ramucirumab 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
human origin	4917	947687-13-0

Description:

Molecule	Description
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

Molecule

Description

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:

None

ADMET properties:

None

Approvals:

Date	Agency	Company
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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Malignant neoplasm progression	296.38	41.12	105	1762	82016	63405139
Ascites	119.90	41.12	45	1822	40683	63446472
Nephrotic syndrome	66.82	41.12	18	1849	5558	63481597
Disease progression	60.18	41.12	40	1827	122718	63364437
Proteinuria	59.33	41.12	22	1845	19123	63468032
Neutropenia	55.98	41.12	44	1823	174961	63312194
Death	51.68	41.12	59	1808	374322	63112833
Gastrointestinal perforation	45.28	41.12	12	1855	3479	63483676
Neutrophil count decreased	41.92	41.12	24	1843	56382	63430773

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Malignant neoplasm progression	420.25	29.79	196	3407	87850	34865478
Febrile neutropenia	101.22	29.79	95	3508	136754	34816574
Interstitial lung disease	89.63	29.79	65	3538	65217	34888111
Neutrophil count decreased	63.59	29.79	48	3555	51056	34902272
Gastric perforation	62.87	29.79	19	3584	2501	34950827
Disease progression	61.20	29.79	65	3538	108012	34845316
Neutropenia	59.90	29.79	77	3526	156701	34796627
Decreased appetite	56.29	29.79	77	3526	166315	34787013
Tumour haemorrhage	55.73	29.79	18	3585	2944	34950384
Proteinuria	51.74	29.79	29	3574	18613	34934715
Neuropathy peripheral	46.94	29.79	50	3553	83213	34870115
Metastases to liver	39.94	29.79	22	3581	13641	34939687
Peritonitis	36.25	29.79	22	3581	16343	34936985
Death	33.38	29.79	103	3500	397946	34555382
Ascites	31.72	29.79	31	3572	46540	34906788

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Malignant neoplasm progression	580.86	30.88	245	4989	135745	79603409
Ascites	136.88	30.88	76	5158	75486	79663668
Disease progression	126.17	30.88	101	5133	184261	79554893
Febrile neutropenia	126.02	30.88	111	5123	230888	79508266
Interstitial lung disease	120.85	30.88	81	5153	112519	79626635
Neutrophil count decreased	109.06	30.88	71	5163	93888	79645266
Neutropenia	107.10	30.88	112	5122	287598	79451556
Proteinuria	106.92	30.88	49	5185	32453	79706701
Tumour haemorrhage	83.85	30.88	24	5210	4120	79735034
Neuropathy peripheral	79.09	30.88	69	5165	141236	79597918
Decreased appetite	78.44	30.88	104	5130	342314	79396840
Gastric perforation	75.53	30.88	22	5212	4015	79735139
Nephrotic syndrome	67.57	30.88	26	5208	11148	79728006
Peritonitis	67.10	30.88	34	5200	28002	79711152
Gastrointestinal perforation	54.66	30.88	19	5215	6118	79733036
Pyogenic granuloma	52.68	30.88	11	5223	504	79738650
Therapy partial responder	47.25	30.88	23	5211	17374	79721780
Glomerular vascular disorder	37.11	30.88	7	5227	189	79738965
Death	36.50	30.88	100	5134	566414	79172740
Haematotoxicity	34.74	30.88	18	5216	15501	79723653
Pneumonitis	34.55	30.88	30	5204	60830	79678324
Epistaxis	32.00	30.88	38	5196	111477	79627677
Tumour perforation	31.78	30.88	7	5227	414	79738740

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01FG02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES VEGF/VEGFR (Vascular Endothelial Growth Factor) inhibitors
FDA MoA	N0000020032	VEGFR2 Inhibitors
FDA EPC	N0000191009	Vascular Endothelial Growth Factor Receptor 2 Antagonist

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

Disease	Relation	SNOMED_ID	DOID
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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN	ANTIBODY BINDING	Kd	10.30		IUPHAR	DRUG LABEL

External reference:

ID	Source
D99YVK4L0X	UNII
D09371	KEGG_DRUG
4033300	VUID
N0000190752	NUI
4033300	VANDF
C2742502	UMLSCUI
CHEMBL1743062	ChEMBL_ID
DB05578	DRUGBANK_ID
9098	INN_ID
C543333	MESH_SUPPLEMENTAL_RECORD_UI
7390	IUPHAR_LIGAND_ID
1535922	RXNORM
219168	MMSL
30265	MMSL
d08252	MMSL
015502	NDDF
704259004	SNOMEDCT_US
704260009	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
CYRAMZA	HUMAN PRESCRIPTION DRUG LABEL	1	0002-7669	SOLUTION	10 mg	INTRAVENOUS	BLA	28 sections
CYRAMZA	HUMAN PRESCRIPTION DRUG LABEL	1	0002-7669	SOLUTION	10 mg	INTRAVENOUS	BLA	28 sections
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
CYRAMZA	HUMAN PRESCRIPTION DRUG LABEL	1	0002-7678	SOLUTION	10 mg	INTRAVENOUS	BLA	28 sections
CYRAMZA	HUMAN PRESCRIPTION DRUG LABEL	1	0002-7678	SOLUTION	10 mg	INTRAVENOUS	BLA	28 sections