Peringatan Keamanan

In the event of an overdose via overapplication of sofpironium bromide topical gel, prescribing information recommends washing the area with soap and water.^L51108 Patients experiencing an overdose are likely to exhibit anticholinergic toxicities, including mydriasis (pupil dilation), blurred vision, urinary retention, and temperature dysregulation. Symptoms attributed to sofpironium overdose should be treated symptomatically.^L51108

Sofpironium

DB19325

small molecule approved investigational

Deskripsi

Sofpironium is a "soft" anticholinergic analog of glycopyrronium that has been modified with a readily hydrolyzable ester moiety.^L51109 Soft drugs are designed to reduce systemic toxicity while enhancing local efficacy by employing retrometabolic drug design, in which a molecule contains a metabolically sensitive moiety that promotes rapid metabolism to inactive metabolites after exerting activity at its target site.^A264153 Sofpironium is rapidly converted to a less active metabolite, BBI-4010, after exerting its activity, thereby limiting the incidence and/or severity of systemic anticholinergic effects.L51108,L51109

Sofpironium bromide (Sofdra) was approved by the FDA in June 2024 for the topical treatment of primary axillary hyperhidrosis.L51103,L51108 It has also been available in Japan since 2020 under the brand name Ecclock.^L51103

Struktur Molekul 2D

Berat 390.499

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 _in vitro_ half-life sofpironium in human plasma has been measured at 3.86 hours.[L51109]

Volume Distribusi -

Klirens (Clearance) -

Absorpsi

Following a single topical administration of sofpironium in adult patients, the mean plasma C_max was 2.71 ng/mL, the AUC_0-t was 45.1 ng.hr/mL, and the t_max was 5.34 hours.^L51108 Following a single topical administration of sofpironium in pediatric patients (9 to 16 years of age), the mean plasma C_max was 1.30 ng/mL, the AUC_0-t was 14.6 ng.hr/mL, and the t_max was 4.0 hours.^L51108

Metabolisme

Sofpironium is metabolized by non-enzymatic hydrolysis, oxidative metabolism via CYP2D6 and CYP3A4, and glycine conjugation.^L51108 As a product of retrometabolic drug design, sofpironium includes a metabolically labile ester moiety that is readily hydrolyzed (by plasma paraoxonase 1 (PON1))^A264154 to produce BBI-4010, a less active anticholinergic agent, thereby limiting the risk of systemic adverse effects.^L51109 In plasma, the major component was sofpironium (38%) followed by BBI-4010 (20%).^L51108

Rute Eliminasi

Urinary excretion of sofpironium and BBI-4010 were less than 0.5% of the applied dose.^L51108

Interaksi Obat

188 Data

Tramadol	Sofpironium may increase the anticholinergic activities of Tramadol.
Trospium	Sofpironium may increase the anticholinergic activities of Trospium.
Oxyphenonium	Sofpironium may increase the anticholinergic activities of Oxyphenonium.
Butabarbital	Sofpironium may increase the anticholinergic activities of Butabarbital.
Butalbital	Sofpironium may increase the anticholinergic activities of Butalbital.
Benzatropine	Sofpironium may increase the anticholinergic activities of Benzatropine.
Ziprasidone	Sofpironium may increase the anticholinergic activities of Ziprasidone.
Disopyramide	Sofpironium may increase the anticholinergic activities of Disopyramide.
Talbutal	Sofpironium may increase the anticholinergic activities of Talbutal.
Pentobarbital	Sofpironium may increase the anticholinergic activities of Pentobarbital.
Amitriptyline	Sofpironium may increase the anticholinergic activities of Amitriptyline.
Ipratropium	Sofpironium may increase the anticholinergic activities of Ipratropium.
Methadone	Sofpironium may increase the anticholinergic activities of Methadone.
Olanzapine	Sofpironium may increase the anticholinergic activities of Olanzapine.
Metixene	Sofpironium may increase the anticholinergic activities of Metixene.
Terfenadine	Sofpironium may increase the anticholinergic activities of Terfenadine.
Buclizine	Sofpironium may increase the anticholinergic activities of Buclizine.
Clozapine	Sofpironium may increase the anticholinergic activities of Clozapine.
Doxylamine	Sofpironium may increase the anticholinergic activities of Doxylamine.
Trihexyphenidyl	Sofpironium may increase the anticholinergic activities of Trihexyphenidyl.
Oxyphencyclimine	Sofpironium may increase the anticholinergic activities of Oxyphencyclimine.
Procyclidine	Sofpironium may increase the anticholinergic activities of Procyclidine.
Profenamine	Sofpironium may increase the anticholinergic activities of Profenamine.
Metocurine iodide	Sofpironium may increase the anticholinergic activities of Metocurine iodide.
Secobarbital	Sofpironium may increase the anticholinergic activities of Secobarbital.
Promazine	Sofpironium may increase the anticholinergic activities of Promazine.
Hyoscyamine	Sofpironium may increase the anticholinergic activities of Hyoscyamine.
Cyproheptadine	Sofpironium may increase the anticholinergic activities of Cyproheptadine.
Imipramine	Sofpironium may increase the anticholinergic activities of Imipramine.
Methscopolamine bromide	Sofpironium may increase the anticholinergic activities of Methscopolamine bromide.
Metharbital	Sofpironium may increase the anticholinergic activities of Metharbital.
Fluoxetine	Sofpironium may increase the anticholinergic activities of Fluoxetine.
Chlorpromazine	Sofpironium may increase the anticholinergic activities of Chlorpromazine.
Gallamine triethiodide	Sofpironium may increase the anticholinergic activities of Gallamine triethiodide.
Darifenacin	Sofpironium may increase the anticholinergic activities of Darifenacin.
Tridihexethyl	Sofpironium may increase the anticholinergic activities of Tridihexethyl.
Triflupromazine	Sofpironium may increase the anticholinergic activities of Triflupromazine.
Dextromethorphan	Sofpironium may increase the anticholinergic activities of Dextromethorphan.
Anisotropine methylbromide	Sofpironium may increase the anticholinergic activities of Anisotropine methylbromide.
Nortriptyline	Sofpironium may increase the anticholinergic activities of Nortriptyline.
Amoxapine	Sofpironium may increase the anticholinergic activities of Amoxapine.
Cisatracurium	Sofpironium may increase the anticholinergic activities of Cisatracurium.
Atropine	Sofpironium may increase the anticholinergic activities of Atropine.
Thiopental	Sofpironium may increase the anticholinergic activities of Thiopental.
Nicardipine	Sofpironium may increase the anticholinergic activities of Nicardipine.
Mecamylamine	Sofpironium may increase the anticholinergic activities of Mecamylamine.
Pirenzepine	Sofpironium may increase the anticholinergic activities of Pirenzepine.
Paroxetine	Sofpironium may increase the anticholinergic activities of Paroxetine.
Azatadine	Sofpironium may increase the anticholinergic activities of Azatadine.
Procaine	Sofpironium may increase the anticholinergic activities of Procaine.
Homatropine methylbromide	Sofpironium may increase the anticholinergic activities of Homatropine methylbromide.
Rocuronium	Sofpironium may increase the anticholinergic activities of Rocuronium.
Atracurium besylate	Sofpironium may increase the anticholinergic activities of Atracurium besylate.
Meclizine	Sofpironium may increase the anticholinergic activities of Meclizine.
Scopolamine	Sofpironium may increase the anticholinergic activities of Scopolamine.
Isoflurane	Sofpironium may increase the anticholinergic activities of Isoflurane.
Benzquinamide	Sofpironium may increase the anticholinergic activities of Benzquinamide.
Clidinium	Sofpironium may increase the anticholinergic activities of Clidinium.
Propiomazine	Sofpironium may increase the anticholinergic activities of Propiomazine.
Propantheline	Sofpironium may increase the anticholinergic activities of Propantheline.
Primidone	Sofpironium may increase the anticholinergic activities of Primidone.
Dicyclomine	Sofpironium may increase the anticholinergic activities of Dicyclomine.
Tropicamide	Sofpironium may increase the anticholinergic activities of Tropicamide.
Biperiden	Sofpironium may increase the anticholinergic activities of Biperiden.
Brompheniramine	Sofpironium may increase the anticholinergic activities of Brompheniramine.
Methylphenobarbital	Sofpironium may increase the anticholinergic activities of Methylphenobarbital.
Cocaine	Sofpironium may increase the anticholinergic activities of Cocaine.
Quinidine	Sofpironium may increase the anticholinergic activities of Quinidine.
Amantadine	Sofpironium may increase the anticholinergic activities of Amantadine.
Maprotiline	Sofpironium may increase the anticholinergic activities of Maprotiline.
Methantheline	Sofpironium may increase the anticholinergic activities of Methantheline.
Hexafluronium	Sofpironium may increase the anticholinergic activities of Hexafluronium.
Cycrimine	Sofpironium may increase the anticholinergic activities of Cycrimine.
Desloratadine	Sofpironium may increase the anticholinergic activities of Desloratadine.
Cyclopentolate	Sofpironium may increase the anticholinergic activities of Cyclopentolate.
Glycopyrronium	Sofpironium may increase the anticholinergic activities of Glycopyrronium.
Tolterodine	Sofpironium may increase the anticholinergic activities of Tolterodine.
Oxybutynin	Sofpironium may increase the anticholinergic activities of Oxybutynin.
Promethazine	Sofpironium may increase the anticholinergic activities of Promethazine.
Diphenhydramine	Sofpironium may increase the anticholinergic activities of Diphenhydramine.
Pentolinium	Sofpironium may increase the anticholinergic activities of Pentolinium.
Trimethaphan	Sofpironium may increase the anticholinergic activities of Trimethaphan.
Doxacurium	Sofpironium may increase the anticholinergic activities of Doxacurium.
Doxepin	Sofpironium may increase the anticholinergic activities of Doxepin.
Flavoxate	Sofpironium may increase the anticholinergic activities of Flavoxate.
Desipramine	Sofpironium may increase the anticholinergic activities of Desipramine.
Orphenadrine	Sofpironium may increase the anticholinergic activities of Orphenadrine.
Phenobarbital	Sofpironium may increase the anticholinergic activities of Phenobarbital.
Escitalopram	Sofpironium may increase the anticholinergic activities of Escitalopram.
Tubocurarine	Sofpironium may increase the anticholinergic activities of Tubocurarine.
Quetiapine	Sofpironium may increase the anticholinergic activities of Quetiapine.
Mivacurium	Sofpironium may increase the anticholinergic activities of Mivacurium.
Levacetylmethadol	Sofpironium may increase the anticholinergic activities of Levacetylmethadol.
Diphenidol	Sofpironium may increase the anticholinergic activities of Diphenidol.
Aripiprazole	Sofpironium may increase the anticholinergic activities of Aripiprazole.
Chlorprothixene	Sofpironium may increase the anticholinergic activities of Chlorprothixene.
Fenoterol	Sofpironium may increase the anticholinergic activities of Fenoterol.
Metocurine	Sofpironium may increase the anticholinergic activities of Metocurine.
Pancuronium	Sofpironium may increase the anticholinergic activities of Pancuronium.
Pipecuronium	Sofpironium may increase the anticholinergic activities of Pipecuronium.

Target Protein

Muscarinic acetylcholine receptor M3 CHRM3

Muscarinic acetylcholine receptor CHRM1

Referensi & Sumber

Synthesis reference: Marubayashi K, Watanabe M, & Brinkman HR. (2021). Crystalline form of sofpironium bromide and preparation method thereof. (US Patent No. US11584715B2). U.S. Patent and Trademark Office.

Artikel (PubMed)

PMID: 33410265
Yokozeki H, Fujimoto T, Abe Y, Igarashi M, Ishikoh A, Omi T, Kanda H, Kitahara H, Kinoshita M, Nakasu I, Hattori N, Horiuchi Y, Maruyama R, Mizutani H, Murakami Y, Watanabe C, Kume A, Hanafusa T, Hamaguchi M, Yoshioka A, Egami Y, Matsuo K, Matsuda T, Akamatsu M, Yorozuya T, Takayama S: A phase 3, multicenter, randomized, double-blind, vehicle-controlled, parallel-group study of 5% sofpironium bromide (BBI-4000) gel in Japanese patients with primary axillary hyperhidrosis. J Dermatol. 2021 Mar;48(3):279-288. doi: 10.1111/1346-8138.15668. Epub 2021 Jan 7.
PMID: 35389593
Armstrong A, Reddy R, Chadha D, Kircik L: SUPPLEMENT ARTICLE: A Novel Drug Delivery Method: Retrometabolic Drug Design. J Drugs Dermatol. 2022 Apr 1;21(4):s5-s10.
PMID: 30954525
Samir A, Ohura K, Bodor N, Imai T: Identification of Major Esterase Involved in Hydrolysis of Soft Anticholinergic (2R3'R-SGM) Designed From Glycopyrrolate in Human and Rat Tissues. J Pharm Sci. 2019 Aug;108(8):2791-2797. doi: 10.1016/j.xphs.2019.03.030. Epub 2019 Apr 5.

Link

Contoh Produk & Brand

Produk: 1 • International brands: 0

Produk

Sofdra

Gel • 87 mg/0.67mL • Topical • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.