absorbed dose will undergo hepatic metabolism. The major metabolite of saxagliptin, 5-hydroxy saxagliptin, is also a DPP4 inhibitor, which is one-half as potent as saxagliptin.

Rute Eliminasi

Saxagliptin is eliminated by both renal and hepatic pathways. Following a single 50 mg dose of 14C-saxagliptin, 24%, 36%, and 75% of the dose was excreted in the urine as saxagliptin, its active metabolite, and total radioactivity, respectively. A total of 22% of the administered radioactivity was recovered in feces representing the fraction of the saxagliptin dose excreted in bile and/or unabsorbed drug from the gastrointestinal tract.

Interaksi Makanan

1 Data
  • 1. Take with food. Food increases total drug exposure.

Interaksi Obat

1444 Data
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Saxagliptin.
Aspartame The excretion of Saxagliptin can be decreased when combined with Aspartame.
Pravastatin The excretion of Saxagliptin can be decreased when combined with Pravastatin.
Valproic acid The excretion of Saxagliptin can be decreased when combined with Valproic acid.
Aminohippuric acid The excretion of Saxagliptin can be decreased when combined with Aminohippuric acid.
Lansoprazole The excretion of Saxagliptin can be decreased when combined with Lansoprazole.
Zidovudine The excretion of Saxagliptin can be decreased when combined with Zidovudine.
Guanidine The excretion of Saxagliptin can be decreased when combined with Guanidine.
Oxytetracycline The excretion of Saxagliptin can be decreased when combined with Oxytetracycline.
Leucovorin The excretion of Saxagliptin can be decreased when combined with Leucovorin.
Esomeprazole The excretion of Saxagliptin can be decreased when combined with Esomeprazole.
Tetracycline The excretion of Saxagliptin can be decreased when combined with Tetracycline.
Dinoprostone The excretion of Saxagliptin can be decreased when combined with Dinoprostone.
Famotidine The excretion of Saxagliptin can be decreased when combined with Famotidine.
Minocycline The excretion of Saxagliptin can be decreased when combined with Minocycline.
Mercaptopurine The excretion of Saxagliptin can be decreased when combined with Mercaptopurine.
Novobiocin The excretion of Saxagliptin can be decreased when combined with Novobiocin.
Benzylpenicillin The excretion of Saxagliptin can be decreased when combined with Benzylpenicillin.
Melatonin The excretion of Saxagliptin can be decreased when combined with Melatonin.
Ouabain The excretion of Saxagliptin can be decreased when combined with Ouabain.
Cilastatin The excretion of Saxagliptin can be decreased when combined with Cilastatin.
Tazobactam The excretion of Saxagliptin can be decreased when combined with Tazobactam.
trans-2-hydroxycinnamic acid The excretion of Saxagliptin can be decreased when combined with trans-2-hydroxycinnamic acid.
Topiroxostat The excretion of Saxagliptin can be decreased when combined with Topiroxostat.
Cholic Acid The excretion of Saxagliptin can be decreased when combined with Cholic Acid.
Glutaric Acid The excretion of Saxagliptin can be decreased when combined with Glutaric Acid.
Benzoic acid The excretion of Saxagliptin can be decreased when combined with Benzoic acid.
Taurocholic acid The excretion of Saxagliptin can be decreased when combined with Taurocholic acid.
Caprylic acid The excretion of Saxagliptin can be decreased when combined with Caprylic acid.
Ataluren The excretion of Saxagliptin can be decreased when combined with Ataluren.
Teriflunomide The excretion of Saxagliptin can be decreased when combined with Teriflunomide.
Dabrafenib The serum concentration of Saxagliptin can be decreased when it is combined with Dabrafenib.
Dolutegravir The excretion of Saxagliptin can be decreased when combined with Dolutegravir.
Lenvatinib The excretion of Saxagliptin can be decreased when combined with Lenvatinib.
Cabotegravir The excretion of Saxagliptin can be decreased when combined with Cabotegravir.
Letermovir The metabolism of Saxagliptin can be decreased when combined with Letermovir.
Rucaparib The metabolism of Saxagliptin can be decreased when combined with Rucaparib.
Pradigastat The excretion of Saxagliptin can be decreased when combined with Pradigastat.
Enasidenib The excretion of Saxagliptin can be decreased when combined with Enasidenib.
Ivosidenib The metabolism of Saxagliptin can be increased when combined with Ivosidenib.
Linezolid The excretion of Saxagliptin can be decreased when combined with Linezolid.
Cefotiam The excretion of Saxagliptin can be decreased when combined with Cefotiam.
Indomethacin The excretion of Saxagliptin can be decreased when combined with Indomethacin.
Cefalotin The excretion of Saxagliptin can be decreased when combined with Cefalotin.
Tenoxicam The excretion of Saxagliptin can be decreased when combined with Tenoxicam.
Cefotaxime The excretion of Saxagliptin can be decreased when combined with Cefotaxime.
Piroxicam The excretion of Saxagliptin can be decreased when combined with Piroxicam.
Methotrexate The excretion of Saxagliptin can be decreased when combined with Methotrexate.
Cephalexin The excretion of Saxagliptin can be decreased when combined with Cephalexin.
Diclofenac The excretion of Saxagliptin can be decreased when combined with Diclofenac.
Acyclovir The excretion of Saxagliptin can be decreased when combined with Acyclovir.
Phenylbutazone The excretion of Saxagliptin can be decreased when combined with Phenylbutazone.
Cefaclor The excretion of Saxagliptin can be decreased when combined with Cefaclor.
Ketoprofen The excretion of Saxagliptin can be decreased when combined with Ketoprofen.
Ibuprofen The excretion of Saxagliptin can be decreased when combined with Ibuprofen.
Cefadroxil The excretion of Saxagliptin can be decreased when combined with Cefadroxil.
Ceftriaxone The excretion of Saxagliptin can be decreased when combined with Ceftriaxone.
Cefamandole The excretion of Saxagliptin can be decreased when combined with Cefamandole.
Cefazolin The excretion of Saxagliptin can be decreased when combined with Cefazolin.
Cefoperazone The excretion of Saxagliptin can be decreased when combined with Cefoperazone.
Ceftizoxime The excretion of Saxagliptin can be decreased when combined with Ceftizoxime.
Cefacetrile The excretion of Saxagliptin can be decreased when combined with Cefacetrile.
Ceftibuten The excretion of Saxagliptin can be decreased when combined with Ceftibuten.
Cefaloridine The excretion of Saxagliptin can be decreased when combined with Cefaloridine.
Pantoprazole The excretion of Saxagliptin can be decreased when combined with Pantoprazole.
Ganciclovir The excretion of Saxagliptin can be decreased when combined with Ganciclovir.
Gemfibrozil The excretion of Saxagliptin can be decreased when combined with Gemfibrozil.
Baricitinib Saxagliptin may decrease the excretion rate of Baricitinib which could result in a higher serum level.
Favipiravir The excretion of Saxagliptin can be decreased when combined with Favipiravir.
Tafamidis The excretion of Saxagliptin can be decreased when combined with Tafamidis.
Lipoic acid The risk or severity of hypoglycemia can be increased when Lipoic acid is combined with Saxagliptin.
Moxifloxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Moxifloxacin.
Grepafloxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Grepafloxacin.
Enoxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Enoxacin.
Pefloxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Pefloxacin.
Ciprofloxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Ciprofloxacin.
Trovafloxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Trovafloxacin.
Nalidixic acid The therapeutic efficacy of Saxagliptin can be increased when used in combination with Nalidixic acid.
Rosoxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Rosoxacin.
Cinoxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Cinoxacin.
Lomefloxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Lomefloxacin.
Gatifloxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Gatifloxacin.
Norfloxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Norfloxacin.
Levofloxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Levofloxacin.
Gemifloxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Gemifloxacin.
Ofloxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Ofloxacin.
Sparfloxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Sparfloxacin.
Temafloxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Temafloxacin.
Fleroxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Fleroxacin.
Technetium Tc-99m ciprofloxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Garenoxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Garenoxacin.
Nemonoxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Nemonoxacin.
Flumequine The therapeutic efficacy of Saxagliptin can be increased when used in combination with Flumequine.
Enrofloxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Enrofloxacin.
Orbifloxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Orbifloxacin.
Sarafloxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Sarafloxacin.
Difloxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Difloxacin.
Pazufloxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Pazufloxacin.
Prulifloxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Prulifloxacin.
Delafloxacin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Delafloxacin.

Target Protein

Dipeptidyl peptidase 4 DPP4

Referensi & Sumber

Synthesis reference: Jack Z. Gougoutas, Mary F. Malley, John D. DiMarco, Xiaotian S. Yin, Chenkou Wei, Jurong Yu, Truc Chi Vu, Gregory Scott Jones, Scott A. Savage, "CRYSTAL FORMS OF SAXAGLIPTIN AND PROCESSES FOR PREPARING SAME." U.S. Patent US20090054303, issued February 26, 2009.
Artikel (PubMed)
  • PMID: 18355324
    Rosenstock J, Sankoh S, List JF: Glucose-lowering activity of the dipeptidyl peptidase-4 inhibitor saxagliptin in drug-naive patients with type 2 diabetes. Diabetes Obes Metab. 2008 May;10(5):376-86. doi: 10.1111/j.1463-1326.2008.00876.x. Epub 2008 Mar 18.
  • PMID: 18227430
    Metzler WJ, Yanchunas J, Weigelt C, Kish K, Klei HE, Xie D, Zhang Y, Corbett M, Tamura JK, He B, Hamann LG, Kirby MS, Marcinkeviciene J: Involvement of DPP-IV catalytic residues in enzyme-saxagliptin complex formation. Protein Sci. 2008 Feb;17(2):240-50. doi: 10.1110/ps.073253208.
  • PMID: 17848846
    Crepaldi G, Carruba M, Comaschi M, Del Prato S, Frajese G, Paolisso G: Dipeptidyl peptidase 4 (DPP-4) inhibitors and their role in Type 2 diabetes management. J Endocrinol Invest. 2007 Jul-Aug;30(7):610-4.
  • PMID: 17073841
    Barnett A: DPP-4 inhibitors and their potential role in the management of type 2 diabetes. Int J Clin Pract. 2006 Nov;60(11):1454-70.
  • PMID: 21042540
    Kulasa K, Edelman S: Saxagliptin: the evidence for its place in the treatment of type 2 diabetes mellitus. Core Evid. 2010 Oct 21;5:23-37.
  • PMID: 23263796
    Russell S: Incretin-based therapies for type 2 diabetes mellitus: a review of direct comparisons of efficacy, safety and patient satisfaction. Int J Clin Pharm. 2013 Apr;35(2):159-72. doi: 10.1007/s11096-012-9729-9. Epub 2012 Dec 22.
  • PMID: 23137182
    Ali S, Fonseca V: Saxagliptin overview: special focus on safety and adverse effects. Expert Opin Drug Saf. 2013 Jan;12(1):103-9. doi: 10.1517/14740338.2013.741584. Epub 2012 Nov 9.
  • PMID: 22686547
    Golightly LK, Drayna CC, McDermott MT: Comparative clinical pharmacokinetics of dipeptidyl peptidase-4 inhibitors. Clin Pharmacokinet. 2012 Aug 1;51(8):501-14. doi: 10.2165/11632930-000000000-00000.

Contoh Produk & Brand

Produk: 81 • International brands: 0
Produk
  • Apo-saxagliptin
    Tablet • 2.5 mg • Oral • Canada • Generic • Approved
  • Apo-saxagliptin
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Kombiglyze XR
    Tablet, film coated, extended release • - • Oral • US • Approved
  • Kombiglyze XR
    Tablet, film coated, extended release • - • Oral • US • Approved
  • Kombiglyze XR
    Tablet, film coated, extended release • - • Oral • US • Approved
  • Kombiglyze XR
    Tablet, film coated, extended release • - • Oral • US • Approved
  • Kombiglyze XR
    Tablet, film coated, extended release • - • Oral • US • Approved
  • Kombiglyze XR
    Tablet, film coated, extended release • - • Oral • US • Approved
Menampilkan 8 dari 81 produk.

Sekuens Gen/Protein (FASTA)

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