All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

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

Drug dosage:

Dose	Unit	Route
41	mg	P

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

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

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	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 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	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 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	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:

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	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|

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

Orange Book exclusivity data (new drug applications)

None

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
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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