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

Stem definition	Drug id	CAS RN
	4233	343306-71-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: sugammadex bridion sugammadex sodium ORG 25969	Sugammadex is a modified gamma cyclodextrin which is a Selective Relaxant Binding Agent. It forms a complex with the neuromuscular blocking agents rocuronium or vecuronium in plasma and thereby reduces the amount of neuromuscular blocking agent available to bind to nicotinic receptors in the neuromuscular junction. This results in the reversal of neuromuscular blockade induced by rocuronium or vecuronium. Molecular weight: 2002.12 Formula: C72H112O48S8 CLOGP: -11.90 LIPINSKI: 3 HAC: 48 HDO: 24 TPSA: 769.76 ALOGS: -1.88 ROTB: 40

Molecule

Description

Molfile Inchi Smiles

Synonyms:

sugammadex
bridion
sugammadex sodium
ORG 25969

Sugammadex is a modified gamma cyclodextrin which is a Selective Relaxant Binding Agent. It forms a complex with the neuromuscular blocking agents rocuronium or vecuronium in plasma and thereby reduces the amount of neuromuscular blocking agent available to bind to nicotinic receptors in the neuromuscular junction. This results in the reversal of neuromuscular blockade induced by rocuronium or vecuronium.

Molecular weight: 2002.12
Formula: C72H112O48S8
CLOGP: -11.90
LIPINSKI: 3
HAC: 48
HDO: 24
TPSA: 769.76
ALOGS: -1.88
ROTB: 40

Drug dosage:

None

ADMET properties:

Property	Value	Reference
Vd (Volume of distribution)	0.18 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	1.28 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	2.53 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
July 25, 2008	EMA	MERCK SHARP & DOHME LIMITED
Dec. 15, 2015	FDA	ORGANON USA INC

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
Recurrence of neuromuscular blockade	178.85	51.37	22	1161	81	50603860
Anaphylactic reaction	158.87	51.37	56	1127	53999	50549942
Bronchospasm	104.49	51.37	30	1153	14824	50589117
Bradycardia	103.37	51.37	43	1140	64383	50539558
Anaphylactic shock	99.65	51.37	31	1152	20124	50583817
Neuromuscular block prolonged	71.02	51.37	12	1171	499	50603442
Clonus	60.72	51.37	15	1168	4160	50599781
Hyperreflexia	57.68	51.37	15	1168	5103	50598838
Maternal exposure during pregnancy	54.39	51.37	38	1145	159740	50444201
Hypoventilation	51.57	51.37	13	1170	3908	50600033

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
Anaphylactic reaction	171.62	69.86	55	946	27518	29546008
Anaphylactic shock	163.55	69.86	45	956	13291	29560235
Recurrence of neuromuscular blockade	147.45	69.86	20	981	118	29573408
Negative pressure pulmonary oedema	137.85	69.86	20	981	203	29573323
Bronchospasm	106.50	69.86	30	971	9579	29563947
Cardiac arrest	99.35	69.86	51	950	85540	29487986
Neuromuscular block prolonged	88.09	69.86	15	986	448	29573078
Bradycardia	81.52	69.86	41	960	65588	29507938
Kounis syndrome	78.67	69.86	17	984	1812	29571714

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
Anaphylactic reaction	292.73	46.96	103	2069	68561	64427999
Recurrence of neuromuscular blockade	230.08	46.96	31	2141	173	64496387
Anaphylactic shock	228.05	46.96	70	2102	30258	64466302
Bradycardia	153.33	46.96	76	2096	118143	64378417
Neuromuscular block prolonged	147.67	46.96	26	2146	951	64495609
Bronchospasm	145.79	46.96	46	2126	21636	64474924
Negative pressure pulmonary oedema	137.49	46.96	20	2152	207	64496353
Cardiac arrest	128.96	46.96	74	2098	153990	64342570
Oxygen saturation decreased	82.90	46.96	49	2123	107127	64389433
Kounis syndrome	80.53	46.96	19	2153	3006	64493554
Hypoventilation	72.17	46.96	20	2152	5986	64490574
Delayed recovery from anaesthesia	59.01	46.96	13	2159	1515	64495045
Hypotension	55.59	46.96	66	2106	380908	64115652
Maternal exposure during pregnancy	51.88	46.96	35	2137	95849	64400711
Clonus	49.70	46.96	15	2157	6052	64490508
Laryngospasm	48.50	46.96	13	2159	3432	64493128
Hyperreflexia	47.27	46.96	15	2157	7133	64489427

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	V03AB35	VARIOUS ALL OTHER THERAPEUTIC PRODUCTS ALL OTHER THERAPEUTIC PRODUCTS Antidotes
FDA CS	M0081434	gamma-Cyclodextrins
CHEBI has role	CHEBI:51372	neuromuscular agent

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

Disease	Relation	SNOMED_ID	DOID
Reversal of neuromuscular blockade	indication	241703000

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.58	acidic
pKa2	7.94	acidic
pKa3	8.0	acidic
pKa4	8.0	acidic
pKa5	8.0	acidic
pKa6	8.0	acidic
pKa7	8.0	acidic
pKa8	8.0	acidic
pKa9	13.29	acidic
pKa10	13.65	acidic
pKa11	13.89	acidic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 200MG BASE/2ML (EQ 100MG BASE/ML)	BRIDION	ORGANON SUB MERCK	N022225	Dec. 15, 2015	RX	SOLUTION	INTRAVENOUS	RE44733	Jan. 27, 2026	REVERSAL OF DRUG-INDUCED NEUROMUSCULAR BLOCK
EQ 500MG BASE/5ML (EQ 100MG BASE/ML)	BRIDION	ORGANON SUB MERCK	N022225	Dec. 15, 2015	RX	SOLUTION	INTRAVENOUS	RE44733	Jan. 27, 2026	REVERSAL OF DRUG-INDUCED NEUROMUSCULAR BLOCK

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 200MG BASE/2ML (EQ 100MG BASE/ML)	BRIDION	ORGANON SUB MERCK	N022225	Dec. 15, 2015	RX	SOLUTION	INTRAVENOUS	June 9, 2023	REVISIONS TO THE USE IN SPECIFIC POPULATIONS SECTION OF THE PACKAGE INSERT TO INCLUDE THE RESULT OF STUDY P146 TO FULFILL THE REQUIREMENTS OF PMR 3003-4
EQ 500MG BASE/5ML (EQ 100MG BASE/ML)	BRIDION	ORGANON SUB MERCK	N022225	Dec. 15, 2015	RX	SOLUTION	INTRAVENOUS	June 9, 2023	REVISIONS TO THE USE IN SPECIFIC POPULATIONS SECTION OF THE PACKAGE INSERT TO INCLUDE THE RESULT OF STUDY P146 TO FULFILL THE REQUIREMENTS OF PMR 3003-4
EQ 200MG BASE/2ML (EQ 100MG BASE/ML)	BRIDION	ORGANON SUB MERCK	N022225	Dec. 15, 2015	RX	SOLUTION	INTRAVENOUS	June 25, 2024	NEW PATIENT POPULATION
EQ 500MG BASE/5ML (EQ 100MG BASE/ML)	BRIDION	ORGANON SUB MERCK	N022225	Dec. 15, 2015	RX	SOLUTION	INTRAVENOUS	June 25, 2024	NEW PATIENT POPULATION

Bioactivity Summary:

None

External reference:

ID	Source
D05940	KEGG_DRUG
343306-79-6	SECONDARY_CAS_RN
4035288	VANDF
C1700695	UMLSCUI
CHEBI:90953	CHEBI
CHEMBL2111107	ChEMBL_ID
CHEMBL2107374	ChEMBL_ID
D000077122	MESH_DESCRIPTOR_UI
DB06206	DRUGBANK_ID
8528	INN_ID
361LPM2T56	UNII
6918584	PUBCHEM_CID
1726987	RXNORM
159483	MMSL
26064	MMSL
31376	MMSL
31381	MMSL
d07361	MMSL
012914	NDDF
012915	NDDF
1172425006	SNOMEDCT_US
442340006	SNOMEDCT_US
442379000	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
BRIDION	HUMAN PRESCRIPTION DRUG LABEL	1	0006-5423	INJECTION, SOLUTION	100 mg	INTRAVENOUS	NDA	29 sections
BRIDION	HUMAN PRESCRIPTION DRUG LABEL	1	0006-5423	INJECTION, SOLUTION	100 mg	INTRAVENOUS	NDA	29 sections
BRIDION	HUMAN PRESCRIPTION DRUG LABEL	1	0006-5425	INJECTION, SOLUTION	100 mg	INTRAVENOUS	NDA	29 sections
BRIDION	HUMAN PRESCRIPTION DRUG LABEL	1	0006-5425	INJECTION, SOLUTION	100 mg	INTRAVENOUS	NDA	29 sections
BRIDION	HUMAN PRESCRIPTION DRUG LABEL	1	71872-7187	INJECTION, SOLUTION	100 mg	INTRAVENOUS	NDA	28 sections