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

Stem definitionDrug idCAS RN
antisense oligonucleotides 5319 1492984-65-2

Description:

MoleculeDescription

Synonyms:

  • inotersen
  • inotersen sodium
  • tegsedi
  • ISIS 420915
Inotersen is an antisense oligonucleotide that causes degradation of mutant and wild-type TTR mRNA through binding to the TTR mRNA, which results in a reduction of serum TTR protein and TTR protein deposits in tissues.
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

DoseUnitRoute
41 mg P

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
July 6, 2018 EMA Akcea Therapeutics Ireland Limited
Oct. 5, 2018 FDA AKCEA THERAPS

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
Urine protein/creatinine ratio increased 365.48 40.47 53 1844 617 63486508
Protein urine present 288.74 40.47 60 1837 6060 63481065
Urinary casts 259.67 40.47 40 1857 715 63486410
Bacterial test positive 250.10 40.47 52 1845 5255 63481870
Urine leukocyte esterase positive 245.84 40.47 48 1849 3531 63483594
Urine abnormality 230.08 40.47 51 1846 6968 63480157
Urinary occult blood positive 208.16 40.47 25 1872 50 63487075
Urinary sediment present 197.70 40.47 37 1860 2166 63484959
White blood cells urine positive 194.14 40.47 42 1855 5116 63482009
Nitrite urine present 168.86 40.47 29 1868 1037 63486088
Glomerular filtration rate decreased 168.28 40.47 45 1852 13396 63473729
Creatinine urine abnormal 160.66 40.47 19 1878 31 63487094
Red blood cells urine positive 137.72 40.47 29 1868 3097 63484028
Crystal urine present 137.13 40.47 26 1871 1628 63485497
Blood creatinine abnormal 98.88 40.47 22 1875 3034 63484091
Urine protein/creatinine ratio abnormal 81.13 40.47 10 1887 27 63487098
Platelet count decreased 71.67 40.47 44 1853 116078 63371047
Vitamin A decreased 67.64 40.47 8 1889 13 63487112
Urine ketone body present 64.65 40.47 15 1882 2488 63484637
Creatinine urine decreased 64.26 40.47 10 1887 190 63486935
Glucose urine present 63.75 40.47 12 1885 720 63486405
Creatinine urine increased 60.38 40.47 10 1887 285 63486840
Blood creatinine increased 50.88 40.47 32 1865 87812 63399313

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
Urine protein/creatinine ratio increased 466.01 40.93 70 1953 512 34954396
Protein urine present 390.67 40.93 84 1939 5144 34949764
Urine abnormality 341.35 40.93 64 1959 1935 34952973
Urinary casts 338.21 40.93 51 1972 382 34954526
Bacterial test positive 301.68 40.93 62 1961 3031 34951877
Urine protein/creatinine ratio abnormal 266.90 40.93 33 1990 32 34954876
Glomerular filtration rate decreased 254.05 40.93 71 1952 12890 34942018
Urinary occult blood positive 225.11 40.93 29 1994 50 34954858
Urine ketone body present 222.91 40.93 41 1982 1107 34953801
Urine leukocyte esterase positive 187.40 40.93 31 1992 440 34954468
Creatinine urine abnormal 184.01 40.93 21 2002 0 34954908
Crystal urine present 158.12 40.93 27 1996 468 34954440
Platelet count decreased 141.68 40.93 87 1936 119630 34835278
White blood cells urine positive 126.38 40.93 26 1997 1266 34953642
Red blood cells urine positive 112.15 40.93 25 1998 1784 34953124
Blood creatinine increased 109.52 40.93 68 1955 94908 34860000
Nitrite urine present 97.81 40.93 15 2008 126 34954782
Glucose urine present 78.67 40.93 17 2006 1048 34953860
Urinary sediment present 73.50 40.93 13 2010 278 34954630
Aspartate aminotransferase abnormal 66.47 40.93 14 2009 763 34954145
Urinary casts present 61.31 40.93 7 2016 0 34954908
Prealbumin decreased 44.18 40.93 7 2016 74 34954834
Glomerulonephritis 43.98 40.93 12 2011 1966 34952942
Mean cell haemoglobin decreased 40.97 40.93 11 2012 1695 34953213

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
Urine protein/creatinine ratio increased 793.19 41.84 121 4034 1113 79739120
Protein urine present 661.32 41.84 143 4012 9969 79730264
Urinary casts 571.39 41.84 91 4064 1128 79739105
Bacterial test positive 535.78 41.84 114 4041 7335 79732898
Urine abnormality 530.22 41.84 115 4040 8104 79732129
Glomerular filtration rate decreased 418.72 41.84 116 4039 22586 79717647
Urinary occult blood positive 404.32 41.84 54 4101 161 79740072
Urine leukocyte esterase positive 389.26 41.84 79 4076 4012 79736221
Creatinine urine abnormal 341.23 41.84 40 4115 16 79740217
Urine protein/creatinine ratio abnormal 324.81 41.84 43 4112 117 79740116
White blood cells urine positive 298.02 41.84 68 4087 6007 79734226
Crystal urine present 273.65 41.84 53 4102 2107 79738126
Urine ketone body present 258.54 41.84 55 4100 3510 79736723
Urinary sediment present 247.25 41.84 50 4105 2485 79737748
Nitrite urine present 244.45 41.84 44 4111 1165 79739068
Red blood cells urine positive 235.05 41.84 54 4101 4909 79735324
Platelet count decreased 216.08 41.84 131 4024 194533 79545700
Blood creatinine increased 155.64 41.84 98 4057 154959 79585274
Blood creatinine abnormal 133.29 41.84 34 4121 4783 79735450
Glucose urine present 132.45 41.84 28 4127 1728 79738505
Vitamin A decreased 92.22 41.84 12 4143 27 79740206
Creatinine urine decreased 89.96 41.84 15 4140 249 79739984
Creatinine urine increased 78.45 41.84 15 4140 554 79739679
Aspartate aminotransferase abnormal 77.00 41.84 18 4137 1758 79738475
Glomerulonephritis 74.56 41.84 20 4135 3413 79736820
Pyuria 71.97 41.84 18 4137 2334 79737899
Urinary casts present 67.97 41.84 10 4145 69 79740164
Prealbumin decreased 67.72 41.84 11 4144 154 79740079
Fungal test positive 57.64 41.84 13 4142 1083 79739150
Mean cell volume increased 54.58 41.84 18 4137 6235 79733998
Urine albumin/creatinine ratio increased 54.05 41.84 11 4144 562 79739671
Alanine aminotransferase abnormal 52.12 41.84 19 4136 8848 79731385
Red blood cell burr cells present 47.01 41.84 7 4148 53 79740180
Mean cell haemoglobin concentration decreased 43.27 41.84 14 4141 4565 79735668
Red blood cell count decreased 42.20 41.84 30 4125 57483 79682750

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N07XX15 NERVOUS SYSTEM
OTHER NERVOUS SYSTEM DRUGS
OTHER NERVOUS SYSTEM DRUGS
Other nervous system drugs
MeSH PA D015335 Molecular Probes
MeSH PA D020319 Oligodeoxyribonucleotides, Antisense
MeSH PA D016376 Oligonucleotides, Antisense
FDA CS M0025055 Oligonucleotides, Antisense
FDA PE N0000008852 Decreased RNA Integrity
FDA PE N0000009531 Increased Protein Breakdown
FDA EPC N0000191626 Antisense Oligonucleotide
FDA EPC N0000193849 Transthyretin-directed RNA Interaction

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

DiseaseRelationSNOMED_IDDOID
Polyneuropathy in amyloidosis indication 193187004
Glomerulonephritis contraindication 36171008 DOID:2921
Thrombocytopenic disorder contraindication 302215000 DOID:1588




🐶 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
EQ 284MG BASE/1.5ML (EQ 189.3MG BASE/ML) TEGSEDI AKCEA THERAPS N211172 Oct. 5, 2018 RX SOLUTION SUBCUTANEOUS 9399774 April 29, 2031 TREATMENT OF POLYNEUROPATHY OF HEREDITARY TRANSTHYRETIN AMYLOIDOSIS

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 284MG BASE/1.5ML (EQ 189.3MG BASE/ML) TEGSEDI AKCEA THERAPS N211172 Oct. 5, 2018 RX SOLUTION SUBCUTANEOUS Oct. 5, 2023 NEW CHEMICAL ENTITY
EQ 284MG BASE/1.5ML (EQ 189.3MG BASE/ML) TEGSEDI AKCEA THERAPS N211172 Oct. 5, 2018 RX SOLUTION SUBCUTANEOUS Oct. 5, 2025 INDICATED FOR THE TREATMENT OF THE POLYNEUROPATHY OF HEREDITARY TRANSTHYRETIN-MEDIATED AMYLOIDOSIS IN ADULTS

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
transthyretin (TTR) mRNA RNA ANTISENSE INHIBITOR UNKNOWN DRUG LABEL

External reference:

IDSource
0IEO0F56LV UNII
1432726-13-0 SECONDARY_CAS_RN
C4731850 UMLSCUI
CHEMBL4297770 ChEMBL_ID
DB14713 DRUGBANK_ID
CHEMBL4297537 ChEMBL_ID
D10940 KEGG_DRUG
10294 INN_ID
017681 NDDF
017682 NDDF
782581008 SNOMEDCT_US
782583006 SNOMEDCT_US
782797001 SNOMEDCT_US
4037952 VANDF
121493436 PUBCHEM_CID
2099289 RXNORM
294316 MMSL
35311 MMSL
d09009 MMSL
C000629536 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Tegsedi HUMAN PRESCRIPTION DRUG LABEL 1 72126-007 INJECTION, SOLUTION 284 mg SUBCUTANEOUS NDA 27 sections
Tegsedi HUMAN PRESCRIPTION DRUG LABEL 1 72126-007 INJECTION, SOLUTION 284 mg SUBCUTANEOUS NDA 27 sections
Tegsedi HUMAN PRESCRIPTION DRUG LABEL 1 72126-007 INJECTION, SOLUTION 284 mg SUBCUTANEOUS NDA 27 sections