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Diroximel

Phase 3

Relapsing Forms of Multiple Sclerosis | Small molecule | Neurology |Biogen Inc.|Last Updated: Mar 19, 2026

Target and mechanism

Molecular targetKEAP1
Target classInhibitor
ModalitySmall molecule

Also known as Diroximel Fumarate

Success Probability

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Market & Valuation

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Trial Design

RandomizedDouble-BlindCONTROLLEDDMC
Total Trials2
Total Enrollment321

FDA Designations

No designations recorded

Clinical trial landscape

Diroximel · 3 trials · 2 indications

Phase 3 2Phase 1 1
NCT07483632A Study to Learn About the Safety of Diroximel Fumarate (DRF) and Dimethyl Fumarate (DMF) and Their Effects on Relapses in Pediatric Participants With Relapsing Forms of Multiple Sclerosis (RMS)Relapsing Forms of Multiple Sclerosis
NOT YET_RECRUITING185 Analytics
NCT05083923A Study of Diroximel Fumarate (DRF) in Adult Participants From the Asia-Pacific Region With Relapsing Forms of Multiple Sclerosis (RMS)Relapsing Forms of Multiple Sclerosis
COMPLETED136 Analytics
PHASE3NOT YET_RECRUITING
A Study to Learn About the Safety of Diroximel Fumarate (DRF) and Dimethyl Fumarate (DMF) and Their Effects on Relapses in Pediatric Participants With Relapsing Forms of Multiple Sclerosis (RMS)
Relapsing Forms of Multiple SclerosisUnlock trial analytics
PHASE3COMPLETED
A Study of Diroximel Fumarate (DRF) in Adult Participants From the Asia-Pacific Region With Relapsing Forms of Multiple Sclerosis (RMS)
Relapsing Forms of Multiple SclerosisUnlock trial analytics

Study Endpoints

Primary Endpoints

TP Cohort A and OLE Period: Number of Participants With Treatment Emergent Adverse Events (TEAEs), Serious Adverse Events (SAEs) and AEs Leading to Treatment Discontinuation
Cohort A: From first dose of study drug up to end of follow-up (up to Week 104), OLE: Baseline (Week 96) up to the end of OLE period (up to Week 196)
TP Cohort B: Annualized Relapse Rate (ARR) Through Week 96
Baseline (Day 1) up to Week 96
Part 1: Number of Participants With Treatment Emergent Adverse Events (TEAEs) and Treatment Emergent Serious Adverse Events (TESAEs)
Baseline (Day 1) up to Week 24 (for prematurely discontinued participants, AEs were reported up to 2 weeks post discontinuation)

An adverse event (AE) was any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal (investigational) product, whether/not related to the medicinal (investigational) product. An AE was considered treatment-emergent if it starts or worsens on or after the date of the first dose of study drug in the study until 1 day after the last dose of treatment, or completion of the safety follow-up visit, if applicable.(i.e. for participants who prematurely discontinued study treatment or withdrew from the study) . An SAE is any untoward medical occurrence that at any dose results in death, is a life-threatening event, requires inpatient hospitalization or prolongation of existing hospitalization, results in a significant disability/incapacity or congenital anomaly, is a medically important event. TEAEs included both serious and non-serious TEAEs.

Part 1: Number of Participants With Potentially Clinically Significant Abnormalities in Laboratory Parameters
Baseline (Day 1) to Week 24

Laboratory assessments included hematology, blood chemistry, and urinalysis parameters. Hematology parameters:basophils, hematocrit, red blood cell, total and differential leukocytes, platelets, lymphocytes, monocytes, neutrophils, eosinophils, hemoglobin. Blood chemistry parameters:sodium, potassium, chloride, glucose, calcium, uric acid, total protein, albumin, creatine phosphokinase, Lipid profile: blood cholesterol,high-density lipoprotein,low-density lipoprotein, and triglycerides,serum follicle-stimulating hormone,Vitamin D,thyroid stimulating hormone,serum pregnancy, HIV/Hepatitis screen,tuberculosis test,alanine aminotransferase,aspartate aminotransferase,Lactate Dehydrogenase,alkaline phosphatase,gamma glutamyl transferase,total bilirubin,blood urea nitrogen,creatinine and bicarbonate. Urinalysis parameters:color,pH,specific gravity,ketones,protein,glucose, bilirubin,nitrite,urobilinogen,occult blood,microscopic examination,urine albumin,beta-2-microglobulin,urine creatinine.

Part 1: Number of Participants With Abnormal Shift in 12-Lead Electrocardiogram (ECG) Values
Baseline (Day 1) to Week 24

The number of participants with shifts to categorical values of ECG interpretation (e.g. abnormal) were presented by each cohort. Abnormal shift includes a shift from normal or unknown to abnormal.

Part 1: Number of Participants With Clinically Relevant Abnormalities in Vital Sign Parameters
Baseline (Day 1) to Week 24

Vital sign assessment included temperature, pulse rate systolic blood pressure, diastolic blood pressure, and respiratory rate. The criteria for determining potentially clinically relevant abnormalities in vital signs included: temperature \< 36 and \> 38 degrees Celsius (C), pulse rate \< 60 and \> 100 beats per minute (bpm), systolic blood pressure (\< 90, \> 140 and \> 160 millimeters of mercury \[mmHg\]), diastolic blood pressure \< 50, \> 90 and \> 100 mmHg, weight (7% or more increase from baseline, 7% or more decrease from baseline) and respiratory rate \< 12 and \> 20 breaths per minute.

Part 1: Number of Participants With Columbia Suicide Severity Rating Scale (C-SSRS) Events
Baseline (Day 1) to Week 24

The C-SSRS was an interview-based rating scale to systematically assess suicidal ideation, suicidal behavior and non-suicidal self-injurious behavior. The C-SSRS includes 'yes' or 'no' responses for assessment of suicidal behavior (preparatory acts or behavior, aborted attempt, interrupted attempt, Suicidal behavior, completed suicide), suicidal ideation (wish to be dead, non-specific active suicidal thoughts, active suicidal ideation with any methods, active suicidal ideation with some intent, active suicidal ideation with specific plan and intent) and non-suicidal self-injurious behavior.

Parts 1 and 2: Number of Participants With TEAEs and TESAEs
From Day 1 up to the end of the study (up to Week 50)

An AE was any unfavorable and unintended sign, symptom, or disease temporally associated with use of medicinal (investigational) product, whether/not related to medicinal (investigational) product. AE was considered treatment-emergent if it starts or worsens on or after the date of the first dose of study drug in the study until 1 day after the last dose of treatment. SAE is any untoward medical occurrence that at any dose results in death, is a life-threatening event, requires inpatient hospitalization or prolongation of existing hospitalization, results in a significant disability/incapacity or congenital anomaly, is a medically important event. TEAEs included both serious and non-serious TEAEs. TEAEs and TESAEs for participants were collected cumulatively for Parts 1 and 2.

Part 2: Number of Participants With Potentially Clinically Significant Abnormalities in Laboratory Parameters
Baseline (Day 1) to Week 48

Laboratory assessments included hematology, blood chemistry, and urinalysis parameters. Hematology parameters:basophils, hematocrit, red blood cell, total and differential leukocytes, platelets, lymphocytes, monocytes, neutrophils, eosinophils, hemoglobin. Blood chemistry parameters:sodium, potassium, chloride, glucose, calcium, uric acid, total protein, albumin, creatine phosphokinase, Lipid profile: blood cholesterol,high-density lipoprotein,low-density lipoprotein, and triglycerides,serum follicle-stimulating hormone,Vitamin D,thyroid stimulating hormone,serum pregnancy, HIV/Hepatitis screen,tuberculosis test,alanine aminotransferase,aspartate aminotransferase,Lactate Dehydrogenase,alkaline phosphatase,gamma glutamyl transferase,total bilirubin,blood urea nitrogen,creatinine and bicarbonate. Urinalysis parameters:color,pH,specific gravity,ketones,protein,glucose, bilirubin,nitrite,urobilinogen,occult blood,microscopic examination,urine albumin,beta-2-microglobulin,urine creatinine.

Part 2: Number of Participants With Abnormal Shift in 12-Lead ECG Values
Baseline (Day 1) to Week 48

The number of participants with shifts to categorical values of ECG interpretation (e.g. abnormal) were presented by each cohort. Abnormal shift includes a shift from normal or unknown to abnormal.

Part 2: Number of Participants With Clinically Relevant Abnormalities in Vital Sign Parameters
Baseline (Day 1) to Week 48

Vital sign assessment included temperature, pulse rate systolic blood pressure, diastolic blood pressure, and respiratory rate. The criteria for determining potentially clinically relevant abnormalities in vital signs included: temperature \< 36 and \> 38 degrees C, pulse rate \< 60 and \> 100 bpm, systolic blood pressure (\< 90, \> 140 and \> 160 mmHg), diastolic blood pressure \< 50, \> 90 and \> 100 mmHg, weight (7% or more increase from baseline, 7% or more decrease from baseline) and respiratory rate \< 12 and \> 20 breaths per minute.

Part 2: Number of Participants With C-SSRS Events
Baseline (Day 1) to Week 48

The C-SSRS was an interview-based rating scale to systematically assess suicidal ideation, suicidal behavior and non-suicidal self-injurious behavior. The C-SSRS includes 'yes' or 'no' responses for assessment of suicidal behavior (preparatory acts or behavior, aborted attempt, interrupted attempt, Suicidal behavior, completed suicide), suicidal ideation (wish to be dead, non-specific active suicidal thoughts, active suicidal ideation with any methods, active suicidal ideation with some intent, active suicidal ideation with specific plan and intent) and non-suicidal self-injurious behavior.

Maximum Observed Concentration (Cmax) of Monomethyl Fumarate (MMF)
Pre-dose and at multiple timepoints post-dose on Days 1 and 5 and post-dose on Days 6, 7 and 8
Area Under the Concentration-Time Curve within a Dosing Interval (AUCtau) of MMF
Pre-dose and at multiple timepoints post-dose on Days 1 and 5 and post-dose on Days 6, 7 and 8

Secondary Endpoints

TP Cohorts A and B: Maximum Observed Concentration at Steady State (Cmax,ss) of Monomethyl Fumarate (MMF)
Predose and at multiple timepoints post dose up to Week 96
TP Cohorts A and B: Minimum Observed Concentration at Steady State (Cmin,ss) of MMF
Predose and at multiple timepoints post dose up to Week 96
TP Cohorts A and B: Cmax,ss of 2-Hydroxyethyl Succinimide (HES)
Predose and at multiple timepoints post dose up to Week 96
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Study Design & Arms

AllocationRANDOMIZED
MaskingQUADRUPLE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
TP Cohort AEXPERIMENTALParticipants weighing ≤ 40 kilograms (kg) will receive DRF 231 milligrams (mg) orally, once daily (QD) (starting dose) on Days 1 to 7 followed by DRF 231 mg orally, BID (twice daily) (maintenance dose) on Day 8 through Week 96.
TP Cohort B: Sub-cohort 1: DRFEXPERIMENTALParticipants weighing \>40 kg will receive DRF/placebo matching fingolimod 231 mg orally, BID (starting dose) on Days 1 to 7 followed by DRF 462 mg orally, BID (maintenance dose) on Day 8 through Week 96.
TP Cohort B: Sub-cohort 1: FingolimodEXPERIMENTALParticipants weighing \>40 kg will receive Fingolimod 0.5 mg orally, QD followed by placebo matching DRF 231 mg (starting dose) orally, BID on Days 1 to 7 followed by placebo matching DRF 462 mg (maintenance dose) orally, BID on Day 8 through Week 96.
TP Cohort B: Sub-cohort 2: DMFEXPERIMENTALParticipants weighing \>40 kg will receive DMF/placebo matching fingolimod 120 mg (starting dose) orally, BID on Days 1 to 7 followed by DMF 240 mg (maintenance dose) orally BID, on Day 8 through Week 96.
TP Cohort B: Sub-cohort 2: FingolimodEXPERIMENTALParticipants weighing \>40 kg will receive Fingolimod 0.5 mg oral QD followed by placebo matching DMF 120 mg (starting dose) orally, BID on Days 1 to 7 followed by placebo matching DMF 240 mg (maintenance dose) orally, BID through Week 96.
Open-label Extension (OLE) Period: Participants from Cohort AEXPERIMENTALParticipants from Cohort A weighing ≤ 40 kg will receive DRF 231 mg orally, BID and participants weighing \>40 kg will receive DRF 462 mg orally, BID up to 192 weeks.
OLE Period: Participants from Cohort BEXPERIMENTALParticipants from Cohort B will receive DRF 231 mg orally, BID for 7 days, followed by the maintenance dose of DRF 462 mg orally, BID up to 192 weeks.
Diroximel Fumarate (DRF)EXPERIMENTALJapanese and Chinese participants will initiate treatment with DRF 231 milligrams (mg), oral capsule, twice daily on Day 1 through Day 7, followed by DRF 462 mg, oral capsules, twice daily from Day 8 up to Week 48.
DRF: Chinese ParticipantsEXPERIMENTALChinese participants will receive DRF Dose 1, oral capsules, twice daily (BID), from Day 1 to Day 4 and DRF Dose 1, oral capsules, once daily (QD), on Day 5.
DRF: Caucasian ParticipantsEXPERIMENTALCaucasian participants will receive DRF Dose 1, oral capsules, BID, from Day 1 to Day 4 and DRF Dose 1, oral capsules, QD, on Day 5.

Interventions

NameTypeDescription
Diroximel FumarateDRUGOral capsule
Dimethyl FumarateDRUGOral capsule
FingolimodDRUGOral capsule
Placebo matching DRFDRUGOral capsule
Placebo matching DMFDRUGOral capsule
Placebo matching fingolimodDRUGOral capsule
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Eligibility Criteria

Age Range10 Years to 17 Years
SexALL
Healthy VolunteersNo

Key Inclusion Criteria: Treatment Period: * Must have a diagnosis of pediatric MS (as defined by the revised consensus definition of pediatric MS). * Must have an Expanded Disability Status Scale (EDSS) score between 0 and 5.0, inclusive. * Must have experienced at least 1 of the following conditi...

Countries:ChinaJapanHong KongNew Zealand
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Frequently asked questions about Diroximel

What is Diroximel used for?

Diroximel, also known as Diroximel Fumarate, is being studied for the treatment of relapsing forms of multiple sclerosis (RMS) in adult and pediatric participants. It is an investigational small molecule developed by Biogen Inc. (BIIB). Clinical trials are evaluating its safety and effects on relapses in this patient population.

What does Diroximel target?

Diroximel is a small molecule being developed for relapsing forms of multiple sclerosis. Its specific molecular target has not been disclosed in the available clinical trial information. The drug is being studied for its effects on disease activity and relapse rates in patients with RMS.

Who makes Diroximel?

Diroximel is being developed by Biogen Inc., a biotechnology company traded on the NASDAQ under the ticker symbol BIIB. Biogen is conducting clinical trials to evaluate the safety and efficacy of Diroximel Fumarate in patients with relapsing forms of multiple sclerosis.

What phase is Diroximel in?

Diroximel is in clinical development, with trials listed in Phase 1 and Phase 3. A Phase 1 study in healthy volunteers has been completed, and a Phase 3 study in adult patients with relapsing forms of multiple sclerosis has also been completed. An additional Phase 3 study in pediatric patients is planned but has not yet started recruiting.

What clinical trials is Diroximel in?

Diroximel has been studied in clinical trials including NCT05083923, a completed Phase 3 study in adults with relapsing forms of multiple sclerosis in China and Japan, and NCT05127564, a completed Phase 1 study in healthy Chinese and Caucasian participants. A third trial, NCT07483632, is a planned Phase 3 study in pediatric patients with RMS.

Is Diroximel the same as Diroximel Fumarate?

Yes, Diroximel is also known as Diroximel Fumarate (DRF). Clinical trials refer to the drug as Diroximel Fumarate, and it is being investigated for the treatment of relapsing forms of multiple sclerosis. Biogen Inc. is the developer of this investigational small molecule.