Peringatan Keamanan

Cases of overdose are represented by an increased risk of bleeding and in these cases, external administration of von Willebrand factor concentrate should be done.FDA label

To this point, there have not been performed studies regarding the effect on fertility, genotoxicity, or carcinogenicity

Caplacizumab

DB06081

biotech approved investigational

Deskripsi

Caplacizumab, firstly called ALX-0081, is a humanized single-variable-domain immunoglobulin consisting of two identical humanized building blocks genetically linked by a three-alanine linker. Caplacizumab was developed by Ablynx, a Sanofi company and FDA approved on February 6, 2019,L5302 and approved previously by the EU in October 2018 as a combination therapy with plasma exchange and immunosuppression.A174634

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The reported half-life is reported to be in the range of 16-27 hours.[F3457]
Volume Distribusi The reported volume of distribution of caplacizumab is 6.33 L.[A174634]
Klirens (Clearance) As the elimination is highly divided among hepatic, target-driven and renal elimination, the calculation of the clearance rate is not significant for drug description.

Absorpsi

After intravenous administration of caplacizumab, the pharmacokinetic profile is non-linear and to follow a non-compartmental model as the pharmacokinetic profile of this drug is dependent on the expression of von Willebrand factor. After administration, caplacizumab is rapidly absorbed with a dose-dependent behavior. The peak concentration was reached after 6-7 hoursA174634 and it presents a very high bioavailability reaching approximately 90%.F3457 The subcutaneous administration of a dose of 10 mg of caplacizumab produced a peak concentration of 528 ng/ml and an AUC of 7951 ng.h/ml.L5314

Metabolisme

Caplacizumab is degraded in the reticuloendothelial system to small peptides and amino acids which can be used for de-novo protein synthesis.A31470

Rute Eliminasi

The elimination of caplacizumab is divided between target-driven disposition which is driven by the binding to the von Willebrand factor and non-target disposition driven by the combination of catabolism and renal elimination.F3457

Interaksi Obat

778 Data
Apixaban The risk or severity of adverse effects can be increased when Caplacizumab is combined with Apixaban.
Dasatinib Dasatinib may increase the anticoagulant activities of Caplacizumab.
Ursodeoxycholic acid The risk or severity of adverse effects can be increased when Caplacizumab is combined with Ursodeoxycholic acid.
Glycochenodeoxycholic Acid The risk or severity of adverse effects can be increased when Caplacizumab is combined with Glycochenodeoxycholic Acid.
Cholic Acid The risk or severity of adverse effects can be increased when Caplacizumab is combined with Cholic Acid.
Glycocholic acid The risk or severity of adverse effects can be increased when Caplacizumab is combined with Glycocholic acid.
Deoxycholic acid The risk or severity of adverse effects can be increased when Caplacizumab is combined with Deoxycholic acid.
Taurocholic acid The risk or severity of adverse effects can be increased when Caplacizumab is combined with Taurocholic acid.
Obeticholic acid The risk or severity of adverse effects can be increased when Caplacizumab is combined with Obeticholic acid.
Chenodeoxycholic acid The risk or severity of adverse effects can be increased when Caplacizumab is combined with Chenodeoxycholic acid.
Taurochenodeoxycholic acid The risk or severity of adverse effects can be increased when Caplacizumab is combined with Taurochenodeoxycholic acid.
Tauroursodeoxycholic acid The risk or severity of adverse effects can be increased when Caplacizumab is combined with Tauroursodeoxycholic acid.
Bamet-UD2 The risk or severity of adverse effects can be increased when Caplacizumab is combined with Bamet-UD2.
Dehydrocholic acid The risk or severity of adverse effects can be increased when Caplacizumab is combined with Dehydrocholic acid.
Hyodeoxycholic Acid The risk or severity of adverse effects can be increased when Caplacizumab is combined with Hyodeoxycholic Acid.
Glucosamine Glucosamine may increase the antiplatelet activities of Caplacizumab.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Caplacizumab is combined with Ibritumomab tiuxetan.
Ibrutinib The risk or severity of adverse effects can be increased when Ibrutinib is combined with Caplacizumab.
Obinutuzumab The risk or severity of adverse effects can be increased when Caplacizumab is combined with Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the antiplatelet activities of Caplacizumab.
Rivaroxaban Caplacizumab may increase the anticoagulant activities of Rivaroxaban.
Tipranavir Tipranavir may increase the antiplatelet activities of Caplacizumab.
Urokinase Caplacizumab may increase the anticoagulant activities of Urokinase.
Vitamin E Vitamin E may increase the antiplatelet activities of Caplacizumab.
Pentosan polysulfate The risk or severity of adverse effects can be increased when Pentosan polysulfate is combined with Caplacizumab.
Diethylstilbestrol Diethylstilbestrol may increase the thrombogenic activities of Caplacizumab.
Chlorotrianisene Chlorotrianisene may increase the thrombogenic activities of Caplacizumab.
Conjugated estrogens Conjugated estrogens may increase the thrombogenic activities of Caplacizumab.
Estrone Estrone may increase the thrombogenic activities of Caplacizumab.
Estradiol Estradiol may increase the thrombogenic activities of Caplacizumab.
Dienestrol Dienestrol may increase the thrombogenic activities of Caplacizumab.
Ethinylestradiol Ethinylestradiol may increase the thrombogenic activities of Caplacizumab.
Mestranol Mestranol may increase the thrombogenic activities of Caplacizumab.
Estriol Estriol may increase the thrombogenic activities of Caplacizumab.
Estrone sulfate Estrone sulfate may increase the thrombogenic activities of Caplacizumab.
Quinestrol Quinestrol may increase the thrombogenic activities of Caplacizumab.
Hexestrol Hexestrol may increase the thrombogenic activities of Caplacizumab.
Tibolone Tibolone may increase the thrombogenic activities of Caplacizumab.
Synthetic Conjugated Estrogens, A Synthetic Conjugated Estrogens, A may increase the thrombogenic activities of Caplacizumab.
Synthetic Conjugated Estrogens, B Synthetic Conjugated Estrogens, B may increase the thrombogenic activities of Caplacizumab.
Polyestradiol phosphate Polyestradiol phosphate may increase the thrombogenic activities of Caplacizumab.
Esterified estrogens Esterified estrogens may increase the thrombogenic activities of Caplacizumab.
Zeranol Zeranol may increase the thrombogenic activities of Caplacizumab.
Equol Equol may increase the thrombogenic activities of Caplacizumab.
Promestriene Promestriene may increase the thrombogenic activities of Caplacizumab.
Methallenestril Methallenestril may increase the thrombogenic activities of Caplacizumab.
Epimestrol Epimestrol may increase the thrombogenic activities of Caplacizumab.
Moxestrol Moxestrol may increase the thrombogenic activities of Caplacizumab.
Estradiol acetate Estradiol acetate may increase the thrombogenic activities of Caplacizumab.
Estradiol benzoate Estradiol benzoate may increase the thrombogenic activities of Caplacizumab.
Estradiol cypionate Estradiol cypionate may increase the thrombogenic activities of Caplacizumab.
Estradiol valerate Estradiol valerate may increase the thrombogenic activities of Caplacizumab.
Biochanin A Biochanin A may increase the thrombogenic activities of Caplacizumab.
Formononetin Formononetin may increase the thrombogenic activities of Caplacizumab.
Estetrol Estetrol may increase the thrombogenic activities of Caplacizumab.
Limaprost Limaprost may increase the antiplatelet activities of Caplacizumab.
Omega-3 fatty acids Omega-3 fatty acids may increase the antiplatelet activities of Caplacizumab.
Tositumomab The risk or severity of adverse effects can be increased when Caplacizumab is combined with Tositumomab.
Lepirudin The risk or severity of bleeding can be increased when Caplacizumab is combined with Lepirudin.
Bivalirudin The risk or severity of bleeding can be increased when Caplacizumab is combined with Bivalirudin.
Alteplase The risk or severity of bleeding can be increased when Caplacizumab is combined with Alteplase.
Reteplase The risk or severity of bleeding can be increased when Caplacizumab is combined with Reteplase.
Anistreplase The risk or severity of bleeding can be increased when Caplacizumab is combined with Anistreplase.
Tenecteplase The risk or severity of bleeding can be increased when Caplacizumab is combined with Tenecteplase.
Abciximab The risk or severity of bleeding can be increased when Caplacizumab is combined with Abciximab.
Drotrecogin alfa The risk or severity of bleeding can be increased when Caplacizumab is combined with Drotrecogin alfa.
Streptokinase The risk or severity of bleeding can be increased when Caplacizumab is combined with Streptokinase.
Dicoumarol The risk or severity of bleeding can be increased when Caplacizumab is combined with Dicoumarol.
Argatroban The risk or severity of bleeding can be increased when Caplacizumab is combined with Argatroban.
Ardeparin The risk or severity of bleeding can be increased when Caplacizumab is combined with Ardeparin.
Phenindione The risk or severity of bleeding can be increased when Caplacizumab is combined with Phenindione.
Fondaparinux The risk or severity of bleeding can be increased when Caplacizumab is combined with Fondaparinux.
Warfarin The risk or severity of bleeding can be increased when Caplacizumab is combined with Warfarin.
Phenprocoumon The risk or severity of bleeding can be increased when Caplacizumab is combined with Phenprocoumon.
Dipyridamole The risk or severity of bleeding can be increased when Caplacizumab is combined with Dipyridamole.
Heparin The risk or severity of bleeding can be increased when Caplacizumab is combined with Heparin.
Enoxaparin The risk or severity of bleeding can be increased when Caplacizumab is combined with Enoxaparin.
Epoprostenol The risk or severity of bleeding can be increased when Caplacizumab is combined with Epoprostenol.
Acenocoumarol The risk or severity of bleeding can be increased when Caplacizumab is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of bleeding can be increased when Caplacizumab is combined with 4-hydroxycoumarin.
Coumarin The risk or severity of bleeding can be increased when Caplacizumab is combined with Coumarin.
Ximelagatran The risk or severity of bleeding can be increased when Caplacizumab is combined with Ximelagatran.
Desmoteplase The risk or severity of bleeding can be increased when Caplacizumab is combined with Desmoteplase.
Defibrotide The risk or severity of bleeding can be increased when Caplacizumab is combined with Defibrotide.
Ancrod The risk or severity of bleeding can be increased when Caplacizumab is combined with Ancrod.
Beraprost The risk or severity of bleeding can be increased when Caplacizumab is combined with Beraprost.
Prasugrel The risk or severity of bleeding can be increased when Caplacizumab is combined with Prasugrel.
Sulodexide The risk or severity of bleeding can be increased when Caplacizumab is combined with Sulodexide.
Semuloparin The risk or severity of bleeding can be increased when Caplacizumab is combined with Semuloparin.
Idraparinux The risk or severity of bleeding can be increased when Caplacizumab is combined with Idraparinux.
Cangrelor The risk or severity of bleeding can be increased when Caplacizumab is combined with Cangrelor.
Astaxanthin The risk or severity of bleeding can be increased when Caplacizumab is combined with Astaxanthin.
Otamixaban The risk or severity of bleeding can be increased when Caplacizumab is combined with Otamixaban.
Amediplase The risk or severity of bleeding can be increased when Caplacizumab is combined with Amediplase.
Danaparoid The risk or severity of bleeding can be increased when Caplacizumab is combined with Danaparoid.
Dalteparin The risk or severity of bleeding can be increased when Caplacizumab is combined with Dalteparin.
Tinzaparin The risk or severity of bleeding can be increased when Caplacizumab is combined with Tinzaparin.
(R)-warfarin The risk or severity of bleeding can be increased when Caplacizumab is combined with (R)-warfarin.
Ethyl biscoumacetate The risk or severity of bleeding can be increased when Caplacizumab is combined with Ethyl biscoumacetate.
Nadroparin The risk or severity of bleeding can be increased when Caplacizumab is combined with Nadroparin.

Target Protein

von Willebrand factor VWF

Referensi & Sumber

Artikel (PubMed)
  • PMID: 30298461
    Duggan S: Caplacizumab: First Global Approval. Drugs. 2018 Oct;78(15):1639-1642. doi: 10.1007/s40265-018-0989-0.
  • PMID: 30656273
    Coppo P, Cuker A, George JN: Thrombotic thrombocytopenic purpura: Toward targeted therapy and precision medicine. Res Pract Thromb Haemost. 2018 Nov 16;3(1):26-37. doi: 10.1002/rth2.12160. eCollection 2019 Jan.
  • PMID: 28445600
    Peyvandi F, Scully M, Kremer Hovinga JA, Knobl P, Cataland S, De Beuf K, Callewaert F, De Winter H, Zeldin RK: Caplacizumab reduces the frequency of major thromboembolic events, exacerbations and death in patients with acquired thrombotic thrombocytopenic purpura. J Thromb Haemost. 2017 Jul;15(7):1448-1452. doi: 10.1111/jth.13716. Epub 2017 Jun 5.
  • PMID: 26863353
    Peyvandi F, Scully M, Kremer Hovinga JA, Cataland S, Knobl P, Wu H, Artoni A, Westwood JP, Mansouri Taleghani M, Jilma B, Callewaert F, Ulrichts H, Duby C, Tersago D: Caplacizumab for Acquired Thrombotic Thrombocytopenic Purpura. N Engl J Med. 2016 Feb 11;374(6):511-22. doi: 10.1056/NEJMoa1505533.
  • PMID: 16478695
    Tabrizi MA, Tseng CM, Roskos LK: Elimination mechanisms of therapeutic monoclonal antibodies. Drug Discov Today. 2006 Jan;11(1-2):81-8. doi: 10.1016/S1359-6446(05)03638-X.

Contoh Produk & Brand

Produk: 5 • International brands: 0
Produk
  • Cablivi
    Kit; Powder, for solution • 11 mg / vial • Intravenous; Subcutaneous • Canada • Approved
  • Cablivi
    Injection, powder, for solution • 10 mg • Intravenous; Subcutaneous • EU • Approved
  • Cablivi
    Injection, powder, for solution • 10 mg • Intravenous; Subcutaneous • EU • Approved
  • Cablivi
    Injection, powder, for solution • 10 mg • Intravenous; Subcutaneous • EU • Approved
  • Cablivi
    Injection, powder, lyophilized, for solution; Kit • 11 mg/1mL • Intravenous; Subcutaneous • US • Approved

Sekuens Gen/Protein (FASTA)

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