Peringatan Keamanan

There is no information regarding the LD₅₀ of padeliporfin.

There is limited clinical information on padeliporfin overdose. In clinical studies, healthy subjects were exposed to doses up to 15 mg/kg of padeliporfin di-potassium (corresponding to 13.73 mg/kg of padeliporfin) without light activation and 23 patients have been treated with 6 mg/kg of padeliporfin di-potassium (corresponding to 5.49 mg/kg of padeliporfin) without significant safety issues. However, prolonged photosensitization is possible and precautions against light exposure should be maintained for an additional 24 hours. An overdose of the laser light may increase the risk of undesirable extraprostatic necrosis.^L39794

Padeliporfin

DB15575

small molecule approved experimental

Deskripsi

Padeliporfin is a water-soluble chlorophyll derivative and cytotoxic photosensitizer used for vascular-targeted photodynamic therapy for malignancies.^A244559 Vascular-targeted photodynamic therapy (VTP), or vascular targeted photochemotherapy, is a focal treatment for localized prostate cancer. It aims to destroy only cancerous lesions of the prostate, rather than ablating the entire prostate gland.^A244699 Padeliporfin was first approved by the European Commission on November 10, 2017, for the treatment of low-risk prostate cancer in adults meeting certain clinical criteria.^L39799

Struktur Molekul 2D

Berat 840.26

Wujud liquid

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 estimated half-life is 1.19 hrs ± 0.08 at 4 mg/kg of padeliporfin di-potassium.[L39794]

Volume Distribusi In healthy men receiving 1.25 to 15 mg/kg of padeliporfin di-potassium, the mean volume of distribution (V<sub>d</sub>) ranged from 0.064 to 0.279 L/kg. In patients with localized prostate cancer treated with 2 and 4 mg/kg of padeliporfin di-potassium, the mean V<sub>d</sub> ranged from 0.09 to 0.10 L/kg.[L39794] Upon administration, padeliporfin remain confined within the circulation even at high doses, with minimal extravasation to other tissues.[A244699]

Klirens (Clearance) Following administration of 1.25-15 mg/kg of padeliporfin di-potassium in healthy men, clearance of padeliporfin di-potassium ranged from 0.0245 to 0.088 L/h/kg. In patients with localised prostate cancer treated with 4 mg/kg and 2 mg/kg of padeliporfin di-potassium, clearance was 0.04 L/h/kg and 0.06 L/h/kg, respectively.[L39794]

Absorpsi

After intravenous bolus injection at a dose of 6 mg/kg into healthy mice, the C_max of padeliporfin was about 52 mg/L, with a T_max of two minutes.^A244699

Metabolisme

In human liver microsomes and S9 fractions, padeliporfin underwent minimal metabolism. No metabolites of padeliporfin have been identified yet as a radiolabeled study has not been performed.^L39794

Rute Eliminasi

In healthy subjects, urinary excretion of padeliporfin was very low, accounting for less than 0.2% of the dose. Fecal elimination is a suspected predominant route of elimination.^L39794

Interaksi Obat

162 Data

Riboflavin	Riboflavin may increase the photosensitizing activities of Padeliporfin.
Metoprolol	Metoprolol may increase the photosensitizing activities of Padeliporfin.
Cyproheptadine	Cyproheptadine may increase the photosensitizing activities of Padeliporfin.
Verteporfin	Verteporfin may increase the photosensitizing activities of Padeliporfin.
Methoxsalen	Methoxsalen may increase the photosensitizing activities of Padeliporfin.
Porfimer sodium	Porfimer sodium may increase the photosensitizing activities of Padeliporfin.
Carprofen	Carprofen may increase the photosensitizing activities of Padeliporfin.
Clofazimine	Clofazimine may increase the photosensitizing activities of Padeliporfin.
Aminolevulinic acid	Aminolevulinic acid may increase the photosensitizing activities of Padeliporfin.
Methyl aminolevulinate	Methyl aminolevulinate may increase the photosensitizing activities of Padeliporfin.
Levofloxacin	Levofloxacin may increase the photosensitizing activities of Padeliporfin.
Methotrimeprazine	Methotrimeprazine may increase the photosensitizing activities of Padeliporfin.
Tiaprofenic acid	Tiaprofenic acid may increase the photosensitizing activities of Padeliporfin.
Benzophenone	Benzophenone may increase the photosensitizing activities of Padeliporfin.
Protoporphyrin	Protoporphyrin may increase the photosensitizing activities of Padeliporfin.
Trioxsalen	Trioxsalen may increase the photosensitizing activities of Padeliporfin.
Acetophenone	Acetophenone may increase the photosensitizing activities of Padeliporfin.
Febuxostat	Febuxostat may increase the photosensitizing activities of Padeliporfin.
Nilotinib	Nilotinib may increase the photosensitizing activities of Padeliporfin.
Motexafin lutetium	Motexafin lutetium may increase the photosensitizing activities of Padeliporfin.
Motexafin gadolinium	Motexafin gadolinium may increase the photosensitizing activities of Padeliporfin.
Hexaminolevulinate	Hexaminolevulinate may increase the photosensitizing activities of Padeliporfin.
Rostaporfin	Rostaporfin may increase the photosensitizing activities of Padeliporfin.
Vemurafenib	Vemurafenib may increase the photosensitizing activities of Padeliporfin.
Dabrafenib	Dabrafenib may increase the photosensitizing activities of Padeliporfin.
Cyamemazine	Cyamemazine may increase the photosensitizing activities of Padeliporfin.
Methylene blue	Methylene blue may increase the photosensitizing activities of Padeliporfin.
Titanium dioxide	Titanium dioxide may increase the photosensitizing activities of Padeliporfin.
Temoporfin	Temoporfin may increase the photosensitizing activities of Padeliporfin.
Talaporfin	Talaporfin may increase the photosensitizing activities of Padeliporfin.
Bergapten	Bergapten may increase the photosensitizing activities of Padeliporfin.
Dihematoporphyrin ether	Dihematoporphyrin ether may increase the photosensitizing activities of Padeliporfin.
Hemoporfin	Hemoporfin may increase the photosensitizing activities of Padeliporfin.
Fosdenopterin	Fosdenopterin may increase the photosensitizing activities of Padeliporfin.
Lepirudin	The risk or severity of bleeding can be increased when Lepirudin is combined with Padeliporfin.
Bivalirudin	The risk or severity of bleeding can be increased when Bivalirudin is combined with Padeliporfin.
Alteplase	The risk or severity of bleeding can be increased when Alteplase is combined with Padeliporfin.
Urokinase	The risk or severity of bleeding can be increased when Urokinase is combined with Padeliporfin.
Reteplase	The risk or severity of bleeding can be increased when Reteplase is combined with Padeliporfin.
Anistreplase	The risk or severity of bleeding can be increased when Anistreplase is combined with Padeliporfin.
Tenecteplase	The risk or severity of bleeding can be increased when Tenecteplase is combined with Padeliporfin.
Abciximab	The risk or severity of bleeding can be increased when Abciximab is combined with Padeliporfin.
Drotrecogin alfa	The risk or severity of bleeding can be increased when Drotrecogin alfa is combined with Padeliporfin.
Streptokinase	The risk or severity of bleeding can be increased when Streptokinase is combined with Padeliporfin.
Dicoumarol	The risk or severity of bleeding can be increased when Dicoumarol is combined with Padeliporfin.
Argatroban	The risk or severity of bleeding can be increased when Argatroban is combined with Padeliporfin.
Ardeparin	The risk or severity of bleeding can be increased when Ardeparin is combined with Padeliporfin.
Phenindione	The risk or severity of bleeding can be increased when Phenindione is combined with Padeliporfin.
Fondaparinux	The risk or severity of bleeding can be increased when Fondaparinux is combined with Padeliporfin.
Warfarin	The risk or severity of bleeding can be increased when Warfarin is combined with Padeliporfin.
Pentosan polysulfate	The risk or severity of bleeding can be increased when Pentosan polysulfate is combined with Padeliporfin.
Phenprocoumon	The risk or severity of bleeding can be increased when Phenprocoumon is combined with Padeliporfin.
Edetic acid	The risk or severity of bleeding can be increased when Edetic acid is combined with Padeliporfin.
Dipyridamole	The risk or severity of bleeding can be increased when Dipyridamole is combined with Padeliporfin.
Heparin	The risk or severity of bleeding can be increased when Heparin is combined with Padeliporfin.
Enoxaparin	The risk or severity of bleeding can be increased when Enoxaparin is combined with Padeliporfin.
Epoprostenol	The risk or severity of bleeding can be increased when Epoprostenol is combined with Padeliporfin.
Acenocoumarol	The risk or severity of bleeding can be increased when Acenocoumarol is combined with Padeliporfin.
4-hydroxycoumarin	The risk or severity of bleeding can be increased when 4-hydroxycoumarin is combined with Padeliporfin.
Coumarin	The risk or severity of bleeding can be increased when Coumarin is combined with Padeliporfin.
Ximelagatran	The risk or severity of bleeding can be increased when Ximelagatran is combined with Padeliporfin.
Desmoteplase	The risk or severity of bleeding can be increased when Desmoteplase is combined with Padeliporfin.
Defibrotide	The risk or severity of bleeding can be increased when Defibrotide is combined with Padeliporfin.
Ancrod	The risk or severity of bleeding can be increased when Ancrod is combined with Padeliporfin.
Beraprost	The risk or severity of bleeding can be increased when Beraprost is combined with Padeliporfin.
Fibrinolysin	The risk or severity of bleeding can be increased when Fibrinolysin is combined with Padeliporfin.
SR-123781A	The risk or severity of bleeding can be increased when SR-123781A is combined with Padeliporfin.
Prasugrel	The risk or severity of bleeding can be increased when Prasugrel is combined with Padeliporfin.
Rivaroxaban	The risk or severity of bleeding can be increased when Rivaroxaban is combined with Padeliporfin.
Sulodexide	The risk or severity of bleeding can be increased when Sulodexide is combined with Padeliporfin.
Semuloparin	The risk or severity of bleeding can be increased when Semuloparin is combined with Padeliporfin.
Idraparinux	The risk or severity of bleeding can be increased when Idraparinux is combined with Padeliporfin.
Cangrelor	The risk or severity of bleeding can be increased when Cangrelor is combined with Padeliporfin.
Astaxanthin	The risk or severity of bleeding can be increased when Astaxanthin is combined with Padeliporfin.
Apixaban	The risk or severity of bleeding can be increased when Apixaban is combined with Padeliporfin.
Otamixaban	The risk or severity of bleeding can be increased when Otamixaban is combined with Padeliporfin.
Amediplase	The risk or severity of bleeding can be increased when Amediplase is combined with Padeliporfin.
Dabigatran etexilate	The risk or severity of bleeding can be increased when Dabigatran etexilate is combined with Padeliporfin.
Danaparoid	The risk or severity of bleeding can be increased when Danaparoid is combined with Padeliporfin.
Dalteparin	The risk or severity of bleeding can be increased when Dalteparin is combined with Padeliporfin.
Tinzaparin	The risk or severity of bleeding can be increased when Tinzaparin is combined with Padeliporfin.
Ferulic acid	The risk or severity of bleeding can be increased when Ferulic acid is combined with Padeliporfin.
(R)-warfarin	The risk or severity of bleeding can be increased when (R)-warfarin is combined with Padeliporfin.
Ethyl biscoumacetate	The risk or severity of bleeding can be increased when Ethyl biscoumacetate is combined with Padeliporfin.
Nadroparin	The risk or severity of bleeding can be increased when Nadroparin is combined with Padeliporfin.
Triflusal	The risk or severity of bleeding can be increased when Triflusal is combined with Padeliporfin.
Ticagrelor	The risk or severity of bleeding can be increased when Ticagrelor is combined with Padeliporfin.
Ditazole	The risk or severity of bleeding can be increased when Ditazole is combined with Padeliporfin.
Vorapaxar	The risk or severity of bleeding can be increased when Vorapaxar is combined with Padeliporfin.
Edoxaban	The risk or severity of bleeding can be increased when Edoxaban is combined with Padeliporfin.
Sodium citrate	The risk or severity of bleeding can be increased when Sodium citrate is combined with Padeliporfin.
Dextran	The risk or severity of bleeding can be increased when Dextran is combined with Padeliporfin.
Bemiparin	The risk or severity of bleeding can be increased when Bemiparin is combined with Padeliporfin.
Reviparin	The risk or severity of bleeding can be increased when Reviparin is combined with Padeliporfin.
Parnaparin	The risk or severity of bleeding can be increased when Parnaparin is combined with Padeliporfin.
Certoparin	The risk or severity of bleeding can be increased when Certoparin is combined with Padeliporfin.
Desirudin	The risk or severity of bleeding can be increased when Desirudin is combined with Padeliporfin.
Antithrombin Alfa	The risk or severity of bleeding can be increased when Antithrombin Alfa is combined with Padeliporfin.
Protocatechualdehyde	The risk or severity of bleeding can be increased when Protocatechualdehyde is combined with Padeliporfin.
Protein C	The risk or severity of bleeding can be increased when Protein C is combined with Padeliporfin.

Referensi & Sumber

Artikel (PubMed)

PMID: 33228126
Nogueira L, Tracey AT, Alvim R, Reisz P, Scherz A, Coleman JA, Kim K: Developments in Vascular-Targeted Photodynamic Therapy for Urologic Malignancies. Molecules. 2020 Nov 19;25(22). pii: molecules25225417. doi: 10.3390/molecules25225417.
PMID: 27019798
Bugaj AM: Vascular targeted photochemotherapy using padoporfin and padeliporfin as a method of the focal treatment of localised prostate cancer - clinician's insight. World J Methodol. 2016 Mar 26;6(1):65-76. doi: 10.5662/wjm.v6.i1.65. eCollection 2016 Mar 26.

Link

Contoh Produk & Brand

Produk: 2 • International brands: 0

Produk

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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.