Ekulizumab

Ekulizumab
Klinički podaci
Prodajno ime	Soliris, Soliris (Alexion Pharmaceuticals)
Drugs.com	Monografija
Način primene	Intravenozno
Farmakokinetički podaci
Poluvreme eliminacije	82 h

Identifikatori
CAS broj	219685-50-4^Y
ATC kod	None
DrugBank	DB01257^Y
ChEMBL	CHEMBL1201828^Y
Hemijski podaci
Molarna masa	148 kDa

Ekulizumab (INN i USAN; prodajno ime Soliris) jeste humanizovano monoklonalno antitelo. Ono je prvo u klasi terminalnih inhibitora komplementa, kao i prva terapija koja je odobrena za lečenje paroksizmalne noćne hemoglobinurije (PNH), retke, progresivne, i u pojedinim slučajevima smrtonosne bolesti karakterisane prekomernim uništavanjem crvenih krvnih zrnaca (hemolizom).^[1]^[2]^[3]^[4]^[5]^[6]^[7]

Reference

^ Hillmen, Young, Schubert, P, N, J; et al. (2006). „The complement inhibitor eculizumab in paroxysmal nocturnal hemoglobinuria”. N Engl J Med. 355 (12): 1233—1243. PMID 16990386. doi:10.1056/NEJMMoa061648. CS1 одржавање: Експлицитна употреба et al. (веза)CS1 одржавање: Вишеструка имена: списак аутора (веза)
^ Hillmen P, Young NS, Schubert J, Brodsky RA, Socie G, Muus P, Roth A, Szer J, Elebute MO, Nakamura R, Browne P, Risitano AM, Hill A, Schrezenmeier H, Fu CL, Maciejewski J, Rollins SA, Mojcik CF, Rother RP, Luzzatto L: The complement inhibitor eculizumab in paroxysmal nocturnal hemoglobinuria. N Engl J Med. 2006 Sep 21;355(12):1233-43. PMID 16990386
^ Thomas TC, Rollins SA, Rother RP, Giannoni MA, Hartman SL, Elliott EA, Nye SH, Matis LA, Squinto SP, Evans MJ: Inhibition of complement activity by humanized anti-C5 antibody and single-chain Fv. Mol Immunol. 1996 Dec;33(17-18):1389-401. PMID 9171898
^ Dmytrijuk A, Robie-Suh K, Cohen MH, Rieves D, Weiss K, Pazdur R: FDA report: eculizumab (Soliris) for the treatment of patients with paroxysmal nocturnal hemoglobinuria. Oncologist. 2008 Sep;13(9):993-1000. Epub 2008 Sep 10. PMID 18784156
^ Rother RP, Rollins SA, Mojcik CF, Brodsky RA, Bell L: Discovery and development of the complement inhibitor eculizumab for the treatment of paroxysmal nocturnal hemoglobinuria. Nat Biotechnol. 2007 Nov;25(11):1256-64. PMID 17989688
^ Knox C, Law V, Jewison T, Liu P, Ly S, Frolkis A, Pon A, Banco K, Mak C, Neveu V, Djoumbou Y, Eisner R, Guo AC, Wishart DS (2011). „DrugBank 3.0: a comprehensive resource for omics research on drugs”. Nucleic Acids Res. 39 (Database issue): D1035—41. PMC 3013709 . PMID 21059682. doi:10.1093/nar/gkq1126. уреди
^ David S. Wishart; Craig Knox; An Chi Guo; Dean Cheng; Savita Shrivastava; Dan Tzur; Bijaya Gautam; Murtaza Hassanali (2008). „DrugBank: a knowledgebase for drugs, drug actions and drug targets”. Nucleic acids research. 36 (Database issue): D901—6. PMC 2238889 . PMID 18048412. doi:10.1093/nar/gkm958. уреди

Literatura

Hardman JG, Limbird LE, Gilman AG (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10. изд.). New York: McGraw-Hill. ISBN 0071354697. doi:10.1036/0071422803.
Thomas L. Lemke; David A. Williams, ур. (2007). Foye's Principles of Medicinal Chemistry (6. изд.). Baltimore: Lippincott Willams & Wilkins. ISBN 0781768799.

Spoljašnje veze

Eculizumab

Imunomodulatori: Imunosupresivni lekovi / Imunosupresanti (L04)

Intracelularni
(inicijacija)

Antimetaboliti	inhibitor sinteze purinа: Azatioprin • Mikofenolna kiselina/Mikofenolat mofetil inhibitor sinteze pirimidina: Leflunomid • Teriflunomid antifolat: Metotreksat
Makrolidi/ drugi IL-2 inhibitori	FKBP/Ciklofilin/Kalcineurin: Takrolimus • Ciklosporin • Pimekrolimus Abetimus • Gusperimus
TNF-α inhibitor	Talidomid • Lenalidomid

Intracelularni
(recepcija)

Antagonisti IL-1 receptora	Anakinra
mTOR	Sirolimus • Deforolimus • Everolimus • Temsirolimus • Zotarolimus • Biolimus A9

Ekstracelularni

Antitela

Monoklonalna

Serum cilj (non-celularni)	Dopunska komponenta 5 (Eculizumab) • TNF (Infliksimab, Adalimumab, Certolizumab pegol, Afelimomab, Golimumab) • Interleukin 5 (Mepolizumab) • Imunoglobulin E (Omalizumab) • BAYX (Nerelimomab) Interferon (Faralimomab) IL-6 (Elsilimomab) IL-12 i IL-13 (Lebrikizumab, Ustekinumab)
Celularni ciljevi	CD3 (Muromonab-CD3, Oteliksizumab, Teplizumab, Visilizumab) • CD4 (Klenoliksimab, Keliksimab, Zanolimumab) • CD11a (Efalizumab) • CD18 (Erlizumab) • CD20 (Afutuzumab, Ocrelizumab, Pascolizumab) • CD23 (Lumiliksimab) • CD40 (Teneliksimab, Toralizumab) • CD62L/L-selektin (Aselizumab) • CD80 (Galiksimab) • CD147/Basigin (Gavilimomab) • CD154 (Ruplizumab) BLyS (Belimumab) • CTLA-4 (Ipilimumab, Tremelimumab) • CAT (Bertilimumab, Lerdelimumab, Metelimumab) • Integrin (Natalizumab) • Interleukin-6 receptor (Tocilizumab) • LFA-1 (Odulimomab) IL-2 receptor/CD25 (Basiliksimab, Daklizumab, Inolimomab) T-limfocit (Zolimomab aritoks)
Nesortirani	Atorolimumab, Cedelizumab, Dorliksizumab, Fontolizumab, Gantenerumab, Gomiliksimab, Maslimomab, Morolimumab, Pekselizumab, Reslizumab, Rovelizumab, Siplizumab, Talizumab, Telimomab aritoks, Vapaliksimab, Vepalimomab