Apremilast
OTEZLA
What it isPDE4 inhibitor that raises intracellular cAMP; plaque psoriasis, psoriatic arthritis, and Behcet oral ulcers.
Why this oneIt is oral and requires neither routine laboratory monitoring nor tuberculosis screening, unlike biologic therapy.
What limits itEarly diarrhea, nausea, and weight loss can end treatment; depression is labeled, and efficacy trails biologics.
FDA-approved for
- psoriatic arthritis (2014)
- plaque psoriasis, Behcet oral ulcers
Off-label
- recalcitrant hand and foot dermatitis
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Psoriatic arthritis | adults | 5-day titration (Days 1-5) | 30 mg BID | 30 mg BID |
| Plaque psoriasis | adults | 5-day titration (Days 1-5) | 30 mg BID | 30 mg BID |
| Behçet's disease | adults | 5-day titration (Days 1-5) | 30 mg BID | 30 mg BID |
| Psoriatic arthritis or moderate-severe plaque psoriasis | peds ≥6 y, ≥50 kg | titration | 30 mg BID | 30 mg BID |
| Psoriatic arthritis or moderate-severe plaque psoriasis | peds ≥6 y, 20-<50 kg | titration | 20 mg BID | 20 mg BID |
Titration 5-day up-titration (Days 1-5) to maintenance dose to reduce GI symptoms.
Renal Severe renal impairment: reduce to 30 mg QD (adults & peds ≥50 kg) or 20 mg QD (peds 20-<50 kg); titrate using AM schedule only, skip afternoon doses.
Hepatic No adjustment needed
Instructions
- Swallow tablets whole; OTEZLA XR must not be crushed, split, or chewed.
- May take with or without food.
- Consider dose reduction or suspension for severe diarrhea, nausea, or vomiting.
Cautions
- Hypersensitivity: angioedema and anaphylaxis reported
- Severe diarrhea, nausea, vomiting (higher risk ≥65 y or with volume-depleting/hypotensive drugs)
- Depression, suicidal thoughts/mood changes
- Weight decrease — monitor weight
- Avoid strong CYP450 inducers (rifampin, phenobarbital, carbamazepine, phenytoin) — loss of efficacy
Adverse reactions
- Diarrhea
- Nausea
- Headache
- Upper respiratory tract infection (plaque psoriasis)
- Vomiting
Pregnancy May increase risk of fetal loss (animal embryo-fetal death); advise pregnant women of the risk.
Lactation No human data; detected in animal milk.
NO BOXED WARNINGS
Principal riskDiarrhea and weight loss; depression is labeled
Cost, est. cash$1,000–$15,000+/month
Generic entry2028 est.
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilitySerious infection, cytopenias, hepatic injury and malignancy risk require laboratory and clinical monitoring.
Mechanism of action: Apremilast ballicule
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