Peringatan Keamanan

Odanacatib was found to increase the risk of stroke A19388. No further toxicological studies have been performed.

Odanacatib

DB06670

small molecule investigational

Deskripsi

Odanacatib is an inhibiter of cathepsin K which was originally developed be Merck & Co as a new treatment for osteoporosis A19388. The drug made it to phase III trials before abandoned due to increased stroke.

Struktur Molekul 2D

Berat 525.56
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Apparent half life observed to be 87.3-94.7h [A19389].
Volume Distribusi 100L [A19391]
Klirens (Clearance) Total clearance of 0.8L/h [A19391].

Absorpsi

Tmax of 2-6h A19389. The absolute bioavailabilities observed with 30mg and 50 mg doses are 70% and 30% respectively. When taken with high fat meals the 50mg dose's bioavailability increases to 49% and tmax increases to 10.5h A19391.

Metabolisme

The major metabolite is the product of hydroxylation by CYP3A4 and CYP2C8 A19392. This metabolite is active but is 25 times less effective at inhibiting cathepsin K than odanacatib. The other metabolites are produced through glutathione conjugation, hydrolysis, dealkylation, glucuronidation, oxidation, and cyclization.

Rute Eliminasi

16.9% excreted in urine. 74.5% excreted in feces.

Interaksi Obat

464 Data
Ranolazine The serum concentration of Odanacatib can be increased when it is combined with Ranolazine.
Mifepristone The serum concentration of Odanacatib can be increased when it is combined with Mifepristone.
Lumacaftor The serum concentration of Odanacatib can be decreased when it is combined with Lumacaftor.
Secobarbital The metabolism of Odanacatib can be increased when combined with Secobarbital.
Phenobarbital The metabolism of Odanacatib can be increased when combined with Phenobarbital.
Rifampin The metabolism of Odanacatib can be increased when combined with Rifampicin.
Bexarotene The metabolism of Odanacatib can be decreased when combined with Bexarotene.
Diltiazem The metabolism of Odanacatib can be decreased when combined with Diltiazem.
Medroxyprogesterone acetate The metabolism of Odanacatib can be decreased when combined with Medroxyprogesterone acetate.
Nicardipine The metabolism of Odanacatib can be decreased when combined with Nicardipine.
Irbesartan The metabolism of Odanacatib can be decreased when combined with Irbesartan.
Oxybutynin The metabolism of Odanacatib can be decreased when combined with Oxybutynin.
Fluvastatin The metabolism of Odanacatib can be decreased when combined with Fluvastatin.
Pioglitazone The metabolism of Odanacatib can be decreased when combined with Pioglitazone.
Topiroxostat The metabolism of Odanacatib can be decreased when combined with Topiroxostat.
Abiraterone The metabolism of Odanacatib can be decreased when combined with Abiraterone.
Eltrombopag The metabolism of Odanacatib can be decreased when combined with Eltrombopag.
Teriflunomide The metabolism of Odanacatib can be decreased when combined with Teriflunomide.
Levothyroxine The metabolism of Odanacatib can be decreased when combined with Levothyroxine.
Loratadine The metabolism of Odanacatib can be decreased when combined with Loratadine.
Genistein The metabolism of Odanacatib can be decreased when combined with Genistein.
Trimethoprim The metabolism of Odanacatib can be decreased when combined with Trimethoprim.
Fluticasone propionate The metabolism of Odanacatib can be decreased when combined with Fluticasone propionate.
Clopidogrel The metabolism of Odanacatib can be decreased when combined with Clopidogrel.
Candesartan cilexetil The metabolism of Odanacatib can be decreased when combined with Candesartan cilexetil.
Salmeterol The metabolism of Odanacatib can be decreased when combined with Salmeterol.
Gemfibrozil The metabolism of Odanacatib can be decreased when combined with Gemfibrozil.
Fluticasone The metabolism of Odanacatib can be decreased when combined with Fluticasone.
Mometasone furoate The metabolism of Odanacatib can be decreased when combined with Mometasone furoate.
Felodipine The metabolism of Odanacatib can be decreased when combined with Felodipine.
Vemurafenib The serum concentration of Odanacatib can be increased when it is combined with Vemurafenib.
Apalutamide The serum concentration of Odanacatib can be decreased when it is combined with Apalutamide.
Pitolisant The serum concentration of Odanacatib can be decreased when it is combined with Pitolisant.
Isavuconazole The serum concentration of Odanacatib can be increased when it is combined with Isavuconazole.
Isavuconazonium The serum concentration of Odanacatib can be increased when it is combined with Isavuconazonium.
Fluconazole The metabolism of Odanacatib can be decreased when combined with Fluconazole.
Erythromycin The serum concentration of Odanacatib can be increased when it is combined with Erythromycin.
Reserpine The serum concentration of Odanacatib can be increased when it is combined with Reserpine.
Loxapine The serum concentration of Odanacatib can be increased when it is combined with Loxapine.
Quinine The metabolism of Odanacatib can be decreased when combined with Quinine.
Toremifene The serum concentration of Odanacatib can be increased when it is combined with Toremifene.
Verapamil The metabolism of Odanacatib can be decreased when combined with Verapamil.
Tamoxifen The metabolism of Odanacatib can be decreased when combined with Tamoxifen.
Zonisamide The serum concentration of Odanacatib can be increased when it is combined with Zonisamide.
Carvedilol The serum concentration of Odanacatib can be increased when it is combined with Carvedilol.
Propafenone The serum concentration of Odanacatib can be increased when it is combined with Propafenone.
Lapatinib The serum concentration of Odanacatib can be increased when it is combined with Lapatinib.
Paliperidone The serum concentration of Odanacatib can be increased when it is combined with Paliperidone.
Mibefradil The serum concentration of Odanacatib can be increased when it is combined with Mibefradil.
Biricodar The serum concentration of Odanacatib can be increased when it is combined with Biricodar.
Elacridar The serum concentration of Odanacatib can be increased when it is combined with Elacridar.
Flibanserin The serum concentration of Odanacatib can be increased when it is combined with Flibanserin.
Vandetanib The serum concentration of Odanacatib can be increased when it is combined with Vandetanib.
Zosuquidar The serum concentration of Odanacatib can be increased when it is combined with Zosuquidar.
Tariquidar The serum concentration of Odanacatib can be increased when it is combined with Tariquidar.
Simeprevir The metabolism of Odanacatib can be decreased when combined with Simeprevir.
Brefeldin A The serum concentration of Odanacatib can be increased when it is combined with Brefeldin A.
Ivacaftor The serum concentration of Odanacatib can be increased when it is combined with Ivacaftor.
Crizotinib The serum concentration of Odanacatib can be increased when it is combined with Crizotinib.
Linagliptin The metabolism of Odanacatib can be decreased when combined with Linagliptin.
Regorafenib The serum concentration of Odanacatib can be increased when it is combined with Regorafenib.
Canagliflozin The serum concentration of Odanacatib can be increased when it is combined with Canagliflozin.
Afatinib The serum concentration of Odanacatib can be increased when it is combined with Afatinib.
Ledipasvir The serum concentration of Odanacatib can be increased when it is combined with Ledipasvir.
Vorapaxar The serum concentration of Odanacatib can be increased when it is combined with Vorapaxar.
Suvorexant The serum concentration of Odanacatib can be increased when it is combined with Suvorexant.
Netupitant The metabolism of Odanacatib can be decreased when combined with Netupitant.
Palbociclib The serum concentration of Odanacatib can be increased when it is combined with Palbociclib.
Daclatasvir The serum concentration of Odanacatib can be increased when it is combined with Daclatasvir.
Niguldipine The serum concentration of Odanacatib can be increased when it is combined with Niguldipine.
Rolapitant The serum concentration of Odanacatib can be increased when it is combined with Rolapitant.
Venetoclax The metabolism of Odanacatib can be decreased when combined with Venetoclax.
Asunaprevir The serum concentration of Odanacatib can be increased when it is combined with Asunaprevir.
Velpatasvir The serum concentration of Odanacatib can be increased when it is combined with Velpatasvir.
Neratinib The serum concentration of Odanacatib can be increased when it is combined with Neratinib.
Valspodar The serum concentration of Odanacatib can be increased when it is combined with Valspodar.
Dacomitinib The serum concentration of Odanacatib can be increased when it is combined with Dacomitinib.
Glasdegib The serum concentration of Odanacatib can be increased when it is combined with Glasdegib.
Voxilaprevir The serum concentration of Odanacatib can be increased when it is combined with Voxilaprevir.
Sarecycline The serum concentration of Odanacatib can be increased when it is combined with Sarecycline.
Laniquidar The serum concentration of Odanacatib can be increased when it is combined with Laniquidar.
Pibrentasvir The serum concentration of Odanacatib can be increased when it is combined with Pibrentasvir.
Glecaprevir The serum concentration of Odanacatib can be increased when it is combined with Glecaprevir.
Dexniguldipine The serum concentration of Odanacatib can be increased when it is combined with Dexniguldipine.
ONT-093 The serum concentration of Odanacatib can be increased when it is combined with ONT-093.
Ivosidenib The metabolism of Odanacatib can be increased when combined with Ivosidenib.
Dronedarone The metabolism of Odanacatib can be decreased when combined with Dronedarone.
Lomitapide The serum concentration of Odanacatib can be increased when it is combined with Lomitapide.
Entrectinib The serum concentration of Odanacatib can be increased when it is combined with Entrectinib.
Fedratinib The serum concentration of Odanacatib can be increased when it is combined with Fedratinib.
Norgestimate The serum concentration of Odanacatib can be increased when it is combined with Norgestimate.
Tacrolimus The serum concentration of Odanacatib can be increased when it is combined with Tacrolimus.
Carfilzomib The serum concentration of Odanacatib can be increased when it is combined with Carfilzomib.
Favipiravir The serum concentration of Odanacatib can be increased when it is combined with Favipiravir.
Methylene blue The serum concentration of Odanacatib can be increased when it is combined with Methylene blue.
Ripretinib The serum concentration of Odanacatib can be increased when it is combined with Ripretinib.
Pralsetinib The serum concentration of Odanacatib can be increased when it is combined with Pralsetinib.
Clofazimine The serum concentration of Odanacatib can be increased when it is combined with Clofazimine.
Arsenic trioxide The serum concentration of Odanacatib can be increased when it is combined with Arsenic trioxide.
Mefloquine The serum concentration of Odanacatib can be increased when it is combined with Mefloquine.

Target Protein

Cathepsin K CTSK

Referensi & Sumber

Artikel (PubMed)
  • PMID: 27681784
    Mullard A: Merck &Co. drops osteoporosis drug odanacatib. Nat Rev Drug Discov. 2016 Sep 29;15(10):669. doi: 10.1038/nrd.2016.207.
  • PMID: 24276460
    Anderson MS, Gendrano IN, Liu C, Jeffers S, Mahon C, Mehta A, Mostoller K, Zajic S, Morris D, Lee J, Stoch SA: Odanacatib, a selective cathepsin K inhibitor, demonstrates comparable pharmacodynamics and pharmacokinetics in older men and postmenopausal women. J Clin Endocrinol Metab. 2014 Feb;99(2):552-60. doi: 10.1210/jc.2013-1688. Epub 2013 Nov 25.
  • PMID: 27402726
    Zajic S, Rossenu S, Hreniuk D, Kesisoglou F, McCrea J, Liu F, Sun L, Witter R, Gauthier D, Helmy R, Joss D, Ni T, Stoltz R, Stone J, Stoch SA: The Absolute Bioavailability and Effect of Food on the Pharmacokinetics of Odanacatib: A Stable-Label i.v./Oral Study in Healthy Postmenopausal Women. Drug Metab Dispos. 2016 Sep;44(9):1450-8. doi: 10.1124/dmd.116.069906. Epub 2016 Jul 11.
  • PMID: 24553380
    Kassahun K, McIntosh I, Koeplinger K, Sun L, Talaty JE, Miller DL, Dixon R, Zajic S, Stoch SA: Disposition and metabolism of the cathepsin K inhibitor odanacatib in humans. Drug Metab Dispos. 2014 May;42(5):818-27. doi: 10.1124/dmd.113.056580. Epub 2014 Feb 19.
  • PMID: 22228398
    Boonen S, Rosenberg E, Claessens F, Vanderschueren D, Papapoulos S: Inhibition of cathepsin K for treatment of osteoporosis. Curr Osteoporos Rep. 2012 Mar;10(1):73-9. doi: 10.1007/s11914-011-0085-9.
  • PMID: 18226527
    Gauthier JY, Chauret N, Cromlish W, Desmarais S, Duong LT, Falgueyret JP, Kimmel DB, Lamontagne S, Leger S, LeRiche T, Li CS, Masse F, McKay DJ, Nicoll-Griffith DA, Oballa RM, Palmer JT, Percival MD, Riendeau D, Robichaud J, Rodan GA, Rodan SB, Seto C, Therien M, Truong VL, Venuti MC, Wesolowski G, Young RN, Zamboni R, Black WC: The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8. doi: 10.1016/j.bmcl.2007.12.047. Epub 2008 Jan 15.
  • PMID: 20337585
    Black WC: Peptidomimetic inhibitors of cathepsin K. Curr Top Med Chem. 2010;10(7):745-51.

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