Aflibercept

Vascular Endothelial Growth Factor Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Aflibercept is a drug in the Vascular Endothelial Growth Factor Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2011. Its mechanism of action is classified as Vascular Endothelial Growth Factor Inhibitors. DrugCentral lists 3 molecular targets, including VEGFA, VEGFB and PGF. Recorded indications include Branch retinal vein occlusion with macular edema, Central retinal vein occlusion with macular edema, Exudative age-related macular degeneration and Macular edema due to diabetes mellitus.

• Drug class: Vascular Endothelial Growth Factor Inhibitor.
• Mechanism of action: Vascular Endothelial Growth Factor Inhibitors.
• Molecular targets: VEGFA, VEGFB and PGF (3 listed in DrugCentral).
• Indications: Branch retinal vein occlusion with macular edema, Central retinal vein occlusion with macular edema, Exudative age-related macular degeneration, Macular edema due to diabetes mellitus and Metastasis from malignant tumor of colon and others.
• ATC code: L01XX44 (Other antineoplastic agents).

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (8)

• Branch retinal vein occlusion with macular edema
• Central retinal vein occlusion with macular edema
• Exudative age-related macular degeneration
• Macular edema due to diabetes mellitus
• Metastasis from malignant tumor of colon
• Myopic choroidal neovascularization
• Neovascular glaucoma
• Retinopathy of prematurity

Contraindications (1)

• Uveitis

Mechanism & targets

• Mechanism of action (MoA): Vascular Endothelial Growth Factor Inhibitors
• Established pharmacologic class: Vascular Endothelial Growth Factor Inhibitor

Molecular targets (3)

Target	Gene	Action	Activity
Vascular endothelial growth factor A	VEGFA	inhibitor	Kd 12.30
Vascular endothelial growth factor B	VEGFB	inhibitor	Kd 11.72
Placenta growth factor	PGF	inhibitor	Kd 10.41

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2020-03-25	PMDA	—	Bayer Yakuhin, Ltd	Yes
2012-11-22	EMA	—	Bayer AG
2011-11-18	FDA	—	REGENERON PHARMACEUTICALS

ATC classification

ATC code	Therapeutic hierarchy
L01XX44	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › OTHER ANTINEOPLASTIC AGENTS › Other antineoplastic agents
S01LA05	SENSORY ORGANS › OPHTHALMOLOGICALS › OCULAR VASCULAR DISORDER AGENTS › Antineovascularisation agents

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Endophthalmitis	4415.5
Visual acuity reduced	2967.1
Blindness	2630.1
Blindness transient	2309.8
Eye inflammation	2064.0
Visual impairment	1762.5
Intraocular pressure increased	1756.6
Blindness unilateral	1742.3
Non-infectious endophthalmitis	1713.9
Retinal haemorrhage	1702.0
Vitritis	1611.2
Death	1382.6

Chemical structure

• Molecular formula: —
• Molecular weight: —
• CAS number: 862111-32-8
• InChIKey: —
• PubChem CID: —

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Aflibercept used for?

DrugCentral lists the following indications for Aflibercept: Branch retinal vein occlusion with macular edema, Central retinal vein occlusion with macular edema, Exudative age-related macular degeneration, Macular edema due to diabetes mellitus, Metastasis from malignant tumor of colon, Myopic choroidal neovascularization, Neovascular glaucoma and Retinopathy of prematurity.

How does Aflibercept work?

Aflibercept is classified as Vascular Endothelial Growth Factor Inhibitors; its molecular targets in DrugCentral include VEGFA (inhibitor), VEGFB (inhibitor) and PGF (inhibitor).

When was Aflibercept first approved?

Aflibercept was first approved by the FDA in 2011.

What drug class does Aflibercept belong to?

Aflibercept is in the Vascular Endothelial Growth Factor Inhibitor class.

Sources

• DrugCentral drug card 4916 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1742982 — compound record and bioactivity
• DrugBank DB08885 — drug record
• FDA UNII 15C2VL427D — substance identity
• DailyMed: FDA labels for Aflibercept — current prescribing information (label search)
• UniProt P15692 (VEGFA) — target protein
• UniProt P49765 (VEGFB) — target protein
• UniProt P49763 (PGF) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

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