Alirocumab

DB09302

biotech approved

Deskripsi

Alirocumab is a biopharmaceutical that obtained FDA approval in July 2015 as a second line treatment for high cholesterol in adults whose LDL-cholesterol (LDL-C) is not controlled by the combination of diet and statin treatment. It is a human monoclonal antibody part of the family of the PCSK9 inhibitors which are a novel class of anticholesterol therapeutics. From this family, it was the first agent to receive FDA approval. The FDA approval was contingent on the completion of further clinical trials to better determine efficacy and safety. PCSK9 inhibition facilitates more LDL-C clearance from the blood.

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) In monotherapy, the median half-life of alirocumab at steady state was 17–20 days in patients receiving alirocumab at SC doses of 75 or 150 mg every 2 weeks. As statin therapy increases the production of PCSK9, statin co-administration is thought to shorten alirocumab half-life; therefore the median apparent half-life of alirocumab was reduced to 12 days at equivalent alirocumab doses. However, this difference is not considered clinically significant and does not change dosing recommendations.
Volume Distribusi Alirocumab is mainly distributed through the circulatory system, with minimal extravascular distribution.
Klirens (Clearance) -

Absorpsi

Following subcutaneous (SC) administration, alirocumab is absorbed into the bloodstream and maximum concentrations are reached at a median time of 3-7 days. The absolute availability after SC administration was 85%.

Metabolisme

Antibodies are generally metabolized by the reticuloendothelial system and degraded into small peptides and individual amino acids - therefore specific metabolism studies were not conducted. Alirocumab did not show evidence of affecting CYP 450 enzymes or transporter proteins in co-administration with statins.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

373 Data
Diethylstilbestrol Diethylstilbestrol may increase the thrombogenic activities of Alirocumab.
Chlorotrianisene Chlorotrianisene may increase the thrombogenic activities of Alirocumab.
Conjugated estrogens Conjugated estrogens may increase the thrombogenic activities of Alirocumab.
Estrone Estrone may increase the thrombogenic activities of Alirocumab.
Estradiol Estradiol may increase the thrombogenic activities of Alirocumab.
Dienestrol Dienestrol may increase the thrombogenic activities of Alirocumab.
Ethinylestradiol Ethinylestradiol may increase the thrombogenic activities of Alirocumab.
Mestranol Mestranol may increase the thrombogenic activities of Alirocumab.
Estriol Estriol may increase the thrombogenic activities of Alirocumab.
Estrone sulfate Estrone sulfate may increase the thrombogenic activities of Alirocumab.
Quinestrol Quinestrol may increase the thrombogenic activities of Alirocumab.
Hexestrol Hexestrol may increase the thrombogenic activities of Alirocumab.
Tibolone Tibolone may increase the thrombogenic activities of Alirocumab.
Synthetic Conjugated Estrogens, A Synthetic Conjugated Estrogens, A may increase the thrombogenic activities of Alirocumab.
Synthetic Conjugated Estrogens, B Synthetic Conjugated Estrogens, B may increase the thrombogenic activities of Alirocumab.
Polyestradiol phosphate Polyestradiol phosphate may increase the thrombogenic activities of Alirocumab.
Esterified estrogens Esterified estrogens may increase the thrombogenic activities of Alirocumab.
Zeranol Zeranol may increase the thrombogenic activities of Alirocumab.
Equol Equol may increase the thrombogenic activities of Alirocumab.
Promestriene Promestriene may increase the thrombogenic activities of Alirocumab.
Methallenestril Methallenestril may increase the thrombogenic activities of Alirocumab.
Epimestrol Epimestrol may increase the thrombogenic activities of Alirocumab.
Moxestrol Moxestrol may increase the thrombogenic activities of Alirocumab.
Estradiol acetate Estradiol acetate may increase the thrombogenic activities of Alirocumab.
Estradiol benzoate Estradiol benzoate may increase the thrombogenic activities of Alirocumab.
Estradiol cypionate Estradiol cypionate may increase the thrombogenic activities of Alirocumab.
Estradiol valerate Estradiol valerate may increase the thrombogenic activities of Alirocumab.
Biochanin A Biochanin A may increase the thrombogenic activities of Alirocumab.
Formononetin Formononetin may increase the thrombogenic activities of Alirocumab.
Estetrol Estetrol may increase the thrombogenic activities of Alirocumab.
Cetuximab The risk or severity of adverse effects can be increased when Cetuximab is combined with Alirocumab.
Human immunoglobulin G The risk or severity of adverse effects can be increased when Human immunoglobulin G is combined with Alirocumab.
Omalizumab The risk or severity of adverse effects can be increased when Omalizumab is combined with Alirocumab.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Alirocumab.
Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Alirocumab.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Alirocumab.
Indium In-111 satumomab pendetide The risk or severity of adverse effects can be increased when Indium In-111 satumomab pendetide is combined with Alirocumab.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Alirocumab.
Trastuzumab The risk or severity of adverse effects can be increased when Trastuzumab is combined with Alirocumab.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Alirocumab.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Alirocumab.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Alirocumab.
Digoxin Immune Fab (Ovine) The risk or severity of adverse effects can be increased when Digoxin Immune Fab (Ovine) is combined with Alirocumab.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Alirocumab.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Alirocumab.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Alirocumab.
Capromab pendetide The risk or severity of adverse effects can be increased when Capromab pendetide is combined with Alirocumab.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Alirocumab.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Alirocumab.
Natalizumab The risk or severity of adverse effects can be increased when Natalizumab is combined with Alirocumab.
Palivizumab The risk or severity of adverse effects can be increased when Palivizumab is combined with Alirocumab.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Alirocumab.
Bevacizumab The risk or severity of adverse effects can be increased when Bevacizumab is combined with Alirocumab.
Technetium Tc-99m arcitumomab The risk or severity of adverse effects can be increased when Technetium Tc-99m arcitumomab is combined with Alirocumab.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Alirocumab.
Panitumumab The risk or severity of adverse effects can be increased when Panitumumab is combined with Alirocumab.
Ranibizumab The risk or severity of adverse effects can be increased when Ranibizumab is combined with Alirocumab.
Galiximab The risk or severity of adverse effects can be increased when Galiximab is combined with Alirocumab.
Pexelizumab The risk or severity of adverse effects can be increased when Pexelizumab is combined with Alirocumab.
Afelimomab The risk or severity of adverse effects can be increased when Afelimomab is combined with Alirocumab.
Epratuzumab The risk or severity of adverse effects can be increased when Epratuzumab is combined with Alirocumab.
Bectumomab The risk or severity of adverse effects can be increased when Bectumomab is combined with Alirocumab.
Oregovomab The risk or severity of adverse effects can be increased when Oregovomab is combined with Alirocumab.
IGN311 The risk or severity of adverse effects can be increased when IGN311 is combined with Alirocumab.
Adecatumumab The risk or severity of adverse effects can be increased when Adecatumumab is combined with Alirocumab.
Labetuzumab The risk or severity of adverse effects can be increased when Labetuzumab is combined with Alirocumab.
Matuzumab The risk or severity of adverse effects can be increased when Matuzumab is combined with Alirocumab.
Fontolizumab The risk or severity of adverse effects can be increased when Fontolizumab is combined with Alirocumab.
Bavituximab The risk or severity of adverse effects can be increased when Bavituximab is combined with Alirocumab.
CR002 The risk or severity of adverse effects can be increased when CR002 is combined with Alirocumab.
Rozrolimupab The risk or severity of adverse effects can be increased when Rozrolimupab is combined with Alirocumab.
Girentuximab The risk or severity of adverse effects can be increased when Girentuximab is combined with Alirocumab.
Obiltoxaximab The risk or severity of adverse effects can be increased when Obiltoxaximab is combined with Alirocumab.
XTL-001 The risk or severity of adverse effects can be increased when XTL-001 is combined with Alirocumab.
NAV 1800 The risk or severity of adverse effects can be increased when NAV 1800 is combined with Alirocumab.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Alirocumab.
Otelixizumab The risk or severity of adverse effects can be increased when Otelixizumab is combined with Alirocumab.
AMG 108 The risk or severity of adverse effects can be increased when AMG 108 is combined with Alirocumab.
Iratumumab The risk or severity of adverse effects can be increased when Iratumumab is combined with Alirocumab.
Enokizumab The risk or severity of adverse effects can be increased when Enokizumab is combined with Alirocumab.
Ramucirumab The risk or severity of adverse effects can be increased when Ramucirumab is combined with Alirocumab.
Farletuzumab The risk or severity of adverse effects can be increased when Farletuzumab is combined with Alirocumab.
Veltuzumab The risk or severity of adverse effects can be increased when Veltuzumab is combined with Alirocumab.
Ustekinumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Alirocumab.
Trastuzumab emtansine The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Alirocumab.
PRO-542 The risk or severity of adverse effects can be increased when PRO-542 is combined with Alirocumab.
TNX-901 The risk or severity of adverse effects can be increased when TNX-901 is combined with Alirocumab.
Inotuzumab ozogamicin The risk or severity of adverse effects can be increased when Inotuzumab ozogamicin is combined with Alirocumab.
RI 624 The risk or severity of adverse effects can be increased when RI 624 is combined with Alirocumab.
Stamulumab The risk or severity of adverse effects can be increased when MYO-029 is combined with Alirocumab.
CT-011 The risk or severity of adverse effects can be increased when CT-011 is combined with Alirocumab.
Leronlimab The risk or severity of adverse effects can be increased when Leronlimab is combined with Alirocumab.
Glembatumumab vedotin The risk or severity of adverse effects can be increased when Glembatumumab vedotin is combined with Alirocumab.
Olaratumab The risk or severity of adverse effects can be increased when Olaratumab is combined with Alirocumab.
IPH 2101 The risk or severity of adverse effects can be increased when IPH 2101 is combined with Alirocumab.
TB-402 The risk or severity of adverse effects can be increased when TB-402 is combined with Alirocumab.
Caplacizumab The risk or severity of adverse effects can be increased when Caplacizumab is combined with Alirocumab.
IMC-1C11 The risk or severity of adverse effects can be increased when IMC-1C11 is combined with Alirocumab.
Eldelumab The risk or severity of adverse effects can be increased when Eldelumab is combined with Alirocumab.
Lumiliximab The risk or severity of adverse effects can be increased when Lumiliximab is combined with Alirocumab.

Target Protein

Proprotein convertase subtilisin/kexin type 9 PCSK9

Referensi & Sumber

Artikel (PubMed)
  • PMID: 26563849
    Farnier M: An evaluation of alirocumab for the treatment of hypercholesterolemia. Expert Rev Cardiovasc Ther. 2015 Dec;13(12):1307-23. doi: 10.1586/14779072.2015.1111759. Epub 2015 Nov 13.
  • PMID: 26455563
    Devito F, Zito A, Ricci G, Carbonara R, Dentamaro I, Cortese F, Carbonara S, Ciccone MM: Focus on alirocumab: A PCSK9 antibody to treat hypercholesterolemia. Pharmacol Res. 2015 Dec;102:168-75. doi: 10.1016/j.phrs.2015.09.021. Epub 2015 Oct 8.
  • PMID: 26393853
    Authors unspecified: Alirocumab (Praluent) to Lower LDL-Cholesterol. JAMA. 2015 Sep 22-29;314(12):1284-5. doi: 10.1001/jama.2015.11372.

Contoh Produk & Brand

Produk: 37 • International brands: 0
Produk
  • Praluent
    Injection, solution • 75 mg/1mL • Subcutaneous • US • Approved
  • Praluent
    Injection, solution • 150 mg/1mL • Subcutaneous • US • Approved
  • Praluent
    Injection, solution • 75 mg/1mL • Subcutaneous • US • Approved
  • Praluent
    Injection, solution • 150 mg/1mL • Subcutaneous • US • Approved
  • Praluent
    Injection, solution • 75 mg/1mL • Subcutaneous • US • Approved
  • Praluent
    Injection, solution • 150 mg/1mL • Subcutaneous • US • Approved
  • Praluent
    Injection, solution • 75 mg/1mL • Subcutaneous • US • Approved
  • Praluent
    Injection, solution • 150 mg/1mL • Subcutaneous • US • Approved
Menampilkan 8 dari 37 produk.

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