diroximel fumarate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 5502 | 1577222-14-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
The mechanism by which diroximel fumarate exerts therapeutic effects in MS is not fully understood. Diroximel fumarate acts via the major active metabolite, monomethyl fumarate. Preclinical studies indicate that the pharmacodynamic responses of monomethyl fumarate appears to be mediated, at least in part, through activation of the Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) transcriptional pathway. Dimethyl fumarate has been shown to up regulate Nrf2-dependent antioxidant genes in patients.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.92 | g | O |
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 15, 2021 | EMA | BIOGEN NETHERLANDS B.V. | |
| Oct. 29, 2019 | FDA | BIOGEN INC |
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 |
|---|---|---|---|---|---|---|
| Flushing | 301.54 | 37.19 | 102 | 1631 | 74985 | 63412304 |
| Multiple sclerosis relapse | 186.71 | 37.19 | 64 | 1669 | 48414 | 63438875 |
| Chromaturia | 59.99 | 37.19 | 21 | 1712 | 16696 | 63470593 |
| Drug ineffective | 43.08 | 37.19 | 90 | 1643 | 1044675 | 62442614 |
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 |
|---|---|---|---|---|---|---|
| Multiple sclerosis relapse | 75.38 | 51.03 | 18 | 260 | 13115 | 34943538 |
| Flushing | 54.98 | 51.03 | 17 | 261 | 32403 | 34924250 |
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 |
|---|---|---|---|---|---|---|
| Flushing | 240.07 | 41.44 | 72 | 828 | 88196 | 79655292 |
| Multiple sclerosis relapse | 104.76 | 41.44 | 33 | 867 | 46500 | 79696988 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L04AX09 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS IMMUNOSUPPRESSANTS IMMUNOSUPPRESSANTS Other immunosuppressants |
| CHEBI has role | CHEBI:22586 | antioxidants |
| CHEBI has role | CHEBI:49103 | drug metabolites |
| CHEBI has role | CHEBI:50846 | Immunologic factor |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Relapsing forms of multiple sclerosis | indication | 426373005 | DOID:2378 |
| Progressive multifocal leukoencephalopathy | contraindication | 22255007 | DOID:643 |
🐶 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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 231MG | VUMERITY | BIOGEN INC | N211855 | Oct. 29, 2019 | RX | CAPSULE, DELAYED RELEASE | ORAL | 10080733 | Sept. 20, 2033 | METHOD OF TREATING MULTIPLE SCLEROSIS |
| 231MG | VUMERITY | BIOGEN INC | N211855 | Oct. 29, 2019 | RX | CAPSULE, DELAYED RELEASE | ORAL | 9090558 | Sept. 20, 2033 | METHOD OF TREATING MULTIPLE SCLEROSIS |
| 95MG | BAFIERTAM | BANNER LIFE SCIENCES | N210296 | April 28, 2020 | RX | CAPSULE, DELAYED RELEASE | ORAL | 10098863 | Feb. 27, 2035 | METHOD OF TREATING MULTIPLE SCLEROSIS |
| 95MG | BAFIERTAM | BANNER LIFE SCIENCES | N210296 | April 28, 2020 | RX | CAPSULE, DELAYED RELEASE | ORAL | 10105336 | Feb. 27, 2035 | METHOD OF TREATING MULTIPLE SCLEROSIS |
| 95MG | BAFIERTAM | BANNER LIFE SCIENCES | N210296 | April 28, 2020 | RX | CAPSULE, DELAYED RELEASE | ORAL | 9326965 | Feb. 27, 2035 | METHOD OF TREATING MULTIPLE SCLEROSIS |
| 95MG | BAFIERTAM | BANNER LIFE SCIENCES | N210296 | April 28, 2020 | RX | CAPSULE, DELAYED RELEASE | ORAL | 9511043 | Feb. 27, 2035 | METHOD OF TREATING MULTIPLE SCLEROSIS |
| 95MG | BAFIERTAM | BANNER LIFE SCIENCES | N210296 | April 28, 2020 | RX | CAPSULE, DELAYED RELEASE | ORAL | 9636318 | Feb. 27, 2035 | METHOD OF TREATING MULTIPLE SCLEROSIS |
| 95MG | BAFIERTAM | BANNER LIFE SCIENCES | N210296 | April 28, 2020 | RX | CAPSULE, DELAYED RELEASE | ORAL | 9814691 | Feb. 27, 2035 | METHOD OF TREATING MULTIPLE SCLEROSIS |
| 95MG | BAFIERTAM | BANNER LIFE SCIENCES | N210296 | April 28, 2020 | RX | CAPSULE, DELAYED RELEASE | ORAL | 9814692 | Feb. 27, 2035 | METHOD OF TREATING MULTIPLE SCLEROSIS |
| 95MG | BAFIERTAM | BANNER LIFE SCIENCES | N210296 | April 28, 2020 | RX | CAPSULE, DELAYED RELEASE | ORAL | 9820961 | Feb. 27, 2035 | METHOD OF TREATING MULTIPLE SCLEROSIS |
| 95MG | BAFIERTAM | BANNER LIFE SCIENCES | N210296 | April 28, 2020 | RX | CAPSULE, DELAYED RELEASE | ORAL | 10918616 | June 3, 2035 | METHOD OF TREATING MULTIPLE SCLEROSIS |
| 95MG | BAFIERTAM | BANNER LIFE SCIENCES | N210296 | April 28, 2020 | RX | CAPSULE, DELAYED RELEASE | ORAL | 10918615 | Aug. 12, 2035 | METHOD OF TREATING MULTIPLE SCLEROSIS |
| 95MG | BAFIERTAM | BANNER LIFE SCIENCES | N210296 | April 28, 2020 | RX | CAPSULE, DELAYED RELEASE | ORAL | 11590095 | March 18, 2036 | METHOD OF TREATING MULTIPLE SCLEROSIS |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Hydroxycarboxylic acid receptor 2 | GPCR | AGONIST | Ki | 6.74 | IUPHAR | ||||
| Nuclear factor erythroid 2-related factor 2 | Transcription factor | ACTIVATOR | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| CHEBI:167450 | CHEBI |
| CHEMBL3989944 | ChEMBL_ID |
| C000722501 | MESH_SUPPLEMENTAL_RECORD_UI |
| C509058 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10525 | IUPHAR_LIGAND_ID |
| DB14783 | DRUGBANK_ID |
| DB14219 | DRUGBANK_ID |
| 018178 | NDDF |
| 018377 | NDDF |
| 4038911 | VANDF |
| 4039606 | VANDF |
| D11154 | KEGG_DRUG |
| C5139729 | UMLSCUI |
| C3848524 | UMLSCUI |
| CHEMBL589586 | ChEMBL_ID |
| 10356 | INN_ID |
| 1010557002 | SNOMEDCT_US |
| 1010563006 | SNOMEDCT_US |
| 1268407006 | SNOMEDCT_US |
| 1268477005 | SNOMEDCT_US |
| 11163 | INN_ID |
| 2756-87-8 | SECONDARY_CAS_RN |
| 73330464 | PUBCHEM_CID |
| 5369209 | PUBCHEM_CID |
| 1546433 | RXNORM |
| 326412 | MMSL |
| 37634 | MMSL |
| 38425 | MMSL |
| d09422 | MMSL |
| d09557 | MMSL |
| 5786 | IUPHAR_LIGAND_ID |
| K0N0Z40J3W | UNII |
| 45IUB1PX8R | UNII |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Vumerity | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64406-020 | CAPSULE | 231 mg | ORAL | NDA | 28 sections |
| Vumerity | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64406-020 | CAPSULE | 231 mg | ORAL | NDA | 28 sections |
| Vumerity | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64406-020 | CAPSULE | 231 mg | ORAL | NDA | 28 sections |
| BAFIERTAM | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69387-001 | CAPSULE | 95 mg | ORAL | NDA | 28 sections |
| BAFIERTAM | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69387-001 | CAPSULE | 95 mg | ORAL | NDA | 28 sections |
| BAFIERTAM | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69387-001 | CAPSULE | 95 mg | ORAL | NDA | 28 sections |