Peringatan Keamanan

There is limited information on the overdosage profile of pafolacianine.

Pafolacianine

DB15413

small molecule approved investigational

Deskripsi

Pafolacianine, or OTL38, is a folate analogue conjugated with a fluorescent dye that absorbs light in the near-infrared (NIR) spectrum ^A242572 within a range of 760 nm to 785 nm, with a peak absorption of 776 nm. It emits fluorescence within a range of 790 nm to 815 nm with a peak emission of 796 nm.^L39332 The longer wavelength allows for deeper penetration of the fluorescent light through tissues for better imaging and detection of tumours. Pafolacianine targets the folate receptor alpha (FR?) which is upregulated in numerous epithelial malignancies.^A242572

On November 29, 2021, the FDA approved pafolacianine as an adjunct imaging agent for intraoperative identification of malignant lesions in adult patients with ovarian cancer.^L39332 It is currently under investigation for use in FR?-positive pituitary adenoma, lung cancer,^A242577 and renal-cell carcinoma, which is thought to be the second-highest folate receptor-expressing cancer.^A242572

Struktur Molekul 2D

Berat 1326.49

Wujud -

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 pafolacianine is 0.44 ± 0.23 hours.[L39332]

Volume Distribusi The mean volume of distribution (V<sub>z</sub>) is 17.1 ± 5.99 L, indicating distribution into tissues.[L39332] During intraoperative molecular imaging for surgically resectable pulmonary adenocarcinoma, pafolacianine accumulated in nearly 70% of squamous cell carcinomas.[A242577]

Klirens (Clearance) The mean plasma clearance is 28.6 ± 4.97 L/hr.[L39332]

Absorpsi

The mean C_max of pafolacianine was 59.1 ± 5.94 ng/mL and AUC_inf was 63.6 ± 12.6 ng x hr/mL.^L39332

Metabolisme

The metabolism of pafolacianine is unknown; however, pafolacianine is not metabolized by cytochrome P450 (CYP) enzymes.^L39332

Rute Eliminasi

Following a single intravenous infusion of radiolabeled pafolacianine sodium, approximately 35% of the dose was recovered in urine (19.1%) and in feces (15.8%) after approximately 3-5 weeks.^L39332

Interaksi Obat

10 Data

Glucarpidase	The serum concentration of the active metabolites of Pafolacianine can be reduced when Pafolacianine is used in combination with Glucarpidase resulting in a loss in efficacy.
Tetrahydrofolic acid	Tetrahydrofolic acid may decrease effectiveness of Pafolacianine as a diagnostic agent.
Folic acid	Folic acid may decrease effectiveness of Pafolacianine as a diagnostic agent.
Leucovorin	Leucovorin may decrease effectiveness of Pafolacianine as a diagnostic agent.
(6S)-5,6,7,8-tetrahydrofolic acid	(6S)-5,6,7,8-tetrahydrofolic acid may decrease effectiveness of Pafolacianine as a diagnostic agent.
Triglu-5-formyl-tetrahydrofolate	Triglu-5-formyl-tetrahydrofolate may decrease effectiveness of Pafolacianine as a diagnostic agent.
(6R)-Folinic acid	(6R)-Folinic acid may decrease effectiveness of Pafolacianine as a diagnostic agent.
5-methyltetrahydrofolic acid	5-methyltetrahydrofolic acid may decrease effectiveness of Pafolacianine as a diagnostic agent.
Levomefolic acid	Levomefolic acid may decrease effectiveness of Pafolacianine as a diagnostic agent.
Levoleucovorin	Levoleucovorin may decrease effectiveness of Pafolacianine as a diagnostic agent.

Target Protein

Folate receptor alpha FOLR1

Referensi & Sumber

Artikel (PubMed)

PMID: 27868096
Shum CF, Bahler CD, Low PS, Ratliff TL, Kheyfets SV, Natarajan JP, Sandusky GE, Sundaram CP: Novel Use of Folate-Targeted Intraoperative Fluorescence, OTL38, in Robot-Assisted Laparoscopic Partial Nephrectomy: Report of the First Three Cases. J Endourol Case Rep. 2016 Nov 1;2(1):189-197. doi: 10.1089/cren.2016.0104. eCollection 2016.
PMID: 31362825
Randall LM, Wenham RM, Low PS, Dowdy SC, Tanyi JL: A phase II, multicenter, open-label trial of OTL38 injection for the intra-operative imaging of folate receptor-alpha positive ovarian cancer. Gynecol Oncol. 2019 Oct;155(1):63-68. doi: 10.1016/j.ygyno.2019.07.010. Epub 2019 Jul 27.
PMID: 32292641
Bahler CD, Maniar V, Marley KN, Kheyfets SV, Shum CF, Sundaram CP: OTL-38-Guided Fluorescent Imaging in Renal Cell Cancer Robotic Partial Nephrectomy. J Endourol B Videourol. 2017 Feb 6;31(3). pii: 10.1089/vid.2016.0068. doi: 10.1089/vid.2016.0068. eCollection 2017.
PMID: 29568374
Predina JD, Newton AD, Xia L, Corbett C, Connolly C, Shin M, Sulyok LF, Litzky L, Deshpande C, Nie S, Kularatne SA, Low PS, Singhal S: An open label trial of folate receptor-targeted intraoperative molecular imaging to localize pulmonary squamous cell carcinomas. Oncotarget. 2018 Feb 5;9(17):13517-13529. doi: 10.18632/oncotarget.24399. eCollection 2018 Mar 2.

Link

FDA Approved Drug Products: CYTALUX (pafolacianine) injection, for intravenous use

Contoh Produk & Brand

Produk: 1 • International brands: 0

Produk

Cytalux

Injection • 3.2 mg/1.6mL • Intravenous • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.