Peringatan Keamanan

Toxicity information, including information regarding overdosage, is currently unavailable.L44451 Symptoms of teprotumumab overdose are likely to be consistent with its adverse effect profile.

Teprotumumab

DB06343

biotech approved investigational

Deskripsi

Teprotumumab is a fully human IgG1 monoclonal antibody directed against the human insulin-like growth factor-1 receptor.L11359 Following a clinical trial in which its efficacy in the treatment of thyroid eye disease (TED) was assessed, it received "breakthrough therapy" designation from the FDA in 2016A190129 and was approved by the FDA in January 2020 for the treatment of TED.L11350 Thyroid eye disease is a potentially debilitating complication of Graves' Disease involving inflammation and tissue remodeling behind the eye, and previous treatment options typically involved multiple invasive surgeries - teprotumumab is the first drug ever approved for the treatment of TED and therefore represents a significant step forward in the treatment this disease.L11350

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of teprotumumab is 20 ± 5 days.[L44451]
Volume Distribusi Following the standard dosing regimen, the mean central and peripheral volumes of distribution are approximately 3.26 ± 0.87 L and 4.32 ± 0.67 L, respectively.[L44451]
Klirens (Clearance) The estimated mean clearance of teprotumumab is 0.27 L/day.[L44451] The inter-compartment clearance is 0.74 L/day.[L44451]

Absorpsi

In a population of 40 patients receiving standard dosing in two clinical trials of teprotumumab, utilizing a two-compartment pharmacokinetic model, the AUC and Cmax were estimated to be 138 ± 34 mg•hr/mL and 632 ± 139 mcg/mL, respectively.L44451

Metabolisme

The metabolism of teprotumumab has not been fully characterized. As a protein, its metabolism is expected to involve proteolysis to smaller proteins and peptides.L44451

Rute Eliminasi

Data regarding specific route(s) of elimination are unavailable at this time.

Interaksi Obat

767 Data
Dulaglutide The therapeutic efficacy of Dulaglutide can be decreased when used in combination with Teprotumumab.
Insulin human The therapeutic efficacy of Insulin human can be decreased when used in combination with Teprotumumab.
Insulin lispro The therapeutic efficacy of Insulin lispro can be decreased when used in combination with Teprotumumab.
Insulin glargine The therapeutic efficacy of Insulin glargine can be decreased when used in combination with Teprotumumab.
Insulin pork The therapeutic efficacy of Insulin pork can be decreased when used in combination with Teprotumumab.
Troglitazone The therapeutic efficacy of Troglitazone can be decreased when used in combination with Teprotumumab.
Glimepiride The therapeutic efficacy of Glimepiride can be decreased when used in combination with Teprotumumab.
Sulfisoxazole The therapeutic efficacy of Sulfisoxazole can be decreased when used in combination with Teprotumumab.
Disopyramide The therapeutic efficacy of Disopyramide can be decreased when used in combination with Teprotumumab.
Acarbose The therapeutic efficacy of Acarbose can be decreased when used in combination with Teprotumumab.
Sulfadiazine The therapeutic efficacy of Sulfadiazine can be decreased when used in combination with Teprotumumab.
Rosiglitazone The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Teprotumumab.
Acetohexamide The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Teprotumumab.
Quinine The therapeutic efficacy of Quinine can be decreased when used in combination with Teprotumumab.
Miglitol The therapeutic efficacy of Miglitol can be decreased when used in combination with Teprotumumab.
Chlorpropamide The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Teprotumumab.
Nateglinide The therapeutic efficacy of Nateglinide can be decreased when used in combination with Teprotumumab.
Pentamidine The therapeutic efficacy of Pentamidine can be decreased when used in combination with Teprotumumab.
Mifepristone The therapeutic efficacy of Mifepristone can be decreased when used in combination with Teprotumumab.
Tolazamide The therapeutic efficacy of Tolazamide can be decreased when used in combination with Teprotumumab.
Repaglinide The therapeutic efficacy of Repaglinide can be decreased when used in combination with Teprotumumab.
Phenformin The therapeutic efficacy of Phenformin can be decreased when used in combination with Teprotumumab.
Sulfamethoxazole The risk or severity of myelosuppression can be increased when Sulfamethoxazole is combined with Teprotumumab.
Glyburide The therapeutic efficacy of Glyburide can be decreased when used in combination with Teprotumumab.
Glipizide The therapeutic efficacy of Glipizide can be decreased when used in combination with Teprotumumab.
Gliclazide The therapeutic efficacy of Gliclazide can be decreased when used in combination with Teprotumumab.
Tolbutamide The therapeutic efficacy of Tolbutamide can be decreased when used in combination with Teprotumumab.
Pioglitazone The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Teprotumumab.
Bromocriptine The therapeutic efficacy of Bromocriptine can be decreased when used in combination with Teprotumumab.
Gliquidone The therapeutic efficacy of Gliquidone can be decreased when used in combination with Teprotumumab.
Mitiglinide The therapeutic efficacy of Mitiglinide can be decreased when used in combination with Teprotumumab.
Sitagliptin The therapeutic efficacy of Sitagliptin can be decreased when used in combination with Teprotumumab.
Sunitinib The risk or severity of adverse effects can be increased when Sunitinib is combined with Teprotumumab.
Exenatide The therapeutic efficacy of Exenatide can be decreased when used in combination with Teprotumumab.
Mecasermin The therapeutic efficacy of Mecasermin can be decreased when used in combination with Teprotumumab.
Pramlintide The therapeutic efficacy of Pramlintide can be decreased when used in combination with Teprotumumab.
Glisoxepide The therapeutic efficacy of Glisoxepide can be decreased when used in combination with Teprotumumab.
Insulin aspart The therapeutic efficacy of Insulin aspart can be decreased when used in combination with Teprotumumab.
Insulin detemir The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Teprotumumab.
Insulin glulisine The therapeutic efficacy of Insulin glulisine can be decreased when used in combination with Teprotumumab.
Glymidine The therapeutic efficacy of Glymidine can be decreased when used in combination with Teprotumumab.
AICA ribonucleotide The therapeutic efficacy of AICA ribonucleotide can be decreased when used in combination with Teprotumumab.
Buformin The therapeutic efficacy of Buformin can be decreased when used in combination with Teprotumumab.
Vildagliptin The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Teprotumumab.
Voglibose The therapeutic efficacy of Voglibose can be decreased when used in combination with Teprotumumab.
NN344 The therapeutic efficacy of NN344 can be decreased when used in combination with Teprotumumab.
AMG-222 The therapeutic efficacy of AMG-222 can be decreased when used in combination with Teprotumumab.
Bisegliptin The therapeutic efficacy of Bisegliptin can be decreased when used in combination with Teprotumumab.
Alogliptin The therapeutic efficacy of Alogliptin can be decreased when used in combination with Teprotumumab.
Dapagliflozin The therapeutic efficacy of Dapagliflozin can be decreased when used in combination with Teprotumumab.
Saxagliptin The therapeutic efficacy of Saxagliptin can be decreased when used in combination with Teprotumumab.
Liraglutide The therapeutic efficacy of Liraglutide can be decreased when used in combination with Teprotumumab.
Gosogliptin The therapeutic efficacy of Gosogliptin can be decreased when used in combination with Teprotumumab.
Linagliptin The therapeutic efficacy of Linagliptin can be decreased when used in combination with Teprotumumab.
Canagliflozin The therapeutic efficacy of Canagliflozin can be decreased when used in combination with Teprotumumab.
Glibornuride The therapeutic efficacy of Glibornuride can be decreased when used in combination with Teprotumumab.
Benfluorex The therapeutic efficacy of Benfluorex can be decreased when used in combination with Teprotumumab.
Empagliflozin The therapeutic efficacy of Empagliflozin can be decreased when used in combination with Teprotumumab.
Albiglutide The therapeutic efficacy of Albiglutide can be decreased when used in combination with Teprotumumab.
Lobeglitazone The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Teprotumumab.
Netoglitazone The therapeutic efficacy of Netoglitazone can be decreased when used in combination with Teprotumumab.
Rivoglitazone The therapeutic efficacy of Rivoglitazone can be decreased when used in combination with Teprotumumab.
Ciglitazone The therapeutic efficacy of Ciglitazone can be decreased when used in combination with Teprotumumab.
Lixisenatide The therapeutic efficacy of Lixisenatide can be decreased when used in combination with Teprotumumab.
Insulin beef The therapeutic efficacy of Insulin beef can be decreased when used in combination with Teprotumumab.
Insulin degludec The therapeutic efficacy of Insulin degludec can be decreased when used in combination with Teprotumumab.
Insulin peglispro The therapeutic efficacy of Insulin peglispro can be decreased when used in combination with Teprotumumab.
Insulin tregopil The therapeutic efficacy of Insulin tregopil can be decreased when used in combination with Teprotumumab.
Ipragliflozin The therapeutic efficacy of Ipragliflozin can be decreased when used in combination with Teprotumumab.
Dutogliptin The therapeutic efficacy of Dutogliptin can be decreased when used in combination with Teprotumumab.
Allicin The therapeutic efficacy of Allicin can be decreased when used in combination with Teprotumumab.
Tofogliflozin The therapeutic efficacy of Tofogliflozin can be decreased when used in combination with Teprotumumab.
Ertugliflozin The therapeutic efficacy of Ertugliflozin can be decreased when used in combination with Teprotumumab.
2,4-thiazolidinedione The therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Teprotumumab.
Teneligliptin The therapeutic efficacy of Teneligliptin can be decreased when used in combination with Teprotumumab.
Omarigliptin The therapeutic efficacy of Omarigliptin can be decreased when used in combination with Teprotumumab.
Carmegliptin The therapeutic efficacy of Carmegliptin can be decreased when used in combination with Teprotumumab.
Gemigliptin The therapeutic efficacy of Gemigliptin can be decreased when used in combination with Teprotumumab.
Anagliptin The therapeutic efficacy of Anagliptin can be decreased when used in combination with Teprotumumab.
Evogliptin The therapeutic efficacy of Evogliptin can be decreased when used in combination with Teprotumumab.
Sotagliflozin The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Teprotumumab.
Balaglitazone The therapeutic efficacy of Balaglitazone can be decreased when used in combination with Teprotumumab.
Remogliflozin etabonate The therapeutic efficacy of Remogliflozin etabonate can be decreased when used in combination with Teprotumumab.
Carbutamide The therapeutic efficacy of Carbutamide can be decreased when used in combination with Teprotumumab.
Guar gum The therapeutic efficacy of Guar gum can be decreased when used in combination with Teprotumumab.
Metahexamide The therapeutic efficacy of Metahexamide can be decreased when used in combination with Teprotumumab.
Semaglutide The therapeutic efficacy of Semaglutide can be decreased when used in combination with Teprotumumab.
Taspoglutide The therapeutic efficacy of Taspoglutide can be decreased when used in combination with Teprotumumab.
Englitazone The therapeutic efficacy of Englitazone can be decreased when used in combination with Teprotumumab.
Tirzepatide The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Teprotumumab.
Gastric inhibitory polypeptide The therapeutic efficacy of Gastric inhibitory polypeptide can be decreased when used in combination with Teprotumumab.
Torasemide The risk or severity of ototoxicity can be increased when Torasemide is combined with Teprotumumab.
Furosemide The risk or severity of ototoxicity can be increased when Furosemide is combined with Teprotumumab.
Etacrynic acid The risk or severity of ototoxicity can be increased when Etacrynic acid is combined with Teprotumumab.
Tobramycin The risk or severity of ototoxicity can be increased when Tobramycin is combined with Teprotumumab.
Metformin The therapeutic efficacy of Metformin can be decreased when used in combination with Teprotumumab.
Neomycin The risk or severity of ototoxicity can be increased when Teprotumumab is combined with Neomycin.
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Teprotumumab.
Etanercept The risk or severity of adverse effects can be increased when Etanercept is combined with Teprotumumab.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Teprotumumab.

Target Protein

Insulin-like growth factor 1 receptor IGF1R

Referensi & Sumber

Artikel (PubMed)
  • PMID: 31814726
    Wang Y, Patel A, Douglas RS: Thyroid Eye Disease: How A Novel Therapy May Change The Treatment Paradigm. Ther Clin Risk Manag. 2019 Nov 11;15:1305-1318. doi: 10.2147/TCRM.S193018. eCollection 2019.
  • PMID: 31823232
    Hodgson NM, Rajaii F: Current Understanding of the Progression and Management of Thyroid Associated Orbitopathy: A Systematic Review. Ophthalmol Ther. 2019 Dec 10. pii: 10.1007/s40123-019-00226-9. doi: 10.1007/s40123-019-00226-9.
  • PMID: 28467880
    Smith TJ, Kahaly GJ, Ezra DG, Fleming JC, Dailey RA, Tang RA, Harris GJ, Antonelli A, Salvi M, Goldberg RA, Gigantelli JW, Couch SM, Shriver EM, Hayek BR, Hink EM, Woodward RM, Gabriel K, Magni G, Douglas RS: Teprotumumab for Thyroid-Associated Ophthalmopathy. N Engl J Med. 2017 May 4;376(18):1748-1761. doi: 10.1056/NEJMoa1614949.
  • PMID: 30575804
    Douglas RS: Teprotumumab, an insulin-like growth factor-1 receptor antagonist antibody, in the treatment of active thyroid eye disease: a focus on proptosis. Eye (Lond). 2019 Feb;33(2):183-190. doi: 10.1038/s41433-018-0321-y. Epub 2018 Dec 21.
  • PMID: 30385883
    Smith TJ: The insulin-like growth factor-I receptor and its role in thyroid-associated ophthalmopathy. Eye (Lond). 2019 Feb;33(2):200-205. doi: 10.1038/s41433-018-0265-2. Epub 2018 Nov 1.
  • PMID: 29273685
    Mohyi M, Smith TJ: IGF1 receptor and thyroid-associated ophthalmopathy. J Mol Endocrinol. 2018 Jul;61(1):T29-T43. doi: 10.1530/JME-17-0276. Epub 2017 Dec 22.

Contoh Produk & Brand

Produk: 1 • International brands: 0
Produk
  • Tepezza
    Injection, powder, lyophilized, for solution • 500 mg/1 • Intravenous • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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