Aflibercept

Aflibercept
Klinički podaci
Prodajno ime	Eylea, Zaltrap
Drugs.com	Monografija
Način primene	Intraokularno
Farmakokinetički podaci
Poluvreme eliminacije	7,13 dana

Identifikatori
CAS broj	862111-32-8^Y
ATC kod	S01LA05 (WHO)
DrugBank	DB08885^Y
Hemijski podaci
Formula	C₄₃₁₈H₆₇₈₈N₁₁₆₄O₁₃₀₄S₃₂
Molarna masa	96.90 kDa

Aflibercept je rekombinantni fuzioni protein koji se sastoji od dve glavne komponente: vezujućeg dela vaskularnog endotelnog faktora rasta (VEGF) iz ekstracelularnih domena ljudskih VEGF receptora 1 i 2, koji su spojeni sa Fc porcijom ljudskog IgG1. Aflibercept je oftalmički agens, koji se koristi u lečenju makularnog edema nakon centralne retinalne venske okcluzije (CRVO) i neovaskularne starosne makularne degeneracije (AMD). FDA je odobrila primenu ovog leka novembera 2011 a EMA novembera 2012.^[1]^[2]^[3]^[4]

Reference

^ Freund KB, Mrejen S, Gallego-Pinazo R: An update on the pharmacotherapy of neovascular age-related macular degeneration. Expert Opin Pharmacother. 2013 Jun;14(8):1017-28. doi: 10.1517/14656566.2013.787410. Epub 2013 Apr 8. PMID 23560774
^ Thai HT, Veyrat-Follet C, Mentre F, Comets E: Population pharmacokinetic analysis of free and bound aflibercept in patients with advanced solid tumors. Cancer Chemother Pharmacol. 2013 May 15. PMID 23673444
^ 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.
^ 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.

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

Aflibercept

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