Peringatan Keamanan

Patients experiencing an overdose of finerenone may experience hyperkalemia.L34739 In the even of an overdose, immediately stop taking finerenone.L34739 Treat patients with symptomatic and supportive treatment, including treatment for hyperkalemia if it develops.L34739 Hemodialysis is not expected to remove finerenone from the blood due to its high plasma protein binding.L34739

Finerenone

DB16165

small molecule approved investigational

Deskripsi

Finerenone, or BAY 94-8862, is a mineralocorticoid receptor antagonist indicated to reduce the risk of sustained decline in glomerular filtration rate, end stage kidney disease, cardiovascular death, heart attacks, and hospitalization due to heart failure in adults with chronic kidney disease associated with type II diabetes mellitus.A236519,L34739 Patients with kidney disease, would originally be given spironolactone or eplerenone to antagonize the mineraclocorticoid receptor.A236544 Spironolactone has low selectivity and affinity for the receptor; it dissociates quickly and can also have effects at the androgen, progesterone, and glucocorticoid receptors.A236544 Eplerenone is more selective and has longer lasting effects.A236544 More selective nonsteroidal mineralocorticoid antagonists such as apararenone, esaxerenone, and finerenone were later developed.A236544 So far, finerenone is the only nonsteroidal mineralocorticoid receptor antagonist to be FDA approved.A236544,L34739

Finerenone was granted FDA approval on 9 July 2021,L34739 followed by the EMA approval on 11 March 2022.L41449

Struktur Molekul 2D

Berat 378.432
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of a 10 mg dose of finerenone in 4 healthy men was 17.4 hours in plasma and 12.3 hours in whole blood.[A236519] The terminal half life of finerenone is approximately 2-3 hours.[L34739]
Volume Distribusi The volume of distribution of finerenone as steady state is 52.6L.[L34739]
Klirens (Clearance) The systemic clearance of finerenone is approximately 25 L/h.[L34739]

Absorpsi

A 10 mg oral dose of finerenone reaches a Cmax of 351 µg/L, with a Tmax of 1.5 hours, and an AUC of 2820 µg\*h/L in plasma.A236519 The same dose of finerenone reaches a Cmax of 226 µg/L, with a Tmax of 1.5 hours, and an AUC of 1840 µg\*h/L in whole blood.A236519 Regular doses of 20 mg of finerenone reach a geometric mean steady state Cmax of 160 µg/L with an AUC of 686 µg\*h/L.L34739

Metabolisme

Finerenone is approximately 90% metabolized by CYP3A4, and 10% metabolized by CYP2C8.A236519,L34739 There is a minor contribution to metabolism by CYP1A1.A236519 Finerenone has no active metabolites.A236524 Finerenone is aromatized to the M1 metabolite by CYP3A4 and CYP2C8, which is further hydroxylated by CYP3A4 to the M2 metabolite, and finally oxidized bye CYP3A4 to the M3 metabolite.A236519 Alternatively, finerenone can undergo epoxidation and possibly hydrolysis by CYP3A4 and CYP2C8 to form the M4 metabolite, which is hydroxylated again by CYP3A4 to the M5 metabolite, and oxidized to the M8 metabolite.A236519 Finerenone can also be hydroxylated by CYP2C8 to the M7 metabolite, and further oxidized to the M9 metabolite.A236519 The M10 metabolite is formed by the demethylation, oxidation, and ring opening of finerenone.A236519 The M13 metabolite is formed through de-ethylation of finerenone by CYP1A1, and the M14 metabolite is formed through an undefined multi-step process involving CYP2C8 and CYP3A4.A236519

Rute Eliminasi

The majority of the dose recovered in urine was in the form of the M2, M3 (47.8%), and M4 metabolites; <1.3% of the dose recovered in the urine was as the unchanged parent compound.A236519 The majority of the dose recovered in the feces was as the M5 metabolite, with only 0.2% eliminated as the unchanged parent compound.A236519 The M1 metabolite made up <1.5% of the recovered dose in urine and feces.A236519 Finerenone is not expected to be metabolized by the intestinal microflora.A236519

Interaksi Makanan

2 Data
  • 1. Avoid grapefruit products. Grapefruit products may increase exposure to finerenone, increasing the risk and severity of adverse effects.
  • 2. Take with or without food. Food does not have a clinically significant effect on area under the curve.

Interaksi Obat

1224 Data
Mifepristone The serum concentration of Finerenone can be increased when it is combined with Mifepristone.
Secobarbital The metabolism of Finerenone can be increased when combined with Secobarbital.
Troglitazone The metabolism of Finerenone can be decreased when combined with Troglitazone.
Spironolactone The risk or severity of hyperkalemia can be increased when Finerenone is combined with Spironolactone.
Trimethoprim The metabolism of Finerenone can be decreased when combined with Trimethoprim.
Levothyroxine The metabolism of Finerenone can be decreased when combined with Levothyroxine.
Loratadine The metabolism of Finerenone can be decreased when combined with Loratadine.
Medroxyprogesterone acetate The metabolism of Finerenone can be decreased when combined with Medroxyprogesterone acetate.
Pioglitazone The metabolism of Finerenone can be decreased when combined with Pioglitazone.
Genistein The metabolism of Finerenone can be decreased when combined with Genistein.
Eltrombopag The metabolism of Finerenone can be decreased when combined with Eltrombopag.
Teriflunomide The metabolism of Finerenone can be decreased when combined with Teriflunomide.
Clopidogrel The metabolism of Finerenone can be decreased when combined with Clopidogrel.
Candesartan cilexetil The metabolism of Finerenone can be decreased when combined with Candesartan cilexetil.
Salmeterol The metabolism of Finerenone can be decreased when combined with Salmeterol.
Felodipine The metabolism of Finerenone can be decreased when combined with Felodipine.
Gemfibrozil The metabolism of Finerenone can be decreased when combined with Gemfibrozil.
Trametinib Finerenone may increase the excretion rate of Trametinib which could result in a lower serum level and potentially a reduction in efficacy.
Mometasone furoate The metabolism of Finerenone can be decreased when combined with Mometasone furoate.
Icosapent The risk or severity of hyperkalemia can be increased when Icosapent is combined with Finerenone.
Valsartan The risk or severity of hyperkalemia can be increased when Valsartan is combined with Finerenone.
Ramipril The risk or severity of hyperkalemia can be increased when Ramipril is combined with Finerenone.
Esmolol The risk or severity of hyperkalemia can be increased when Esmolol is combined with Finerenone.
Betaxolol The risk or severity of hyperkalemia can be increased when Betaxolol is combined with Finerenone.
Succinylcholine The risk or severity of hyperkalemia can be increased when Succinylcholine is combined with Finerenone.
Mesalazine The risk or severity of hyperkalemia can be increased when Mesalazine is combined with Finerenone.
Metoprolol The risk or severity of hyperkalemia can be increased when Metoprolol is combined with Finerenone.
Olmesartan The risk or severity of hyperkalemia can be increased when Olmesartan is combined with Finerenone.
Indomethacin The risk or severity of hyperkalemia can be increased when Indomethacin is combined with Finerenone.
Atenolol The risk or severity of hyperkalemia can be increased when Atenolol is combined with Finerenone.
Timolol The risk or severity of hyperkalemia can be increased when Timolol is combined with Finerenone.
Amlodipine The risk or severity of hyperkalemia can be increased when Amlodipine is combined with Finerenone.
Triamterene The risk or severity of hyperkalemia can be increased when Triamterene is combined with Finerenone.
Digoxin The risk or severity of hyperkalemia can be increased when Digoxin is combined with Finerenone.
Nimodipine The risk or severity of hyperkalemia can be increased when Nimodipine is combined with Finerenone.
Nisoldipine The risk or severity of hyperkalemia can be increased when Nisoldipine is combined with Finerenone.
Ardeparin The risk or severity of hyperkalemia can be increased when Ardeparin is combined with Finerenone.
Nabumetone The risk or severity of hyperkalemia can be increased when Nabumetone is combined with Finerenone.
Tenoxicam The risk or severity of hyperkalemia can be increased when Tenoxicam is combined with Finerenone.
Sotalol The risk or severity of hyperkalemia can be increased when Sotalol is combined with Finerenone.
Fosinopril The risk or severity of hyperkalemia can be increased when Fosinopril is combined with Finerenone.
Tolmetin The risk or severity of hyperkalemia can be increased when Tolmetin is combined with Finerenone.
Trandolapril The risk or severity of hyperkalemia can be increased when Trandolapril is combined with Finerenone.
Lercanidipine The risk or severity of hyperkalemia can be increased when Lercanidipine is combined with Finerenone.
Benazepril The risk or severity of hyperkalemia can be increased when Benazepril is combined with Finerenone.
Lamotrigine The risk or severity of hyperkalemia can be increased when Lamotrigine is combined with Finerenone.
Cinnarizine The risk or severity of hyperkalemia can be increased when Cinnarizine is combined with Finerenone.
Propranolol The risk or severity of hyperkalemia can be increased when Propranolol is combined with Finerenone.
Fenoprofen The risk or severity of hyperkalemia can be increased when Fenoprofen is combined with Finerenone.
Valdecoxib The risk or severity of hyperkalemia can be increased when Valdecoxib is combined with Finerenone.
Enalapril The risk or severity of hyperkalemia can be increased when Enalapril is combined with Finerenone.
Ethosuximide The risk or severity of hyperkalemia can be increased when Ethosuximide is combined with Finerenone.
Amiloride The risk or severity of hyperkalemia can be increased when Amiloride is combined with Finerenone.
Labetalol The risk or severity of hyperkalemia can be increased when Labetalol is combined with Finerenone.
Sulindac The risk or severity of hyperkalemia can be increased when Sulindac is combined with Finerenone.
Bisoprolol The risk or severity of hyperkalemia can be increased when Bisoprolol is combined with Finerenone.
Magnesium sulfate The risk or severity of dehydration can be increased when Finerenone is combined with Magnesium sulfate.
Moexipril The risk or severity of hyperkalemia can be increased when Moexipril is combined with Finerenone.
Nitrofurantoin The risk or severity of hyperkalemia can be increased when Nitrofurantoin is combined with Finerenone.
Eplerenone The risk or severity of hyperkalemia can be increased when Eplerenone is combined with Finerenone.
Flurbiprofen The risk or severity of hyperkalemia can be increased when Flurbiprofen is combined with Finerenone.
Lisinopril The risk or severity of hyperkalemia can be increased when Lisinopril is combined with Finerenone.
Pentamidine The risk or severity of hyperkalemia can be increased when Pentamidine is combined with Finerenone.
Mannitol The risk or severity of dehydration can be increased when Finerenone is combined with Mannitol.
Etodolac The risk or severity of hyperkalemia can be increased when Etodolac is combined with Finerenone.
Mefenamic acid The risk or severity of hyperkalemia can be increased when Mefenamic acid is combined with Finerenone.
Perindopril The risk or severity of hyperkalemia can be increased when Perindopril is combined with Finerenone.
Sulfasalazine The risk or severity of hyperkalemia can be increased when Sulfasalazine is combined with Finerenone.
Phenylbutazone The risk or severity of hyperkalemia can be increased when Phenylbutazone is combined with Finerenone.
Meloxicam The therapeutic efficacy of Finerenone can be decreased when used in combination with Meloxicam.
Carprofen The risk or severity of hyperkalemia can be increased when Carprofen is combined with Finerenone.
Levomenthol The risk or severity of hyperkalemia can be increased when Levomenthol is combined with Finerenone.
Diflunisal The risk or severity of hyperkalemia can be increased when Diflunisal is combined with Finerenone.
Alprenolol The risk or severity of hyperkalemia can be increased when Alprenolol is combined with Finerenone.
Eprosartan The risk or severity of hyperkalemia can be increased when Eprosartan is combined with Finerenone.
Quinapril The risk or severity of hyperkalemia can be increased when Quinapril is combined with Finerenone.
Omapatrilat The risk or severity of hyperkalemia can be increased when Omapatrilat is combined with Finerenone.
Zonisamide The risk or severity of hyperkalemia can be increased when Zonisamide is combined with Finerenone.
Salicylic acid The risk or severity of hyperkalemia can be increased when Salicylic acid is combined with Finerenone.
Meclofenamic acid The risk or severity of hyperkalemia can be increased when Meclofenamic acid is combined with Finerenone.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Finerenone which could result in a higher serum level.
Pindolol The risk or severity of hyperkalemia can be increased when Pindolol is combined with Finerenone.
Telmisartan The risk or severity of hyperkalemia can be increased when Telmisartan is combined with Finerenone.
Oxaprozin The risk or severity of hyperkalemia can be increased when Oxaprozin is combined with Finerenone.
Balsalazide The risk or severity of hyperkalemia can be increased when Balsalazide is combined with Finerenone.
Nitrendipine The risk or severity of hyperkalemia can be increased when Nitrendipine is combined with Finerenone.
Perhexiline The risk or severity of hyperkalemia can be increased when Perhexiline is combined with Finerenone.
Heparin The risk or severity of hyperkalemia can be increased when Heparin is combined with Finerenone.
Carvedilol The risk or severity of hyperkalemia can be increased when Carvedilol is combined with Finerenone.
Rescinnamine The risk or severity of hyperkalemia can be increased when Rescinnamine is combined with Finerenone.
Propafenone The risk or severity of hyperkalemia can be increased when Propafenone is combined with Finerenone.
Acebutolol The risk or severity of hyperkalemia can be increased when Acebutolol is combined with Finerenone.
Captopril The risk or severity of hyperkalemia can be increased when Captopril is combined with Finerenone.
Nadolol The risk or severity of hyperkalemia can be increased when Nadolol is combined with Finerenone.
Dantrolene The risk or severity of hyperkalemia can be increased when Dantrolene is combined with Finerenone.
Enoxaparin The risk or severity of hyperkalemia can be increased when Enoxaparin is combined with Finerenone.
Bepridil The risk or severity of hyperkalemia can be increased when Bepridil is combined with Finerenone.
Lumiracoxib The risk or severity of hyperkalemia can be increased when Lumiracoxib is combined with Finerenone.
Bevantolol The risk or severity of hyperkalemia can be increased when Bevantolol is combined with Finerenone.
Practolol The risk or severity of hyperkalemia can be increased when Practolol is combined with Finerenone.

Target Protein

Mineralocorticoid receptor NR3C2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 30171161
    Gerisch M, Heinig R, Engelen A, Lang D, Kolkhof P, Radtke M, Platzek J, Lovis K, Rohde G, Schwarz T: Biotransformation of Finerenone, a Novel Nonsteroidal Mineralocorticoid Receptor Antagonist, in Dogs, Rats, and Humans, In Vivo and In Vitro. Drug Metab Dispos. 2018 Nov;46(11):1546-1555. doi: 10.1124/dmd.118.083337. Epub 2018 Aug 31.
  • PMID: 33857953
    Epstein M: Aldosterone and Mineralocorticoid Receptor Signaling as Determinants of Cardiovascular and Renal Injury: From Hans Selye to the Present. Am J Nephrol. 2021;52(3):209-216. doi: 10.1159/000515622. Epub 2021 Apr 15.
  • PMID: 34015478
    Filippatos G, Bakris GL, Pitt B, Agarwal R, Rossing P, Ruilope LM, Butler J, Lam CSP, Kolkhof P, Roberts L, Tasto C, Joseph A, Anker SD: Finerenone Reduces New-Onset Atrial Fibrillation in Patients With Chronic Kidney Disease and Type 2 Diabetes. J Am Coll Cardiol. 2021 Jul 13;78(2):142-152. doi: 10.1016/j.jacc.2021.04.079. Epub 2021 May 17.
  • PMID: 34026868
    Li Z, Zhao H, Wang J: Metabolism and Chronic Inflammation: The Links Between Chronic Heart Failure and Comorbidities. Front Cardiovasc Med. 2021 May 5;8:650278. doi: 10.3389/fcvm.2021.650278. eCollection 2021.
  • PMID: 19617444
    Yang J, Young MJ: The mineralocorticoid receptor and its coregulators. J Mol Endocrinol. 2009 Aug;43(2):53-64. doi: 10.1677/JME-09-0031.
  • PMID: 34208285
    Vodosek Hojs N, Bevc S, Ekart R, Piko N, Petreski T, Hojs R: Mineralocorticoid Receptor Antagonists in Diabetic Kidney Disease. Pharmaceuticals (Basel). 2021 Jun 11;14(6). pii: ph14060561. doi: 10.3390/ph14060561.

Contoh Produk & Brand

Produk: 14 • International brands: 1
Produk
  • Kerendia
    Tablet • 20 mg • Oral • Canada • Approved
  • Kerendia
    Tablet, film coated • 10 mg • Oral • EU • Approved
  • Kerendia
    Tablet, film coated • 10 mg • Oral • EU • Approved
  • Kerendia
    Tablet, film coated • 10 mg • Oral • EU • Approved
  • Kerendia
    Tablet, film coated • 10 mg/1 • Oral • US • Approved
  • Kerendia
    Tablet, film coated • 10 mg • Oral • EU • Approved
  • Kerendia
    Tablet, film coated • 20 mg/1 • Oral • US • Approved
  • Kerendia
    Tablet, film coated • 10 mg • Oral • EU • Approved
Menampilkan 8 dari 14 produk.
International Brands
  • Kerendia — Bayer

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul