perflutren 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
perfluorinated compounds used as blood substitutes and/or diagnostic agents 2104 76-19-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • luminity
  • perflutren
  • octafluoropropane
  • perfluoropropane
Perflutren lipid microspheres exhibit lower acoustic impedance than blood and enhance the intrinsic backscatter of blood. These physical acoustic properties of activated perflutren provide contrast enhancement of the left ventricular chamber and aid delineation of the left ventricular endocardial border during echocardiography.
  • Molecular weight: 188.02
  • Formula: C3F8
  • CLOGP: 2.85
  • LIPINSKI: 0
  • HAC: 0
  • HDO: 0
  • TPSA:
  • ALOGS: -3.11
  • ROTB: 2

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 1.60 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 590.71 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 0.02 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,ACVRL1,AKT2,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,IKBKB,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIK3CG,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 55
kinase-selectivity-class AXL,GRK2,PDK1,PDK2,PIK3CD,PIK3CG 6
pfas-class PFAS structural alert (1 = True, 0 = False) 1

Approvals:

DateAgencyCompanyOrphan
July 31, 2001 FDA LANTHEUS MEDCL

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
Back pain 1090.28 54.33 383 2195 316792 90309077
Muscle spasms 213.67 54.33 115 2463 251768 90374101
Flushing 200.41 54.33 80 2498 88411 90537458
Dyspnoea 155.86 54.33 155 2423 880800 89745069
Contrast media reaction 113.11 54.33 21 2557 1230 90624639
Neck pain 110.22 54.33 57 2521 113906 90511963
Chest pain 106.26 54.33 81 2497 319564 90306305
Pain in extremity 71.09 54.33 75 2503 450454 90175415

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
Back pain 921.40 60.90 312 1679 141464 42477880
Muscle spasms 284.71 60.90 117 1874 85927 42533417
Flushing 117.15 60.90 49 1942 36979 42582365
Urticaria 109.75 60.90 58 1933 73978 42545366
Neck pain 99.20 60.90 41 1950 29973 42589371
Anaphylactic reaction 97.65 60.90 45 1946 42698 42576646
Contrast media reaction 81.51 60.90 17 1974 1099 42618245
Pain in extremity 76.35 60.90 60 1931 150544 42468800

FDA Adverse Event Reporting System (Geriatric)

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
Back pain 1813.18 59.44 634 3749 370362 110214554
Muscle spasms 466.89 59.44 224 4159 277933 110306983
Flushing 303.03 59.44 124 4259 104612 110480304
Contrast media reaction 183.93 59.44 37 4346 2361 110582555
Neck pain 175.10 59.44 89 4294 123041 110461875
Dyspnoea 164.33 59.44 209 4174 1106663 109478253
Pain in extremity 130.98 59.44 126 4257 486992 110097924
Chest pain 117.73 59.44 106 4277 376269 110208647
Anaphylactic reaction 115.77 59.44 66 4317 114234 110470682
Flank pain 100.89 59.44 37 4346 23093 110561823
Urticaria 98.04 59.44 89 4294 318768 110266148
Unresponsive to stimuli 93.12 59.44 47 4336 63743 110521173

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC V08DA01 VARIOUS
CONTRAST MEDIA
ULTRASOUND CONTRAST MEDIA
Ultrasound contrast media
ATC V08DA04 VARIOUS
CONTRAST MEDIA
ULTRASOUND CONTRAST MEDIA
Ultrasound contrast media
FDA MoA N0000010259 Ultrasound Contrast Activity
MeSH PA D003287 Contrast Media
MeSH PA D064907 Diagnostic Uses of Chemicals
FDA EPC N0000175864 Contrast Agent for Ultrasound Imaging
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:35610 antineoplastic agent

Related Drugs by ATC class:

V08DA Ultrasound contrast media 4 drugs

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

DiseaseRelationSNOMED_IDDOID
Echocardiography indication 40701008




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
13.04MG/2ML (6.52MG/ML) DEFINITY LANTHEUS MEDCL N021064 July 31, 2001 RX INJECTABLE INTRAVENOUS 10583207 Dec. 28, 2035 METHOD OF USING THE DRUG SUBSTANCE/DRUG PRODUCT FOR ULTRASOUND IMAGING
13.04MG/2ML (6.52MG/ML) DEFINITY RT LANTHEUS MEDCL N021064 Nov. 17, 2020 RX INJECTABLE INTRAVENOUS 10583207 Dec. 28, 2035 METHOD OF USING THE DRUG SUBSTANCE/DRUG PRODUCT FOR ULTRASOUND IMAGING
13.04MG/2ML (6.52MG/ML) DEFINITY RT LANTHEUS MEDCL N021064 Nov. 17, 2020 RX INJECTABLE INTRAVENOUS 11395856 Dec. 28, 2035 METHOD OF USING THE DRUG SUBSTANCE/DRUG PRODUCT FOR ULTRASOUND IMAGING
13.04MG/2ML (6.52MG/ML) DEFINITY LANTHEUS MEDCL N021064 July 31, 2001 RX INJECTABLE INTRAVENOUS 10583208 March 16, 2037 METHOD OF USING THE DRUG SUBSTANCE/DRUG PRODUCT FOR ULTRASOUND IMAGING
13.04MG/2ML (6.52MG/ML) DEFINITY RT LANTHEUS MEDCL N021064 Nov. 17, 2020 RX INJECTABLE INTRAVENOUS 10583208 March 16, 2037 METHOD OF USING THE DRUG SUBSTANCE/DRUG PRODUCT FOR ULTRASOUND IMAGING
13.04MG/2ML (6.52MG/ML) DEFINITY LANTHEUS MEDCL N021064 July 31, 2001 RX INJECTABLE INTRAVENOUS 11266750 March 16, 2037 METHOD OF USING THE DRUG SUBSTANCE/DRUG PRODUCT FOR ULTRASOUND IMAGING
13.04MG/2ML (6.52MG/ML) DEFINITY RT LANTHEUS MEDCL N021064 Nov. 17, 2020 RX INJECTABLE INTRAVENOUS 11266750 March 16, 2037 METHOD OF USING THE DRUG SUBSTANCE/DRUG PRODUCT FOR ULTRASOUND IMAGING
13.04MG/2ML (6.52MG/ML) DEFINITY LANTHEUS MEDCL N021064 July 31, 2001 RX INJECTABLE INTRAVENOUS 11529431 March 16, 2037 METHOD OF USING THE DRUG SUBSTANCE/DRUG PRODUCT FOR ULTRASOUND IMAGING
13.04MG/2ML (6.52MG/ML) DEFINITY RT LANTHEUS MEDCL N021064 Nov. 17, 2020 RX INJECTABLE INTRAVENOUS 11529431 March 16, 2037 METHOD OF USING THE DRUG SUBSTANCE/DRUG PRODUCT FOR ULTRASOUND IMAGING
13.04MG/2ML (6.52MG/ML) DEFINITY LANTHEUS MEDCL N021064 July 31, 2001 RX INJECTABLE INTRAVENOUS 11857646 March 16, 2037 METHOD OF USING THE DRUG SUBSTANCE/DRUG PRODUCT FOR ULTRASOUND IMAGING
13.04MG/2ML (6.52MG/ML) DEFINITY RT LANTHEUS MEDCL N021064 Nov. 17, 2020 RX INJECTABLE INTRAVENOUS 11857646 March 16, 2037 METHOD OF USING THE DRUG SUBSTANCE/DRUG PRODUCT FOR ULTRASOUND IMAGING
13.04MG/2ML (6.52MG/ML) DEFINITY LANTHEUS MEDCL N021064 July 31, 2001 RX INJECTABLE INTRAVENOUS 11925695 March 16, 2037 METHOD OF USING THE DRUG SUBSTANCE/DRUG PRODUCT FOR ULTRASOUND IMAGING
13.04MG/2ML (6.52MG/ML) DEFINITY RT LANTHEUS MEDCL N021064 Nov. 17, 2020 RX INJECTABLE INTRAVENOUS 11925695 March 16, 2037 METHOD OF USING THE DRUG SUBSTANCE/DRUG PRODUCT FOR ULTRASOUND IMAGING
13.04MG/2ML (6.52MG/ML) DEFINITY LANTHEUS MEDCL N021064 July 31, 2001 RX INJECTABLE INTRAVENOUS 12161730 March 16, 2037 METHOD OF USING THE DRUG SUBSTANCE/DRUG PRODUCT FOR ULTRASOUND IMAGING
13.04MG/2ML (6.52MG/ML) DEFINITY RT LANTHEUS MEDCL N021064 Nov. 17, 2020 RX INJECTABLE INTRAVENOUS 12161730 March 16, 2037 METHOD OF USING THE DRUG SUBSTANCE/DRUG PRODUCT FOR ULTRASOUND IMAGING
13.04MG/2ML (6.52MG/ML) DEFINITY LANTHEUS MEDCL N021064 July 31, 2001 RX INJECTABLE INTRAVENOUS 9789210 March 16, 2037 METHOD OF USING THE DRUG SUBSTANCE/DRUG PRODUCT FOR ULTRASOUND IMAGING
13.04MG/2ML (6.52MG/ML) DEFINITY RT LANTHEUS MEDCL N021064 Nov. 17, 2020 RX INJECTABLE INTRAVENOUS 9789210 March 16, 2037 METHOD OF USING THE DRUG SUBSTANCE/DRUG PRODUCT FOR ULTRASOUND IMAGING
13.04MG/2ML (6.52MG/ML) DEFINITY LANTHEUS MEDCL N021064 July 31, 2001 RX INJECTABLE INTRAVENOUS 10588988 May 4, 2037 METHOD OF USING THE DRUG SUBSTANCE/DRUG PRODUCT FOR ULTRASOUND IMAGING
13.04MG/2ML (6.52MG/ML) DEFINITY RT LANTHEUS MEDCL N021064 Nov. 17, 2020 RX INJECTABLE INTRAVENOUS 10588988 May 4, 2037 METHOD OF USING THE DRUG SUBSTANCE/DRUG PRODUCT FOR ULTRASOUND IMAGING

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
4024282 VUID
N0000148772 NUI
D01738 KEGG_DRUG
4021302 VANDF
4021353 VANDF
4024282 VANDF
C0937858 UMLSCUI
CHEBI:31980 CHEBI
CHEMBL1663 ChEMBL_ID
DB00556 DRUGBANK_ID
6432 PUBCHEM_CID
C042852 MESH_SUPPLEMENTAL_RECORD_UI
7932 INN_ID
CK0N3WH0SR UNII
283753 RXNORM
16500 MMSL
d04796 MMSL
009302 NDDF
409291008 SNOMEDCT_US
409292001 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
OptisonPerflutren Protein-Type A Microspheres HUMAN PRESCRIPTION DRUG LABEL 2 0407-2707 INJECTION, SOLUTION 0.22 mg INTRAVENOUS NDA 28 sections
Definity HUMAN PRESCRIPTION DRUG LABEL 1 11994-011 INJECTION, SUSPENSION 6.52 mg INTRAVENOUS NDA 28 sections
DEFINITY RT HUMAN PRESCRIPTION DRUG LABEL 1 11994-017 INJECTION, SUSPENSION 6.52 mg INTRAVENOUS NDA 28 sections