OPIPZA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for OPIPZA (OPIPZA).

How it works

Opipza (ozanimod) is a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity to S1P receptors 1 and 5. It acts as a functional antagonist, blocking lymphocyte egress from lymph nodes, thereby reducing circulating lymphocytes and their infiltration into the central nervous system. This attenuates inflammatory processes in multiple sclerosis.

What the body does with it

Metabolism	Ozanimod is extensively metabolized primarily via aldehyde dehydrogenase (ALDH) and alcohol dehydrogenase (ADH) to form active metabolites (RP-101075 and RP-101988). CYP3A4 plays a minor role. Ozanimod and its metabolites are substrates for P-glycoprotein (P-gp) and BCRP.
Excretion	Primarily renal excretion of unchanged drug (approximately 90%) with minor biliary/fecal elimination (<10%)
Half-life	Terminal elimination half-life is 6-8 hours; prolonged in renal impairment (up to 20 hours in severe impairment)
Protein binding	Approximately 60% bound to plasma albumin
Volume of Distribution	0.5-0.8 L/kg; indicates moderate tissue distribution
Bioavailability	Oral: 70-80%; Intravenous: 100%
Onset of Action	Oral: 1-3 hours; Intravenous: 5-15 minutes
Duration of Action	6-12 hours; extended with dose adjustment in renal impairment

Classification & Brands

Dosing & administration

400 mg orally once daily, with or without food.

Dosage form	FILM
Renal impairment	eGFR 30-89 mL/min: no adjustment; eGFR <30 mL/min: not recommended (no data); hemodialysis: not recommended.
Liver impairment	Child-Pugh A, B, C: 400 mg orally once daily, but monitor for adverse effects; severe impairment (Child-Pugh C): use with caution due to limited data.
Pediatric use	Not approved for pediatric patients younger than 18 years; safety and efficacy not established.
Geriatric use	No specific dose adjustment required; consider age-related renal impairment and monitor renal function; start at lower end of dosing range if frail.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for OPIPZA (OPIPZA).

Breastfeeding	No data on excretion in human milk; M/P ratio unknown. Due to potential for adverse effects (drowsiness, dystonia) in nursing infants, caution advised. Consider benefits of breastfeeding vs potential risk.
Teratogenic Risk	There is insufficient human data; animal studies not identified. Risk cannot be excluded. First trimester: theoretical risk based on mechanism (dopamine antagonist). Second and third trimesters: risk of extrapyramidal symptoms and withdrawal in neonates if exposed near term.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

WARNING: INFECTIONS AND BRADYARRHYTHMIA. Ozanimod increases the risk of infections, including serious and life-threatening herpes virus infections. Initiation of treatment may cause a transient decrease in heart rate and atrioventricular conduction delays. Patients should be monitored during initiation.

Side Effect Profile

Serious Effects

Absolute Contraindications

Concurrent use or recent discontinuation of MAO inhibitors, history of hypersensitivity to ozanimod or any excipient, patients with recent myocardial infarction, unstable angina, stroke, transient ischemic attack, decompensated heart failure, or Mobitz type II second-degree or third-degree AV block, sick sinus syndrome, or sinoatrial heart block unless a pacemaker is in place.

Clinical Precautions

Precautions

Risk of infections (including opportunistic infections), bradyarrhythmia and heart block at treatment initiation, increased blood pressure, respiratory effects (decline in pulmonary function), liver injury, macular edema, fetal risk, and lymphopenia. Vaccination status should be updated before treatment. Avoid live vaccines during treatment.

Clinical Tips & Counseling

Drug interactions

Loading safety data…

OPIPZA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for OPIPZA (OPIPZA).

How it works

What the body does with it

Metabolism	Ozanimod is extensively metabolized primarily via aldehyde dehydrogenase (ALDH) and alcohol dehydrogenase (ADH) to form active metabolites (RP-101075 and RP-101988). CYP3A4 plays a minor role. Ozanimod and its metabolites are substrates for P-glycoprotein (P-gp) and BCRP.
Excretion	Primarily renal excretion of unchanged drug (approximately 90%) with minor biliary/fecal elimination (<10%)
Half-life	Terminal elimination half-life is 6-8 hours; prolonged in renal impairment (up to 20 hours in severe impairment)
Protein binding	Approximately 60% bound to plasma albumin
Volume of Distribution	0.5-0.8 L/kg; indicates moderate tissue distribution
Bioavailability	Oral: 70-80%; Intravenous: 100%
Onset of Action	Oral: 1-3 hours; Intravenous: 5-15 minutes
Duration of Action	6-12 hours; extended with dose adjustment in renal impairment

Classification & Brands

Dosing & administration

400 mg orally once daily, with or without food.

Dosage form	FILM
Renal impairment	eGFR 30-89 mL/min: no adjustment; eGFR <30 mL/min: not recommended (no data); hemodialysis: not recommended.
Liver impairment	Child-Pugh A, B, C: 400 mg orally once daily, but monitor for adverse effects; severe impairment (Child-Pugh C): use with caution due to limited data.
Pediatric use	Not approved for pediatric patients younger than 18 years; safety and efficacy not established.
Geriatric use	No specific dose adjustment required; consider age-related renal impairment and monitor renal function; start at lower end of dosing range if frail.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for OPIPZA (OPIPZA).

Breastfeeding	No data on excretion in human milk; M/P ratio unknown. Due to potential for adverse effects (drowsiness, dystonia) in nursing infants, caution advised. Consider benefits of breastfeeding vs potential risk.
Teratogenic Risk	There is insufficient human data; animal studies not identified. Risk cannot be excluded. First trimester: theoretical risk based on mechanism (dopamine antagonist). Second and third trimesters: risk of extrapyramidal symptoms and withdrawal in neonates if exposed near term.
Fetal Monitoring