Overview
11 DESCRIPTION VUMERITY contains diroximel fumarate. The chemical name of diroximel fumarate is 2-Butenedioic acid (2E)-, 1-[2-(2,5-dioxo-1-pyrrolidinyl)ethyl] 4-methyl ester, which has a molecular formula of C 11 H 13 NO 6 and molecular weight of 255.22. Diroximel fumarate has the following structure: Diroximel fumarate is a white to off-white powder that is slightly soluble in water.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action The mechanism by which diroximel fumarate exerts its therapeutic effect in multiple sclerosis is unknown. MMF, the active metabolite of diroximel fumarate, has been shown to activate the nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway in vitro and in vivo in animals and humans. The Nrf2 pathway is involved in the cellular response to oxidative stress. MMF has been identified as a nicotinic acid receptor agonist in vitro . 12.2 Pharmacodynamics Cardiac Electrophysiology At a dose 2 times the maximum recommended dose, VUMERITY does not prolong the QTc interval to any clinically relevant extent. 12.
Indications
- 1 INDICATIONS AND USAGE VUMERITY is indicated for the treatment of relapsing forms of multiple sclerosis (MS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults. VUMERITY is indicated for the treatment of relapsing forms of multiple sclerosis (MS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults. ( 1 )
Common Doses
- 231 mg
- 462 mg
- 325 mg
- 30 g
Dosage
2 DOSAGE AND ADMINISTRATION Blood tests are required prior to initiation of VUMERITY ( 2.1 ) Starting dose: 231 mg twice a day, orally, for 7 days ( 2.2 ) Maintenance dose after 7 days: 462 mg (administered as two 231 mg capsules) twice a day, orally ( 2.2 ) Swallow VUMERITY capsules whole and intact. Do not crush, chew, or sprinkle capsule contents on food ( 2.3 ) Avoid administration of VUMERITY with a high-fat, high-calorie meal/snack ( 2.3 ) Avoid co-administration of VUMERITY with alcohol ( 2.3 ) 2.
Contraindications
- 4 CONTRAINDICATIONS VUMERITY is contraindicated in patients With known hypersensitivity to diroximel fumarate, dimethyl fumarate, or to any of the excipients of VUMERITY. Reactions may include anaphylaxis and angioedema [see Warnings and Precautions ( 5.1 )]. Taking dimethyl fumarate [see Drug Interactions ( 7.1 )] . Known hypersensitivity to diroximel fumarate, dimethyl fumarate, or to any of the excipients of VUMERITY ( 4 ) Co-administration with dimethyl fumarate ( 4 )
Side Effects
- 6 ADVERSE REACTIONS The following important adverse reactions are described elsewhere in labeling: Anaphylaxis and Angioedema [see Warnings and Precautions ( 5.1 )] Progressive Multifocal Leukoencephalopathy [see Warnings and Precautions Section ( 5.2 )] Herpes Zoster and Other Serious Opportunistic Infections [see Warnings and Precautions ( 5.3 )] Lymphopenia [see Warnings and Precautions ( 5.4 )] Liver Injury [see Warnings and Precautions ( 5.6 )] Flushing [see Warnings and Precautions ( 5.6 )] Serious Gastrointestinal Reactions [see Warnings and Precautions ( 5.
Interactions
- 7 DRUG INTERACTIONS 7.1 Concomitant Dimethyl Fumarate VUMERITY is contraindicated in patients currently taking dimethyl fumarate, which is also metabolized to monomethyl fumarate. VUMERITY may be initiated the day following discontinuation of dimethyl fumarate [see Contraindications ( 4 )] .