Drug intelligence / Profile preview

aflibercept + mLV5FU2

Development stage
Unknown
Lead developer
Regeneron Pharmaceuticals
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Intravitreal
01

Overview

Aflibercept is a recombinant fusion protein that acts as a decoy receptor for vascular endothelial growth factor A (VEGF-A), VEGF-B, and placenta growth factor (PlGF). By binding these ligands and preventing their interaction with VEGFR-1 and VEGFR-2 on endothelial cells, aflibercept inhibits angiogenesis and vascular permeability. It is primarily used to treat neovascular (wet) age-related macular degeneration (AMD), diabetic macular edema (DME), diabetic retinopathy (DR), macular edema following retinal vein occlusion (RVO), and retinopathy of prematurity (ROP)[1][2][3][4][5][6]. Systemically administered ziv-aflibercept in combination with chemotherapy regimens such as FOLFIRI or modified LV5FU2 is indicated for metastatic colorectal cancer resistant to or progressed after oxaliplatin-based therapy[2]. mLV5FU2 refers to a modified regimen of leucovorin plus 5-fluorouracil ("modified de Gramont" protocol). 5-fluorouracil is an antimetabolite that inhibits thymidylate synthase leading to impaired DNA synthesis; leucovorin enhances its efficacy by stabilizing the binding of 5-FU's active metabolite to thymidylate synthase. The combination "aflibercept + mLV5FU2" is used in oncology—specifically metastatic colorectal cancer—where aflibercept’s antiangiogenic effect complements the cytotoxic action of fluoropyrimidine-based chemotherapy.

Brand names
AhzantiveEnzeevuOpuvizPavbluYesafili
Other names
ziv-aflibercept
02

Targets

VEGFB (Vascular endothelial growth factor B)PGF (Placental Growth Factor)VEGFA (Vascular endothelial growth factor A)TS (Thymidylate synthase)

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