Estradiol dienanthate

DB13955

small molecule approved investigational vet_approved

Deskripsi

Estradiol Dienanthate is a pro-drug ester of DB00783, a naturally occurring hormone that circulates endogenously within the human body. Estradiol is the most potent form of all mammalian estrogenic steroids and acts as the major female sex hormone. As a pro-drug of estradiol, estradiol benzoate therefore has the same downstream effects within the body through binding to the Estrogen Receptor (ER) including ER? and ER? subtypes, which are located in various tissues including in the breasts, uterus, ovaries, skin, prostate, bone, fat, and brain.

Estradiol is commonly produced with an ester side-chain as endogenous estradiol has very low oral bioavailability on its own (2-10%). First-pass metabolism by the gut and the liver quickly degrades the estradiol molecule before it gets a chance to enter systemic circulation and exert its estrogenic effects A12102. Esterification of estradiol aims to improves absorption and bioavailability after oral administration (such as with Estradiol valerate) or to sustain release from depot intramuscular injections (such as with Estradiol Cypionate) through improved lipophilicity. Following absorption, the esters are cleaved, resulting in the release of endogenous estradiol, or 17?-estradiol. Ester pro-drugs of estradiol are therefore considered to be bioidentical forms of estrogen T84.

Estradiol dienanthate is not currently available in any commercially available products in Canada or the US.

Struktur Molekul 2D

Berat 496.732
Wujud -

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) -
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Exogenous estrogens are metabolized using the same mechanism as endogenous estrogens. Estrogens are partially metabolized by cytochrome P450.

Rute Eliminasi

Estradiol, estrone and estriol are excreted in the urine along with glucuronide and sulfate conjugates.

Interaksi Obat

1460 Data
Tizanidine The serum concentration of Tizanidine can be increased when it is combined with Estradiol dienanthate.
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Estradiol dienanthate.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Estradiol dienanthate.
Deferasirox The serum concentration of Estradiol dienanthate can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Estradiol dienanthate can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Estradiol dienanthate can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Estradiol dienanthate can be decreased when it is combined with Teriflunomide.
Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Estradiol dienanthate.
Mifepristone The serum concentration of Estradiol dienanthate can be increased when it is combined with Mifepristone.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Estradiol dienanthate.
Perampanel The metabolism of Perampanel can be increased when combined with Estradiol dienanthate.
Warfarin The metabolism of Warfarin can be increased when combined with Estradiol dienanthate.
Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Estradiol dienanthate.
(R)-warfarin The metabolism of (R)-warfarin can be increased when combined with Estradiol dienanthate.
R,S-Warfarin alcohol The metabolism of R,S-Warfarin alcohol can be increased when combined with Estradiol dienanthate.
S,R-Warfarin alcohol The metabolism of S,R-Warfarin alcohol can be increased when combined with Estradiol dienanthate.
(S)-Warfarin The metabolism of (S)-Warfarin can be increased when combined with Estradiol dienanthate.
Zidovudine The metabolism of Estradiol dienanthate can be increased when combined with Zidovudine.
Lamotrigine The metabolism of Estradiol dienanthate can be increased when combined with Lamotrigine.
Ethinylestradiol The metabolism of Estradiol dienanthate can be increased when combined with Ethinylestradiol.
Testosterone propionate The metabolism of Estradiol dienanthate can be increased when combined with Testosterone propionate.
Abiraterone The serum concentration of Estradiol dienanthate can be increased when it is combined with Abiraterone.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Estradiol dienanthate.
Cyproterone acetate The metabolism of Estradiol dienanthate can be increased when combined with Cyproterone acetate.
Erlotinib The serum concentration of Erlotinib can be decreased when it is combined with Estradiol dienanthate.
Primidone The metabolism of Estradiol dienanthate can be increased when combined with Primidone.
Albendazole The metabolism of Estradiol dienanthate can be increased when combined with Albendazole.
Caffeine The metabolism of Estradiol dienanthate can be decreased when combined with Caffeine.
Moxifloxacin The metabolism of Estradiol dienanthate can be decreased when combined with Moxifloxacin.
Mexiletine The metabolism of Estradiol dienanthate can be decreased when combined with Mexiletine.
Alosetron The metabolism of Estradiol dienanthate can be decreased when combined with Alosetron.
Gatifloxacin The metabolism of Estradiol dienanthate can be decreased when combined with Gatifloxacin.
Simeprevir The metabolism of Estradiol dienanthate can be decreased when combined with Simeprevir.
Lobeglitazone The metabolism of Estradiol dienanthate can be decreased when combined with Lobeglitazone.
Pazufloxacin The metabolism of Estradiol dienanthate can be decreased when combined with Pazufloxacin.
Lidocaine The metabolism of Estradiol dienanthate can be decreased when combined with Lidocaine.
Osilodrostat The metabolism of Estradiol dienanthate can be decreased when combined with Osilodrostat.
Fluoxetine The metabolism of Estradiol dienanthate can be decreased when combined with Fluoxetine.
Nabilone The metabolism of Estradiol dienanthate can be decreased when combined with Nabilone.
Felbamate The metabolism of Estradiol dienanthate can be decreased when combined with Felbamate.
Sulfinpyrazone The metabolism of Estradiol dienanthate can be decreased when combined with Sulfinpyrazone.
Iproniazid The metabolism of Estradiol dienanthate can be decreased when combined with Iproniazid.
Medical Cannabis The metabolism of Estradiol dienanthate can be decreased when combined with Medical Cannabis.
Troglitazone The metabolism of Estradiol dienanthate can be decreased when combined with Troglitazone.
Imatinib The metabolism of Estradiol dienanthate can be decreased when combined with Imatinib.
Valproic acid The metabolism of Estradiol dienanthate can be decreased when combined with Valproic acid.
Fluconazole The metabolism of Estradiol dienanthate can be decreased when combined with Fluconazole.
Floxuridine The metabolism of Estradiol dienanthate can be decreased when combined with Floxuridine.
Nicardipine The metabolism of Estradiol dienanthate can be decreased when combined with Nicardipine.
Miconazole The metabolism of Estradiol dienanthate can be decreased when combined with Miconazole.
Gemfibrozil The metabolism of Estradiol dienanthate can be decreased when combined with Gemfibrozil.
Sulfaphenazole The metabolism of Estradiol dienanthate can be decreased when combined with Sulfaphenazole.
Secobarbital The metabolism of Estradiol dienanthate can be increased when combined with Secobarbital.
Bexarotene The metabolism of Estradiol dienanthate can be decreased when combined with Bexarotene.
Spironolactone Spironolactone may increase the excretion rate of Estradiol dienanthate which could result in a lower serum level and potentially a reduction in efficacy.
Medroxyprogesterone acetate The metabolism of Estradiol dienanthate can be decreased when combined with Medroxyprogesterone acetate.
Irbesartan The metabolism of Estradiol dienanthate can be decreased when combined with Irbesartan.
Oxybutynin The metabolism of Estradiol dienanthate can be decreased when combined with Oxybutynin.
Fluvastatin The metabolism of Estradiol dienanthate can be decreased when combined with Fluvastatin.
Pioglitazone The metabolism of Estradiol dienanthate can be decreased when combined with Pioglitazone.
Topiroxostat The metabolism of Estradiol dienanthate can be decreased when combined with Topiroxostat.
Trimethoprim The metabolism of Estradiol dienanthate can be decreased when combined with Trimethoprim.
Quinine The metabolism of Estradiol dienanthate can be decreased when combined with Quinine.
Loratadine The metabolism of Estradiol dienanthate can be decreased when combined with Loratadine.
Levothyroxine The metabolism of Estradiol dienanthate can be decreased when combined with Levothyroxine.
Fluticasone propionate The metabolism of Estradiol dienanthate can be decreased when combined with Fluticasone propionate.
Clopidogrel The metabolism of Estradiol dienanthate can be decreased when combined with Clopidogrel.
Candesartan cilexetil The metabolism of Estradiol dienanthate can be decreased when combined with Candesartan cilexetil.
Salmeterol The metabolism of Estradiol dienanthate can be decreased when combined with Salmeterol.
Fluticasone furoate The metabolism of Estradiol dienanthate can be decreased when combined with Fluticasone furoate.
Trametinib Trametinib may decrease the excretion rate of Estradiol dienanthate which could result in a higher serum level.
Fluticasone The metabolism of Estradiol dienanthate can be decreased when combined with Fluticasone.
Mometasone furoate The metabolism of Estradiol dienanthate can be decreased when combined with Mometasone furoate.
Felodipine The metabolism of Estradiol dienanthate can be decreased when combined with Felodipine.
Osimertinib The serum concentration of Estradiol dienanthate can be decreased when it is combined with Osimertinib.
Tipiracil The excretion of Tipiracil can be decreased when combined with Estradiol dienanthate.
Vemurafenib The serum concentration of Estradiol dienanthate can be increased when it is combined with Vemurafenib.
Pitolisant The serum concentration of Estradiol dienanthate can be decreased when it is combined with Pitolisant.
Folic acid Estradiol dienanthate may decrease the excretion rate of Folic acid which could result in a higher serum level.
Pravastatin Estradiol dienanthate may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Conjugated estrogens Estradiol dienanthate may decrease the excretion rate of Conjugated estrogens which could result in a higher serum level.
Cerivastatin Estradiol dienanthate may decrease the excretion rate of Cerivastatin which could result in a higher serum level.
Celecoxib Estradiol dienanthate may decrease the excretion rate of Celecoxib which could result in a higher serum level.
Sumatriptan Estradiol dienanthate may decrease the excretion rate of Sumatriptan which could result in a higher serum level.
Mycophenolate mofetil Estradiol dienanthate may decrease the excretion rate of Mycophenolate mofetil which could result in a higher serum level.
Nitrofurantoin Estradiol dienanthate may decrease the excretion rate of Nitrofurantoin which could result in a higher serum level.
Riluzole Estradiol dienanthate may decrease the excretion rate of Riluzole which could result in a higher serum level.
Sulfasalazine Estradiol dienanthate may decrease the excretion rate of Sulfasalazine which could result in a higher serum level.
Ezetimibe Estradiol dienanthate may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Topotecan Estradiol dienanthate may decrease the excretion rate of Topotecan which could result in a higher serum level.
Rosuvastatin Estradiol dienanthate may decrease the excretion rate of Rosuvastatin which could result in a higher serum level.
Alvocidib Estradiol dienanthate may decrease the excretion rate of Alvocidib which could result in a higher serum level.
Camptothecin Estradiol dienanthate may decrease the excretion rate of Camptothecin which could result in a higher serum level.
Apixaban Estradiol dienanthate may decrease the excretion rate of Apixaban which could result in a higher serum level.
Dolutegravir Estradiol dienanthate may decrease the excretion rate of Dolutegravir which could result in a higher serum level.
Riociguat Estradiol dienanthate may decrease the excretion rate of Riociguat which could result in a higher serum level.
Sofosbuvir Estradiol dienanthate may decrease the excretion rate of Sofosbuvir which could result in a higher serum level.
Lenvatinib Estradiol dienanthate may decrease the excretion rate of Lenvatinib which could result in a higher serum level.
Fimasartan Estradiol dienanthate may decrease the excretion rate of Fimasartan which could result in a higher serum level.
Talazoparib The serum concentration of Talazoparib can be increased when it is combined with Estradiol dienanthate.

Target Protein

Estrogen receptor ESR1
Estrogen receptor beta ESR2
Nuclear receptor subfamily 1 group I member 2 NR1I2
Neuronal acetylcholine receptor subunit alpha-4 CHRNA4
Nuclear receptor coactivator 2 NCOA2
G-protein coupled estrogen receptor 1 GPER1
ATP synthase subunit a MT-ATP6
Beclin-1 BECN1
17-beta-hydroxysteroid dehydrogenase type 2 HSD17B2
Estrogen-related receptor gamma ESRRG

Referensi & Sumber

Artikel (PubMed)
  • PMID: 10843196
    Pentikainen V, Erkkila K, Suomalainen L, Parvinen M, Dunkel L: Estradiol acts as a germ cell survival factor in the human testis in vitro. J Clin Endocrinol Metab. 2000 May;85(5):2057-67.
  • PMID: 8098802
    Sharpe RM, Skakkebaek NE: Are oestrogens involved in falling sperm counts and disorders of the male reproductive tract? Lancet. 1993 May 29;341(8857):1392-5.
  • PMID: 11792932
    Raman JD, Schlegel PN: Aromatase inhibitors for male infertility. J Urol. 2002 Feb;167(2 Pt 1):624-9.
  • PMID: 9211678
    Carani C, Qin K, Simoni M, Faustini-Fustini M, Serpente S, Boyd J, Korach KS, Simpson ER: Effect of testosterone and estradiol in a man with aromatase deficiency. N Engl J Med. 1997 Jul 10;337(2):91-5.
  • PMID: 7488136
    Behl C, Widmann M, Trapp T, Holsboer F: 17-beta estradiol protects neurons from oxidative stress-induced cell death in vitro. Biochem Biophys Res Commun. 1995 Nov 13;216(2):473-82.
  • PMID: 17135036
    Schmidt JW, Wollner D, Curcio J, Riedlinger J, Kim LS: Hormone replacement therapy in menopausal women: Past problems and future possibilities. Gynecol Endocrinol. 2006 Oct;22(10):564-77.
  • PMID: 17573901
    Foresta C, Zuccarello D, Biagioli A, De Toni L, Prana E, Nicoletti V, Ambrosini G, Ferlin A: Oestrogen stimulates endothelial progenitor cells via oestrogen receptor-alpha. Clin Endocrinol (Oxf). 2007 Oct;67(4):520-5. Epub 2007 Jun 15.
  • PMID: 17124377
    Garcia-Segura LM, Sanz A, Mendez P: Cross-talk between IGF-I and estradiol in the brain: focus on neuroprotection. Neuroendocrinology. 2006;84(4):275-9. Epub 2006 Nov 23.
Menampilkan 8 dari 9 artikel.
Textbook
  • ISBN: 978-3-642-60107-1
    W. KuhnzH. BlodeH. Zimmermann (1993). Pharmacokinetics of Exogenous Natural and Synthetic Estrogens and Antiestrogens. In: Estrogens and Antiestrogens II.. Springer, Berlin, Heidelberg.

Contoh Produk & Brand

Produk: 1 • International brands: 0
Produk
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    Liquid • - • Intramuscular • Canada • Approved

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