Peringatan Keamanan

LD50 information for obeticholic acid is not readily available in the literature.L12633

The maximum documented exposure to obeticholic acid was 500 mg in healthy research volunteers. Doses of 250 mg have been administered to healthy volunteers for 12 consecutive days. Pruritus and reversible transaminase liver elevations were observed. In PBC patients who received 25mg daily to 50mg daily (2.5 to 5 times the maximum recommended dose), dose-dependent transaminase and bilirubin elevations, ascites, primary biliary cholangitis aggravation, and new-onset jaundice were reported.L12720

In the case of an overdose with obeticholic acid, clinical monitoring and supportive care should be offered as they are required.L12720

Obeticholic acid

DB05990

small molecule approved

Deskripsi

Primary biliary cirrhosis, or PBC, is a progressive and chronic condition that leads to hepatic injury often resulting in end-stage liver failure that requires liver transplantation.A192786

Obeticholic acid is a farnesoid-X receptor (FXR) agonist used to treat this condition, possibly allowing for increased survival.A18696 In 2016, it was granted approval to treat primary biliary cholangitis in combination with ursodeoxycholic acid, which was previously the mainstay treatment for this condition.A18696,L12633 In May 2021, the FDA updated its prescribing information to contraindicate the use of obeticholic acid in patients with PBC and advanced cirrhosis (e.g. those with portal hypertension or hepatic decompensation) due to a risk of liver failure, in some cases requiring liver transplantation.L34650

Obeticholic acid is currently being considered for FDA approval to treat fibrosis caused by non-alcoholic liver steatohepatitis (NASH). The NDA from Intercept Pharmaceuticals was approved in November 2019 and obeticholic acid is expected to be granted full approval for this indication in 2020.L12636

Struktur Molekul 2D

Berat 420.6252
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The biological half-life of obeticholic acid is reported to be 24 hours.[L12738]
Volume Distribusi The volume of distribution of obeticholic acid is 618 L.[L12633,L12720]
Klirens (Clearance) Clearance information for obeticholic acid is not readily available in the literature.[L12633,L12720]

Absorpsi

Obeticholic acid is absorbed in the gastrointestinal tract. The Cmax of obeticholic acid occurs at approximately 1.5 hours after an oral dose and ranges from 28.8-53.7 ng/mL at doses of 5-10mg.L12735 The median Tmax for both the conjugates of obeticholic acid is about 10 hours.L12633 One product monograph reports a Tmax of 4.5h for both 5 and 10mg doses. The AUC ranged from 236.6-568.1 ng/h/mL with 5mg to 10 mg doses.L12735

Metabolisme

The metabolism of obeticholic acid occurs in the liver. Obeticholic acid is conjugated with glycine or taurine, followed by secretion into bile. The conjugates are then absorbed in the small intestine and then re-enter the liver via enterohepatic circulation. The intestinal microbiota in the ileum converts conjugated obeticholic acid in a deconjugated form that may be either reabsorbed or eliminated. Glycine conjugates account for 13.8% of the metabolites and taurine conjugates account for 12.3%. Another metabolite, 3-glucuronide, may also be formed, but displays little pharmacological activity.L12633

Rute Eliminasi

About 87% of an orally administered dose is accounted for in the feces. Less than 3% of the dose can be recovered in the urine.L12633,L12720

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

373 Data
Lepirudin The risk or severity of bleeding and bruising can be increased when Lepirudin is combined with Obeticholic acid.
Bivalirudin The risk or severity of bleeding and bruising can be increased when Bivalirudin is combined with Obeticholic acid.
Alteplase The risk or severity of bleeding and bruising can be increased when Alteplase is combined with Obeticholic acid.
Urokinase The risk or severity of bleeding and bruising can be increased when Urokinase is combined with Obeticholic acid.
Reteplase The risk or severity of bleeding and bruising can be increased when Reteplase is combined with Obeticholic acid.
Anistreplase The risk or severity of bleeding and bruising can be increased when Anistreplase is combined with Obeticholic acid.
Tenecteplase The risk or severity of bleeding and bruising can be increased when Tenecteplase is combined with Obeticholic acid.
Drotrecogin alfa The risk or severity of bleeding and bruising can be increased when Drotrecogin alfa is combined with Obeticholic acid.
Streptokinase The risk or severity of bleeding and bruising can be increased when Streptokinase is combined with Obeticholic acid.
Dicoumarol The risk or severity of bleeding and bruising can be increased when Dicoumarol is combined with Obeticholic acid.
Argatroban The risk or severity of bleeding and bruising can be increased when Argatroban is combined with Obeticholic acid.
Ardeparin The risk or severity of bleeding and bruising can be increased when Ardeparin is combined with Obeticholic acid.
Phenindione The risk or severity of bleeding and bruising can be increased when Phenindione is combined with Obeticholic acid.
Fondaparinux The risk or severity of bleeding and bruising can be increased when Fondaparinux is combined with Obeticholic acid.
Pentosan polysulfate The risk or severity of bleeding and bruising can be increased when Pentosan polysulfate is combined with Obeticholic acid.
Phenprocoumon The risk or severity of bleeding and bruising can be increased when Phenprocoumon is combined with Obeticholic acid.
Heparin The risk or severity of bleeding and bruising can be increased when Heparin is combined with Obeticholic acid.
Enoxaparin The risk or severity of bleeding and bruising can be increased when Enoxaparin is combined with Obeticholic acid.
4-hydroxycoumarin The risk or severity of bleeding and bruising can be increased when 4-hydroxycoumarin is combined with Obeticholic acid.
Coumarin The risk or severity of bleeding and bruising can be increased when Coumarin is combined with Obeticholic acid.
Ximelagatran The risk or severity of bleeding and bruising can be increased when Ximelagatran is combined with Obeticholic acid.
Desmoteplase The risk or severity of bleeding and bruising can be increased when Desmoteplase is combined with Obeticholic acid.
Ancrod The risk or severity of bleeding and bruising can be increased when Ancrod is combined with Obeticholic acid.
Rivaroxaban The risk or severity of bleeding and bruising can be increased when Rivaroxaban is combined with Obeticholic acid.
Sulodexide The risk or severity of bleeding and bruising can be increased when Sulodexide is combined with Obeticholic acid.
Semuloparin The risk or severity of bleeding and bruising can be increased when Semuloparin is combined with Obeticholic acid.
Idraparinux The risk or severity of bleeding and bruising can be increased when Idraparinux is combined with Obeticholic acid.
Astaxanthin The risk or severity of bleeding and bruising can be increased when Astaxanthin is combined with Obeticholic acid.
Apixaban The risk or severity of bleeding and bruising can be increased when Apixaban is combined with Obeticholic acid.
Otamixaban The risk or severity of bleeding and bruising can be increased when Otamixaban is combined with Obeticholic acid.
Amediplase The risk or severity of bleeding and bruising can be increased when Amediplase is combined with Obeticholic acid.
Dabigatran etexilate The risk or severity of bleeding and bruising can be increased when Dabigatran etexilate is combined with Obeticholic acid.
Danaparoid The risk or severity of bleeding and bruising can be increased when Danaparoid is combined with Obeticholic acid.
Dalteparin The risk or severity of bleeding and bruising can be increased when Dalteparin is combined with Obeticholic acid.
Tinzaparin The risk or severity of bleeding and bruising can be increased when Tinzaparin is combined with Obeticholic acid.
Ethyl biscoumacetate The risk or severity of bleeding and bruising can be increased when Ethyl biscoumacetate is combined with Obeticholic acid.
Nadroparin The risk or severity of bleeding and bruising can be increased when Nadroparin is combined with Obeticholic acid.
Ditazole The risk or severity of bleeding and bruising can be increased when Ditazole is combined with Obeticholic acid.
Edoxaban The risk or severity of bleeding and bruising can be increased when Edoxaban is combined with Obeticholic acid.
Sodium citrate The risk or severity of bleeding and bruising can be increased when Sodium citrate is combined with Obeticholic acid.
Dextran The risk or severity of bleeding and bruising can be increased when Dextran is combined with Obeticholic acid.
Bemiparin The risk or severity of bleeding and bruising can be increased when Bemiparin is combined with Obeticholic acid.
Parnaparin The risk or severity of bleeding and bruising can be increased when Parnaparin is combined with Obeticholic acid.
Desirudin The risk or severity of bleeding and bruising can be increased when Desirudin is combined with Obeticholic acid.
Antithrombin Alfa The risk or severity of bleeding and bruising can be increased when Antithrombin Alfa is combined with Obeticholic acid.
Protein C The risk or severity of bleeding and bruising can be increased when Protein C is combined with Obeticholic acid.
Antithrombin III human The risk or severity of bleeding and bruising can be increased when Antithrombin III human is combined with Obeticholic acid.
Letaxaban The risk or severity of bleeding and bruising can be increased when Letaxaban is combined with Obeticholic acid.
Darexaban The risk or severity of bleeding and bruising can be increased when Darexaban is combined with Obeticholic acid.
Betrixaban The risk or severity of bleeding and bruising can be increased when Betrixaban is combined with Obeticholic acid.
Nafamostat The risk or severity of bleeding and bruising can be increased when Nafamostat is combined with Obeticholic acid.
Monteplase The risk or severity of bleeding and bruising can be increased when Monteplase is combined with Obeticholic acid.
Gabexate The risk or severity of bleeding and bruising can be increased when Gabexate is combined with Obeticholic acid.
Fluindione The risk or severity of bleeding and bruising can be increased when Fluindione is combined with Obeticholic acid.
Protein S human The risk or severity of bleeding and bruising can be increased when Protein S human is combined with Obeticholic acid.
Brinase The risk or severity of bleeding and bruising can be increased when Brinase is combined with Obeticholic acid.
Clorindione The risk or severity of bleeding and bruising can be increased when Clorindione is combined with Obeticholic acid.
Diphenadione The risk or severity of bleeding and bruising can be increased when Diphenadione is combined with Obeticholic acid.
Tioclomarol The risk or severity of bleeding and bruising can be increased when Tioclomarol is combined with Obeticholic acid.
Melagatran The risk or severity of bleeding and bruising can be increased when Melagatran is combined with Obeticholic acid.
Saruplase The risk or severity of bleeding and bruising can be increased when Saruplase is combined with Obeticholic acid.
Tocopherylquinone The risk or severity of bleeding and bruising can be increased when Tocopherylquinone is combined with Obeticholic acid.
Dabigatran The risk or severity of bleeding and bruising can be increased when Dabigatran is combined with Obeticholic acid.
Troxerutin The risk or severity of bleeding and bruising can be increased when Troxerutin is combined with Obeticholic acid.
Edetic acid The risk or severity of bleeding and bruising can be increased when Edetic acid is combined with Obeticholic acid.
Reviparin The risk or severity of bleeding and bruising can be increased when Reviparin is combined with Obeticholic acid.
Dermatan sulfate The risk or severity of bleeding and bruising can be increased when Dermatan sulfate is combined with Obeticholic acid.
SR-123781A The risk or severity of bleeding and bruising can be increased when SR-123781A is combined with Obeticholic acid.
Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Obeticholic acid.
Eptifibatide The risk or severity of adverse effects can be increased when Eptifibatide is combined with Obeticholic acid.
Ticlopidine The risk or severity of adverse effects can be increased when Ticlopidine is combined with Obeticholic acid.
Clopidogrel The risk or severity of adverse effects can be increased when Clopidogrel is combined with Obeticholic acid.
Tirofiban The risk or severity of adverse effects can be increased when Tirofiban is combined with Obeticholic acid.
Pentoxifylline The risk or severity of adverse effects can be increased when Pentoxifylline is combined with Obeticholic acid.
Acetylsalicylic acid The risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Obeticholic acid.
Dipyridamole The risk or severity of adverse effects can be increased when Dipyridamole is combined with Obeticholic acid.
Sulfinpyrazone The risk or severity of adverse effects can be increased when Sulfinpyrazone is combined with Obeticholic acid.
Cilostazol The risk or severity of adverse effects can be increased when Cilostazol is combined with Obeticholic acid.
Ridogrel The risk or severity of adverse effects can be increased when Ridogrel is combined with Obeticholic acid.
Epoprostenol The risk or severity of adverse effects can be increased when Epoprostenol is combined with Obeticholic acid.
Resveratrol The risk or severity of adverse effects can be increased when Resveratrol is combined with Obeticholic acid.
Nimesulide The risk or severity of adverse effects can be increased when Nimesulide is combined with Obeticholic acid.
Tesmilifene The risk or severity of adverse effects can be increased when Tesmilifene is combined with Obeticholic acid.
Defibrotide The risk or severity of adverse effects can be increased when Defibrotide is combined with Obeticholic acid.
Beraprost The risk or severity of adverse effects can be increased when Beraprost is combined with Obeticholic acid.
Ibudilast The risk or severity of adverse effects can be increased when Ibudilast is combined with Obeticholic acid.
Andrographolide The risk or severity of adverse effects can be increased when Andrographolide is combined with Obeticholic acid.
Caplacizumab The risk or severity of adverse effects can be increased when Caplacizumab is combined with Obeticholic acid.
Prasugrel The risk or severity of adverse effects can be increased when Prasugrel is combined with Obeticholic acid.
Cangrelor The risk or severity of adverse effects can be increased when Cangrelor is combined with Obeticholic acid.
Tranilast The risk or severity of adverse effects can be increased when Tranilast is combined with Obeticholic acid.
Triflusal The risk or severity of adverse effects can be increased when Triflusal is combined with Obeticholic acid.
Ticagrelor The risk or severity of adverse effects can be increased when Ticagrelor is combined with Obeticholic acid.
Icosapent ethyl The risk or severity of adverse effects can be increased when Icosapent ethyl is combined with Obeticholic acid.
Vorapaxar The risk or severity of adverse effects can be increased when Vorapaxar is combined with Obeticholic acid.
Trapidil The risk or severity of adverse effects can be increased when Trapidil is combined with Obeticholic acid.
Naftopidil The risk or severity of adverse effects can be increased when Naftopidil is combined with Obeticholic acid.
Sarpogrelate The risk or severity of adverse effects can be increased when Sarpogrelate is combined with Obeticholic acid.
Ifetroban The risk or severity of adverse effects can be increased when Ifetroban is combined with Obeticholic acid.
Nitroaspirin The risk or severity of adverse effects can be increased when Nitroaspirin is combined with Obeticholic acid.

Target Protein

Bile acid receptor NR1H4

Referensi & Sumber

Synthesis reference: He XL, Wang LT, Gu XZ, Xiao JX, Qiu WW. A facile synthesis of ursodeoxycholic acid and obeticholic acid from cholic acid.J.steroids.2018.10.009. Epub 2018 Oct 31.
Artikel (PubMed)
  • PMID: 27406083
    Markham A, Keam SJ: Obeticholic Acid: First Global Approval. Drugs. 2016 Aug;76(12):1221-6. doi: 10.1007/s40265-016-0616-x.
  • PMID: 31813639
    Eslam M, Alvani R, Shiha G: Obeticholic acid: towards first approval for NASH. Lancet. 2019 Dec 14;394(10215):2131-2133. doi: 10.1016/S0140-6736(19)32963-0. Epub 2019 Dec 5.
  • PMID: 30844895
    Manne V, Kowdley KV: Obeticholic acid in primary biliary cholangitis: where we stand. Curr Opin Gastroenterol. 2019 May;35(3):191-196. doi: 10.1097/MOG.0000000000000525.
  • PMID: 17641080
    Jones DE: Pathogenesis of primary biliary cirrhosis. Gut. 2007 Nov;56(11):1615-24. doi: 10.1136/gut.2007.122150. Epub 2007 Jul 19.
  • PMID: 31061656
    Onofrio FQ, Hirschfield GM, Gulamhusein AF: A Practical Review of Primary Biliary Cholangitis for the Gastroenterologist. Gastroenterol Hepatol (N Y). 2019 Mar;15(3):145-154.
  • PMID: 27621676
    Bowlus CL: Obeticholic acid for the treatment of primary biliary cholangitis in adult patients: clinical utility and patient selection. Hepat Med. 2016 Sep 1;8:89-95. doi: 10.2147/HMER.S91709. eCollection 2016.
  • PMID: 27743502
    Edwards JE, LaCerte C, Peyret T, Gosselin NH, Marier JF, Hofmann AF, Shapiro D: Modeling and Experimental Studies of Obeticholic Acid Exposure and the Impact of Cirrhosis Stage. Clin Transl Sci. 2016 Dec;9(6):328-336. doi: 10.1111/cts.12421. Epub 2016 Oct 15.

Contoh Produk & Brand

Produk: 8 • International brands: 1
Produk
  • Ocaliva
    Tablet • 5 mg • Oral • Canada • Approved
  • Ocaliva
    Tablet • 10 mg • Oral • Canada • Approved
  • Ocaliva
    Tablet, film coated • 5 mg • Oral • EU
  • Ocaliva
    Tablet, film coated • 10 mg • Oral • EU
  • Ocaliva
    Tablet, film coated • 5 mg • Oral • EU
  • Ocaliva
    Tablet, film coated • 5 mg/1 • Oral • US • Approved
  • Ocaliva
    Tablet, film coated • 10 mg/1 • Oral • US • Approved
  • Ocaliva
    Tablet, film coated • 10 mg • Oral • EU
International Brands
  • Ocaliva

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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