Peringatan Keamanan

While durlobactam is removable by hemodialysis, there is limited clinical information regarding the use of hemodialysis to treat overdosage.^L47336

Durlobactam

DB16704

small molecule approved investigational

Deskripsi

Durlobactam is a diazabicyclooctane non-beta-lactam, beta-lactamase inhibitor. It is typically given in combination with sulbactam to protect it from degradation by certain serine-beta-lactamases.^L47336 The combination product of durlobactam and sulbactam was first approved by the FDA in May 2023.^A263306 It is used to treat hospital-acquired bacterial pneumonia and ventilator-associated bacterial pneumonia (HABP/VABP), caused by susceptible isolates of Acinetobacter baumannii-calcoaceticus complex.^L47336

Struktur Molekul 2D

Berat 277.25

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 elimination half-life of durlobactam was calculated to be 2.52 ± 0.77 h.[L47336]

Volume Distribusi The volume of distribution of durlobactam as stead state (<sub>ss</sub>) was estimated to be 30.3 ± 12.9 L.[L47336]

Klirens (Clearance) The clearance of durlobactam was calculated to be 9.96 ± 3.11 L/h.[L47336]

Absorpsi

Durlobactam demonstrated dose-proportional pharmacokinetics across the dose range studied (0.25 times the recommended single dose to 2 times the recommended single dose infused over 3 hours every 6 hours), with the C_max, AUC_0-24, and AUC_0-6/ELF plasma ratio calculated to be 29.2 ± 13.2 µg/mL, 471 ± 240 h.µg/mL, and 0.37 respectively.^L47336

Metabolisme

Durlobactam is minimally metabolized.^L47336

Rute Eliminasi

The major route of elimination of durlobactam is through the kidney, with 78% of durlobactam excreted unchanged in the urine.^L47336

Interaksi Obat

53 Data

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

Target Protein

Beta-lactamase CTX-M

Referensi & Sumber

Artikel (PubMed)

PMID: 34349751
Shapiro AB, Moussa SH, McLeod SM, Durand-Reville T, Miller AA: Durlobactam, a New Diazabicyclooctane beta-Lactamase Inhibitor for the Treatment of Acinetobacter Infections in Combination With Sulbactam. Front Microbiol. 2021 Jul 19;12:709974. doi: 10.3389/fmicb.2021.709974. eCollection 2021.
PMID: 37125470
Papp-Wallace KM, McLeod SM, Miller AA: Durlobactam, a Broad-Spectrum Serine beta-lactamase Inhibitor, Restores Sulbactam Activity Against Acinetobacter Species. Clin Infect Dis. 2023 May 1;76(Suppl 2):S194-S201. doi: 10.1093/cid/ciad095.
PMID: 37523122
Keam SJ: Sulbactam/Durlobactam: First Approval. Drugs. 2023 Sep;83(13):1245-1252. doi: 10.1007/s40265-023-01920-6.

Link

FDA Approved Drug Products: XACDURO (sulbactam for injection; durlobactam for injection), co-packaged for intravenous use

Contoh Produk & Brand

Produk: 1 • International brands: 0

Produk

Xacduro

Injection, powder, for solution; Injection, powder, lyophilized, for solution; Kit • - • Intravenous • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.