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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

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

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 304.29 37.47 46 2009 966 90625426
Bacterial test positive 256.09 37.47 51 2004 5488 90620904
Protein urine present 255.94 37.47 53 2002 6931 90619461
Urinary casts 237.60 37.47 36 2019 766 90625626
Urine leukocyte esterase positive 237.37 37.47 44 2011 3238 90623154
Urine abnormality 210.87 37.47 46 2009 7691 90618701
Urinary sediment present 208.36 37.47 37 2018 2137 90624255
White blood cells urine positive 195.99 37.47 42 2013 6456 90619936
Urinary occult blood positive 183.66 37.47 22 2033 63 90626329
Nitrite urine present 169.41 37.47 28 2027 1051 90625341
Creatinine urine abnormal 165.90 37.47 19 2036 31 90626361
Glomerular filtration rate decreased 151.29 37.47 41 2014 16891 90609501
Red blood cells urine positive 126.95 37.47 26 2029 3199 90623193
Crystal urine present 120.68 37.47 22 2033 1468 90624924
Blood creatinine abnormal 87.34 37.47 20 2035 4137 90622255
Vitamin A decreased 86.22 37.47 12 2043 136 90626256
Creatinine urine decreased 77.35 37.47 12 2043 298 90626094
Platelet count decreased 76.16 37.47 44 2011 136925 90489467
Urine protein/creatinine ratio abnormal 73.41 37.47 9 2046 33 90626359
Glucose urine present 57.95 37.47 11 2044 913 90625479
Urine ketone body present 57.49 37.47 13 2042 2539 90623853
Blood creatinine increased 57.44 37.47 33 2022 101353 90525039
Creatinine urine increased 42.42 37.47 7 2048 259 90626133

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 378.85 44.98 58 1593 759 42618925
Protein urine present 333.62 44.98 70 1581 5731 42613953
Urinary casts 274.16 44.98 41 1610 451 42619233
Urine abnormality 268.70 44.98 50 1601 2189 42617495
Bacterial test positive 236.31 44.98 48 1603 3327 42616357
Glomerular filtration rate decreased 228.62 44.98 63 1588 16288 42603396
Urine protein/creatinine ratio abnormal 219.15 44.98 28 1623 79 42619605
Creatinine urine abnormal 198.83 44.98 22 1629 3 42619681
Urinary occult blood positive 170.80 44.98 23 1628 108 42619576
Urine leukocyte esterase positive 156.70 44.98 25 1626 429 42619255
Urine ketone body present 153.61 44.98 29 1622 1365 42618319
Crystal urine present 141.93 44.98 23 1628 437 42619247
Platelet count decreased 129.64 44.98 75 1576 138506 42481178
White blood cells urine positive 97.80 44.98 20 1631 1421 42618263
Blood creatinine increased 90.73 44.98 55 1596 109948 42509736
Red blood cells urine positive 86.60 44.98 19 1632 1891 42617793
Glucose urine present 64.11 44.98 14 1637 1361 42618323
Aspartate aminotransferase abnormal 63.39 44.98 13 1638 935 42618749
Urinary sediment present 58.20 44.98 10 1641 273 42619411
Urinary casts present 54.96 44.98 6 1645 0 42619684
Nitrite urine present 52.51 44.98 9 1642 242 42619442

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 657.07 34.47 101 3857 1472 110583869
Protein urine present 569.14 34.47 121 3837 11363 110573978
Urinary casts 492.62 34.47 77 3881 1255 110584086
Bacterial test positive 481.54 34.47 99 3859 7878 110577463
Urine abnormality 462.85 34.47 98 3860 8998 110576343
Glomerular filtration rate decreased 373.06 34.47 103 3855 28853 110556488
Creatinine urine abnormal 364.13 34.47 40 3918 6 110585335
Urine leukocyte esterase positive 361.81 34.47 69 3889 3717 110581624
Urinary occult blood positive 333.54 34.47 45 3913 236 110585105
Urine protein/creatinine ratio abnormal 279.73 34.47 37 3921 162 110585179
White blood cells urine positive 275.98 34.47 62 3896 7462 110577879
Urinary sediment present 247.25 34.47 47 3911 2481 110582860
Crystal urine present 245.88 34.47 45 3913 1929 110583412
Nitrite urine present 212.23 34.47 37 3921 1198 110584143
Platelet count decreased 208.45 34.47 119 3839 230324 110355017
Red blood cells urine positive 202.53 34.47 45 3913 5140 110580201
Urine ketone body present 192.91 34.47 41 3917 3805 110581536
Blood creatinine increased 142.85 34.47 86 3872 182803 110402538
Glucose urine present 112.48 34.47 24 3934 2265 110583076
Blood creatinine abnormal 104.32 34.47 27 3931 5865 110579476
Creatinine urine decreased 97.60 34.47 16 3942 354 110584987
Vitamin A decreased 94.91 34.47 14 3944 150 110585191
Aspartate aminotransferase abnormal 67.51 34.47 17 3941 3308 110582033
Prealbumin decreased 62.19 34.47 10 3948 195 110585146
Urinary casts present 59.48 34.47 9 3949 116 110585225
Creatinine urine increased 59.11 34.47 11 3947 515 110584826
Fungal test positive 56.40 34.47 12 3946 1115 110584226
Red blood cell count decreased 51.31 34.47 31 3927 65892 110519449
Pyuria 51.02 34.47 13 3945 2650 110582691
Alanine aminotransferase abnormal 50.17 34.47 17 3941 9317 110576024
Red blood cell burr cells present 44.36 34.47 6 3952 32 110585309
Mean cell volume increased 44.10 34.47 15 3943 8315 110577026
Red cell distribution width increased 39.68 34.47 17 3941 17585 110567756
Urine analysis abnormal 38.80 34.47 13 3945 6884 110578457
Haematocrit decreased 38.75 34.47 26 3932 66091 110519250
Platelet count increased 36.07 34.47 18 3940 26316 110559025
Urine albumin/creatinine ratio abnormal 36.01 34.47 6 3952 147 110585194

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 D016376 Oligonucleotides, Antisense
MeSH PA D020319 Oligodeoxyribonucleotides, 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

Related Drugs by ATC class:

N07XX Other nervous system drugs 23 drugs
amifampridinearimoclomoldeutetrabenazinedextromethorphanedaravoneeplontersenfampridinelaquinimodlevacetylleucineomaveloxolonepatisiranphenylbutanoic acid show all 23 →

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 DISCN SOLUTION SUBCUTANEOUS 9399774 April 29, 2031 TREATMENT OF POLYNEUROPATHY OF HEREDITARY TRANSTHYRETIN AMYLOIDOSIS

Orange Book exclusivity data (new drug applications)

None

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
4037952 VANDF
C4731850 UMLSCUI
CHEBI:757219 CHEBI
CHEMBL4297770 ChEMBL_ID
DB14713 DRUGBANK_ID
CHEMBL4297537 ChEMBL_ID
D10940 KEGG_DRUG
10294 INN_ID
C000629536 MESH_SUPPLEMENTAL_RECORD_UI
13543 IUPHAR_LIGAND_ID
782581008 SNOMEDCT_US
782583006 SNOMEDCT_US
782797001 SNOMEDCT_US
294316 MMSL
35311 MMSL
d09009 MMSL
121493437 PUBCHEM_CID
017681 NDDF
017682 NDDF
2099289 RXNORM

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Tegsedi HUMAN PRESCRIPTION DRUG LABEL 1 61434-031 INJECTION, SOLUTION 284 mg SUBCUTANEOUS Export only 1 sections
Tegsedi HUMAN PRESCRIPTION DRUG LABEL 1 72126-007 INJECTION, SOLUTION 284 mg SUBCUTANEOUS NDA 28 sections