Peringatan Keamanan

The oral LD50 is 4000 mg/kg in mice and rats. The subcutaneous LD50 is 2880 mg/kg in mice and rats.L41509

There is limited information on testosterone undecanoate overdose. There was one report of acute overdose from an approved injectable testosterone product, which resulted in increased serum testosterone levels of up to 11,400 ng/dL with a cerebrovascular accident.L35970 There was one case of overdose following administration of oral testosterone undecanoate capsules: this patient inadvertently took a 20% higher dose than the maximum recommended dose but did not report any adverse reactions.L8932 Overdose should be managed with discontinuation of the drug in combination with appropriate symptomatic and supportive care.L35970

The abuse of anabolic androgenic steroids can result in serious adverse reactions, such as cardiac arrest, myocardial infarction, hypertrophic cardiomyopathy, congestive heart failure, cerebrovascular accident, hepatotoxicity, and psychiatric manifestations, including major depression, mania, paranoia, psychosis, delusions, hallucinations, hostility, and aggression. Men receiving testosterone have experienced transient ischemic attacks, convulsions, hypomania, irritability, dyslipidemias, testicular atrophy, subfertility, and infertility.L35970

Testosterone undecanoate

DB13946

small molecule approved investigational

Deskripsi

Testosterone undecanoate is the ester prodrug of testosterone and has a mid-chain fatty acid at the carbon 17? position.L35970 It was developed via fatty acid esterification of testosterone in order to achieve orally administer testosterone.A246594 There are oral and intramuscular formulations available for testosterone undecanoate: both formulations are indicated for testosterone replacement therapy in adult males with hypogonadism.L35970,L8932,L41355

Testosterone is a critical male hormone that is responsible for the normal growth and development of the male sex organs and for the maintenance of secondary sex characteristics. Male hypogonadism, resulting from insufficient testosterone secretion, can result symptoms and signs of testosterone deficiency, such as decreased libido, erectile dysfunction, and loss of muscle and bone mass. Testosterone replacement therapy aims to restore the levels of testosterone, thereby improving symptoms and signs of testosterone deficiency.A246614,L35970

Struktur Molekul 2D

Berat 456.711
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of testosterone undecanoate is approximately two hours. Once testosterone is formed from testosterone undecanoate, the half life of testosterone can vary and the reported values in the literature remain inconsistent, ranging from 10 to to 100 minutes.[L35970,L41355] Testosterone undecanoate in castor oil for intramuscular injection had a half life of 33.9 days, allowing it to maintain serum levels in the normal range for over 6 weeks.[A176954]
Volume Distribusi There is no information available.
Klirens (Clearance) While there is limited information available, an earlier study reports a metabolic clearance rate of 24.5 mL/min/kg for testosterone following oral administration of 25 mg testosterone and 40 mg testosterone undecanoate in women.[A31633]

Absorpsi

Testosterone undecanoate is a lipophilic molecule that is absorbed into the intestinal lymphatic system after oral administration. It is then released into the general blood circulation by the thoracic duct, thereby bypassing the portal circulation and first-pass metabolism in the liver,A246594,L41355 unlike endogenous testosterone.A246614 Following oral administration of 237 mg twice per day in males with hypogonadism, the mean (SD) Cmax was 1008 (581) ng/dL.L8932 Tmax is about five hours following oral administration.L41355 Decreased testosterone exposure was observed when administered without food.L8932,L41355 Following intramuscular administration of 750 mg testosterone undecanoate, serum testosterone concentrations reached a maximum after a median of seven days (range of four to 42 days), which then slowly declined. The mean (SD) Cmax was about 90.9 (68.8) ng/dL on the fourth day following injection of testosterone undecanoate. Steady-state serum testosterone concentration was achieved with the third injection at 14 weeks. At 42 days following the injection, testosterone undecanoate was nearly undetectable.L35970

Metabolisme

Testosterone undecanoate can be reduced to dihydrotestosterone undecanoate via 5?-reductase.L41355 In the circulation, the ester bond linking testosterone to the undecanoic acid is cleaved by endogenous non-specific esterases.A246594,L35970 Like all fatty acids, the undecanoic side chain undergoes ?-oxidation to form acetyl coenzyme A (CoA) and, finally, propionyl CoA.A246594,L8932 Testosterone is metabolized to various 17-keto steroids through two different pathways to form major active metabolites, estradiol and dihydrotestosterone (DHT).L35970

Rute Eliminasi

About 90% of a testosterone dose given intramuscularly is excreted in the urine as glucuronic and sulfuric acid-conjugates of testosterone or as metabolites. About 6% of a dose is excreted in the feces, mostly in the unconjugated form. Inactivation of testosterone occurs primarily in the liver.L35970

Interaksi Makanan

1 Data
  • 1. Take with food. Food enhances the systemic exposure of testosterone undecanoate administered as oral capsules.

Interaksi Obat

1219 Data
Eliglustat The metabolism of Eliglustat can be decreased when combined with Testosterone undecanoate.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Testosterone undecanoate.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Testosterone undecanoate.
Colchicine The metabolism of Colchicine can be decreased when combined with Testosterone undecanoate.
Fentanyl Testosterone undecanoate may increase the hypertensive activities of Fentanyl.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Testosterone undecanoate.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Testosterone undecanoate.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Testosterone undecanoate.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Testosterone undecanoate.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Testosterone undecanoate.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Testosterone undecanoate.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Testosterone undecanoate.
Mifepristone Testosterone undecanoate may increase the hypoglycemic activities of Mifepristone.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Testosterone undecanoate.
Perampanel The metabolism of Perampanel can be increased when combined with Testosterone undecanoate.
Prasterone The serum concentration of Testosterone undecanoate can be increased when it is combined with Prasterone.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Testosterone undecanoate.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Testosterone undecanoate.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Testosterone undecanoate.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Testosterone undecanoate.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Testosterone undecanoate.
Erlotinib The serum concentration of Erlotinib can be decreased when it is combined with Testosterone undecanoate.
Glimepiride Testosterone undecanoate may increase the hypoglycemic activities of Glimepiride.
Acetohexamide Testosterone undecanoate may increase the hypoglycemic activities of Acetohexamide.
Miglitol Testosterone undecanoate may increase the hypoglycemic activities of Miglitol.
Phenformin Testosterone undecanoate may increase the hypoglycemic activities of Phenformin.
Gliclazide Testosterone undecanoate may increase the hypoglycemic activities of Gliclazide.
Gliquidone Testosterone undecanoate may increase the hypoglycemic activities of Gliquidone.
Mitiglinide Testosterone undecanoate may increase the hypoglycemic activities of Mitiglinide.
Exenatide Testosterone undecanoate may increase the hypoglycemic activities of Exenatide.
Mecasermin Testosterone undecanoate may increase the hypoglycemic activities of Mecasermin.
Pramlintide Testosterone undecanoate may increase the hypoglycemic activities of Pramlintide.
Glisoxepide Testosterone undecanoate may increase the hypoglycemic activities of Glisoxepide.
Glymidine Testosterone undecanoate may increase the hypoglycemic activities of Glymidine.
AICA ribonucleotide Testosterone undecanoate may increase the hypoglycemic activities of AICA ribonucleotide.
Buformin Testosterone undecanoate may increase the hypoglycemic activities of Buformin.
Vildagliptin Testosterone undecanoate may increase the hypoglycemic activities of Vildagliptin.
Voglibose Testosterone undecanoate may increase the hypoglycemic activities of Voglibose.
AMG-222 Testosterone undecanoate may increase the hypoglycemic activities of AMG-222.
Bisegliptin Testosterone undecanoate may increase the hypoglycemic activities of Bisegliptin.
Liraglutide Testosterone undecanoate may increase the hypoglycemic activities of Liraglutide.
Gosogliptin Testosterone undecanoate may increase the hypoglycemic activities of Gosogliptin.
Glibornuride Testosterone undecanoate may increase the hypoglycemic activities of Glibornuride.
Benfluorex Testosterone undecanoate may increase the hypoglycemic activities of Benfluorex.
Albiglutide Testosterone undecanoate may increase the hypoglycemic activities of Albiglutide.
Dulaglutide Testosterone undecanoate may increase the hypoglycemic activities of Dulaglutide.
Ipragliflozin Testosterone undecanoate may increase the hypoglycemic activities of Ipragliflozin.
Dutogliptin Testosterone undecanoate may increase the hypoglycemic activities of Dutogliptin.
Allicin Testosterone undecanoate may increase the hypoglycemic activities of Allicin.
Tofogliflozin Testosterone undecanoate may increase the hypoglycemic activities of Tofogliflozin.
2,4-thiazolidinedione Testosterone undecanoate may increase the hypoglycemic activities of 2,4-thiazolidinedione.
Teneligliptin Testosterone undecanoate may increase the hypoglycemic activities of Teneligliptin.
Omarigliptin Testosterone undecanoate may increase the hypoglycemic activities of Omarigliptin.
Carmegliptin Testosterone undecanoate may increase the hypoglycemic activities of Carmegliptin.
Gemigliptin Testosterone undecanoate may increase the hypoglycemic activities of Gemigliptin.
Anagliptin Testosterone undecanoate may increase the hypoglycemic activities of Anagliptin.
Evogliptin Testosterone undecanoate may increase the hypoglycemic activities of Evogliptin.
Sotagliflozin Testosterone undecanoate may increase the hypoglycemic activities of Sotagliflozin.
Remogliflozin etabonate Testosterone undecanoate may increase the hypoglycemic activities of Remogliflozin etabonate.
Carbutamide Testosterone undecanoate may increase the hypoglycemic activities of Carbutamide.
Guar gum Testosterone undecanoate may increase the hypoglycemic activities of Guar gum.
Metahexamide Testosterone undecanoate may increase the hypoglycemic activities of Metahexamide.
Semaglutide Testosterone undecanoate may increase the hypoglycemic activities of Semaglutide.
Taspoglutide Testosterone undecanoate may increase the hypoglycemic activities of Taspoglutide.
Englitazone Testosterone undecanoate may increase the hypoglycemic activities of Englitazone.
Tirzepatide Testosterone undecanoate may increase the hypoglycemic activities of Tirzepatide.
Gastric inhibitory polypeptide Testosterone undecanoate may increase the hypoglycemic activities of Gastric inhibitory polypeptide.
Empagliflozin Testosterone undecanoate may increase the hypoglycemic activities of Empagliflozin.
Acarbose Testosterone undecanoate may increase the hypoglycemic activities of Acarbose.
Fluvoxamine Fluvoxamine may decrease the excretion rate of Testosterone undecanoate which could result in a higher serum level.
Troglitazone Testosterone undecanoate may increase the hypoglycemic activities of Troglitazone.
Fluconazole Fluconazole may decrease the excretion rate of Testosterone undecanoate which could result in a higher serum level.
Floxuridine Floxuridine may decrease the excretion rate of Testosterone undecanoate which could result in a higher serum level.
Gemfibrozil Gemfibrozil may decrease the excretion rate of Testosterone undecanoate which could result in a higher serum level.
Secobarbital Secobarbital may decrease the excretion rate of Testosterone undecanoate which could result in a higher serum level.
Spironolactone Spironolactone may increase the excretion rate of Testosterone undecanoate which could result in a lower serum level and potentially a reduction in efficacy.
Medroxyprogesterone acetate Medroxyprogesterone acetate may decrease the excretion rate of Testosterone undecanoate which could result in a higher serum level.
Pioglitazone Testosterone undecanoate may increase the hypoglycemic activities of Pioglitazone.
Quinine Testosterone undecanoate may increase the hypoglycemic activities of Quinine.
Trimethoprim Trimethoprim may decrease the excretion rate of Testosterone undecanoate which could result in a higher serum level.
Trametinib Trametinib may decrease the excretion rate of Testosterone undecanoate which could result in a higher serum level.
Dextrose, unspecified form The serum concentration of Dextrose, unspecified form can be decreased when it is combined with Testosterone undecanoate.
Propranolol Testosterone undecanoate may increase the excretion rate of Propranolol which could result in a lower serum level and potentially a reduction in efficacy.
Flunisolide The risk or severity of edema formation can be increased when Testosterone undecanoate is combined with Flunisolide.
Beclomethasone dipropionate The risk or severity of edema formation can be increased when Testosterone undecanoate is combined with Beclomethasone dipropionate.
Fluocinolone acetonide The risk or severity of edema formation can be increased when Testosterone undecanoate is combined with Fluocinolone acetonide.
Triamcinolone The risk or severity of edema formation can be increased when Testosterone undecanoate is combined with Triamcinolone.
Fludrocortisone The risk or severity of edema formation can be increased when Testosterone undecanoate is combined with Fludrocortisone.
Trilostane The risk or severity of edema formation can be increased when Testosterone undecanoate is combined with Trilostane.
Corticotropin The risk or severity of edema formation can be increased when Testosterone undecanoate is combined with Corticotropin.
Cortisone acetate The risk or severity of edema formation can be increased when Testosterone undecanoate is combined with Cortisone acetate.
Paramethasone The risk or severity of edema formation can be increased when Testosterone undecanoate is combined with Paramethasone.
Ciclesonide The risk or severity of edema formation can be increased when Testosterone undecanoate is combined with Ciclesonide.
Fluprednidene The risk or severity of edema formation can be increased when Testosterone undecanoate is combined with Fluprednidene.
Tixocortol The risk or severity of edema formation can be increased when Testosterone undecanoate is combined with Tixocortol.
Fluprednisolone The risk or severity of edema formation can be increased when Testosterone undecanoate is combined with Fluprednisolone.
Meprednisone The risk or severity of edema formation can be increased when Testosterone undecanoate is combined with Meprednisone.
Dexamethasone isonicotinate The risk or severity of edema formation can be increased when Testosterone undecanoate is combined with Dexamethasone isonicotinate.
Melengestrol The risk or severity of edema formation can be increased when Testosterone undecanoate is combined with Melengestrol.
Deflazacort The risk or severity of edema formation can be increased when Testosterone undecanoate is combined with Deflazacort.

Target Protein

Androgen receptor AR

Referensi & Sumber

Artikel (PubMed)
  • PMID: 28031910
    Lachance S, Dhingra O, Bernstein J, Gagnon S, Savard C, Pelletier N, Boudreau N, Levesque A: Importance of measuring testosterone in enzyme-inhibited plasma for oral testosterone undecanoate androgen replacement therapy clinical trials. Future Sci OA. 2015 Nov 1;1(4):FSO55. doi: 10.4155/fso.15.55. eCollection 2015 Nov.
  • PMID: 32382745
    Swerdloff RS, Wang C, White WB, Kaminetsky J, Gittelman MC, Longstreth JA, Dudley RE, Danoff TM: A New Oral Testosterone Undecanoate Formulation Restores Testosterone to Normal Concentrations in Hypogonadal Men. J Clin Endocrinol Metab. 2020 Aug 1;105(8). pii: 5834353. doi: 10.1210/clinem/dgaa238.
  • PMID: 32068334
    Barbonetti A, D'Andrea S, Francavilla S: Testosterone replacement therapy. Andrology. 2020 Nov;8(6):1551-1566. doi: 10.1111/andr.12774. Epub 2020 Mar 9.
  • PMID: 27057074
    Davey RA, Grossmann M: Androgen Receptor Structure, Function and Biology: From Bench to Bedside. Clin Biochem Rev. 2016 Feb;37(1):3-15.
  • PMID: 3770015
    Tauber U, Schroder K, Dusterberg B, Matthes H: Absolute bioavailability of testosterone after oral administration of testosterone-undecanoate and testosterone. Eur J Drug Metab Pharmacokinet. 1986 Apr-Jun;11(2):145-9.

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