Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMT3D5I)

• Drug Name: Aflibercept Drug Info
• Synonyms: Ziv-Aflibercept; Zaltrap (TN); VEGF Trap; VEGF Trap-Eye

Indication

Disease Entry	ICD 11	Status	REF
Central retinal vein occlusion with macular edema		Approved	[1]
Diabetic macular edema	9B71.02	Approved	[2]
Exudative age-related macular degeneration	9B78.3Z	Approved	[3]
Metastasis from malignant tumor of colon		Approved	[4]
Metastatic colorectal cancer	2B91	Approved	[5]

• Cross-matching ID: TTD Drug ID: DMT3D5I

Molecule-Related Drug Atlas

Drug(s) Targeting Vascular endothelial growth factor A (VEGFA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Brolucizumab	DMW8QNG	Wet age-related macular degeneration	9B78.3Z	Approved	[6]
Faricimab	DM83SEB	Diabetic macular edema	9B71.02	Approved	[7]
Ranibizumab	DMSYPNW	Central retinal vein occlusion with macular edema		Approved	[8]
Bevacizumab	DMSD1UN	Adenocarcinoma	2D40	Approved	[9]
Avastin+/-Tarceva	DMA86FL	Non-small-cell lung cancer	2C25.Y	Phase 3	[10]
PTC299	DMP9TKE	Rheumatoid arthritis	FA20	Phase 2	[11]
RG7221	DM8J9DC	Colorectal cancer	2B91.Z	Phase 2	[12]
RO5520985	DMD3WNP	Colorectal cancer	2B91.Z	Phase 2	[13]
Abicipar pegol	DM59OJ2	Diabetic macular edema	9B71.02	Phase 2	[14]
MP0250	DMR3VCY	Non-small-cell lung cancer	2C25.Y	Phase 1/2	[15]

Drug(s) Targeting Vascular endothelial growth factor B (VEGFB)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CSL346	DMDWJCT	Diabetic kidney disease	GB61.Z	Phase 2	[16]

Drug(s) Targeting Placenta growth factor (PlGF)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
RO-5323441	DMUB3OY	Solid tumour/cancer	2A00-2F9Z	Phase 2	[17]
TB-403	DMDPBMH	Glioblastoma of brain	2A00.00	Phase 2	[18]
SFLT-01	DMD2GKF	Macular degeneration	9B78.3	Phase 1	[19]
R7334	DMVA186	Macular degeneration	9B78.3	Phase 1	[20]
2-Methyl-2,4-Pentanediol	DMD45CU	Discovery agent	N.A.	Investigative	[21]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Placenta growth factor (PlGF)	TT48I1Y	PLGF_HUMAN	Modulator	[5]
Vascular endothelial growth factor A (VEGFA)	TTOHSBA	VEGFA_HUMAN	Modulator	[5]
Vascular endothelial growth factor B (VEGFB)	TTPJQHE	VEGFB_HUMAN	Modulator	[5]

References

• [1] A review of neovascular glaucoma. Etiopathogenesis and treatment. Rom J Ophthalmol. 2021 Oct-Dec;65(4):315-329.
• [2] Aflibercept versus Faricimab in the Treatment of Neovascular Age-Related Macular Degeneration and Diabetic Macular Edema: A Review. Int J Mol Sci. 2022 Aug 20;23(16):9424.
• [3] Efficacy and Safety of Intravitreal Aflibercept Treat-and-Extend Regimens in Exudative Age-Related Macular Degeneration: 52- and 96-Week Findings from ALTAIR : A Randomized Controlled Trial. Adv Ther. 2020 Mar;37(3):1173-1187.
• [4] A Comparison of Folinic Acid, Fluorouracil and Irinotecan (FOLFIRI) plus Bevacizumab and FOLFIRI plus Aflibercept as Second-line Treatment for Metastatic Colorectal Cancer. Clin Oncol (R Coll Radiol). 2022 Aug;34(8):e323-e328.
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [6] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [7] Faricimab: an investigational agent targeting the Tie-2/angiopoietin pathway and VEGF-A for the treatment of retinal diseases. Expert Opin Investig Drugs. 2021 Mar;30(3):193-200.
• [8] Development of ranibizumab, an anti-vascular endothelial growth factor antigen binding fragment, as therapy for neovascular age-related macular degeneration. Retina. 2006 Oct;26(8):859-70.
• [9] FDA Approved Drug Products from FDA Official Website. 2004. Application Number: (ANDA) 125085.
• [10] Clinical pipeline report, company report or official report of Genentech (2009).
• [11] Phase I and pharmacokinetic trial of PTC299 in pediatric patients with refractory or recurrent central nervous system tumors: a PBTC study.J Neurooncol.2015 Jan;121(1):217-24.
• [12] Bispecific antibodies and their applications
• [13] Bispecific antibodies rise again. Nat Rev Drug Discov. 2014 Nov;13(11):799-801.
• [14] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [15] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [16] ClinicalTrials.gov (NCT04419467) A Phase 2a, Double-blind, Randomized, Placebo-controlled, Proof of Concept Study of Vascular Endothelial Growth Factor (VEGF)-B Blockade With the Monoclonal Antibody CSL346 in Subjects With Diabetic Kidney Disease. U.S.National Institutes of Health.
• [17] RO5323441, a humanized monoclonal antibody against the placenta growth factor, blocks PlGF-induced VEGFR-1 phosphorylation in vitro and tumor growth in vivo. Cancer Research. 01/2011.
• [18] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [19] sFLT01: a novel fusion protein with antiangiogenic activity. Mol Cancer Ther. 2011 Mar;10(3):404-15.
• [20] Clinical pipeline report, company report or official report of Roche (2009).
• [21] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.