Peringatan Keamanan

There is limited information on the acute toxicity (LD₅₀) or overdose of enmetazobactam. Symptoms of overdose may include encephalopathy (disturbance of consciousness including confusion, hallucinations, stupor, and coma), myoclonus, seizures, neuromuscular excitability and nonconvulsive status epilepticus. Enmetazobactam can be removed by hemodialysis.^L50117

Enmetazobactam

DB18716

small molecule approved

Deskripsi

Enmetazobactam is a penicillanic acid sulfone extended-spectrum beta (?)-lactamase (ESBL) inhibitor.^A263266 Because ESBL enzymes can hydrolyze important antibiotics such as penicillins, broad-spectrum cephalosporins and monobactams, ESBL-producing bacteria poses challenges in the treatment of serious infections.^A263276

The combination product of enmetazobactam and cefepime was first approved by the FDA on February 23, 2024, for the treatment of complicated urinary tract infections.^L50126 Enmetazobactam is used as cefepime-sparing therapy by preventing its breakdown by ESBL.

Struktur Molekul 2D

Berat 314.32

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 mean (SD) half-life is 2.6 (1.1) hours in patients with cUTI and eGFR greater than or equal to 60 mL/min.[L50117]

Volume Distribusi Mean (SD) steady state volume of distribution (Vss) is 25.26 (9.97) L in patients with cUTI and eGFR greater than or equal to 60 mL/min..[L50117]

Klirens (Clearance) The mean (SD) clearance is 7.6 (2.9) L/h in patients with cUTI and eGFR greater than or equal to 60 mL/min.[L50117]

Absorpsi

The mean (SD) C_max is 19.8 (6.3) µg/mL in patients with cUTI and eGFR greater than or equal to 60 mL/min. The mean AUC_0-last is 75.3 (30.8) ?gxh/mL.^L50117

Metabolisme

Enmetazobactam is minimally metabolized.^L50117

Rute Eliminasi

About 90% of enmetazobactam is excreted unchanged in urine.^L50117

Interaksi Obat

53 Data

BCG vaccine	The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Enmetazobactam.
Typhoid vaccine	The therapeutic efficacy of Typhoid vaccine can be decreased when used in combination with Enmetazobactam.
Dicoumarol	The risk or severity of bleeding can be increased when Enmetazobactam is combined with Dicoumarol.
Phenindione	The risk or severity of bleeding can be increased when Enmetazobactam is combined with Phenindione.
Warfarin	The risk or severity of bleeding can be increased when Enmetazobactam is combined with Warfarin.
Phenprocoumon	The risk or severity of bleeding can be increased when Enmetazobactam is combined with Phenprocoumon.
Acenocoumarol	The risk or severity of bleeding can be increased when Enmetazobactam is combined with Acenocoumarol.
4-hydroxycoumarin	The risk or severity of bleeding can be increased when Enmetazobactam is combined with 4-hydroxycoumarin.
Coumarin	The risk or severity of bleeding can be increased when Enmetazobactam is combined with Coumarin.
(R)-warfarin	The risk or severity of bleeding can be increased when Enmetazobactam is combined with (R)-warfarin.
Ethyl biscoumacetate	The risk or severity of bleeding can be increased when Enmetazobactam is combined with Ethyl biscoumacetate.
Fluindione	The risk or severity of bleeding can be increased when Enmetazobactam is combined with Fluindione.
Clorindione	The risk or severity of bleeding can be increased when Enmetazobactam is combined with Clorindione.
Diphenadione	The risk or severity of bleeding can be increased when Enmetazobactam is combined with Diphenadione.
Tioclomarol	The risk or severity of bleeding can be increased when Enmetazobactam is combined with Tioclomarol.
(S)-Warfarin	The risk or severity of bleeding can be increased when Enmetazobactam is combined with (S)-Warfarin.
Vibrio cholerae CVD 103-HgR strain live antigen	The therapeutic efficacy of Vibrio cholerae CVD 103-HgR strain live antigen can be decreased when used in combination with Enmetazobactam.
Estetrol	The therapeutic efficacy of Estetrol can be decreased when used in combination with Enmetazobactam.
Lidocaine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Lidocaine.
Ropivacaine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Ropivacaine.
Bupivacaine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Bupivacaine.
Cinchocaine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Cinchocaine.
Dyclonine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Dyclonine.
Procaine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Procaine.
Prilocaine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Prilocaine.
Proparacaine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Proparacaine.
Meloxicam	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Meloxicam.
Oxybuprocaine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Oxybuprocaine.
Cocaine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Cocaine.
Mepivacaine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Mepivacaine.
Levobupivacaine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Levobupivacaine.
Diphenhydramine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Diphenhydramine.
Benzocaine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Benzocaine.
Chloroprocaine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Chloroprocaine.
Phenol	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Phenol.
Tetrodotoxin	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Tetrodotoxin.
Ambroxol	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Ambroxol.
Benzyl alcohol	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Benzyl alcohol.
Capsaicin	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Capsaicin.
Etidocaine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Etidocaine.
Articaine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Articaine.
Tetracaine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Tetracaine.
Propoxycaine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Propoxycaine.
Pramocaine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Pramocaine.
Butamben	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Butamben.
Butacaine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Butacaine.
Oxetacaine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Oxetacaine.
Ethyl chloride	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Ethyl chloride.
Butanilicaine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Butanilicaine.
Metabutethamine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Metabutethamine.
Quinisocaine	The risk or severity of methemoglobinemia can be increased when Enmetazobactam is combined with Quinisocaine.
Cisatracurium	Enmetazobactam may increase the neuromuscular blocking activities of Cisatracurium.
Fecal microbiota	The therapeutic efficacy of Fecal microbiota can be decreased when used in combination with Enmetazobactam.

Target Protein

Extended-spectrum beta-lactamase PER-1 per1

Beta-lactamase blaZ

Referensi & Sumber

Artikel (PubMed)

PMID: 32253212
Bernhard F, Odedra R, Sordello S, Cardin R, Franzoni S, Charrier C, Belley A, Warn P, Machacek M, Knechtle P: Pharmacokinetics-Pharmacodynamics of Enmetazobactam Combined with Cefepime in a Neutropenic Murine Thigh Infection Model. Antimicrob Agents Chemother. 2020 May 21;64(6):e00078-20. doi: 10.1128/AAC.00078-20. Print 2020 May 21.
PMID: 16223952
Paterson DL, Bonomo RA: Extended-spectrum beta-lactamases: a clinical update. Clin Microbiol Rev. 2005 Oct;18(4):657-86. doi: 10.1128/CMR.18.4.657-686.2005.
PMID: 12558458
Rupp ME, Fey PD: Extended spectrum beta-lactamase (ESBL)-producing Enterobacteriaceae: considerations for diagnosis, prevention and drug treatment. Drugs. 2003;63(4):353-65. doi: 10.2165/00003495-200363040-00002.

Link

Contoh Produk & Brand

Produk: 2 • International brands: 0

Produk

Exblifep

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

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

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.