ramucirumab 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
human origin 4917 947687-13-0

Description:

MoleculeDescription

Synonyms:

  • ramucirumab
  • cyramza
  • IMC-1121B
Ramucirumab is a vascular endothelial growth factor receptor 2 antagonist that specifically binds VEGF Receptor 2 and blocks binding of VEGFR ligands, VEGF-A, VEGF-C, and VEGF-D. As a result, ramucirumab inhibits ligand-stimulated activation of VEGF Receptor 2, thereby inhibiting ligand-induced proliferation, and migration of human endothelial cells. Ramucirumab inhibited angiogenesis in an in vivo animal model.
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

DoseUnitRoute
40 mg P

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

DateAgencyCompanyOrphan
March 26, 2015 PMDA Eli Lilly Japan K.K.
Dec. 19, 2014 EMA Eli Lilly Nederland B.V.
April 21, 2014 FDA ELI LILLY AND CO

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Malignant neoplasm progression 378.63 38.74 132 2322 106738 90519255
Ascites 138.23 38.74 51 2403 47689 90578304
Disease progression 111.95 38.74 63 2391 156552 90469441
Nephrotic syndrome 101.06 38.74 26 2428 7313 90618680
Neutropenia 88.61 38.74 62 2392 224842 90401151
Proteinuria 71.46 38.74 26 2428 23265 90602728
Death 60.93 38.74 68 2386 456483 90169510
Neuropathy peripheral 59.11 38.74 40 2414 136930 90489063
Haemoptysis 55.75 38.74 24 2430 33296 90592697
Neutrophil count decreased 54.30 38.74 30 2424 71502 90554491
Chylothorax 50.49 38.74 9 2445 440 90625553
Gastrointestinal perforation 48.36 38.74 13 2441 4319 90621674
Pyogenic granuloma 46.47 38.74 8 2446 319 90625674
Anaemia 39.35 38.74 48 2406 352754 90273239

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Malignant neoplasm progression 511.00 28.72 243 4372 108157 42508563
Disease progression 104.30 28.72 101 4514 143555 42473165
Interstitial lung disease 103.96 28.72 78 4537 78384 42538336
Febrile neutropenia 91.12 28.72 106 4509 185597 42431123
Neutrophil count decreased 77.24 28.72 60 4555 63355 42553365
Neutropenia 77.10 28.72 101 4514 199330 42417390
Decreased appetite 73.38 28.72 97 4518 193040 42423680
Gastric perforation 66.29 28.72 21 4594 3072 42613648
Tumour haemorrhage 62.94 28.72 21 4594 3617 42613103
Proteinuria 60.13 28.72 35 4580 22948 42593772
Neuropathy peripheral 59.87 28.72 64 4551 101789 42514931
Ascites 59.13 28.72 49 4566 56629 42560091
Metastases to liver 51.19 28.72 28 4587 16298 42600422
Fulminant type 1 diabetes mellitus 45.28 28.72 13 4602 1361 42615359
Pneumonitis 39.24 28.72 34 4581 41684 42575036
Peritonitis 37.50 28.72 24 4591 18609 42598111
Death 34.18 28.72 120 4495 471065 42145655
Therapy partial responder 31.19 28.72 22 4593 19999 42596721
Recall phenomenon 30.37 28.72 8 4607 608 42616112
Nephrotic syndrome 30.25 28.72 16 4599 8702 42608018
Stomatitis 30.17 28.72 32 4583 50297 42566423
Metastases to lung 28.81 28.72 17 4598 11407 42605313

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Malignant neoplasm progression 776.64 30.09 318 6498 174249 110408234
Disease progression 244.50 30.09 164 6652 243870 110338613
Ascites 186.77 30.09 98 6718 92710 110489773
Neutropenia 160.67 30.09 153 6663 374467 110208016
Interstitial lung disease 152.23 30.09 99 6717 139235 110443248
Neutrophil count decreased 137.17 30.09 88 6728 120853 110461630
Febrile neutropenia 129.31 30.09 126 6690 316641 110265842
Proteinuria 127.84 30.09 58 6758 39960 110542523
Neuropathy peripheral 116.66 30.09 93 6723 179184 110403299
Nephrotic syndrome 107.25 30.09 38 6778 13793 110568690
Tumour haemorrhage 101.78 30.09 29 6787 5216 110577267
Decreased appetite 96.67 30.09 132 6684 475714 110106769
Gastric perforation 81.21 30.09 24 6792 4905 110577578
Pyogenic granuloma 70.56 30.09 14 6802 529 110581954
Peritonitis 67.10 30.09 35 6781 32572 110549911
Therapy partial responder 65.64 30.09 36 6780 37025 110545458
Gastrointestinal perforation 55.95 30.09 20 6796 7436 110575047
Death 52.83 30.09 126 6690 698743 109883740
Polyneuropathy 50.97 30.09 29 6787 31983 110550500
Pneumonitis 50.32 30.09 40 6776 76491 110505992
Fulminant type 1 diabetes mellitus 50.08 30.09 14 6802 2349 110580134
Chylothorax 49.60 30.09 12 6804 1144 110581339
Metastases to liver 43.16 30.09 27 6789 35359 110547124
Epistaxis 38.95 30.09 44 6772 130328 110452155
Metastases to peritoneum 38.17 30.09 14 6802 5596 110576887
Haemoptysis 37.97 30.09 33 6783 71321 110511162
Glomerular vascular disorder 36.22 30.09 7 6809 230 110582253
Haematotoxicity 36.00 30.09 20 6796 21062 110561421
Anaemia 32.31 30.09 90 6726 546996 110035487
Peripheral sensory neuropathy 31.74 30.09 17 6799 16663 110565820
Neoplasm progression 30.64 30.09 28 6788 64567 110517916

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01FG02 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES
VEGF/VEGFR (Vascular Endothelial Growth Factor / -Receptor) inhibitors
FDA MoA N0000020032 VEGFR2 Inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D006131 Growth Inhibitors
MeSH PA D006133 Growth Substances
MeSH PA D020533 Angiogenesis Inhibitors
FDA EPC N0000191009 Vascular Endothelial Growth Factor Receptor 2 Antagonist
CHEBI has role CHEBI:35610 antineoplastic agent

Related Drugs by ATC class:

L01FG VEGF/VEGFR (Vascular Endothelial Growth Factor / -Receptor) inhibitors 1 drug
bevacizumab

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Liver cell carcinoma indication 109841003 DOID:684
Non-small cell lung cancer indication 254637007 DOID:3908
Malignant tumor of stomach indication 363349007 DOID:10534
Adenocarcinoma of stomach indication 408647009 DOID:3717
Malignant neoplasm of colon and/or rectum indication 781382000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Vascular endothelial growth factor receptor 2 Kinase ANTIBODY BINDING Kd 10.30 IUPHAR DRUG LABEL

External reference:

IDSource
D99YVK4L0X UNII
D09371 KEGG_DRUG
4033300 VUID
N0000190752 NUI
4033300 VANDF
C2742502 UMLSCUI
CHEBI:750139 CHEBI
CHEMBL1743062 ChEMBL_ID
DB05578 DRUGBANK_ID
D000096662 MESH_DESCRIPTOR_UI
9098 INN_ID
7390 IUPHAR_LIGAND_ID
1535922 RXNORM
219168 MMSL
30265 MMSL
d08252 MMSL
015502 NDDF
704259004 SNOMEDCT_US
704260009 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
CYRAMZA HUMAN PRESCRIPTION DRUG LABEL 1 0002-7669 SOLUTION 10 mg INTRAVENOUS BLA 28 sections
CYRAMZA HUMAN PRESCRIPTION DRUG LABEL 1 0002-7678 SOLUTION 10 mg INTRAVENOUS BLA 28 sections