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

Stem definitionDrug idCAS RN
4233 343306-71-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • sugammadex
  • bridion
  • sugammadex sodium
  • ORG 25969
A gamma-cyclodextrin that functions as a reversal agent for the neuromuscular blocker ROCURONIUM BROMIDE.
  • 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:

PropertyValueReference
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:

DateAgencyCompanyOrphan
Dec. 15, 2015 FDA ORGANON USA INC

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
Recurrence of neuromuscular blockade 171.75 51.22 21 972 82 46684987
Anaphylactic reaction 145.71 51.22 51 942 53061 46632008
Bronchospasm 83.52 51.22 25 968 15682 46669387
Bradycardia 76.16 51.22 34 959 66264 46618805
Anaphylactic shock 69.15 51.22 23 970 20251 46664818
Clonus 62.49 51.22 15 978 4065 46681004
Hyperreflexia 58.72 51.22 15 978 5239 46679830
Hypoventilation 52.20 51.22 13 980 4097 46680972

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
Anaphylactic reaction 140.92 64.30 46 838 27936 29923658
Negative pressure pulmonary oedema 132.69 64.30 19 865 203 29951391
Recurrence of neuromuscular blockade 126.57 64.30 17 867 108 29951486
Anaphylactic shock 117.02 64.30 34 850 13959 29937635
Cardiac arrest 84.71 64.30 45 839 92805 29858789
Neuromuscular block prolonged 79.21 64.30 13 871 356 29951238
Bronchospasm 77.02 64.30 23 861 10315 29941279
Kounis syndrome 76.69 64.30 16 868 1657 29949937
Oxygen saturation decreased 66.34 64.30 30 854 43410 29908184

Pharmacologic Action:

SourceCodeDescription
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 (View source of the data)

DiseaseRelationSNOMED_IDDOID
Reversal of neuromuscular blockade indication 241703000

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (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)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
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

Bioactivity Summary:

None

External reference:

IDSource
D05940 KEGG_DRUG
343306-79-6 SECONDARY_CAS_RN
4035288 VANDF
C2699711 UMLSCUI
CHEBI:90952 CHEBI
CHEMBL2107374 ChEMBL_ID
CHEMBL2111107 ChEMBL_ID
D000077122 MESH_DESCRIPTOR_UI
6918584 PUBCHEM_CID
8528 INN_ID
DB06206 DRUGBANK_ID
361LPM2T56 UNII
1726987 RXNORM
159483 MMSL
26064 MMSL
31376 MMSL
31381 MMSL
d07361 MMSL
012914 NDDF
012915 NDDF
442340006 SNOMEDCT_US
442379000 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
BRIDION HUMAN PRESCRIPTION DRUG LABEL 1 0006-5423 INJECTION, SOLUTION 100 mg INTRAVENOUS NDA 28 sections
BRIDION HUMAN PRESCRIPTION DRUG LABEL 1 0006-5425 INJECTION, SOLUTION 100 mg INTRAVENOUS NDA 28 sections
BRIDION HUMAN PRESCRIPTION DRUG LABEL 1 71872-7187 INJECTION, SOLUTION 100 mg INTRAVENOUS NDA 28 sections