Peringatan Keamanan

Most common adverse effects involved application site reactions such as transient burning and warm sensation. Other adverse effects observed in clinical trials are eye irritation, arthralgia, aggravated osteoarthritis, burning sensation, headache, cough and sneezing. Oral LD50 in mouse is >87.5 mg/kg in male and <60 mg/kg in females. Oral LD50 in rats is >90 mg/kg in males and >60 mg/kg in females.^L877

Zucapsaicin

DB09120

small molecule approved investigational

Deskripsi

Zucapsaicin, the cis-isomer of capsaicin, is a topical analgesic used to treat osteoarthritis of the knee and other neuropathic pain. It is a modulator of transient receptor potential cation channel subfamily V member 1 (TRPV-1), also known as the vanilloid or capsaicin receptor 1, that reduces pain and improves articular functions. Zucapsaicin has also been evaluated for the management of several conditions manifested by chronic nerve pain. These conditions include herpes simplex (HSV) infections, cluster headaches, migraine, and osteoarthritis of the knee. Zucapsaicin was approved by the Health Canada in 2010 as topical cream marketed under the brand name Zuacta but currently not FDA-approved.

Struktur Molekul 2D

Berat 305.4119

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) In rats, the elimination half life of zucapsaicin and its metabolites is approximately 7 to 11 hours [L877].

Volume Distribusi -

Klirens (Clearance) -

Absorpsi

Zucapsaicin displays low systemic absorption and localizes at the area of application. In animal studies, systemic absorption is 0.075% ^L877.

Metabolisme

In vitro studies demonstrates weak to moderate inhibitiory effects on various cytochrome P450 enzymes, although not clinically significant due to low systemic absorption.

Rute Eliminasi

In rat studies, zucapsaicin and its metabolites are slowly excreted into urine and feces (up to 2/3), with minimal elimination via exhalation following dermal administration ^L877.

Interaksi Obat

7 Data

Belzutifan	The serum concentration of Belzutifan can be increased when it is combined with Zucapsaicin.
Mavacamten	The serum concentration of Mavacamten can be increased when it is combined with Zucapsaicin.
Pirfenidone	The metabolism of Pirfenidone can be decreased when combined with Zucapsaicin.
Roflumilast	The serum concentration of Roflumilast can be increased when it is combined with Zucapsaicin.
Clobazam	The serum concentration of Clobazam can be increased when it is combined with Zucapsaicin.
Fezolinetant	The serum concentration of Fezolinetant can be increased when it is combined with Zucapsaicin.
Vorasidenib	The metabolism of Vorasidenib can be decreased when combined with Zucapsaicin.

Target Protein

Transient receptor potential cation channel subfamily V member 1 TRPV1

Referensi & Sumber

Synthesis reference: 1. Gannett PM, Nagel DL, Reilly PJ, Lawson T, Sharpe J, Toth B: The Capsaicinoids: Their Separation, Synthesis, and Mutagenicity. J. Org. Chem., 1988, 53 (5), pp 1064–1071. 2. Kaga H, Miura M, Orito K: A facile procedure for synthesis of capsaicin. J. Org. Chem., 1989, 54 (14), pp 3477–3478.

Artikel (PubMed)

PMID: 25171227
Salat K, Jakubowska A, Kulig K: Zucapsaicin for the treatment of neuropathic pain. Expert Opin Investig Drugs. 2014 Oct;23(10):1433-40. doi: 10.1517/13543784.2014.956079. Epub 2014 Aug 29.
PMID: 19821411
Derry S, Lloyd R, Moore RA, McQuay HJ: Topical capsaicin for chronic neuropathic pain in adults. Cochrane Database Syst Rev. 2009 Oct 7;(4):CD007393. doi: 10.1002/14651858.CD007393.pub2.
PMID: 20693293
Studer M, McNaughton PA: Modulation of single-channel properties of TRPV1 by phosphorylation. J Physiol. 2010 Oct 1;588(Pt 19):3743-56. doi: 10.1113/jphysiol.2010.190611. Epub 2010 Aug 6.
PMID: 21204507
Rosenbaum T, Simon SA: TRPV1 Receptors and Signal Transduction .

Link

Health Canada Product Monograph: Zuacta (zucapsaicin) topical cream

Contoh Produk & Brand

Produk: 1 • International brands: 1

Produk

Zuacta

Cream • 0.075 % w/w • Topical • Canada • Approved

International Brands

Civanex

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.