Peringatan Keamanan

There is no information available regarding the overdosage and acute toxicity of lotilaner.

Lotilaner

DB17992

small molecule approved vet_approved

Deskripsi

Lotilaner is an ectoparasiticide that is a member of the isoxazoline family of compounds.^L47546 Lotilaner has largely been used for veterinary uses as an antiparasitic agent to treat flea and tick infestations in animals.A260746, L47556 Lotilaner consists of two enantiomers: the S-enantiomer is active in vivo, while the R-enantiomer is reported to exhibit low biological activity. The active ingredient found in drug products of lotilaner is the S-enantiomer.^A260741

On July 25, 2023, lotilaner was approved by the FDA for the treatment of Demodex blepharitis, making it the first and only approved therapeutic for this condition.^L47551

Struktur Molekul 2D

Berat 596.75

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 effective half-life in healthy subjects, which is based on the accumulation ratio over the dosing interval of 12 hours, is 264 hours (11 days).[L47546]

Volume Distribusi No information is available.

Klirens (Clearance) No information is available.

Absorpsi

T_max is about two hours after a single ocular administration on Day 1 and one hour after the last drug administration on Day 42. In healthy subjects, the peak concentration (C_max) in whole blood increased after 42 days of repeated ocular administration, from 0.596 to 17.8 ng/mL. The total exposure (AUC_0-12) also increased from 5.75 to 149 hr x ng/mL.^L47546 In patients with Demodex blepharitis who received lotilaner twice daily for 42 days, the mean systemic exposure at the end of treatment was 12.0 ng/mL, with a range of 0.4-46.1 ng/mL.^L47546

Metabolisme

In cats, mininal metabolism of lotilaner was observed.^A260736 Lotilaner is not metabolized by CYP enzymes.^L47546

Rute Eliminasi

No information is available.

Interaksi Obat

0 Data

Tidak ada data.

Target Protein

Gaba-gated chloride channel, putative 8239847

Referensi & Sumber

Artikel (PubMed)

PMID: 30001724
Toutain CE, Seewald W, Jung M: Pharmacokinetics of lotilaner following a single oral or intravenous administration in cats. Parasit Vectors. 2018 Jul 13;11(1):412. doi: 10.1186/s13071-018-2966-6.
PMID: 29089046
Rufener L, Danelli V, Bertrand D, Sager H: The novel isoxazoline ectoparasiticide lotilaner (Credelio): a non-competitive antagonist specific to invertebrates gamma-aminobutyric acid-gated chloride channels (GABACls). Parasit Vectors. 2017 Nov 1;10(1):530. doi: 10.1186/s13071-017-2470-4.
PMID: 33600484
Lamassiaude N, Toubate B, Neveu C, Charnet P, Dupuy C, Debierre-Grockiego F, Dimier-Poisson I, Charvet CL: The molecular targets of ivermectin and lotilaner in the human louse Pediculus humanus humanus: New prospects for the treatment of pediculosis. PLoS Pathog. 2021 Feb 18;17(2):e1008863. doi: 10.1371/journal.ppat.1008863. eCollection 2021 Feb.

Link

Contoh Produk & Brand

Produk: 1 • International brands: 0

Produk

Xdemvy

Solution / drops • 2.5 mg/1mL • Ophthalmic • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.