Peringatan Keamanan

In case of overdose, general supportive treatments should be initiated and hemodialysis to remove varobactam may be performed.FDA Label In a pharmacokinetic study, mild lethargy observed in the highest-dose group.^A32054

Vaborbactam

DB12107

small molecule approved investigational

Deskripsi

Vaborbactam is a ?-lactamase inhibitor based on a cyclic boronic acid pharmacophore.^A32053 It has been used in trials investigating the treatment of bacterial infections in subjects with varying degrees of renal insufficiency. In August 2017, a combination antibacterial therapy under the market name Vabomere was approved by the FDA for the treatment of adult patients with complicated urinary tract infections (cUTI). Vabomere consists of vaborbactam and Meropenem for intravenous administration. Vaborbactam is added to the therapy to reduce the extent meropenem degradation by inhibiting the serine beta-lactamases expressed by the microorganism of target.Label The treatment aims to resolve infection-related symptoms of cUTI and achieve negative urine culture, when the infections are proven or strongly suspected to be caused by susceptible bacteria.

Struktur Molekul 2D

Berat 297.13

Wujud solid

Peta Jejaring Molekuler

Obat Target Gen Interaksi Enzim Transporter Carrier

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

1. Pendahuluan & Konsep

Fitur visualisasi ini dikembangkan menggunakan pendekatan Graph Theory untuk memetakan hubungan polifarmasi dan molekuler. Entitas (Obat, Target, Gen) direpresentasikan sebagai Simpul (Nodes), sedangkan hubungan biologisnya sebagai Sisi (Edges).

2. Sumber Data (Validasi)

Data Obat: Diekstraksi dari elemen drugbank-id dan name pada skema XML DrugBank.
Target Protein: Diambil dari elemen targets/target yang memuat polipeptida sasaran.
Genetik: Disinkronisasi dari sub-elemen gene-name dan varian snp-effects.
Genetik: Jumlah titik node dibatasi pada maksimal 10 (Slice=10) interaksi untuk menghindari tumpukan data.

3. Algoritma Visualisasi

Tata letak grafik menggunakan algoritma Force-Directed Graph (Barnes-Hut). Model fisika ini menerapkan gaya tolak-menolak antar simpul (Gravitasi: -3000) agar tidak tumpang tindih, serta gaya pegas (Spring: 0.04) pada garis penghubung untuk fleksibilitas interaksi.

4. Legenda Visual

Obat Utama (Pusat Analisis)

Target Protein (Mekanisme)

Gen (Faktor Genetik)

Metode ini mendukung analisis Precision Medicine dan evaluasi risiko Drug-Drug Interaction (DDI).

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of vaborbactam in healthy subjects following multiple 2 g dose administration as a 3-hour infusion was 1.68 hours. The half life of vaborbactam following administration of 2 g by 3 hour infusion was 2.25 hours.[FDA Label]

Volume Distribusi The steady-state volume of distribution of vaborbactam in patients was 18.6 L.[FDA Label]

Klirens (Clearance) The mean renal clearance for vaborbactam was 8.9 L/h. The mean non-renal clearance for vaborbactam was 2.0 L/h indicating nearly complete elimination of vaborbactam by the renal route.[FDA Label] The clearance of vaborbactam in healthy subjects following administration of multiple doses of 2 g as a 3-hour infusion was 10.9 L/h. The clearance of vaborbactam in patients following administration of 2 g by 3 hour infusion was 7.95 L/h.[FDA Label]

Absorpsi

The peak plasma concentrations (Cmax) and AUC of vaborbactam increase in a dose-proportional manner. In healthy adult subjects, the Cmax following administration of multiple 2 g dose as a 3-hour infusion was 55.6 mg/L and AUC was 588 mg•h/L. In patients with the same dosing regimen, the Cmax was 71.3 mg/L and AUC was 835 mg•h/L at steady state.FDA Label The exposure of vaborbactam in terms of Cmax and AUC are not expected to change with repeated dosing, and there was no evidence of accumulation of vaborbactam in plasma in a repeated dosing study.^A32054

Metabolisme

Vaborbactam does not undergo metabolism.FDA Label

Rute Eliminasi

Vaborbactam predominantly undergoes renal excretion, where about 75 to 95% of the dose is excreted unchanged in the urine over a 24 to 48 hour period.FDA Label

Interaksi Obat

726 Data

Cyclosporine	Cyclosporine may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Icosapent	Icosapent may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cefotiam	Cefotiam may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Mesalazine	Mesalazine may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cefmenoxime	Cefmenoxime may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cefmetazole	Cefmetazole may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Pamidronic acid	Pamidronic acid may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Tenofovir disoproxil	Tenofovir disoproxil may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Indomethacin	Indomethacin may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cidofovir	Cidofovir may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cefpiramide	Cefpiramide may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Ceftazidime	Ceftazidime may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Loracarbef	Loracarbef may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cefalotin	Cefalotin may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Nabumetone	Nabumetone may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Ketorolac	Ketorolac may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Tenoxicam	Tenoxicam may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Celecoxib	Celecoxib may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cefotaxime	Cefotaxime may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Tolmetin	Tolmetin may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Foscarnet	Foscarnet may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Rofecoxib	Rofecoxib may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Piroxicam	Piroxicam may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Methotrexate	Methotrexate may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cephalexin	Cephalexin may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Fenoprofen	Fenoprofen may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Valaciclovir	Valaciclovir may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Valdecoxib	Valdecoxib may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Diclofenac	Diclofenac may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Sulindac	Sulindac may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Bacitracin	Bacitracin may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Amphotericin B	Amphotericin B may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cephaloglycin	Cephaloglycin may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Flurbiprofen	Flurbiprofen may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Adefovir dipivoxil	Adefovir dipivoxil may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Pentamidine	Pentamidine may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Etodolac	Etodolac may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Mefenamic acid	Mefenamic acid may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Acyclovir	Acyclovir may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Naproxen	Naproxen may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Sulfasalazine	Sulfasalazine may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Phenylbutazone	Phenylbutazone may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Meloxicam	Meloxicam may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Carprofen	Carprofen may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cefaclor	Cefaclor may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Diflunisal	Diflunisal may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Tacrolimus	Tacrolimus may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Ceforanide	Ceforanide may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Salicylic acid	Salicylic acid may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Meclofenamic acid	Meclofenamic acid may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Acetylsalicylic acid	Acetylsalicylic acid may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Carboplatin	Carboplatin may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Oxaprozin	Oxaprozin may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Ketoprofen	Ketoprofen may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Balsalazide	Balsalazide may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Ibuprofen	Ibuprofen may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cefditoren	Cefditoren may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Atazanavir	Atazanavir may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Colistimethate	Colistimethate may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cefuroxime	Cefuroxime may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cefapirin	Cefapirin may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cefadroxil	Cefadroxil may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cefprozil	Cefprozil may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Ceftriaxone	Ceftriaxone may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Olsalazine	Olsalazine may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Lumiracoxib	Lumiracoxib may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cefamandole	Cefamandole may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cefazolin	Cefazolin may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cefonicid	Cefonicid may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cefoperazone	Cefoperazone may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cefotetan	Cefotetan may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cefoxitin	Cefoxitin may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Ceftizoxime	Ceftizoxime may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cefradine	Cefradine may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Magnesium salicylate	Magnesium salicylate may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Salsalate	Salsalate may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Choline magnesium trisalicylate	Choline magnesium trisalicylate may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cefepime	Cefepime may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cefacetrile	Cefacetrile may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Ceftibuten	Ceftibuten may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cefpodoxime	Cefpodoxime may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Antrafenine	Antrafenine may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Aminophenazone	Aminophenazone may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Antipyrine	Antipyrine may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Tiaprofenic acid	Tiaprofenic acid may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Lopinavir	Lopinavir may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Etoricoxib	Etoricoxib may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Hydrolyzed Cephalothin	Hydrolyzed Cephalothin may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cephalothin Group	Cephalothin Group may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Oxyphenbutazone	Oxyphenbutazone may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Latamoxef	Latamoxef may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Nimesulide	Nimesulide may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Benoxaprofen	Benoxaprofen may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Metamizole	Metamizole may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Zomepirac	Zomepirac may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Ceftobiprole	Ceftobiprole may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Cimicoxib	Cimicoxib may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Ceftaroline fosamil	Ceftaroline fosamil may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Lornoxicam	Lornoxicam may decrease the excretion rate of Vaborbactam which could result in a higher serum level.
Aceclofenac	Aceclofenac may decrease the excretion rate of Vaborbactam which could result in a higher serum level.

Target Protein

Beta-lactamase ampC

Beta-lactamase blaZ

Carbapenem-hydrolyzing beta-lactamase KPC bla

Beta-lactamase KPC-2

Beta-lactamase CTX-M

Beta-lactamase blaSHV

Beta-lactamase SHV-1 bla

Beta-lactamase TEM bla

Beta-lactamase MIR-1

Beta-lactamase fox-7

Referensi & Sumber

Artikel (PubMed)

PMID: 27381386
Castanheira M, Rhomberg PR, Flamm RK, Jones RN: Effect of the beta-Lactamase Inhibitor Vaborbactam Combined with Meropenem against Serine Carbapenemase-Producing Enterobacteriaceae. Antimicrob Agents Chemother. 2016 Aug 22;60(9):5454-8. doi: 10.1128/AAC.00711-16. Print 2016 Sep.
PMID: 28848018
Lomovskaya O, Sun D, Rubio-Aparicio D, Nelson K, Tsivkovski R, Griffith DC, Dudley MN: Vaborbactam: Spectrum of Beta-Lactamase Inhibition and Impact of Resistance Mechanisms on Activity in Enterobacteriaceae. Antimicrob Agents Chemother. 2017 Oct 24;61(11). pii: AAC.01443-17. doi: 10.1128/AAC.01443-17. Print 2017 Nov.
PMID: 27527080
Griffith DC, Loutit JS, Morgan EE, Durso S, Dudley MN: Phase 1 Study of the Safety, Tolerability, and Pharmacokinetics of the beta-Lactamase Inhibitor Vaborbactam (RPX7009) in Healthy Adult Subjects. Antimicrob Agents Chemother. 2016 Sep 23;60(10):6326-32. doi: 10.1128/AAC.00568-16. Print 2016 Oct.

Contoh Produk & Brand

Produk: 3 • International brands: 0

Produk

Vabomere

Injection, powder, for solution • - • Intravenous • US • Approved
Vabomere

Injection, powder, for solution • - • Intravenous • US • Approved
Vaborem

Injection, powder, for solution • - • Intravenous • EU • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.