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

Stem definition	Drug id	CAS RN
primate origin	5454	2423948-94-9

Description:

Molecule	Description
Molfile Synonyms: etesevimab LY-CoV016 LY3832479 JS016 CB6 NP005	FDA issued an Emergency Use Authorization (EUA) for etesevimab and bamlanivimab on February 9, 2021 that permits combined use of the drugs for the treatment of mild to moderate COVID-19. The EUA of bamlanivimab ALONE was revoked by FDA but the use of bamlanivimab in a combined regimen with etesevimab remains unchanged. Etesevimab is a recombinant neutralizing human IgG1kappa mAb to the spike protein of SARS-CoV-2, with amino acid substitutions in the Fc region (L234A, L235A) to reduce effector function. Etesevimab binds the spike protein and blocks spike protein attachment to the human ACE2 receptor with an IC50value of 0.32 nM (0.046 μg/mL). Bamlanivimab and etesevimab bind to different but overlapping epitopes in the receptor binding domain (RBD) of the S-protein. Using both antibodies together is expected to reduce the risk of viral resistance. Molecular weight: Formula: CLOGP: LIPINSKI: None HAC: None HDO: None TPSA: ALOGS: ROTB: None

Molecule

Description

Molfile

Synonyms:

etesevimab
LY-CoV016
LY3832479
JS016
CB6
NP005

FDA issued an Emergency Use Authorization (EUA) for etesevimab and bamlanivimab on February 9, 2021 that permits combined use of the drugs for the treatment of mild to moderate COVID-19. The EUA of bamlanivimab ALONE was revoked by FDA but the use of bamlanivimab in a combined regimen with etesevimab remains unchanged. Etesevimab is a recombinant neutralizing human IgG1kappa mAb to the spike protein of SARS-CoV-2, with amino acid substitutions in the Fc region (L234A, L235A) to reduce effector function. Etesevimab binds the spike protein and blocks spike protein attachment to the human ACE2 receptor with an IC50value of 0.32 nM (0.046 μg/mL). Bamlanivimab and etesevimab bind to different but overlapping epitopes in the receptor binding domain (RBD) of the S-protein. Using both antibodies together is expected to reduce the risk of viral resistance.

Molecular weight:
Formula:
CLOGP:
LIPINSKI: None
HAC: None
HDO: None
TPSA:
ALOGS:
ROTB: None

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Nov. 9, 2020	FDA	Eli Lilly and Company

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
Infusion related reaction	461.51	55.79	183	1348	245338	63242153
Flushing	269.93	55.79	91	1440	74996	63412495
Dyspnoea	198.99	55.79	146	1385	661167	62826324
Chest discomfort	197.19	55.79	80	1451	109889	63377602
COVID-19 pneumonia	100.33	55.79	29	1502	14180	63473311
Oxygen saturation decreased	59.79	55.79	33	1498	88552	63398939

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
Infusion related reaction	261.40	50.50	79	670	52978	34903204
COVID-19 pneumonia	188.30	50.50	48	701	16919	34939263
Flushing	84.24	50.50	30	719	32390	34923792

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
Infusion related reaction	703.14	53.46	258	2077	229979	79512074
Flushing	361.77	53.46	124	2211	88144	79653909
COVID-19 pneumonia	263.50	53.46	75	2260	28774	79713279
Chest discomfort	223.64	53.46	99	2236	137945	79604108
Dyspnoea	215.34	53.46	185	2150	856840	78885213
Oxygen saturation decreased	99.34	53.46	56	2279	128991	79613062
Back pain	84.03	53.46	70	2265	304110	79437943
Acute respiratory failure	66.00	53.46	33	2302	59508	79682545
Chest pain	61.84	53.46	57	2278	282247	79459806
Hyperhidrosis	61.73	53.46	44	2291	151448	79590605

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

None

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

Disease	Relation	SNOMED_ID	DOID
COVID-19	indication	840539006

🐶 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
Spike glycoprotein	Glycoprotein		SPIKE_SARS2		Kd	8.19		DRUG LABEL	DRUG LABEL

External reference:

ID	Source
D11944	KEGG_DRUG
N7Q9NLF11I	UNII
C5421804	UMLSCUI
CHEMBL4650488	ChEMBL_ID
DB15897	DRUGBANK_ID
11331	IUPHAR_LIGAND_ID
018633	NDDF
4040109	VANDF
44468170	PUBCHEM_CID
2477854	RXNORM
343519	MMSL
39314	MMSL
d09712	MMSL
C000711968	MESH_SUPPLEMENTAL_RECORD_UI
11873	INN_ID

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Etesevimab	HUMAN PRESCRIPTION DRUG LABEL	1	0002-7950	INJECTION, SOLUTION	35 mg	INTRAVENOUS	Emergency Use Authorization	29 sections
Etesevimab	HUMAN PRESCRIPTION DRUG LABEL	1	0002-7950	INJECTION, SOLUTION	35 mg	INTRAVENOUS	Emergency Use Authorization	29 sections