Peringatan Keamanan

Leuprolide is considered extremely safe, with low dose-related toxicity and comparatively mild adverse effects.A203126 Prostate cancer patients treated with leuprolide at doses as high as 20 mg/day for two years showed no additional adverse effects compared to those receiving 1 mg/day.L13814

Leuprolide

DB00007

biotech approved investigational

Deskripsi

Leuprolide is a synthetic 9-residue peptide analogue of gonadotropin-releasing hormone (GnRH). Unlike the endogenous decapeptide GnRH, leuprolide contains a single D-amino acid (D-leucyl) residue, which helps to increase its circulating half-life from three to four minutes to approximately three hours.A203222 As a GnRH mimic, leuprolide is capable of binding to the GnRH receptor (GnRHR) and inducing downstream modulation of both gonadotropin hormone and sex steroid levels. Prolonged activation of GnRHR results in significant downregulation of sex steroid levels, which is primarily responsible for the clinical efficacy of leuprolide in diverse conditions, including advanced prostate cancer, endometriosis, and central precocious puberty.A203126, A203132

Leuprolide was first approved in 1985 as a daily subcutaneous injection under the tradename Lupron™ by Abbvie Endocrine Inc.L13850 Since this initial approval, various long-acting intramuscular and subcutaneous products have been developed such that patients can be dosed once every six months.L13781, L13790 Leuprolide remains frontline therapy in all conditions for which it is indicated for use.

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Leuprolide has a terminal elimination half-life of approximately three hours.[L10310, L13781, L13784, L13787, L13790, L13814, L34415]
Volume Distribusi Leuprolide has an apparent steady-state volume of distribution of 27 L following intravenous bolus administration to healthy males. The volume of distribution for indicated routes of subcutaneous or intramuscular injection has not been reported.[L10310, L13781, L13784, L13787, L13790, L13814, L34415]
Klirens (Clearance) Leuprolide administered as a 1 mg intravenous bolus in healthy males has a mean systemic clearance between 7.6 and 8.3 L/h.[L10310, L13781, L13784, L13787, L13790, L13814, L34415]

Absorpsi

Leuprolide is typically administered as a single-dose long-acting formulation employing either microsphere or biodegradable solid depot technologies.A203126 Regardless of the exact formulation and initial dose strength, the Cmax is typically achieved by 4-5 hours post-injection and displays large variability in the range of 4.6 - 212 ng/mL. Eventual steady-state kinetics are typically achieved by four weeks, with a narrower range of 0.1 - 2 ng/mL. No studies on the effects of food on absorption have been carried out.L10310, L13781, L13784, L13787, L13790, L13814, L34415

Metabolisme

Radiolabeling studies suggest that leuprolide is primarily metabolized to inactive penta-, tri-, and dipeptide entities, which are likely further metabolized. It is expected that various peptidases encountered throughout systemic circulation are responsible for leuprolide metabolism.L10310, L13781, L13784, L13787, L13790, L13814, L34415

Rute Eliminasi

Following administration of 3.75 mg leuprolide depot suspension to three patients, less than 5% of the initial dose was recovered as unchanged or pentapeptide metabolite in the urine.L10310, L13781, L13784, L13814

Interaksi Obat

1194 Data
Corifollitropin alfa The therapeutic efficacy of Corifollitropin alfa can be increased when used in combination with Leuprolide.
Ivabradine Ivabradine may increase the QTc-prolonging activities of Leuprolide.
Choline C 11 Leuprolide may decrease effectiveness of Choline C 11 as a diagnostic agent.
Capromab pendetide Leuprolide may decrease effectiveness of Capromab pendetide as a diagnostic agent.
Insulin human The therapeutic efficacy of Insulin human can be decreased when used in combination with Leuprolide.
Insulin lispro The therapeutic efficacy of Insulin lispro can be decreased when used in combination with Leuprolide.
Insulin glargine The therapeutic efficacy of Insulin glargine can be decreased when used in combination with Leuprolide.
Insulin pork The therapeutic efficacy of Insulin pork can be decreased when used in combination with Leuprolide.
Troglitazone The therapeutic efficacy of Troglitazone can be decreased when used in combination with Leuprolide.
Glimepiride The therapeutic efficacy of Glimepiride can be decreased when used in combination with Leuprolide.
Acarbose The therapeutic efficacy of Acarbose can be decreased when used in combination with Leuprolide.
Sulfadiazine The therapeutic efficacy of Sulfadiazine can be decreased when used in combination with Leuprolide.
Rosiglitazone The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Leuprolide.
Acetohexamide The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Leuprolide.
Miglitol The therapeutic efficacy of Miglitol can be decreased when used in combination with Leuprolide.
Chlorpropamide The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Leuprolide.
Nateglinide The therapeutic efficacy of Nateglinide can be decreased when used in combination with Leuprolide.
Tolazamide The therapeutic efficacy of Tolazamide can be decreased when used in combination with Leuprolide.
Repaglinide The therapeutic efficacy of Repaglinide can be decreased when used in combination with Leuprolide.
Phenformin The therapeutic efficacy of Phenformin can be decreased when used in combination with Leuprolide.
Glyburide The therapeutic efficacy of Glyburide can be decreased when used in combination with Leuprolide.
Glipizide The therapeutic efficacy of Glipizide can be decreased when used in combination with Leuprolide.
Gliclazide The therapeutic efficacy of Gliclazide can be decreased when used in combination with Leuprolide.
Tolbutamide The therapeutic efficacy of Tolbutamide can be decreased when used in combination with Leuprolide.
Pioglitazone The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Leuprolide.
Gliquidone The therapeutic efficacy of Gliquidone can be decreased when used in combination with Leuprolide.
Mitiglinide The therapeutic efficacy of Mitiglinide can be decreased when used in combination with Leuprolide.
Sitagliptin The therapeutic efficacy of Sitagliptin can be decreased when used in combination with Leuprolide.
Exenatide The therapeutic efficacy of Exenatide can be decreased when used in combination with Leuprolide.
Mecasermin The therapeutic efficacy of Mecasermin can be decreased when used in combination with Leuprolide.
Pramlintide The therapeutic efficacy of Pramlintide can be decreased when used in combination with Leuprolide.
Glisoxepide The therapeutic efficacy of Glisoxepide can be decreased when used in combination with Leuprolide.
Insulin aspart The therapeutic efficacy of Insulin aspart can be decreased when used in combination with Leuprolide.
Insulin detemir The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Leuprolide.
Insulin glulisine The therapeutic efficacy of Insulin glulisine can be decreased when used in combination with Leuprolide.
Glymidine The therapeutic efficacy of Glymidine can be decreased when used in combination with Leuprolide.
AICA ribonucleotide The therapeutic efficacy of AICA ribonucleotide can be decreased when used in combination with Leuprolide.
Buformin The therapeutic efficacy of Buformin can be decreased when used in combination with Leuprolide.
Vildagliptin The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Leuprolide.
Voglibose The therapeutic efficacy of Voglibose can be decreased when used in combination with Leuprolide.
NN344 The therapeutic efficacy of NN344 can be decreased when used in combination with Leuprolide.
AMG-222 The therapeutic efficacy of AMG-222 can be decreased when used in combination with Leuprolide.
Bisegliptin The therapeutic efficacy of Bisegliptin can be decreased when used in combination with Leuprolide.
Alogliptin The therapeutic efficacy of Alogliptin can be decreased when used in combination with Leuprolide.
Dapagliflozin The therapeutic efficacy of Dapagliflozin can be decreased when used in combination with Leuprolide.
Saxagliptin The therapeutic efficacy of Saxagliptin can be decreased when used in combination with Leuprolide.
Liraglutide The therapeutic efficacy of Liraglutide can be decreased when used in combination with Leuprolide.
Gosogliptin The therapeutic efficacy of Gosogliptin can be decreased when used in combination with Leuprolide.
Linagliptin The therapeutic efficacy of Linagliptin can be decreased when used in combination with Leuprolide.
Canagliflozin The therapeutic efficacy of Canagliflozin can be decreased when used in combination with Leuprolide.
Glibornuride The therapeutic efficacy of Glibornuride can be decreased when used in combination with Leuprolide.
Benfluorex The therapeutic efficacy of Benfluorex can be decreased when used in combination with Leuprolide.
Empagliflozin The therapeutic efficacy of Empagliflozin can be decreased when used in combination with Leuprolide.
Albiglutide The therapeutic efficacy of Albiglutide can be decreased when used in combination with Leuprolide.
Dulaglutide The therapeutic efficacy of Dulaglutide can be decreased when used in combination with Leuprolide.
Lobeglitazone The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Leuprolide.
Netoglitazone The therapeutic efficacy of Netoglitazone can be decreased when used in combination with Leuprolide.
Rivoglitazone The therapeutic efficacy of Rivoglitazone can be decreased when used in combination with Leuprolide.
Ciglitazone The therapeutic efficacy of Ciglitazone can be decreased when used in combination with Leuprolide.
Lixisenatide The therapeutic efficacy of Lixisenatide can be decreased when used in combination with Leuprolide.
Insulin beef The therapeutic efficacy of Insulin beef can be decreased when used in combination with Leuprolide.
Insulin degludec The therapeutic efficacy of Insulin degludec can be decreased when used in combination with Leuprolide.
Insulin peglispro The therapeutic efficacy of Insulin peglispro can be decreased when used in combination with Leuprolide.
Insulin tregopil The therapeutic efficacy of Insulin tregopil can be decreased when used in combination with Leuprolide.
Ipragliflozin The therapeutic efficacy of Ipragliflozin can be decreased when used in combination with Leuprolide.
Dutogliptin The therapeutic efficacy of Dutogliptin can be decreased when used in combination with Leuprolide.
Allicin The therapeutic efficacy of Allicin can be decreased when used in combination with Leuprolide.
Tofogliflozin The therapeutic efficacy of Tofogliflozin can be decreased when used in combination with Leuprolide.
Ertugliflozin The therapeutic efficacy of Ertugliflozin can be decreased when used in combination with Leuprolide.
2,4-thiazolidinedione The therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Leuprolide.
Teneligliptin The therapeutic efficacy of Teneligliptin can be decreased when used in combination with Leuprolide.
Omarigliptin The therapeutic efficacy of Omarigliptin can be decreased when used in combination with Leuprolide.
Carmegliptin The therapeutic efficacy of Carmegliptin can be decreased when used in combination with Leuprolide.
Gemigliptin The therapeutic efficacy of Gemigliptin can be decreased when used in combination with Leuprolide.
Anagliptin The therapeutic efficacy of Anagliptin can be decreased when used in combination with Leuprolide.
Evogliptin The therapeutic efficacy of Evogliptin can be decreased when used in combination with Leuprolide.
Sotagliflozin The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Leuprolide.
Balaglitazone The therapeutic efficacy of Balaglitazone can be decreased when used in combination with Leuprolide.
Remogliflozin etabonate The therapeutic efficacy of Remogliflozin etabonate can be decreased when used in combination with Leuprolide.
Carbutamide The therapeutic efficacy of Carbutamide can be decreased when used in combination with Leuprolide.
Guar gum The therapeutic efficacy of Guar gum can be decreased when used in combination with Leuprolide.
Metahexamide The therapeutic efficacy of Metahexamide can be decreased when used in combination with Leuprolide.
Semaglutide The therapeutic efficacy of Semaglutide can be decreased when used in combination with Leuprolide.
Taspoglutide The therapeutic efficacy of Taspoglutide can be decreased when used in combination with Leuprolide.
Englitazone The therapeutic efficacy of Englitazone can be decreased when used in combination with Leuprolide.
Tirzepatide The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Leuprolide.
Gastric inhibitory polypeptide The therapeutic efficacy of Gastric inhibitory polypeptide can be decreased when used in combination with Leuprolide.
Bromocriptine The therapeutic efficacy of Bromocriptine can be decreased when used in combination with Leuprolide.
Citalopram The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Citalopram.
Anagrelide The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Anagrelide.
Disopyramide The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Disopyramide.
Clemastine The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Clemastine.
Ibutilide The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Ibutilide.
Valproic acid The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Valproic acid.
Grepafloxacin The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Grepafloxacin.
Quinine The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Quinine.
Sotalol The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Sotalol.
Erlotinib The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Erlotinib.
Toremifene The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Toremifene.
Imatinib The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Imatinib.

Target Protein

Gonadotropin-releasing hormone receptor GNRHR
Progonadoliberin-1 GNRH1

Referensi & Sumber

Synthesis reference: Daniel Kadzimirzs, Gerhard Jas, Volker Autze, "Solution-Phase Synthesis of Leuprolide and Its Intermediates." U.S. Patent US20090005535, issued January 01, 2009.
Artikel (PubMed)
  • PMID: 27826989
    Hoda MR, Kramer MW, Merseburger AS, Cronauer MV: Androgen deprivation therapy with Leuprolide acetate for treatment of advanced prostate cancer. Expert Opin Pharmacother. 2017 Jan;18(1):105-113. doi: 10.1080/14656566.2016.1258058. Epub 2016 Nov 28.
  • PMID: 29254389
    Ali M, Chaudhry ZT, Al-Hendy A: Successes and failures of uterine leiomyoma drug discovery. Expert Opin Drug Discov. 2018 Feb;13(2):169-177. doi: 10.1080/17460441.2018.1417381. Epub 2017 Dec 18.
  • PMID: 17970643
    Wilson AC, Meethal SV, Bowen RL, Atwood CS: Leuprolide acetate: a drug of diverse clinical applications. Expert Opin Investig Drugs. 2007 Nov;16(11):1851-63. doi: 10.1517/13543784.16.11.1851.
  • PMID: 1984190
    Conn PM, Crowley WF Jr: Gonadotropin-releasing hormone and its analogues. N Engl J Med. 1991 Jan 10;324(2):93-103. doi: 10.1056/NEJM199101103240205.

Contoh Produk & Brand

Produk: 81 • International brands: 6
Produk
  • Camcevi
    - • 42 mg / syr • Subcutaneous • Canada • Approved
  • Camcevi
    Injection, emulsion • 42 mg/0.37g • Subcutaneous • US • Approved
  • Camcevi
    Injection, emulsion • 42 mg/1mL • Subcutaneous • US • Approved
  • Camcevi
    - • 42 mg • Subcutaneous • EU • Approved
  • Eligard
    Kit • 7.5 mg/0.25mL • Subcutaneous • US • Approved
  • Eligard
    Kit • 22.5 mg/0.375mL • Subcutaneous • US • Approved
  • Eligard
    Kit • 30 mg/0.5mL • Subcutaneous • US • Approved
  • Eligard
    Kit • 45 mg/0.375mL • Subcutaneous • US • Approved
Menampilkan 8 dari 81 produk.
International Brands
  • Camcevi — Foresee Pharmaceuticals
  • Leuplin — Takeda
  • LeuProMaxx — Baxter/Teva
  • Memryte — Curaxis
  • Prostap 3 — Takeda UK
  • Prostap SR — Takeda UK

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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