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	212.57	46.90	26	1316	88	56290637
Anaphylactic reaction	175.53	46.90	62	1280	58933	56231792
Bronchospasm	124.73	46.90	35	1307	15634	56275091
Bradycardia	124.31	46.90	50	1292	67454	56223271
Anaphylactic shock	121.94	46.90	37	1305	21703	56269022
Neuromuscular block prolonged	91.66	46.90	15	1327	502	56290223
Hypoventilation	64.67	46.90	16	1326	4376	56286349
Clonus	60.15	46.90	15	1327	4234	56286491
Hyperreflexia	57.00	46.90	15	1327	5235	56285490
Cardiac arrest	52.74	46.90	30	1312	86284	56204441
Maternal exposure during pregnancy	47.86	46.90	38	1304	189515	56101210
Muscle twitching	47.79	46.90	17	1325	16225	56274500

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	201.10	75.65	64	1076	29489	31666715
Recurrence of neuromuscular blockade	189.34	75.65	26	1114	159	31696045
Anaphylactic shock	180.99	75.65	50	1090	14095	31682109
Bronchospasm	140.18	75.65	38	1102	9934	31686270
Negative pressure pulmonary oedema	136.62	75.65	20	1120	203	31696001
Cardiac arrest	114.53	75.65	58	1082	89004	31607200
Bradycardia	94.39	75.65	47	1093	69280	31626924
Neuromuscular block prolonged	87.17	75.65	15	1125	448	31695756
Kounis syndrome	86.41	75.65	19	1121	2065	31694139
Oxygen saturation decreased	77.87	75.65	37	1103	49078	31647126

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	330.06	45.08	116	2339	74858	70851131
Recurrence of neuromuscular blockade	303.05	45.08	41	2414	230	70925759
Anaphylactic shock	272.20	45.08	82	2373	32408	70893581
Bronchospasm	184.11	45.08	56	2399	22736	70903253
Bradycardia	180.09	45.08	87	2368	124528	70801461
Neuromuscular block prolonged	166.90	45.08	29	2426	954	70925035
Cardiac arrest	148.56	45.08	83	2372	159751	70766238
Negative pressure pulmonary oedema	136.93	45.08	20	2435	207	70925782
Kounis syndrome	98.48	45.08	23	2432	3388	70922601
Oxygen saturation decreased	93.31	45.08	55	2400	116374	70809615
Hypoventilation	92.81	45.08	25	2430	6557	70919432
Hypotension	58.96	45.08	71	2384	404310	70521679
Delayed recovery from anaesthesia	58.40	45.08	13	2442	1544	70924445
Laryngospasm	56.85	45.08	15	2440	3628	70922361
Clonus	48.80	45.08	15	2440	6253	70919736
Respiratory arrest	47.13	45.08	27	2428	53906	70872083
Hyperreflexia	46.27	45.08	15	2440	7427	70918562
Maternal exposure during pregnancy	45.17	45.08	35	2420	115310	70810679

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
4035288	VANDF
C1700695	UMLSCUI
CHEBI:90953	CHEBI
CHEMBL2111107	ChEMBL_ID
CHEMBL2107374	ChEMBL_ID
D000077122	MESH_DESCRIPTOR_UI
DB06206	DRUGBANK_ID
8528	INN_ID
343306-79-6	SECONDARY_CAS_RN
361LPM2T56	UNII
6918585	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