Identification

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

Aflibercept is a recombinant fusion protein that comprises of two main components: the vascular endothelial growth factor (VEGF) binding portions from the extracellular domains of human VEGF receptors 1 and 2 which is then fused to the Fc portion of human 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
  • VEGF Trap
  • VEGF Trap-Eye
  • Ziv-Aflibercept
External IDs
AVE 0005 / AVE 005 / AVE-0005
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
EyleaSolution40 mgIntravitrealBayer2013-12-23Not applicableCanada
EyleaInjection, solution40 mg/mLIntravitrealRegeneron Pharmaceuticals2011-11-21Not applicableUs
EyleaInjection, solution40 mg/mlIntravitrealBayer Pharma Ag2012-11-22Not applicableEu
EyleaInjection, solution40 mg/mlIntravitrealBayer Pharma Ag2012-11-22Not applicableEu
ZaltrapSolution200 mgIntravenousSanofi Aventis2014-05-08Not applicableCanada
ZaltrapInjection, solution, concentrate25 mg/mlIntravenousSanofi Aventis Groupe2013-02-01Not applicableEu
ZaltrapSolution, concentrate100 mg/4mLIntravenousSanofi Aventis2012-08-03Not applicableUs
ZaltrapInjection, solution, concentrate25 mg/mlIntravenousSanofi Aventis Groupe2013-02-01Not applicableEu
ZaltrapSolution100 mgIntravenousSanofi Aventis2014-05-08Not applicableCanada
ZaltrapInjection, solution, concentrate25 mg/mlIntravenousSanofi Aventis Groupe2013-02-01Not applicableEu
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.

Structured Indications
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
Human
APlacenta growth factor
binder
Human
AVascular endothelial growth factor B
binder
Human
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
DrugInteractionDrug group
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Aflibercept.Approved
AcetyldigoxinAcetyldigoxin may decrease the cardiotoxic activities of Aflibercept.Experimental
BevacizumabBevacizumab may increase the cardiotoxic activities of Aflibercept.Approved, Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Aflibercept.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Aflibercept.Approved, Investigational
CymarinCymarin may decrease the cardiotoxic activities of Aflibercept.Experimental
DeslanosideDeslanoside may decrease the cardiotoxic activities of Aflibercept.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Aflibercept.Approved, Investigational
DigoxinDigoxin may decrease the cardiotoxic activities of Aflibercept.Approved
Digoxin Immune Fab (Ovine)Digoxin Immune Fab (Ovine) may decrease the cardiotoxic activities of Aflibercept.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Aflibercept.Approved, Investigational
GitoformateGitoformate may decrease the cardiotoxic activities of Aflibercept.Experimental
Lanatoside CLanatoside C may decrease the cardiotoxic activities of Aflibercept.Experimental
MetildigoxinMetildigoxin may decrease the cardiotoxic activities of Aflibercept.Experimental
OleandrinOleandrin may decrease the cardiotoxic activities of Aflibercept.Experimental, Investigational
OuabainOuabain may decrease the cardiotoxic activities of Aflibercept.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Aflibercept.Approved, Vet Approved
PeruvosidePeruvoside may decrease the cardiotoxic activities of Aflibercept.Experimental
ProscillaridinProscillaridin may decrease the cardiotoxic activities of Aflibercept.Experimental
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Aflibercept.Approved, Investigational
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
L01XX44 — AfliberceptS01LA05 — 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
1Active Not RecruitingTreatmentMacular Edema (ME) / Radiation Retinopathy1
1Active Not RecruitingTreatmentNeovascular Age-Related Macular Degeneration1
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
1CompletedTreatmentCancers1
1CompletedTreatmentDiabetic Macular Edema (DME)1
1CompletedTreatmentMacular Degeneration1
1CompletedTreatmentMetastatic Biliary Cancers / Metastatic Breast Cancer (MBC) / Metastatic Colorectal Cancers / Metastatic Gastric Cancers / Metastatic Oesophageal Cancers / Pancreatic Cancer Metastatic1
1CompletedTreatmentNeoplasms3
1CompletedTreatmentNeoplasms Malignant1
1CompletedTreatmentNeoplasms Metastasis / Neoplasms, Colorectal1
1CompletedTreatmentNeovascular Age Related Macular Degeneration1
1CompletedTreatmentNon-Hodgkin's Lymphoma (NHL)1
1CompletedTreatmentTumors, Solid1
1CompletedTreatmentUnspecified Childhood Solid Tumor, Protocol Specific1
1RecruitingTreatmentAdult Solid Neoplasm / Metastatic Melanoma / Metastatic Renal Cell Cancer / Recurrent Colorectal Carcinoma / Recurrent Melanoma / Recurrent Ovarian Carcinoma / Renal Cell Carcinoma Recurrent / Stage IV Ovarian Cancer / Stage IVA Colorectal Cancer / Stage IVA Colorectal Cancer AJCC v7 / Stage IVB Colorectal Cancer / Stage IVB Colorectal Cancer AJCC v71
1RecruitingTreatmentAdvanced Malignant Solid Neoplasm / 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 / Solid Neoplasms / Unresectable Solid Neoplasm1
1RecruitingTreatmentMacular Edema (ME) / Retinal Artery Macroaneurysm1
1TerminatedTreatmentCorneal Neovascularization1
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, 2CompletedTreatmentFallopian Tube Cancer / Malignant Tumor of Peritoneum / Recurrent Ovarian Epithelial Cancer1
1, 2CompletedTreatmentMetastatic Colorectal Cancers1
1, 2CompletedTreatmentNeovascular Age-Related Macular Degeneration1
1, 2Not Yet RecruitingTreatmentCorneal Neovascularization1
1, 2RecruitingPreventionRetinopathy, Diabetic1
1, 2RecruitingTreatmentNeovascular Age-Related Macular Degeneration1
1, 2RecruitingTreatmentProliferative Diabetic Retinopathy (PDR)1
1, 2TerminatedTreatmentMetastatic Colorectal Cancers1
1, 2Unknown StatusTreatmentHistoplasmosis retinitis1
2Active Not RecruitingTreatmentAge-Related Macular Degeneration (AMD) / AMD / Eye Diseases / Macular Degeneration / Macular Degeneration, Age-related, 10 / Neovascular Age-Related Macular Degeneration / Retinal Degenerations / Retinal Diseases1
2Active Not RecruitingTreatmentAge-Related Macular Degeneration (ARMD)1
2Active Not RecruitingTreatmentEsophageal Cancers / Malignant Neoplasm of Stomach1
2Active Not RecruitingTreatmentMacular Oedema / Retinitis Pigmentosa (RP)1
2Active Not RecruitingTreatmentMetastatic 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
2Active Not RecruitingTreatmentMucinous Adenocarcinoma of the Colon / Mucinous Adenocarcinoma of the Rectum / Signet Ring Adenocarcinoma of the Colon / Signet Ring Adenocarcinoma of the Rectum / Stage IV Colon Cancer / Stage IV Rectal Cancer1
2Active Not RecruitingTreatmentMultiple Endocrine Neoplasia Type 1 / Pancreatic Neuroendocrine Carcinoma1
2Active Not RecruitingTreatmentProliferative Diabetic Retinopathy (PDR)1
2Active Not RecruitingTreatmentRectal Carcinoma1
2CompletedTreatmentAdult Anaplastic Astrocytoma / Adult Anaplastic Oligodendroglioma / Adult Giant Cell Glioblastoma / Adult Gliosarcoma / Recurrent Adult Brain Tumor1
2CompletedTreatmentCancer of the Ovary / Neoplasms1
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)2
2CompletedTreatmentExtensive Stage Small Cell Lung Cancer / Recurrent 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 Polypoidal Choroidal Vasculopathy1
2CompletedTreatmentMacular Degeneration2
2CompletedTreatmentMetastatic Breast Cancer (MBC) / Recurrent Breast Cancer / Stage IV Breast Cancer1
2CompletedTreatmentMetastatic Colorectal Cancers2
2CompletedTreatmentNeoplasms Metastasis / Neoplasms, Colorectal1
2CompletedTreatmentNeoplasms, Lung / Pulmonary Diseases1
2CompletedTreatmentNeoplasms, Ovarian1
2CompletedTreatmentNeovascular Age-Related Macular Degeneration3
2CompletedTreatmentRectal Carcinoma1
2CompletedTreatmentRecurrent Colon Cancer / Recurrent Rectal Cancer / Stage IV Colon Cancer / Stage IV Rectal Cancer1
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 RecruitingTreatmentAdverse Effect of Radiation Therapy1
2Not Yet RecruitingTreatmentMetastatic Colorectal Cancers / MSI1
2Not Yet RecruitingTreatmentMetastatic Colorectal Cancers1
2Not Yet RecruitingTreatmentProliferative Diabetic Retinopathy (PDR)1
2Not Yet RecruitingTreatmentRadiation Retinopathy1
2RecruitingPreventionAge-Related Macular Degeneration (ARMD)1
2RecruitingTreatmentCarcinoid Tumors1
2RecruitingTreatmentCystoid Macular Edema / Macular Degeneration / Neovascularization / Recurrent Pterygium / Retinal Neovascularization / Retinal Vein Occlusions(RVO) / Retinopathy, Diabetic / Subfoveal Choroidal Neovascularization1
2RecruitingTreatmentIdiopathic Choroidal Neovascularization1
2RecruitingTreatmentInflammatory Choroidal Neovascularization1
2RecruitingTreatmentMetastatic Colorectal Cancers4
2RecruitingTreatmentNeoplasms, Colorectal1
2RecruitingTreatmentPseudoxanthoma Elasticum1
2RecruitingTreatmentRectal Carcinoma / Rectosigmoid Cancer1
2RecruitingTreatmentRetinopathy, Diabetic1
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
2WithdrawnTreatmentLeukemias1
2WithdrawnTreatmentMetastatic Colorectal Cancers1
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, 3CompletedTreatmentAscites / Neoplasms, Ovarian1
2, 3CompletedTreatmentDiabetic Macular Edema (DME)1
2, 3CompletedTreatmentProliferative Diabetic Retinopathy (PDR)1
2, 3RecruitingBasic ScienceAge Related Macular Degeneration (ARMD)1
2, 3RecruitingTreatmentProliferative Diabetic Retinopathy (PDR) / Vitreous Hemorrhage1
2, 3WithdrawnTreatmentHepatic Metastases / KRAS Mutated Colorectal Cancer / Metastatic Colorectal Cancers1
3Active Not RecruitingTreatmentCentral Retinal Vein Occlusion (CRVO)1
3Active Not RecruitingTreatmentMacular Edema (ME)1
3Active Not RecruitingTreatmentNeovascular Age-Related Macular Degeneration2
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)2
3CompletedTreatmentEye Diseases / Macular Degeneration / Retinal Degenerations / Retinal Diseases / Wet Macular Degeneration1
3CompletedTreatmentGlaucoma, Neovascular1
3CompletedTreatmentGlaucoma / Iris Neovascularization1
3CompletedTreatmentMacular Degeneration3
3CompletedTreatmentMacular Edema (ME)2
3CompletedTreatmentMacular Edema Secondary to Central Retinal Vein Occlusion1
3CompletedTreatmentMetastatic Colorectal Cancers2
3CompletedTreatmentNeoplasms Metastasis / Neoplasms, Colorectal1
3CompletedTreatmentNeoplasms Metastasis / Prostatic Neoplasms1
3CompletedTreatmentPathological Myopia1
3CompletedTreatmentRetinal Vein Occlusions(RVO)1
3Not Yet RecruitingTreatmentDiabetic Macular Edema (DME)1
3Not Yet RecruitingTreatmentOcular Melanoma1
3RecruitingPreventionDiabetic Macular Edema (DME) / Retinopathy, Diabetic1
3RecruitingTreatmentDiabetic Macular Edema (DME)1
3RecruitingTreatmentMacular Degeneration1
3TerminatedTreatmentAge-Related Macular Degeneration (ARMD)1
3TerminatedTreatmentNeoplasms, Pancreatic1
4Active Not RecruitingTreatmentAge Related Macular Degeneration (ARMD)1
4Active Not RecruitingTreatmentAge-Related Macular Degeneration (ARMD)1
4Active Not RecruitingTreatmentBranch Retinal Vein Occlusion / Central Retinal Vein Occlusion (CRVO) / Diabetic Macular Edema (DME) / Retinal Vein Occlusions(RVO)1
4Active Not RecruitingTreatmentCentral Retinal Vein Occlusion (CRVO)1
4Active Not RecruitingTreatmentDiabetic Macular Edema (DME)1
4Active Not RecruitingTreatmentMacular Degeneration1
4Active Not RecruitingTreatmentNeovascular Age-Related Macular Degeneration2
4Active Not RecruitingTreatmentNeovascular Macular Degeneration1
4Active Not RecruitingTreatmentWet Macular Degeneration1
4CompletedBasic ScienceNeovascular Age-Related Macular Degeneration1
4CompletedTreatmentAge Related Macular Degeneration (ARMD)1
4CompletedTreatmentAge-Related Macular Degeneration (ARMD)1
4CompletedTreatmentDiabetic Macular Edema (DME)1
4CompletedTreatmentFibrovascular Pigment Epithelial Detachment1
4CompletedTreatmentMacular Edema (ME)1
4CompletedTreatmentMacular Edema With Central Retinal Vein Occlusions1
4CompletedTreatmentNeovascular Age-Related Macular Degeneration1
4CompletedTreatmentNeovascular Age-Related Macular Degeneration / Polypoidal Choroidal Vasculopathy (PCV)1
4CompletedTreatmentPolypoidal Choroidal Vasculopathy (PCV)1
4CompletedTreatmentRetinal Diseases1
4CompletedTreatmentRetinal Pigment Epithelial Detachment Secondary to Age-related Macular Degeneration1
4CompletedTreatmentSubmacular Vascularized Pigment Epithelial Detachments1
4CompletedTreatmentVisual Impairment Due to Neovascular AMD1
4Enrolling by InvitationTreatmentClinically Significant Diabetic Macular Edema1
4Not Yet RecruitingTreatmentAge Related Macular Degeneration (ARMD) / Diabetic Macular Edema (DME) / Macular Edema (ME) / Retinal Vein Occlusions(RVO)1
4Not Yet RecruitingTreatmentCentral Serous Chorioretinopathy (CSC) / Idiopathic Poplypoidal Choroidal Vasculopathy / Macular Degeneration1
4Not Yet RecruitingTreatmentDiabetic Macular Edema (DME)3
4Not Yet RecruitingTreatmentSymtomatic Macular Polypoidal Choroidal Vasculopathy1
4RecruitingOtherWet Macular Degeneration1
4RecruitingTreatmentAge Related Macular Degeneration (ARMD)1
4RecruitingTreatmentAge-Related Macular Degeneration (ARMD)1
4RecruitingTreatmentCentral Retinal Vein Occlusion (CRVO)1
4RecruitingTreatmentDiabetic Macular Edema (DME)4
4RecruitingTreatmentMacular Degeneration / Wet Macular Degeneration1
4RecruitingTreatmentMacular Diseases1
4RecruitingTreatmentMacular Edema (ME) / Retinopathy, Diabetic1
4RecruitingTreatmentRetinopathy, Diabetic1
4RecruitingTreatmentType 3 Choroidal Neovascularization1
4Unknown StatusPreventionDiabetic Macular Edema (DME)1
4Unknown StatusTreatmentAge Related Macular Degeneration (ARMD) / Pigment Epithelial Detachment1
4Unknown StatusTreatmentChoroidal Retinal Neovascularization1
4Unknown StatusTreatmentPolypoidal Choroidal Vasculopathy Without Active Polyp1
4Unknown StatusTreatmentRetinal Vein Occlusions(RVO)1
4Unknown StatusTreatmentWet Macular Degeneration1
4WithdrawnTreatmentVisual Impairment Due to Diabetic Macular Edema2
Not AvailableActive Not RecruitingNot AvailableAge Related Macular Degeneration (ARMD)1
Not AvailableActive Not RecruitingNot AvailableCentral Retinal Vein1
Not AvailableActive Not RecruitingNot AvailableEye Diseases1
Not AvailableActive Not RecruitingNot AvailableMacular Degeneration2
Not AvailableActive Not RecruitingNot AvailablePolypoidal Choroidal Vasculopathy (PCV)1
Not AvailableActive Not RecruitingNot AvailableRetinal Vein Occlusions(RVO)1
Not AvailableActive Not RecruitingNot AvailableRetinopathy, Diabetic1
Not AvailableActive Not RecruitingNot AvailableSubfoveal Choroidal Neovascularization1
Not AvailableActive Not RecruitingNot AvailableWet Macular Degeneration4
Not AvailableActive Not RecruitingTreatmentPolypoidal Choroidal Vasculopathy (PCV)1
Not AvailableCompletedNot AvailableAMD1
Not AvailableCompletedNot AvailableAge Related Macular Degeneration (ARMD)1
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 AvailableMacular Edema (ME) / Retinal Vein Occlusions(RVO)1
Not AvailableCompletedNot AvailableWet Age-Related Macular Degeneration1
Not AvailableCompletedNot AvailableWet Macular Degeneration2
Not AvailableCompletedTreatmentAge-Related Macular Degeneration (ARMD) / Central Retinal Vein Occlusion (CRVO) / Diabetic Macular Edema (DME)1
Not AvailableCompletedTreatmentGlaucoma, Neovascular1
Not AvailableNo Longer AvailableNot AvailableRetinal Hemangioma1
Not AvailableNot Yet RecruitingNot AvailableDiabetic Macular Edema (DME)1
Not AvailableNot Yet RecruitingNot AvailableMacular Edema (ME)1
Not AvailableNot Yet RecruitingNot AvailableWet Age-Related Macular Degeneration1
Not AvailableNot Yet RecruitingTreatmentVisual Acuity Improvement With Aflibercept Injection1
Not AvailableRecruitingNot AvailableAge Related Macular Degeneration (ARMD)1
Not AvailableRecruitingNot AvailableAge Related Macular Degeneration (ARMD) / Intravitreal Injections1
Not AvailableRecruitingNot AvailableMacular Degeneration1
Not AvailableRecruitingNot AvailableMacular Diseases1
Not AvailableRecruitingNot AvailableMacular Edema (ME)1
Not AvailableRecruitingNot AvailableSubfoveal Choroidal Neovascularization1
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/ml
SolutionIntravitreal40 mg
Injection, solution, concentrateIntravenous25 mg/ml
SolutionIntravenous100 mg
SolutionIntravenous200 mg
Solution, concentrateIntravenous100 mg/4mL
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US7306799No2005-03-252020-05-23Us
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

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
Human
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
Human
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
Human
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 19, 2017 20:33