Stem definition | Drug id | CAS RN |
---|---|---|
antisense oligonucleotides | 5319 | 1492984-65-2 |
Molecule | Description |
---|---|
Synonyms:
|
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.
|
Dose | Unit | Route |
---|---|---|
41 | mg | P |
None
Date | Agency | Company | Orphan |
---|---|---|---|
July 6, 2018 | EMA | Akcea Therapeutics Ireland Limited | |
Oct. 5, 2018 | FDA | AKCEA THERAPS |
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 |
---|---|---|---|---|---|---|
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 |
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 |
---|---|---|---|---|---|---|
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 |
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 |
---|---|---|---|---|---|---|
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 |
None
Source | Code | Description |
---|---|---|
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 |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Polyneuropathy in amyloidosis | indication | 193187004 | |
Glomerulonephritis | contraindication | 36171008 | DOID:2921 |
Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
None
None
None
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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 |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
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 |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
transthyretin (TTR) mRNA | RNA | ANTISENSE INHIBITOR | UNKNOWN | DRUG LABEL |
ID | Source |
---|---|
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 |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
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 |