Identification

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Name
Aflibercept
Accession Number
DB08885
Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Fusion proteins
Description

Aflibercept is a recombinant protein composed of the binding domains of two human vascular endothelial growth factor (VEGF) receptors fused with the Fc region of human immunoglobulin gamma 1 (IgG1). Structurally, Aflibercept is a dimeric glycoprotein with a protein molecular weight of 96.9 kilo Daltons (kDa). It contains approximately 15% glycosylation to give a total molecular weight of 115 kDa. All five putative N-glycosylation sites on each polypeptide chain predicted by the primary sequence can be occupied with carbohydrate and exhibit some degree of chain heterogeneity, including heterogeneity in terminal sialic acid residues, except at the single unsialylated site associated with the Fc domain. Aflibercept, as an ophthalmic agent, is used in the treatment of macular edema following Central Retinal Vein Occlusion (CRVO) and neovascular Age-Related Macular Degeneration (AMD). Ziv-aflibercept, under the brand name Zaltrap, was developed as an injection for treatment of metastatic colorectal cancer. FDA approved in November 18, 2011 and EMA approved in November 2012.

Protein chemical formula
C4318H6788N1164O1304S32
Protein average weight
115000.0 Da (with glycosylation)
Sequences
> Protein sequence for aflibercept
SDTGRPFVEMYSEIPEIIHMTEGRELVIPCRVTSPNITVTLKKFPLDTLIPDGKRIIWDS
RKGFIISNATYKEIGLLTCEATVNGHLYKTNYLTHRQTNTIIDVVLSPSHGIELSVGEKL
VLNCTARTELNVGIDFNWEYPSSKHQHKKLVNRDLKTQSGSEMKKFLSTLTIDGVTRSDQ
GLYTCAASSGLMTKKNSTFVRVHEKDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISR
TPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLN
GKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPS
DIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNH
YTQKSLSLSPG
Download FASTA Format
Synonyms
  • Aflibercept
  • Aflibercept (genetical recombination)
  • Ziv-aflibercept
External IDs
AVE 0005 / AVE 005 / AVE-0005 / AVE0005 / Bay 86-5321 / BAY-865321 / Bay86-5321
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
EyleaInjection, solution40 mg/1mLIntravitrealRegeneron Pharmaceuticals, Inc.2011-11-21Not applicableUs
EyleaInjection, solution40 mg/mlIntravitrealBayer Ag2012-11-22Not applicableEu
EyleaInjection, solution40 mg/mlIntravitrealBayer Ag2012-11-22Not applicableEu
EyleaSolution40 mgIntravitrealBayer2013-12-23Not applicableCanada
ZaltrapInjection, solution, concentrate25 mg/mlIntravenousSanofi Aventis Groupe2013-02-01Not applicableEu
ZaltrapInjection, solution, concentrate25 mg/mlIntravenousSanofi Aventis Groupe2013-02-01Not applicableEu
ZaltrapSolution, concentrate200 mg/8mLIntravenoussanofi-aventis U.S. LLC2012-08-03Not applicableUs
ZaltrapSolution200 mgIntravenousSanofi Aventis2014-05-08Not applicableCanada
ZaltrapSolution, concentrate100 mg/4mLIntravenoussanofi-aventis U.S. LLC2012-08-03Not applicableUs
ZaltrapSolution100 mgIntravenousSanofi Aventis2014-05-08Not applicableCanada
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories
UNII
15C2VL427D
CAS number
862111-32-8

Pharmacology

Indication

The opthalmic agent is used for the treatment of neovascular (wet) age-related mascular degeneration (AMD) and macular edema following central retinal vein occulsion (CRVO). The systemic injection, known as ziv-aflibercept, in combination with 5-fluorouracil, leucovorin, irinotecan-(FOLFIRI), is for the treatment of metastatic colorectal cancer that is resistant to or progressed following treatment with oxaliplatin.

Associated Conditions
Pharmacodynamics

Compared to other anti-VEGF drugs like bevacizumab and ranibizumab, aflibercept has a higher binding affinity to VEGF-A (Kd = 0.5 pM).

Mechanism of action

Ablibercept is a recombinant fusion protein that acts as a decoy receptor for the ligands, vascular endothelial growth factor-A (VEGF-A) and placental growth factor (PIGF). It prevents these ligands to binding to endothelial receptors, VEGFR-1 and VEGFR-2, to suppress neovascularization and decrease vascular permeability. This ultimately will slow vision loss or the progression of metastatic colorectal cancer.

TargetActionsOrganism
AVascular endothelial growth factor A
binder
Humans
APlacenta growth factor
binder
Humans
AVascular endothelial growth factor B
binder
Humans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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Absorption

In patients with wet AMD and CRVO, the mean peak plasma concentration (Cmax) was 0.02 mcg/mL and 0.05 mcg/mL respectively. These concentrations were reached in 1 to 3 days. Aflibercept did not accumulate when administered as repeated doses intravitreally every 4 weeks.

Volume of distribution

After intravenous injection of aflibercept, the volume of distribution is 6 L.

Protein binding
Not Available
Metabolism

Because aflibercept is a protein, it is expected to be broken down via proteolysis into smaller peptides and amino acids. The cytochrome P450 enzyme system is not involved in the metabolism of aflibercept.

Route of elimination

Via kidney and liver

Half life

Intravitreal half-life= 7.13 days in humans; Terminal elimination half-life of free aflibercept in plasma was 5 to 6 days after IV injection of 2 - 4 mg/kg dose.

Clearance

When cancer patients were given 2-9 mg/kg every 2 or 3 week; 1 hour IV infusion of aflibercept the typical estimated clearances were as follows: CL of free aflibercept (CLf) = 0.88 L/day; CL of bound aflibercept (CLf) = 0.19 L/day; Patients clear free aflibercept faster if they had low albumin or high alkaline phosphatase levels.

Toxicity

For all intravitreal VEGF inhibitors, there is increased risk of stroke and myocardial infarction. An increase in intraocular pressure may also occur. When used intravenously, most common adverse reactions were leukopenia, diarrhea, neutropenia, proteinuria, AST increased, stomatitis, fatigue, thrombocytopenia, ALT increased, hypertension, weight decreased, decreased appetite, epistaxis, abdominal pain, dysphonia, serum creatinine increased, and headache.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

References

General References
  1. 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. [PubMed:23560774]
  2. 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 Jul;72(1):167-80. doi: 10.1007/s00280-013-2182-1. Epub 2013 May 15. [PubMed:23673444]
External Links
KEGG Drug
D09574
PubChem Substance
347910379
ChEMBL
CHEMBL1742982
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Aflibercept
ATC Codes
S01LA05 — AfliberceptL01XX44 — Aflibercept
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
  • 52:92.00 — EENT Drugs, Miscellaneous
FDA label
Download (325 KB)
MSDS
Download (91.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Active Not RecruitingTreatmentAb externo surgery Glaucoma / Eye Diseases / Optic nerve damage1
0CompletedTreatmentRetinopathy, Diabetic1
1Active Not RecruitingTreatmentMacular Edema (ME) / Radiation Retinopathy1
1CompletedBasic ScienceDiabetic Macular Edema (DME) / Neovascular Age-Related Macular Degeneration1
1CompletedOtherNeovascular Macular Degeneration1
1CompletedTreatmentAdult Anaplastic Astrocytoma / Adult Anaplastic Oligodendroglioma / Adult Giant Cell Glioblastoma / Adult Glioblastoma / Adult Gliosarcoma / Adult Mixed Glioma / Recurrent Adult Brain Tumor1
1CompletedTreatmentMacular Degeneration1
1CompletedTreatmentMalignancies3
1CompletedTreatmentMalignant Lymphomas / Unspecified Adult Solid Tumor, Protocol Specific2
1CompletedTreatmentMetastatic Biliary Tract Cancer / Metastatic Breast Cancer (MBC) / Metastatic Colorectal Cancers / Metastatic Gastric Cancers / Metastatic Oesophageal Cancers / Pancreatic Cancer Metastatic1
1CompletedTreatmentNeoplasms2
1CompletedTreatmentNeoplasms Malignant2
1CompletedTreatmentNeoplasms Metastasis / Neoplasms, Colorectal1
1CompletedTreatmentNeovascular Age-Related Macular Degeneration1
1CompletedTreatmentNon-Hodgkin's Lymphoma (NHL)1
1CompletedTreatmentPresumed Ocular Histoplasmosis / Subfoveal Choroidal Neovascularization1
1CompletedTreatmentTumors, Solid1
1CompletedTreatmentUnspecified Childhood Solid Tumor, Protocol Specific1
1Not Yet RecruitingTreatmentNeovascular Age-Related Macular Degeneration1
1RecruitingTreatmentAdult Solid Neoplasm / Malignant Solid Neoplasm / Metastatic Kidney Carcinoma / Metastatic Melanoma / Metastatic Renal Cell Cancer / Microsatellite Stable / Recurrent Colorectal Carcinoma / Recurrent Melanoma / Recurrent Ovarian Carcinoma / Refractory Melanoma / Renal Cell Carcinoma Recurrent / Sarcomas / Stage IV Colorectal Cancer AJCC v7 / Stage IV Ovarian Cancer / Stage IV Ovarian Cancer AJCC v6 and v7 / Stage IVA Colorectal Cancer / Stage IVA Colorectal Cancer AJCC v7 / Stage IVB Colorectal Cancer / Stage IVB Colorectal Cancer AJCC v71
1RecruitingTreatmentAdvanced Malignant Solid Neoplasm / Fibrolamellar Carcinoma / Metastatic Malignant Solid Neoplasm / Metastatic Solid Neoplasm / Neoplasms, Advanced Solid / Ovarian Carcinoma / Progressive Neuroendocrine Tumors of pancreatic origin / Recurrent Malignant Solid Neoplasm / Recurrent Solid Neoplasm / Refractory Malignant Solid Neoplasm / Solid Neoplasms / Unresectable Solid Neoplasm1
1RecruitingTreatmentDiabetic Macular Edema (DME) / Neovascular Age-Related Macular Degeneration1
1RecruitingTreatmentMacular Edema (ME) / Retinal Artery Macroaneurysm1
1RecruitingTreatmentNeovascular Age-Related Macular Degeneration / Wet Age-Related Macular Degeneration1
1RecruitingTreatmentPseudophakic Cystoid Macular Edema1
1RecruitingTreatmentWet Age-Related Macular Degeneration1
1TerminatedTreatmentCorneal Neovascularization1
1TerminatedTreatmentNeoplasms1
1Unknown StatusTreatmentAge Related Macular Degeneration (ARMD) / Central Retinal Vein Occlusion (CRVO)1
1, 2CompletedBasic ScienceAge-Related Macular Degeneration (ARMD) / Diabetic Macular Edema (DME) / Retinal Vein Occlusions(RVO)1
1, 2CompletedTreatmentAdvanced Carcinoma / Lung Cancer Non-Small Cell Cancer (NSCLC)1
1, 2CompletedTreatmentCentral Retinal Vein Occlusion (CRVO) / Proliferative Diabetic Retinopathy (PDR)1
1, 2CompletedTreatmentDiabetic Macular Edema (DME)1
1, 2CompletedTreatmentFallopian Tube Cancer / Malignant Tumor of Peritoneum / Recurrent Ovarian Epithelial Cancer1
1, 2CompletedTreatmentMetastatic Colorectal Cancers1
1, 2CompletedTreatmentNeovascular Age-Related Macular Degeneration2
1, 2RecruitingPreventionRetinopathy, Diabetic1
1, 2RecruitingTreatmentDiabetic Macular Edema (DME)1
1, 2RecruitingTreatmentNeovascular Age-Related Macular Degeneration1
1, 2RecruitingTreatmentProliferative Diabetic Retinopathy (PDR)1
1, 2TerminatedTreatmentCorneal Neovascularization1
1, 2TerminatedTreatmentMacular Degeneration1
1, 2TerminatedTreatmentMetastatic Colorectal Cancers1
1, 2Unknown StatusTreatmentHistoplasmosis retinitis1
2Active Not RecruitingTreatmentAdverse Effect of Radiation Therapy1
2Active Not RecruitingTreatmentCarcinoid Tumors1
2Active Not RecruitingTreatmentMacular Oedema / Retinitis Pigmentosa (RP)1
2Active Not RecruitingTreatmentMetastatic Colon Cancer / Mucinous Adenocarcinoma of the Colon / Mucinous Adenocarcinoma of the Rectum / Signet Ring Adenocarcinoma of the Colon / Signet Ring Adenocarcinoma of the Rectum / Stage IV Rectal Cancer1
2Active Not RecruitingTreatmentMetastatic Colorectal Cancers2
2Active Not RecruitingTreatmentNaive Patients With Uncomplicated PDR / Naive Patients With Uncomplicated Proliferative Diabetic Retinopathy1
2Active Not RecruitingTreatmentProliferative Diabetic Retinopathy (PDR)1
2Active Not RecruitingTreatmentRectal Carcinoma1
2Active Not RecruitingTreatmentSubfoveal Choroidal Neovascularization / Wet Macular Degeneration1
2Active Not RecruitingTreatmentWet Age-Related Macular Degeneration / Wet Macular Degeneration1
2CompletedTreatmentAdenocarcinoma of the Bladder / Distal Urethral Cancer / Metastatic Bladder Cancer / Metastatic Transitional Cell Cancer of the Renal Pelvis and Ureter / Proximal Urethral Cancer / Recurrent Bladder Cancer / Recurrent Transitional Cell Cancer of the Renal Pelvis and Ureter / Recurrent Urethral Cancer / Squamous Cell Carcinoma of the Bladder / Stage III Bladder Cancer / Stage III Urethral Cancer / Transitional Cell Carcinoma of the Bladder / Urethral Cancer Associated With Invasive Bladder Cancer1
2CompletedTreatmentAdult Anaplastic Astrocytoma / Adult Anaplastic Oligodendroglioma / Adult Giant Cell Glioblastoma / Adult Gliosarcoma / Recurrent Adult Brain Tumor1
2CompletedTreatmentAge-Related Macular Degeneration (ARMD)2
2CompletedTreatmentCancer of the Ovary / Neoplasms1
2CompletedTreatmentCentral Serous Chorioretinopathy (CSC)1
2CompletedTreatmentCiliary Body and Choroid Melanoma, Medium/Large Size / Extraocular Extension Melanoma / Iris Melanoma / Metastatic Intraocular Melanoma / Recurrent Intraocular Melanoma / Recurrent Melanoma / Stage III Melanoma / Stage IV Melanoma1
2CompletedTreatmentClear Cell Renal Cell Carcinoma / Renal Cell Carcinoma Recurrent / Stage III Renal Cell Cancer / Stage IV Renal Cell Cancer1
2CompletedTreatmentDiabetic Macular Edema (DME)4
2CompletedTreatmentEsophageal Cancers / Malignant Neoplasm of Stomach1
2CompletedTreatmentExtensive Stage Small Cell Lung Cancer / Refractory Small cell lung cancer1
2CompletedTreatmentExudative Age Related Macular Degeneration1
2CompletedTreatmentFallopian Tube Cancer / Female Reproductive Cancer / Ovarian Carcinosarcoma / Ovarian Sarcoma / Recurrent Ovarian Epithelial Cancer / Recurrent Uterine Sarcoma / Stage III Ovarian Epithelial Cancer / Stage III Uterine Sarcoma / Stage IV Ovarian Epithelial Cancer / Stage IV Uterine Sarcoma / Uterine Carcinosarcoma / Uterine Leiomyosarcoma1
2CompletedTreatmentIdiopathic Choroidal Neovascularization1
2CompletedTreatmentIdiopathic Polypoidal Choroidal Vasculopathy1
2CompletedTreatmentInflammatory Choroidal Neovascularization1
2CompletedTreatmentMacular Degeneration2
2CompletedTreatmentMacular Edema (ME) / Retinal Vein Occlusions(RVO)1
2CompletedTreatmentMetastatic Breast Cancer (MBC) / Recurrent Breast Cancer / Stage IV Breast Cancer1
2CompletedTreatmentMetastatic Colon Cancer / Recurrent Colon Cancer / Recurrent Rectal Cancer / Stage IV Rectal Cancer1
2CompletedTreatmentMetastatic Colorectal Cancers4
2CompletedTreatmentMetastatic Melanoma / Recurrent Melanoma / Stage III Cutaneous Melanoma AJCC v7 / Stage IIIA Cutaneous Melanoma AJCC v7 / Stage IIIA Skin Melanoma / Stage IIIB Cutaneous Melanoma AJCC v7 / Stage IIIB Skin Melanoma / Stage IIIC Cutaneous Melanoma AJCC v7 / Stage IIIC Skin Melanoma / Stage IV Cutaneous Melanoma AJCC v6 and v7 / Stage IV Skin Melanoma1
2CompletedTreatmentMultiple Endocrine Neoplasia Type 1 / Pancreatic Neuroendocrine Carcinoma1
2CompletedTreatmentNeoplasms Metastasis / Neoplasms, Colorectal1
2CompletedTreatmentNeoplasms, Lung / Pulmonary Diseases1
2CompletedTreatmentNeoplasms, Ovarian1
2CompletedTreatmentNeovascular Age-Related Macular Degeneration3
2CompletedTreatmentPseudoxanthoma Elasticum1
2CompletedTreatmentRectal Carcinoma1
2CompletedTreatmentRecurrent Endometrial Carcinoma1
2CompletedTreatmentRecurrent Thyroid Gland Carcinoma / Stage III Thyroid Gland Follicular Carcinoma / Stage III Thyroid Gland Papillary Carcinoma / Stage IV Thyroid Gland Follicular Carcinoma / Stage IV Thyroid Gland Papillary Carcinoma1
2CompletedTreatmentUnresectable Metastatic Colorectal Cancer1
2CompletedTreatmentVitreous Hemorrhage1
2Not Yet RecruitingTreatmentCataracts / Diabetic Macular Edema (DME)1
2Not Yet RecruitingTreatmentDiabetic Macular Edema (DME)1
2Not Yet RecruitingTreatmentNeovascular (Wet) Age-Related Macular Degeneration1
2Not Yet RecruitingTreatmentNeovascular Age-Related Macular Degeneration1
2Not Yet RecruitingTreatmentProliferative Diabetic Retinopathy (PDR)1
2RecruitingPreventionAge-Related Macular Degeneration (ARMD)1
2RecruitingTreatmentColorectal Cancers1
2RecruitingTreatmentCystoid Macular Edema / Macular Degeneration / Neovascularization / Recurrent Pterygium / Retinal Neovascularization / Retinal Vein Occlusions(RVO) / Retinopathy, Diabetic / Subfoveal Choroidal Neovascularization1
2RecruitingTreatmentMetastatic Colorectal Cancers / MSI1
2RecruitingTreatmentMetastatic Colorectal Cancers2
2RecruitingTreatmentNeoplasms, Colorectal1
2RecruitingTreatmentNeovascular Age-Related Macular Degeneration1
2RecruitingTreatmentRadiation Retinopathy1
2RecruitingTreatmentRectal Carcinoma / Rectosigmoid Cancer1
2RecruitingTreatmentRetinopathy, Diabetic2
2RecruitingTreatmentUveal Melanoma1
2RecruitingTreatmentWet Macular Degeneration1
2TerminatedTreatmentAge-Related Macular Degeneration (AMD) / AMD / Eye Diseases / Macular Degeneration / Macular Degeneration, Age-related, 10 / Neovascular Age-Related Macular Degeneration / Retinal Degenerations / Retinal Diseases1
2TerminatedTreatmentAge-Related Macular Degeneration (ARMD)1
2TerminatedTreatmentAtypical Chronic Myeloid Leukemia, BCR-ABL1 Negative / Chronic Myelomonocytic Leukemia / De Novo Myelodysplastic Syndromes / Myelodysplastic/Myeloproliferative Neoplasm, Unclassifiable / Previously Treated Myelodysplastic Syndromes / Secondary Myelodysplastic Syndromes1
2TerminatedTreatmentMetastatic Colorectal Cancers2
2TerminatedTreatmentNeovascular Age-Related Macular Degeneration1
2TerminatedTreatmentStage II Multiple Myeloma / Stage III Multiple Myeloma1
2Unknown StatusTreatmentCentral Serous Chorioretinopathy (CSC)1
2WithdrawnTreatmentChoroidal Neovascularization in Angioid Streaks1
2WithdrawnTreatmentColorectal Cancers1
2WithdrawnTreatmentColorectal Cancers / Metastatic Colorectal Cancers1
2WithdrawnTreatmentIdiopathic Polypoidal Choroidal Vasculopathy1
2WithdrawnTreatmentMetastatic Colorectal Cancers2
2WithdrawnTreatmentMucinous Adenocarcinoma of the Colon / Mucinous Adenocarcinoma of the Rectum / Recurrent Colon Cancer / Recurrent Rectal Cancer / Signet Ring Adenocarcinoma of the Colon / Signet Ring Adenocarcinoma of the Rectum / Stage IVA Colon Cancer / Stage IVA Rectal Cancer / Stage IVB Colon Cancer / Stage IVB Rectal Cancer1
2, 3Active Not RecruitingTreatmentProliferative Diabetic Retinopathy (PDR) / Vitreous Hemorrhage1
2, 3CompletedTreatmentAscites / Neoplasms, Ovarian1
2, 3CompletedTreatmentDiabetic Macular Edema (DME)2
2, 3CompletedTreatmentProliferative Diabetic Retinopathy (PDR)1
2, 3RecruitingBasic ScienceAge Related Macular Degeneration (ARMD)1
2, 3RecruitingTreatmentDiabetic Macular Edema (DME)1
2, 3WithdrawnTreatmentHepatic Metastases / KRAS Mutated Colorectal Cancer / Metastatic Colorectal Cancers1
3Active Not RecruitingPreventionDiabetic Macular Edema (DME) / Retinopathy, Diabetic1
3Active Not RecruitingTreatmentCentral Retinal Vein Occlusion (CRVO)1
3Active Not RecruitingTreatmentDiabetic Macular Edema (DME)1
3Active Not RecruitingTreatmentMacular Degeneration1
3Active Not RecruitingTreatmentNonproliferative Diabetic Retinopathy1
3CompletedTreatmentBranch Retinal Vein Occlusion1
3CompletedTreatmentCarcinoma NOS / Non Small Cell Lung1
3CompletedTreatmentDiabetes Mellitus (DM) / Macular Edema (ME)1
3CompletedTreatmentDiabetic Macular Edema (DME)3
3CompletedTreatmentEye Diseases / Macular Degeneration / Retinal Degenerations / Retinal Diseases / Wet Macular Degeneration1
3CompletedTreatmentGlaucoma, Neovascular2
3CompletedTreatmentGlaucoma / Iris Neovascularization1
3CompletedTreatmentMacular Degeneration3
3CompletedTreatmentMacular Edema (ME)3
3CompletedTreatmentMetastatic Colorectal Cancers3
3CompletedTreatmentNeoplasms Metastasis / Neoplasms, Colorectal1
3CompletedTreatmentNeoplasms Metastasis / Prostatic Neoplasms1
3CompletedTreatmentNeovascular Age-Related Macular Degeneration2
3CompletedTreatmentNeovascular Age-Related Macular Degeneration / Subfoveal Choroidal Neovascularization2
3CompletedTreatmentPathological Myopia1
3CompletedTreatmentRetinal Vein Occlusions(RVO)1
3Enrolling by InvitationTreatmentDiabetic Macular Edema (DME)1
3Not Yet RecruitingOtherRetinopathy of Prematurity (ROP)1
3Not Yet RecruitingTreatmentAge-Related Macular Degeneration (ARMD) / Eye Diseases / Macular Degeneration / Retinal Degenerations / Retinal Diseases / Wet Macular Degeneration1
3Not Yet RecruitingTreatmentBranch Retinal Vein Occlusion1
3Not Yet RecruitingTreatmentDiabetic Macular Edema (DME)2
3Not Yet RecruitingTreatmentOcular Melanoma1
3Not Yet RecruitingTreatmentRetinopathy of Prematurity1
3RecruitingTreatmentAge-Related Macular Degeneration (ARMD)1
3RecruitingTreatmentCentral Retinal Vein Occlusion (CRVO)1
3RecruitingTreatmentDiabetic Macular Edema (DME)5
3RecruitingTreatmentMacular Telangiectasia / Patient With Idiopathic Macular Telangiectasia Type 1 Identified1
3RecruitingTreatmentNeovascular Age-Related Macular Degeneration2
3RecruitingTreatmentRetinopathy of Prematurity (ROP)1
3RecruitingTreatmentWet Age-Related Macular Degeneration1
3RecruitingTreatmentWet Macular Degeneration2
3TerminatedTreatmentAge-Related Macular Degeneration (ARMD)1
3TerminatedTreatmentMacular Edema (ME) / Retinal Vein Occlusions(RVO)1
3TerminatedTreatmentNeoplasms, Pancreatic1
4Active Not RecruitingTreatmentAge Related Macular Degeneration (ARMD)1
4Active Not RecruitingTreatmentCentral Retinal Vein Occlusion (CRVO)1
4Active Not RecruitingTreatmentChorioretinal Vascular Disease1
4Active Not RecruitingTreatmentDiabetic Macular Edema (DME)2
4Active Not RecruitingTreatmentNeovascular Age-Related Macular Degeneration2
4Active Not RecruitingTreatmentPolypoidal Choroidal Vasculopathy (PCV)1
4Active Not RecruitingTreatmentRetinopathy, Diabetic1
4CompletedBasic ScienceNeovascular Age-Related Macular Degeneration1
4CompletedPreventionDiabetic Macular Edema (DME)1
4CompletedTreatmentAMD (With Persistent or Recurrent Fluid Despite Monthly Intravitreal Anti-VEGF Therapy) / AMD Who Have Persistent or Recurrent Fluid Despite Monthly Intravitreal Anti-VEGF Therapy1
4CompletedTreatmentAge - Related Macular Degeneration (AMD)1
4CompletedTreatmentAge Related Macular Degeneration (ARMD)2
4CompletedTreatmentAge-Related Macular Degeneration (ARMD)2
4CompletedTreatmentAge-Related Macular Degeneration (ARMD) / Wet Age-Related Macular Degeneration1
4CompletedTreatmentAnti Vascular Endothelial Growth Factor / Macular Degeneration1
4CompletedTreatmentBranch Retinal Vein Occlusion / Central Retinal Vein Occlusion (CRVO) / Diabetic Macular Edema (DME) / Retinal Vein Occlusions(RVO)1
4CompletedTreatmentCentral Retinal Vein Occlusion (CRVO)1
4CompletedTreatmentClinically Significant Diabetic Macular Edema1
4CompletedTreatmentCystoid Macular Edema / Diabetic Macular Edema (DME)1
4CompletedTreatmentDiabetic Macular Edema (DME)7
4CompletedTreatmentDiabetic Vitreous Hemorrhage1
4CompletedTreatmentExudative Macular Degeneration1
4CompletedTreatmentMacular Degeneration1
4CompletedTreatmentMacular Edema (ME)2
4CompletedTreatmentMacular Edema With Central Retinal Vein Occlusions1
4CompletedTreatmentNeovascular Age-Related Macular Degeneration2
4CompletedTreatmentNeovascular Age-Related Macular Degeneration / Polypoidal Choroidal Vasculopathy (PCV)1
4CompletedTreatmentNeovascular Age-Related Macular Degeneration / Visual Impairment Due to Neovascular AMD1
4CompletedTreatmentNeovascular Macular Degeneration1
4CompletedTreatmentPolypoidal Choroidal Vasculopathy (PCV)1
4CompletedTreatmentPolypoidal Choroidal Vasculopathy Without Active Polyp1
4CompletedTreatmentRetinal Diseases1
4CompletedTreatmentRetinal Pigment Epithelial Detachment Secondary to Age-related Macular Degeneration1
4CompletedTreatmentSubmacular Vascularized Pigment Epithelial Detachments1
4CompletedTreatmentType 3 Choroidal Neovascularization1
4CompletedTreatmentWet Macular Degeneration2
4Not Yet RecruitingBasic ScienceDiabetic Macular Edema (DME)1
4Not Yet RecruitingTreatmentAge Related Macular Degeneration (ARMD) / Central Serous Chorioretinopathy (CSC) / Idiopathic Poplypoidal Choroidal Vasculopathy / Macular Degeneration1
4Not Yet RecruitingTreatmentBranch Retinal Vein Occlusion With Macular Edema1
4Not Yet RecruitingTreatmentClinically Significant Macular Edema Due to Diabetes Mellitus1
4Not Yet RecruitingTreatmentDiabetic Macular Edema (DME)1
4Not Yet RecruitingTreatmentNeovascular Age-Related Macular Degeneration1
4RecruitingOtherWet Macular Degeneration1
4RecruitingTreatmentAflibercept / Branch Retinal Vein Occlusion / Branch Retinal Vein Occlusion With Macular Edema / Treat and Extend1
4RecruitingTreatmentAge Related Macular Degeneration (ARMD) / Diabetic Macular Edema (DME) / Macular Edema (ME) / Retinal Vein Occlusions(RVO)1
4RecruitingTreatmentAge Related Macular Degeneration (ARMD) / Polypoidal Choroidal Vasculopathy (PCV)1
4RecruitingTreatmentCataracts / Diabetic Macular Edema (DME)1
4RecruitingTreatmentClinically Significant Macular Edema / Diabetic Macular Edema (DME) / Retinopathy, Diabetic1
4RecruitingTreatmentDiabetic Macular Edema (DME)3
4RecruitingTreatmentMacular Degeneration / Wet Macular Degeneration1
4RecruitingTreatmentMacular Diseases1
4RecruitingTreatmentMacular Edema (ME) / Retinopathy, Diabetic1
4RecruitingTreatmentSymtomatic Macular Polypoidal Choroidal Vasculopathy1
4TerminatedTreatmentAge Related Macular Degeneration (ARMD)1
4Unknown StatusTreatmentAge Related Macular Degeneration (ARMD) / Pigment Epithelial Detachment1
4Unknown StatusTreatmentChoroidal Retinal Neovascularization1
4Unknown StatusTreatmentNeovascular Polypoidal Choroidal Vasculopathy1
4Unknown StatusTreatmentRetinal Vein Occlusions(RVO)1
4WithdrawnTreatmentDiabetic Macular Edema (DME)1
4WithdrawnTreatmentFibrovascular Pigment Epithelial Detachment1
4WithdrawnTreatmentVisual Impairment Due to Diabetic Macular Edema2
Not AvailableActive Not RecruitingNot AvailableDiabetic Macular Edema (DME) / NPDR - Non Proliferative Diabetic Retinopathy / Sleep Apnea Syndrome1
Not AvailableActive Not RecruitingNot AvailableMacular Degeneration / Subfoveal Choroidal Neovascularization1
Not AvailableActive Not RecruitingNot AvailableMacular Edema (ME)1
Not AvailableActive Not RecruitingNot AvailablePolypoidal Choroidal Vasculopathy (PCV)1
Not AvailableActive Not RecruitingNot AvailableRetinopathy, Diabetic1
Not AvailableCompletedNot AvailableAMD1
Not AvailableCompletedNot AvailableAge Related Macular Degeneration (ARMD)2
Not AvailableCompletedNot AvailableAge-Related Macular Degeneration (AMD) / Central Retinal Vein Occlusion (CRVO) / Diabetic Macular Edema (DME)1
Not AvailableCompletedNot AvailableAge-Related Macular Degeneration (ARMD)1
Not AvailableCompletedNot AvailableCentral Retinal Vein / Retinal Vein Occlusions(RVO)1
Not AvailableCompletedNot AvailableDiabetic Macular Edema (DME)1
Not AvailableCompletedNot AvailableDiabetic Macular Edema (DME) / Retinopathy, Diabetic1
Not AvailableCompletedNot AvailableEye Diseases1
Not AvailableCompletedNot AvailableMacular Degeneration5
Not AvailableCompletedNot AvailableMacular Edema (ME) / Retinal Vein Occlusions(RVO)1
Not AvailableCompletedNot AvailableNeovascular Age-Related Macular Degeneration1
Not AvailableCompletedNot AvailablePigment Epithelial Detachment1
Not AvailableCompletedNot AvailableRetinal Vein Occlusions(RVO)1
Not AvailableCompletedNot AvailableSubfoveal Choroidal Neovascularization2
Not AvailableCompletedNot AvailableWet Age-Related Macular Degeneration2
Not AvailableCompletedNot AvailableWet Macular Degeneration6
Not AvailableCompletedTreatmentAge Related Macular Degeneration (ARMD) / Branch Retinal Vein Occlusion With Macular Edema / Central Retinal Vein Occlusion With Macular Edema / Diabetic Macular Edema (DME)1
Not AvailableCompletedTreatmentAge-Related Macular Degeneration (ARMD) / Central Retinal Vein Occlusion (CRVO) / Diabetic Macular Edema (DME)1
Not AvailableCompletedTreatmentAge-Related Macular Degeneration (ARMD) / Macular Degeneration1
Not AvailableCompletedTreatmentChoroid Disease / Subfoveal Choroidal Neovascularization1
Not AvailableCompletedTreatmentDiabetic Macular Edema (DME)2
Not AvailableCompletedTreatmentGlaucoma, Neovascular1
Not AvailableCompletedTreatmentPolypoidal Choroidal Vasculopathy (PCV)1
Not AvailableCompletedTreatmentRetinal Diseases1
Not AvailableNo Longer AvailableNot AvailableRetinal Hemangioma1
Not AvailableNot Yet RecruitingNot AvailableMetastatic Colorectal Cancers1
Not AvailableNot Yet RecruitingNot AvailableRetinal Diseases1
Not AvailableNot Yet RecruitingTreatmentTreatment Naive Patients With Polypoidal Choroidal Vasculopathy (PCV) Diagnosis That Would Likely Benefit From Any Insights Gained From This Study1
Not AvailableRecruitingNot AvailableAge Related Macular Degeneration (ARMD)1
Not AvailableRecruitingNot AvailableAge Related Macular Degeneration (ARMD) / Diabetic Macular Edema (DME) / Intravitreal Injections1
Not AvailableRecruitingNot AvailableDiabetic Macular Edema (DME)1
Not AvailableRecruitingNot AvailableMacular Degeneration2
Not AvailableRecruitingNot AvailableMacular Diseases1
Not AvailableRecruitingNot AvailableMacular Edema (ME)1
Not AvailableRecruitingNot AvailableWet Age-Related Macular Degeneration2
Not AvailableRecruitingTreatmentAge Related Macular Degeneration (ARMD)1
Not AvailableRecruitingTreatmentBranch Retinal Vein Occlusion / Macular Edema (ME)1
Not AvailableRecruitingTreatmentDiabetic Macular Edema (DME) / Visual Acuity Improvement With Aflibercept Injection1
Not AvailableRecruitingTreatmentProliferative Diabetic Retinopathy, Pars Plana Vitrectomy, Intravitreal Bevacizumab / Retinopathy, Diabetic1
Not AvailableTerminatedPreventionMacular Degeneration / Retinal Detachment1
Not AvailableWithdrawnTreatmentNeovascular Age-Related Macular Degeneration1
Not AvailableWithdrawnTreatmentPattern Dystrophy of Macula1
Not AvailableWithdrawnTreatmentRecurrent Colon Cancer / Recurrent Rectal Cancer / Stage IVA Colon Cancer / Stage IVA Rectal Cancer / Stage IVB Colon Cancer / Stage IVB Rectal Cancer1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Injection, solutionIntravitreal40 mg/1mL
Injection, solutionIntravitreal40 mg/ml
SolutionIntravitreal40 mg
Injection, solution, concentrateIntravenous25 mg/ml
SolutionIntravenous100 mg
SolutionIntravenous200 mg
Solution, concentrateIntravenous100 mg/4mL
Solution, concentrateIntravenous200 mg/8mL
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US7306799No2007-12-112020-05-23Us
US7531173No2009-05-122026-02-02Us
US7374758No2008-05-202020-05-23Us
US7608261No2009-10-272027-06-14Us
US7070959No2006-07-042020-05-23Us
US7374757No2008-05-202020-05-23Us
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Liquid
Experimental Properties
PropertyValueSource
water solubility>100 mg/mLMSDS

Taxonomy

Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Binder
General Function
Vascular endothelial growth factor receptor binding
Specific Function
Growth factor active in angiogenesis, vasculogenesis and endothelial cell growth. Induces endothelial cell proliferation, promotes cell migration, inhibits apoptosis and induces permeabilization of...
Gene Name
VEGFA
Uniprot ID
P15692
Uniprot Name
Vascular endothelial growth factor A
Molecular Weight
27042.205 Da
References
  1. Browning DJ, Kaiser PK, Rosenfeld PJ, Stewart MW: Aflibercept for age-related macular degeneration: a game-changer or quiet addition? Am J Ophthalmol. 2012 Aug;154(2):222-6. doi: 10.1016/j.ajo.2012.04.020. [PubMed:22813448]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Binder
General Function
Heparin binding
Specific Function
Growth factor active in angiogenesis and endothelial cell growth, stimulating their proliferation and migration. It binds to the receptor FLT1/VEGFR-1. Isoform PlGF-2 binds NRP1/neuropilin-1 and NR...
Gene Name
PGF
Uniprot ID
P49763
Uniprot Name
Placenta growth factor
Molecular Weight
24788.45 Da
References
  1. Browning DJ, Kaiser PK, Rosenfeld PJ, Stewart MW: Aflibercept for age-related macular degeneration: a game-changer or quiet addition? Am J Ophthalmol. 2012 Aug;154(2):222-6. doi: 10.1016/j.ajo.2012.04.020. [PubMed:22813448]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Binder
General Function
Vascular endothelial growth factor receptor 1 binding
Specific Function
Growth factor for endothelial cells. VEGF-B167 binds heparin and neuropilin-1 whereas the binding to neuropilin-1 of VEGF-B186 is regulated by proteolysis.
Gene Name
VEGFB
Uniprot ID
P49765
Uniprot Name
Vascular endothelial growth factor B
Molecular Weight
21601.56 Da
References
  1. Browning DJ, Kaiser PK, Rosenfeld PJ, Stewart MW: Aflibercept for age-related macular degeneration: a game-changer or quiet addition? Am J Ophthalmol. 2012 Aug;154(2):222-6. doi: 10.1016/j.ajo.2012.04.020. [PubMed:22813448]

Drug created on May 24, 2013 15:16 / Updated on November 11, 2019 07:00