Peringatan Keamanan

Preclinical studies with OM3-CA have shown an absence of a potential carcinogenic effect in males but it is reported to increase the incidence of benign ovarian sex cord-stromal tumors. OM3-CA is not mutagenic, clastogenic and it did not have any effect on fertility.^L2390

Omega-3-carboxylic acids

DB09568

small molecule approved investigational

Deskripsi

The omega-3 carboxylic acid (OM3-CA) is a new formulation of omega-3 fatty acids that present an enhanced bioavailability in the treatment of dyslipidemia. The increased bioavailability is explained because OM3-CA is found in a form of polyunsaturated free fatty acids as opposed to other products whose form is as ethyl esters. It is a complex mixture of the free fatty acids form containing eicosapentaenoic acid and docosahexaenoic acid as the most abundant species found in a proportion of 55% and 20% respectively. The rest of the concentration is represented by docosapentaenoic acid and traces of some other components such as alpha-tocopherol, gelatin, glycerol, sorbitol and purified water.^A25808 It was developed by AstraZeneca Pharmaceuticals and firstly approved by the FDA on May 05, 2014.^L2386

Struktur Molekul 2D

Struktur tidak tersedia

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 half-life of OM3-CA depends on the type of component in which for eicosapentaenoic acid it is estimated to be of approximately 4.7-10.8 hours while for docosahexaenoic acid is reported to be of about 7 hours.[A25808] The half-life of baseline-adjusted at steady-state is of 36 and 46 hours respectively for eicosapentaenoic acid and docosahexaenoic acid.[L2390]

Volume Distribusi This pharmacokinetic property is not available.

Klirens (Clearance) The registered clearance rate at steady-state is of 548 ml/h for eicosapentaenoic acid and 518 ml/h for docohexaenoic acid.[L2390]

Absorpsi

When compared to omega-3 -acid ethyl esters, OM3-CA present a 4-fold higher bioavailability.^A25808 OM3-CA is absorbed directly in the small intestine and the maximal plasma concentration is reached between 4.5-5 hours after initial administration.^A25808 The absorbed dosage is transferred to the general circulation via the lymphatic system and distributed within tissues throughout the body. The absorption speed and extent is highly promoted by the bile. In preclinical studies performed in dogs, the Cmax, tmax and AUC were reported to be 15.1 mcg/ml, 24 hours and 1210.3 mcg.h/ml, respectively.^L2401

Metabolisme

OM3-CA is metabolized in the liver following the normal fatty acid oxidation.^A25808 Once absorbed, they are incorporated into triglycerides, cholesterol esters and phospholipids in tissues. The metabolism is marked by beta-oxidation followed by tricarboxylic acid cycle. It is reported that OM3-CA is an inhibitor of several enzymes such as CYP2C9, CYP2C19 and to a lesser extent to CYP1A2, CYP2E1, CYP3A4. It is thought that the metabolism of OM3-CA is mainly done by CYP3A and CYP4F3B.^L2401

Rute Eliminasi

OM3-CA does not go under renal excretion.^L2390 After the metabolism, all the dose is excreted as CO2 and water in the form of expelled air and the rest is excreted in feces.^L2401

Interaksi Makanan

1 Data

1. Take with or without food. Taking omega-3-carboxylic acids with a high-fat meal may increase the absorption of eicosapentaenoic acid (EPA).

Interaksi Obat

84 Data

Ibrutinib	Omega-3-carboxylic acids may increase the antiplatelet activities of Ibrutinib.
Lepirudin	The therapeutic efficacy of Lepirudin can be increased when used in combination with Omega-3-carboxylic acids.
Bivalirudin	The therapeutic efficacy of Bivalirudin can be increased when used in combination with Omega-3-carboxylic acids.
Alteplase	The therapeutic efficacy of Alteplase can be increased when used in combination with Omega-3-carboxylic acids.
Urokinase	The therapeutic efficacy of Urokinase can be increased when used in combination with Omega-3-carboxylic acids.
Reteplase	The therapeutic efficacy of Reteplase can be increased when used in combination with Omega-3-carboxylic acids.
Anistreplase	The therapeutic efficacy of Anistreplase can be increased when used in combination with Omega-3-carboxylic acids.
Tenecteplase	The therapeutic efficacy of Tenecteplase can be increased when used in combination with Omega-3-carboxylic acids.
Abciximab	The therapeutic efficacy of Abciximab can be increased when used in combination with Omega-3-carboxylic acids.
Drotrecogin alfa	The therapeutic efficacy of Drotrecogin alfa can be increased when used in combination with Omega-3-carboxylic acids.
Streptokinase	The therapeutic efficacy of Streptokinase can be increased when used in combination with Omega-3-carboxylic acids.
Dicoumarol	The therapeutic efficacy of Dicoumarol can be increased when used in combination with Omega-3-carboxylic acids.
Argatroban	The therapeutic efficacy of Argatroban can be increased when used in combination with Omega-3-carboxylic acids.
Ardeparin	The therapeutic efficacy of Ardeparin can be increased when used in combination with Omega-3-carboxylic acids.
Phenindione	The therapeutic efficacy of Phenindione can be increased when used in combination with Omega-3-carboxylic acids.
Fondaparinux	The therapeutic efficacy of Fondaparinux can be increased when used in combination with Omega-3-carboxylic acids.
Warfarin	The therapeutic efficacy of Warfarin can be increased when used in combination with Omega-3-carboxylic acids.
Pentosan polysulfate	The therapeutic efficacy of Pentosan polysulfate can be increased when used in combination with Omega-3-carboxylic acids.
Phenprocoumon	The therapeutic efficacy of Phenprocoumon can be increased when used in combination with Omega-3-carboxylic acids.
Dipyridamole	The therapeutic efficacy of Dipyridamole can be increased when used in combination with Omega-3-carboxylic acids.
Heparin	The therapeutic efficacy of Heparin can be increased when used in combination with Omega-3-carboxylic acids.
Enoxaparin	The therapeutic efficacy of Enoxaparin can be increased when used in combination with Omega-3-carboxylic acids.
Epoprostenol	The therapeutic efficacy of Epoprostenol can be increased when used in combination with Omega-3-carboxylic acids.
Acenocoumarol	The therapeutic efficacy of Acenocoumarol can be increased when used in combination with Omega-3-carboxylic acids.
4-hydroxycoumarin	The therapeutic efficacy of 4-hydroxycoumarin can be increased when used in combination with Omega-3-carboxylic acids.
Coumarin	The therapeutic efficacy of Coumarin can be increased when used in combination with Omega-3-carboxylic acids.
Ximelagatran	The therapeutic efficacy of Ximelagatran can be increased when used in combination with Omega-3-carboxylic acids.
Desmoteplase	The therapeutic efficacy of Desmoteplase can be increased when used in combination with Omega-3-carboxylic acids.
Defibrotide	The therapeutic efficacy of Defibrotide can be increased when used in combination with Omega-3-carboxylic acids.
Ancrod	The therapeutic efficacy of Ancrod can be increased when used in combination with Omega-3-carboxylic acids.
Beraprost	The therapeutic efficacy of Beraprost can be increased when used in combination with Omega-3-carboxylic acids.
Prasugrel	The therapeutic efficacy of Prasugrel can be increased when used in combination with Omega-3-carboxylic acids.
Rivaroxaban	The therapeutic efficacy of Rivaroxaban can be increased when used in combination with Omega-3-carboxylic acids.
Sulodexide	The therapeutic efficacy of Sulodexide can be increased when used in combination with Omega-3-carboxylic acids.
Semuloparin	The therapeutic efficacy of Semuloparin can be increased when used in combination with Omega-3-carboxylic acids.
Idraparinux	The therapeutic efficacy of Idraparinux can be increased when used in combination with Omega-3-carboxylic acids.
Cangrelor	The therapeutic efficacy of Cangrelor can be increased when used in combination with Omega-3-carboxylic acids.
Astaxanthin	The therapeutic efficacy of Astaxanthin can be increased when used in combination with Omega-3-carboxylic acids.
Apixaban	The therapeutic efficacy of Apixaban can be increased when used in combination with Omega-3-carboxylic acids.
Otamixaban	The therapeutic efficacy of Otamixaban can be increased when used in combination with Omega-3-carboxylic acids.
Amediplase	The therapeutic efficacy of Amediplase can be increased when used in combination with Omega-3-carboxylic acids.
Dabigatran etexilate	The therapeutic efficacy of Dabigatran etexilate can be increased when used in combination with Omega-3-carboxylic acids.
Danaparoid	The therapeutic efficacy of Danaparoid can be increased when used in combination with Omega-3-carboxylic acids.
Dalteparin	The therapeutic efficacy of Dalteparin can be increased when used in combination with Omega-3-carboxylic acids.
Tinzaparin	The therapeutic efficacy of Tinzaparin can be increased when used in combination with Omega-3-carboxylic acids.
(R)-warfarin	The therapeutic efficacy of (R)-warfarin can be increased when used in combination with Omega-3-carboxylic acids.
Ethyl biscoumacetate	The therapeutic efficacy of Ethyl biscoumacetate can be increased when used in combination with Omega-3-carboxylic acids.
Nadroparin	The therapeutic efficacy of Nadroparin can be increased when used in combination with Omega-3-carboxylic acids.
Triflusal	The therapeutic efficacy of Triflusal can be increased when used in combination with Omega-3-carboxylic acids.
Ticagrelor	The therapeutic efficacy of Ticagrelor can be increased when used in combination with Omega-3-carboxylic acids.
Ditazole	The therapeutic efficacy of Ditazole can be increased when used in combination with Omega-3-carboxylic acids.
Vorapaxar	The therapeutic efficacy of Vorapaxar can be increased when used in combination with Omega-3-carboxylic acids.
Edoxaban	The therapeutic efficacy of Edoxaban can be increased when used in combination with Omega-3-carboxylic acids.
Sodium citrate	The therapeutic efficacy of Sodium citrate can be increased when used in combination with Omega-3-carboxylic acids.
Dextran	The therapeutic efficacy of Dextran can be increased when used in combination with Omega-3-carboxylic acids.
Bemiparin	The therapeutic efficacy of Bemiparin can be increased when used in combination with Omega-3-carboxylic acids.
Parnaparin	The therapeutic efficacy of Parnaparin can be increased when used in combination with Omega-3-carboxylic acids.
Desirudin	The therapeutic efficacy of Desirudin can be increased when used in combination with Omega-3-carboxylic acids.
Antithrombin Alfa	The therapeutic efficacy of Antithrombin Alfa can be increased when used in combination with Omega-3-carboxylic acids.
Protein C	The therapeutic efficacy of Protein C can be increased when used in combination with Omega-3-carboxylic acids.
Antithrombin III human	The therapeutic efficacy of Antithrombin III human can be increased when used in combination with Omega-3-carboxylic acids.
Letaxaban	The therapeutic efficacy of Letaxaban can be increased when used in combination with Omega-3-carboxylic acids.
Darexaban	The therapeutic efficacy of Darexaban can be increased when used in combination with Omega-3-carboxylic acids.
Betrixaban	The therapeutic efficacy of Betrixaban can be increased when used in combination with Omega-3-carboxylic acids.
Nafamostat	The therapeutic efficacy of Nafamostat can be increased when used in combination with Omega-3-carboxylic acids.
Monteplase	The therapeutic efficacy of Monteplase can be increased when used in combination with Omega-3-carboxylic acids.
Gabexate	The therapeutic efficacy of Gabexate can be increased when used in combination with Omega-3-carboxylic acids.
Fluindione	The therapeutic efficacy of Fluindione can be increased when used in combination with Omega-3-carboxylic acids.
Protein S human	The therapeutic efficacy of Protein S human can be increased when used in combination with Omega-3-carboxylic acids.
Brinase	The therapeutic efficacy of Brinase can be increased when used in combination with Omega-3-carboxylic acids.
Clorindione	The therapeutic efficacy of Clorindione can be increased when used in combination with Omega-3-carboxylic acids.
Diphenadione	The therapeutic efficacy of Diphenadione can be increased when used in combination with Omega-3-carboxylic acids.
Tioclomarol	The therapeutic efficacy of Tioclomarol can be increased when used in combination with Omega-3-carboxylic acids.
Melagatran	The therapeutic efficacy of Melagatran can be increased when used in combination with Omega-3-carboxylic acids.
Saruplase	The therapeutic efficacy of Saruplase can be increased when used in combination with Omega-3-carboxylic acids.
(S)-Warfarin	The therapeutic efficacy of (S)-Warfarin can be increased when used in combination with Omega-3-carboxylic acids.
Tocopherylquinone	The therapeutic efficacy of Tocopherylquinone can be increased when used in combination with Omega-3-carboxylic acids.
Dabigatran	The therapeutic efficacy of Dabigatran can be increased when used in combination with Omega-3-carboxylic acids.
Troxerutin	The therapeutic efficacy of Troxerutin can be increased when used in combination with Omega-3-carboxylic acids.
Edetic acid	The therapeutic efficacy of Edetic acid can be increased when used in combination with Omega-3-carboxylic acids.
Reviparin	The therapeutic efficacy of Reviparin can be increased when used in combination with Omega-3-carboxylic acids.
Dermatan sulfate	The therapeutic efficacy of Dermatan sulfate can be increased when used in combination with Omega-3-carboxylic acids.
SR-123781A	The therapeutic efficacy of SR-123781A can be increased when used in combination with Omega-3-carboxylic acids.
Limaprost	The therapeutic efficacy of Limaprost can be increased when used in combination with Omega-3-carboxylic acids.

Target Protein

Diacylglycerol O-acyltransferase 2 DGAT2

3-hydroxyacyl-CoA dehydrogenase type-2 HSD17B10

Enoyl-CoA hydratase, mitochondrial ECHS1

Hydroxyacyl-coenzyme A dehydrogenase, mitochondrial HADH

Very long chain fatty acid elongase 4 ELOVL4

Lipoprotein lipase LPL

Referensi & Sumber

Artikel (PubMed)

PMID: 28003756
Benes LB, Bassi NS, Davidson MH: Omega-3 carboxylic acids monotherapy and combination with statins in the management of dyslipidemia. Vasc Health Risk Manag. 2016 Dec 12;12:481-490. doi: 10.2147/VHRM.S58149. eCollection 2016.
PMID: 25387209
Weintraub HS: Overview of prescription omega-3 fatty acid products for hypertriglyceridemia. Postgrad Med. 2014 Nov;126(7):7-18. doi: 10.3810/pgm.2014.11.2828.
PMID: 23525082
Brahm A, Hegele RA: Hypertriglyceridemia. Nutrients. 2013 Mar 22;5(3):981-1001. doi: 10.3390/nu5030981.

Link

Contoh Produk & Brand

Produk: 1 • International brands: 0

Produk

Epanova

Capsule, gelatin coated • 1 g/1 • Oral • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.