Peringatan Keamanan

There is no information available regarding acute toxicity (LD₅₀) and overdose of trofinetide.

Trofinetide

DB06045

small molecule approved investigational

Deskripsi

Trofinetide is a novel synthetic analog of glypromate, also known as glycine–proline–glutamate (GPE), a naturally occurring protein in the brain and the N-terminal tripeptide of insulin-like growth factor 1 (IGF-1).^A258438 Trofinetide was approved by the FDA on March 10, 2023, for the treatment of Rett syndrome,L45718,L45748 which is an X-linked neurodevelopmental disorder characterized by a range of cognitive, motor, and autonomic symptoms.^A258438 Trofinetide is believed to work by reducing inflammation and apoptosis of neurons.^A258453

Struktur Molekul 2D

Berat 315.326

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 elimination half-life of orally administered trofinetide in healthy subjects is about 1.5 hours.[L45628]

Volume Distribusi Following oral administration, the apparent volume of distribution of trofinetide in healthy adult subjects was approximately 80 L. Minimal to no accumulation was observed following multiple-dose administration.[L45628]

Klirens (Clearance) No information is available.

Absorpsi

Systemic exposure to trofinetide was dose-proportional across the studied dose range. The T_max is about two to three hours after administration. Based on the mass balance study, at least 84% of the administered oral dose of 12,000 mg trofinetide was absorbed.^L45628 A high-fat meal had negligible effects on drug exposure and reduced the C_max by approximately 20%.^L45628

Metabolisme

Trofinetide is not significantly metabolized by CYP450 enzymes. Hepatic metabolism is not a significant route of trofinetide elimination.^L45628

Rute Eliminasi

Trofinetide is primarily excreted in urine, with minor excretion in feces. Approximately 80% of the dose recovered in urine was in the unchanged parent drug form.^L45628

Interaksi Makanan

1 Data

1. Take with or without food. Food decreases Cmax of trofinetide but has negligible effects on total drug exposure.

Interaksi Obat

242 Data

Lomitapide	The metabolism of Lomitapide can be decreased when combined with Trofinetide.
Eluxadoline	The serum concentration of Eluxadoline can be increased when it is combined with Trofinetide.
Pravastatin	The serum concentration of Pravastatin can be increased when it is combined with Trofinetide.
Valsartan	The serum concentration of Valsartan can be increased when it is combined with Trofinetide.
Erythromycin	The serum concentration of Erythromycin can be increased when it is combined with Trofinetide.
Torasemide	The serum concentration of Torasemide can be increased when it is combined with Trofinetide.
Lovastatin	The metabolism of Lovastatin can be decreased when combined with Trofinetide.
Mesalazine	The serum concentration of Mesalazine can be increased when it is combined with Trofinetide.
Liothyronine	The serum concentration of Liothyronine can be increased when it is combined with Trofinetide.
Conjugated estrogens	The serum concentration of Conjugated estrogens can be increased when it is combined with Trofinetide.
Digoxin	The serum concentration of Digoxin can be increased when it is combined with Trofinetide.
Cerivastatin	The serum concentration of Cerivastatin can be increased when it is combined with Trofinetide.
Raloxifene	The serum concentration of Raloxifene can be increased when it is combined with Trofinetide.
Caspofungin	The serum concentration of Caspofungin can be increased when it is combined with Trofinetide.
Bosentan	The serum concentration of Bosentan can be increased when it is combined with Trofinetide.
Methotrexate	The serum concentration of Methotrexate can be increased when it is combined with Trofinetide.
Enalapril	The serum concentration of Enalapril can be increased when it is combined with Trofinetide.
Simvastatin	The serum concentration of Simvastatin can be increased when it is combined with Trofinetide.
Sumatriptan	The serum concentration of Sumatriptan can be increased when it is combined with Trofinetide.
Mycophenolate mofetil	The serum concentration of Mycophenolate mofetil can be increased when it is combined with Trofinetide.
Penicillamine	The serum concentration of Penicillamine can be increased when it is combined with Trofinetide.
Repaglinide	The serum concentration of Repaglinide can be increased when it is combined with Trofinetide.
Dinoprostone	The serum concentration of Dinoprostone can be increased when it is combined with Trofinetide.
Fexofenadine	The serum concentration of Fexofenadine can be increased when it is combined with Trofinetide.
Ezetimibe	The serum concentration of Ezetimibe can be increased when it is combined with Trofinetide.
Benzylpenicillin	The serum concentration of Benzylpenicillin can be increased when it is combined with Trofinetide.
Atorvastatin	The metabolism of Atorvastatin can be decreased when combined with Trofinetide.
Ouabain	The serum concentration of Ouabain can be increased when it is combined with Trofinetide.
Fluvastatin	The serum concentration of Fluvastatin can be increased when it is combined with Trofinetide.
Rosuvastatin	The serum concentration of Rosuvastatin can be increased when it is combined with Trofinetide.
Liotrix	The serum concentration of Liotrix can be increased when it is combined with Trofinetide.
Cholic Acid	The serum concentration of Cholic Acid can be increased when it is combined with Trofinetide.
Taurocholic acid	The serum concentration of Taurocholic acid can be increased when it is combined with Trofinetide.
Atrasentan	The serum concentration of Atrasentan can be increased when it is combined with Trofinetide.
Simeprevir	The serum concentration of Simeprevir can be increased when it is combined with Trofinetide.
Ambrisentan	The serum concentration of Ambrisentan can be increased when it is combined with Trofinetide.
Axitinib	The serum concentration of Axitinib can be increased when it is combined with Trofinetide.
Gimatecan	The serum concentration of Gimatecan can be increased when it is combined with Trofinetide.
Temocapril	The serum concentration of Temocapril can be increased when it is combined with Trofinetide.
Cholecystokinin	The serum concentration of Cholecystokinin can be increased when it is combined with Trofinetide.
Gadoxetic acid	The serum concentration of Gadoxetic acid can be increased when it is combined with Trofinetide.
Technetium Tc-99m mebrofenin	The serum concentration of Technetium Tc-99m mebrofenin can be increased when it is combined with Trofinetide.
Fimasartan	The serum concentration of Fimasartan can be increased when it is combined with Trofinetide.
Paritaprevir	The serum concentration of Paritaprevir can be increased when it is combined with Trofinetide.
Tenofovir alafenamide	The serum concentration of Tenofovir alafenamide can be increased when it is combined with Trofinetide.
Selexipag	The serum concentration of Selexipag can be increased when it is combined with Trofinetide.
Grazoprevir	The serum concentration of Grazoprevir can be increased when it is combined with Trofinetide.
Asunaprevir	The serum concentration of Asunaprevir can be increased when it is combined with Trofinetide.
Revefenacin	Trofinetide may decrease the excretion rate of Revefenacin which could result in a higher serum level.
Elagolix	The serum concentration of Elagolix can be increased when it is combined with Trofinetide.
Voxilaprevir	The serum concentration of Voxilaprevir can be increased when it is combined with Trofinetide.
Letermovir	The serum concentration of Letermovir can be increased when it is combined with Trofinetide.
Brincidofovir	The serum concentration of Brincidofovir can be increased when it is combined with Trofinetide.
Levosalbutamol	The serum concentration of Levosalbutamol can be increased when it is combined with Trofinetide.
Glecaprevir	The serum concentration of Glecaprevir can be increased when it is combined with Trofinetide.
Belantamab mafodotin	The serum concentration of Belantamab mafodotin can be increased when it is combined with Trofinetide.
Atogepant	The serum concentration of Atogepant can be increased when it is combined with Trofinetide.
Azithromycin	The metabolism of Azithromycin can be decreased when combined with Trofinetide.
Ziprasidone	The metabolism of Ziprasidone can be decreased when combined with Trofinetide.
Methysergide	The metabolism of Methysergide can be decreased when combined with Trofinetide.
Terfenadine	The metabolism of Terfenadine can be decreased when combined with Trofinetide.
Meperidine	The metabolism of Meperidine can be decreased when combined with Trofinetide.
Chlorpromazine	The metabolism of Chlorpromazine can be decreased when combined with Trofinetide.
Albendazole	The metabolism of Albendazole can be decreased when combined with Trofinetide.
Cephalexin	The metabolism of Cephalexin can be decreased when combined with Trofinetide.
Doxazosin	The metabolism of Doxazosin can be decreased when combined with Trofinetide.
Cisapride	The metabolism of Cisapride can be decreased when combined with Trofinetide.
Astemizole	The metabolism of Astemizole can be decreased when combined with Trofinetide.
Norethisterone	The metabolism of Norethisterone can be decreased when combined with Trofinetide.
Fenofibrate	The metabolism of Fenofibrate can be decreased when combined with Trofinetide.
Atazanavir	The metabolism of Atazanavir can be decreased when combined with Trofinetide.
Pimozide	The metabolism of Pimozide can be decreased when combined with Trofinetide.
Amiodarone	The metabolism of Amiodarone can be decreased when combined with Trofinetide.
Fosphenytoin	The metabolism of Fosphenytoin can be decreased when combined with Trofinetide.
Drospirenone	The metabolism of Drospirenone can be decreased when combined with Trofinetide.
Allylestrenol	The metabolism of Allylestrenol can be decreased when combined with Trofinetide.
Zuclopenthixol	The metabolism of Zuclopenthixol can be decreased when combined with Trofinetide.
Roflumilast	The serum concentration of Roflumilast can be increased when it is combined with Trofinetide.
Pretomanid	The metabolism of Pretomanid can be decreased when combined with Trofinetide.
Cobimetinib	The metabolism of Cobimetinib can be decreased when combined with Trofinetide.
Pimavanserin	The metabolism of Pimavanserin can be decreased when combined with Trofinetide.
Lacosamide	The metabolism of Lacosamide can be decreased when combined with Trofinetide.
Fosaprepitant	The metabolism of Fosaprepitant can be decreased when combined with Trofinetide.
Linagliptin	The metabolism of Linagliptin can be decreased when combined with Trofinetide.
Vorapaxar	The metabolism of Vorapaxar can be decreased when combined with Trofinetide.
Suvorexant	The metabolism of Suvorexant can be decreased when combined with Trofinetide.
Netupitant	The metabolism of Netupitant can be decreased when combined with Trofinetide.
Idelalisib	The metabolism of Idelalisib can be decreased when combined with Trofinetide.
Ceritinib	The metabolism of Ceritinib can be decreased when combined with Trofinetide.
Tasimelteon	The metabolism of Tasimelteon can be decreased when combined with Trofinetide.
Nintedanib	The metabolism of Nintedanib can be decreased when combined with Trofinetide.
Osimertinib	The metabolism of Osimertinib can be decreased when combined with Trofinetide.
Dihydroergocornine	The metabolism of Dihydroergocornine can be decreased when combined with Trofinetide.
Isavuconazole	The metabolism of Isavuconazole can be decreased when combined with Trofinetide.
Ribociclib	The metabolism of Ribociclib can be decreased when combined with Trofinetide.
Ebastine	The metabolism of Ebastine can be decreased when combined with Trofinetide.
Infigratinib	The metabolism of Infigratinib can be decreased when combined with Trofinetide.
Duvelisib	The metabolism of Duvelisib can be decreased when combined with Trofinetide.
Dacomitinib	The metabolism of Dacomitinib can be decreased when combined with Trofinetide.
Alpelisib	The metabolism of Alpelisib can be decreased when combined with Trofinetide.

Referensi & Sumber

Artikel (PubMed)

PMID: 35149233
Neul JL, Percy AK, Benke TA, Berry-Kravis EM, Glaze DG, Peters SU, Jones NE, Youakim JM: Design and outcome measures of LAVENDER, a phase 3 study of trofinetide for Rett syndrome. Contemp Clin Trials. 2022 Mar;114:106704. doi: 10.1016/j.cct.2022.106704. Epub 2022 Feb 8.
PMID: 19157421
Bickerdike MJ, Thomas GB, Batchelor DC, Sirimanne ES, Leong W, Lin H, Sieg F, Wen J, Brimble MA, Harris PW, Gluckman PD: NNZ-2566: a Gly-Pro-Glu analogue with neuroprotective efficacy in a rat model of acute focal stroke. J Neurol Sci. 2009 Mar 15;278(1-2):85-90. doi: 10.1016/j.jns.2008.12.003. Epub 2009 Jan 20.
PMID: 29489169
Chahil G, Bollu PC: Rett Syndrome. .

Link

Contoh Produk & Brand

Produk: 2 • International brands: 0

Produk

Daybue

Solution • 200 mg / mL • Oral • Canada • Approved
Daybue

Solution • 200 mg/1mL • Oral • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.