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

Stem definitionDrug idCAS RN
antisense oligonucleotides 5182 1173755-55-9

Description:

MoleculeDescription

Synonyms:

  • eteplirsen
  • Exondys 51
  • AVI-4658
  • AVI 4658
Eteplirsen is designed to bind to exon 51 of dystrophin pre-mRNA, resulting in exclusion of this exon during mRNA processing in patients with genetic mutations that are amenable to exon 51 skipping. Exon skipping is intended to allow for production of an internally truncated dystrophin protein.
  • Molecular weight: 10305.89
  • Formula: C364H569N177O122P30
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA: 3305.26
  • ALOGS:
  • ROTB: None

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

DateAgencyCompanyOrphan
Sept. 19, 2016 FDA SAREPTA THERAPEUTICS INC

FDA Adverse Event Reporting System (Female)

None

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
No adverse event 1993.45 69.58 471 2529 38550 42579785
Product dose omission issue 1884.21 69.58 601 2399 153764 42464571
Intentional dose omission 1195.74 69.58 240 2760 8746 42609589
Poor venous access 644.12 69.58 139 2861 7113 42611222
Device issue 543.01 69.58 136 2864 13373 42604962
Exposure to SARS-CoV-2 187.15 69.58 33 2967 565 42617770
Product distribution issue 120.55 69.58 28 2972 1966 42616369
COVID-19 78.58 69.58 65 2935 115883 42502452
Catheter site pain 77.39 69.58 19 2981 1688 42616647

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
No adverse event 2140.47 75.86 460 2197 73379 110513263
Product dose omission issue 2012.55 75.86 583 2074 321199 110265443
Intentional dose omission 1261.91 75.86 240 2417 19840 110566802
Poor venous access 559.05 75.86 127 2530 24395 110562247
Device issue 536.18 75.86 131 2526 34404 110552238
Exposure to SARS-CoV-2 152.00 75.86 30 2627 2889 110583753
Product distribution issue 123.23 75.86 27 2630 4319 110582323

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC M09AX06 MUSCULO-SKELETAL SYSTEM
OTHER DRUGS FOR DISORDERS OF THE MUSCULO-SKELETAL SYSTEM
OTHER DRUGS FOR DISORDERS OF THE MUSCULO-SKELETAL SYSTEM
Other drugs for disorders of the musculo-skeletal system
MeSH PA D015335 Molecular Probes
MeSH PA D016376 Oligonucleotides, Antisense
FDA CS M0025055 Oligonucleotides, Antisense
FDA EPC N0000191626 Antisense Oligonucleotide

Related Drugs by ATC class:

M09AX Other drugs for disorders of the musculo-skeletal system 11 drugs

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

DiseaseRelationSNOMED_IDDOID
Duchenne muscular dystrophy indication 76670001 DOID:11723




🐶 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
100MG/2ML (50MG/ML) EXONDYS 51 SAREPTA THERAPS INC N206488 Sept. 19, 2016 RX SOLUTION INTRAVENOUS RE48468 Oct. 27, 2028 TREATMENT OF DMD IN PATIENTS HAVING A MUTATION OF THE DMD GENE THAT IS AMENABLE TO EXON 51 SKIPPING
500MG/10ML (50MG/ML) EXONDYS 51 SAREPTA THERAPS INC N206488 Sept. 19, 2016 RX SOLUTION INTRAVENOUS RE48468 Oct. 27, 2028 TREATMENT OF DMD IN PATIENTS HAVING A MUTATION OF THE DMD GENE THAT IS AMENABLE TO EXON 51 SKIPPING
100MG/2ML (50MG/ML) EXONDYS 51 SAREPTA THERAPS INC N206488 Sept. 19, 2016 RX SOLUTION INTRAVENOUS 10337003 March 14, 2034 TREATMENT OF DUCHENNE MUSCULAR DYSTROPHY IN PATIENTS HAVING A MUTATION OF THE DMD GENE THAT IS AMENABLE TO EXON 51 SKIPPING
100MG/2ML (50MG/ML) EXONDYS 51 SAREPTA THERAPS INC N206488 Sept. 19, 2016 RX SOLUTION INTRAVENOUS 10364431 March 14, 2034 RESTORING AN MRNA READING FRAME TO INDUCE DYSTROPHIN PROTEIN PRODUCTION IN PATIENTS HAVING A MUTATION OF THE DMD GENE THAT IS AMENABLE TO EXON 51 SKIPPING
100MG/2ML (50MG/ML) EXONDYS 51 SAREPTA THERAPS INC N206488 Sept. 19, 2016 RX SOLUTION INTRAVENOUS 10364431 March 14, 2034 TREATMENT OF DUCHENNE MUSCULAR DYSTROPHY IN PATIENTS HAVING A MUTATION OF THE DMD GENE THAT IS AMENABLE TO EXON 51 SKIPPING
100MG/2ML (50MG/ML) EXONDYS 51 SAREPTA THERAPS INC N206488 Sept. 19, 2016 RX SOLUTION INTRAVENOUS 9506058 March 14, 2034 RESTORING AN MRNA READING FRAME TO INDUCE DYSTROPHIN PROTEIN PRODUCTION IN PATIENTS HAVING A MUTATION OF THE DMD GENE THAT IS AMENABLE TO EXON 51 SKIPPING
100MG/2ML (50MG/ML) EXONDYS 51 SAREPTA THERAPS INC N206488 Sept. 19, 2016 RX SOLUTION INTRAVENOUS 9506058 March 14, 2034 TREATMENT OF DUCHENNE MUSCULAR DYSTROPHY IN PATIENTS HAVING A MUTATION OF THE DMD GENE THAT IS AMENABLE TO EXON 51 SKIPPING
500MG/10ML (50MG/ML) EXONDYS 51 SAREPTA THERAPS INC N206488 Sept. 19, 2016 RX SOLUTION INTRAVENOUS 10337003 March 14, 2034 TREATMENT OF DUCHENNE MUSCULAR DYSTROPHY IN PATIENTS HAVING A MUTATION OF THE DMD GENE THAT IS AMENABLE TO EXON 51 SKIPPING
500MG/10ML (50MG/ML) EXONDYS 51 SAREPTA THERAPS INC N206488 Sept. 19, 2016 RX SOLUTION INTRAVENOUS 10364431 March 14, 2034 RESTORING AN MRNA READING FRAME TO INDUCE DYSTROPHIN PROTEIN PRODUCTION IN PATIENTS HAVING A MUTATION OF THE DMD GENE THAT IS AMENABLE TO EXON 51 SKIPPING
500MG/10ML (50MG/ML) EXONDYS 51 SAREPTA THERAPS INC N206488 Sept. 19, 2016 RX SOLUTION INTRAVENOUS 10364431 March 14, 2034 TREATMENT OF DUCHENNE MUSCULAR DYSTROPHY IN PATIENTS HAVING A MUTATION OF THE DMD GENE THAT IS AMENABLE TO EXON 51 SKIPPING
500MG/10ML (50MG/ML) EXONDYS 51 SAREPTA THERAPS INC N206488 Sept. 19, 2016 RX SOLUTION INTRAVENOUS 9506058 March 14, 2034 RESTORING AN MRNA READING FRAME TO INDUCE DYSTROPHIN PROTEIN PRODUCTION IN PATIENTS HAVING A MUTATION OF THE DMD GENE THAT IS AMENABLE TO EXON 51 SKIPPING
500MG/10ML (50MG/ML) EXONDYS 51 SAREPTA THERAPS INC N206488 Sept. 19, 2016 RX SOLUTION INTRAVENOUS 9506058 March 14, 2034 TREATMENT OF DUCHENNE MUSCULAR DYSTROPHY IN PATIENTS HAVING A MUTATION OF THE DMD GENE THAT IS AMENABLE TO EXON 51 SKIPPING

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
exon 51 of dystrophin pre-mRNA RNA BINDING AGENT UNKNOWN DRUG LABEL

External reference:

IDSource
AIW6036FAS UNII
4036083 VANDF
C4283710 UMLSCUI
CHEBI:753271 CHEBI
CHEMBL2108278 ChEMBL_ID
D09900 KEGG_DRUG
DB06014 DRUGBANK_ID
9339 INN_ID
C000611335 MESH_SUPPLEMENTAL_RECORD_UI
7534 IUPHAR_LIGAND_ID
724033001 SNOMEDCT_US
763585001 SNOMEDCT_US
244179 MMSL
31970 MMSL
d08476 MMSL
016988 NDDF
1810569 RXNORM

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Exondys 51 HUMAN PRESCRIPTION DRUG LABEL 1 60923-284 INJECTION 50 mg INTRAVENOUS NDA 27 sections
Exondys 51 HUMAN PRESCRIPTION DRUG LABEL 1 60923-363 INJECTION 50 mg INTRAVENOUS NDA 27 sections