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NCT01703988

An Open-label Safety, Tolerability and Dose-Range Finding Study of Multiple Doses of Nusinersen (ISIS 396443) in Participants With Spinal Muscular Atrophy

Completed Phase 1, PHASE2 Results posted Last updated 13 April 2021
What this trial tests

Phase 1, PHASE2 trial testing Nusinersen in Spinal Muscular Atrophy in 34 participants. Completed in 31 January 2015.

Timeline
31 October 2012
Primary endpoint
31 January 2015
31 January 2015

Quick facts

Lead sponsorBiogen
PhasePhase 1, PHASE2
StatusCompleted
Study typeINTERVENTIONAL
Allocationnon randomized
Designparallel
Maskingnone
Primary purposetreatment
Enrollment34
Start date31 October 2012
Primary completion31 January 2015
Estimated completion31 January 2015
Sites4 locations across United States

Drugs / interventions tested

Conditions studied

Sponsor

Biogen — full company profile →

Who can join

Adults 2 to 15, any sex, with Spinal Muscular Atrophy. Patients with the condition only — healthy volunteers not accepted.

Results — posted to ClinicalTrials.gov

Per-arm endpoint measurements with 95% confidence intervals where reported. Source: trial results section.

Number of Participants With Adverse Events (AEs), Serious AEs (SAEs), Discontinuations Due to AEs, and Highest Severity of AEs Primary · Participants were followed for the duration of the study; mean (SD) duration of treatment was 82.9 (15.4) days

An AE is any unfavorable and unintended sign, symptom, or disease temporally associated with the study or use of the investigational drug product, whether or not the AE is considered related to the investigational drug product. An SAE is any AE that, in the view of either the Investigator or Sponsor, meets any of the following criteria: results in death; is life threatening; requires inpatient hospitalization or prolongation of existing hospitalization; results in a persistent or significant incapacity or substantial disruption of the ability to conduct normal life functions; results in congen

Any AE
GroupValue95% CI
Nusinersen 3 mg8
Nusinersen 6 mg6
Nusinersen 9 mg9
Nusinersen 12 mg9
Any drug-related AE
GroupValue95% CI
Nusinersen 3 mg0
Nusinersen 6 mg0
Nusinersen 9 mg0
Nusinersen 12 mg0
Any SAE
GroupValue95% CI
Nusinersen 3 mg2
Nusinersen 6 mg0
Nusinersen 9 mg0
Nusinersen 12 mg1
Discontinued due to an AE
GroupValue95% CI
Nusinersen 3 mg0
Nusinersen 6 mg0
Nusinersen 9 mg0
Nusinersen 12 mg0
Highest severity of AE=mild
GroupValue95% CI
Nusinersen 3 mg2
Nusinersen 6 mg2
Nusinersen 9 mg6
Nusinersen 12 mg5
Highest severity of AE=moderate
GroupValue95% CI
Nusinersen 3 mg4
Nusinersen 6 mg2
Nusinersen 9 mg3
Nusinersen 12 mg4
Highest severity of AE=severe
GroupValue95% CI
Nusinersen 3 mg2
Nusinersen 6 mg2
Nusinersen 9 mg0
Nusinersen 12 mg0
Plasma Pharmacokinetics: Maximal Observed Plasma Drug Concentration (Cmax) Secondary · Day 1 and Day 85
Day 1
GroupValue95% CI
Nusinersen 3 mg51.5± 72.7
Nusinersen 6 mg79.8± 57.2
Nusinersen 9 mg141.0± 52.8
Nusinersen 12 mg208.0± 110.0
Day 85
GroupValue95% CI
Nusinersen 3 mg32.5± 32.3
Nusinersen 6 mg52.8± 33.5
Nusinersen 9 mg127.0± 37.7
Nusinersen 12 mg132.0± 85.6
Plasma Pharmacokinetics: Time to Reach Cmax in Plasma Secondary · Day 1 and Day 85
Day 1
GroupValue95% CI
Nusinersen 3 mg5.092.03 – 12.0
Nusinersen 6 mg5.932.00 – 23.0
Nusinersen 9 mg3.922.00 – 8.03
Nusinersen 12 mg4.051.97 – 12.0
Day 85
GroupValue95% CI
Nusinersen 3 mg6.084.12 – 6.17
Nusinersen 6 mg6.045.97 – 6.25
Nusinersen 9 mg4.122.00 – 6.25
Nusinersen 12 mg5.921.95 – 6.07
Plasma Pharmacokinetics: Plasma Pharmacokinetics: Area Under the Plasma Concentration Time Curve From the Time of the IT Dose to 6 Hours After Dosing (AUC0-6hr) Secondary · Day 1 and Day 85
Day 1
GroupValue95% CI
Nusinersen 3 mg181± 225
Nusinersen 6 mg306± 259
Nusinersen 9 mg601± 249
Nusinersen 12 mg823± 442
Day 85
GroupValue95% CI
Nusinersen 3 mg110± 107
Nusinersen 6 mg179± 135
Nusinersen 9 mg524± 185
Nusinersen 12 mg555± 398
Cerebrospinal Fluid (CSF) Pharmacokinetics: Predose CSF Drug Concentrations Secondary · Day 1, Day 29, and Day 85
Day 1
GroupValue95% CI
Nusinersen 3 mg0.0651± 0.117
Nusinersen 6 mg0.0560± 0.104
Nusinersen 9 mgNA± NA
Nusinersen 12 mgNA± NA
Day 29
GroupValue95% CI
Nusinersen 3 mg1.41± 0.456
Nusinersen 6 mg2.65± 1.44
Nusinersen 12 mg2.22± 0.924
Day 85
GroupValue95% CI
Nusinersen 3 mg2.12± 0.573
Nusinersen 6 mg3.76± 2.05
Nusinersen 9 mg1.50± 0.447
Nusinersen 12 mg3.36± 1.04
Urine Pharmacokinetics: Renal Clearance, Cohort 4 Secondary · Day 1 and Day 85

Renal clearance of nusinersen for participants was assessed in the 12 mg reporting group only, per protocol.

Day 1
GroupValue95% CI
Nusinersen 12 mg0.674± 0.602
Day 85
GroupValue95% CI
Nusinersen 12 mg77.5± 92.5

Adverse events — posted to ClinicalTrials.gov

Time frame: Participants were followed for the duration of the study; mean (SD) duration of treatment was 82.9 (15.4) days.. Reporting threshold: 0%. Adverse-event reports describe events observed during the trial — not all are caused by the drug.

Nusinersen 3 mg
Serious: 2/8 (25%)
Deaths:
Nusinersen 6 mg
Serious: 0/8 (0%)
Deaths:
Nusinersen 9 mg
Serious: 0/9 (0%)
Deaths:
Nusinersen 12 mg
Serious: 1/9 (11%)
Deaths:

Serious adverse events (3 terms)

ReactionSystemNusinersen 3 mgNusinersen 6 mgNusinersen 9 mgNusinersen 12 mg
Drug hypersensitivityImmune system disorders
PneumoniaInfections and infestations
Post lumbar puncture syndromeInjury, poisoning and procedural complications
Other adverse events (89 terms — click to expand)

ReactionSystemNusinersen 3 mgNusinersen 6 mgNusinersen 9 mgNusinersen 12 mg
Post lumbar puncture syndromeInjury, poisoning and procedural complications
NasopharyngitisInfections and infestations
Back painMusculoskeletal and connective tissue disorders
HeadacheNervous system disorders
Puncture site painGeneral disorders
PyrexiaGeneral disorders
Pharyngitis streptococcalInfections and infestations
VomitingGastrointestinal disorders
ConstipationGastrointestinal disorders
NauseaGastrointestinal disorders
Upper respiratory tract infectionInfections and infestations
Viral upper respiratory tract infectionInfections and infestations
Localised infectionInfections and infestations
Otitis mediaInfections and infestations
Arthropod biteInjury, poisoning and procedural complications
PalpitationsCardiac disorders
Ear painEar and labyrinth disorders
ConjunctivitisEye disorders
StrabismusEye disorders
Abdominal discomfortGastrointestinal disorders
DiarrhoeaGastrointestinal disorders
Food poisoningGastrointestinal disorders
Hypoaesthesia oralGastrointestinal disorders
Lip painGastrointestinal disorders
Oral painGastrointestinal disorders
FatigueGeneral disorders
Catheter site haemorrhageGeneral disorders
Catheter site painGeneral disorders
Catheter site related reactionGeneral disorders
Chest discomfortGeneral disorders
ChillsGeneral disorders
Feeling coldGeneral disorders
Gravitational oedemaGeneral disorders
Oedema peripheralGeneral disorders
PainGeneral disorders
Vessel puncture site haematomaGeneral disorders
HypersensitivityImmune system disorders
Seasonal allergyImmune system disorders
PneumoniaInfections and infestations
SinusitisInfections and infestations

Most-reported serious reactions: Drug hypersensitivity, Pneumonia, Post lumbar puncture syndrome.

Data from ClinicalTrials.gov NCT01703988 adverse events section.

Sponsor's own description

This study will test the safety, tolerability, and pharmacokinetics of escalating doses of nusinersen (ISIS 396443) administered into the spinal fluid either two or three times over the duration of the trial, in participants with spinal muscular atrophy (SMA). Four dose levels will be evaluated sequentially. Each dose level will be studied in a cohort of approximately 8 participants, where all participants will receive active drug.

Publications & conference data

8 peer-reviewed publications reference this trial (live from Europe PMC):

  1. Splice-switching antisense oligonucleotides as therapeutic drugs.
    Havens MA, Hastings ML. · · 2016 · cited 402× · PMID 27288447 · DOI 10.1093/nar/gkw533
  2. Nusinersen in later-onset spinal muscular atrophy: Long-term results from the phase 1/2 studies.
    Darras BT, Chiriboga CA, Iannaccone ST, Swoboda KJ, et al · · 2019 · cited 206× · PMID 31019106 · DOI 10.1212/wnl.0000000000007527
  3. Gene-based therapies for neurodegenerative diseases.
    Sun J, Roy S. · · 2021 · cited 126× · PMID 33526943 · DOI 10.1038/s41593-020-00778-1
  4. Antisense oligonucleotides: treating neurodegeneration at the level of RNA.
    DeVos SL, Miller TM. · · 2013 · cited 117× · PMID 23686823 · DOI 10.1007/s13311-013-0194-5
  5. Adverse Drug Reactions and Toxicity of the Food and Drug Administration-Approved Antisense Oligonucleotide Drugs.
    Alhamadani F, Zhang K, Parikh R, Wu H, et al · · 2022 · cited 101× · PMID 35221289 · DOI 10.1124/dmd.121.000418
  6. Requirement of enhanced Survival Motoneuron protein imposed during neuromuscular junction maturation.
    Kariya S, Obis T, Garone C, Akay T, et al · · 2014 · cited 99× · PMID 24463453 · DOI 10.1172/jci72017
  7. An Integrated Safety Analysis of Infants and Children with Symptomatic Spinal Muscular Atrophy (SMA) Treated with Nusinersen in Seven Clinical Trials.
    Darras BT, Farrar MA, Mercuri E, Finkel RS, et al · · 2019 · cited 88× · PMID 31420846 · DOI 10.1007/s40263-019-00656-w
  8. Improved Nucleic Acid Therapy with Advanced Nanoscale Biotechnology.
    Weng Y, Huang Q, Li C, Yang Y, et al · · 2020 · cited 72× · PMID 31927331 · DOI 10.1016/j.omtn.2019.12.004

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