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

Stem definition	Drug id	CAS RN
antisense oligonucleotides	5319	1492984-65-2

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
41	mg	P

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
July 6, 2018	EMA	Akcea Therapeutics Ireland Limited
Oct. 5, 2018	FDA	AKCEA THERAPS

FDA Adverse Event Reporting System (Female)

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

FDA Adverse Event Reporting System (Male)

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

FDA Adverse Event Reporting System (Geriatric)

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

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

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

Disease	Relation	SNOMED_ID	DOID
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 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

Orange Book exclusivity data (new drug applications)

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

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
transthyretin (TTR) mRNA	RNA	P02766	TTHY_HUMAN	ANTISENSE INHIBITOR				UNKNOWN	DRUG LABEL

External reference:

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

Pharmaceutical products:

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