Apremilast

Apremilast is an oral small molecule inhibitor of phosphodiesterase 4 (PDE4) specific for cyclic adenosine monophosphate (cAMP). PDE4 inhibition results in increased intracellular cAMP levels.

• OTEZLA/OTEZLA XR, an inhibitor of phosphodiesterase 4 (PDE4), is indicated for the treatment of: Adult patients with: Active psoriatic arthritis ( 1.1 ) Plaque psoriasis who are candidates for phototherapy or systemic therapy ( 1.2 ) Oral ulcers associated with Behçet's Disease ( 1.3 ) Pediatric patients 6 years of age and older with: Active psoriatic arthritis ( 1.1 ) Moderate to severe plaque psoriasis who are candidates for phototherapy or systemic therapy ( 1.2 ) In the pediatric population, OTEZLA is indicated for patients weighing at least 20 kg, and OTEZLA XR is indicated for patients weighing at least 50 kg. 1.1 Psoriatic Arthritis OTEZLA is indicated for the treatment of adult patients and pediatric patients 6 years of age and older and weighing at least 20 kg with active psoriatic arthritis.ICD-10: L40.50, L40.9

• OTEZLA/OTEZLA XR is contraindicated in patients with a known hypersensitivity to apremilast or to any of the excipients in the formulation [see Warnings and Precautions (5.1) , see Adverse Reactions (6.1) ] .contraindicated

To reduce the risk of gastrointestinal symptoms, titrate to recommended dosage as follows: Adults with Psoriatic Arthritis, Plaque Psoriasis, or Behçet's Disease See Table 1 for the initial titration schedule. Recommended maintenance dosage is OTEZLA 30 mg twice daily or OTEZLA XR 75 mg once daily ( 2.1 ) Pediatric Patients 6 Years of Age and Older and Weighing at Least 20 kg with Psoriatic Arthritis or Moderate to Severe Plaque Psoriasis See Table 2 for the initial titration schedule ( 2.1 ) For patients weighing 50 kg or more : Recommended maintenance dosage is OTEZLA 30 mg twice daily or OTEZLA XR 75 mg once daily ( 2.1 ) For patients weighing 20 kg to less than 50 kg : Recommended maintenance dosage is OTEZLA 20 mg twice daily ( 2.1 ) Dosage in Patients with Severe Renal Impairment : Adult Patients : For initial dosage titration, titrate using only morning schedule listed in Table 1 and skip afternoon doses.

Hypersensitivity : Cases of angioedema and anaphylaxis have been reported during post marketing surveillance. Avoid the use of OTEZLA/OTEZLA XR in patients with known hypersensitivity to apremilast or to any of the excipients in the formulation. If signs or symptoms of serious hypersensitivity reactions develop during treatment, discontinue OTEZLA/OTEZLA XR and institute appropriate therapy ( 5.1 ) Diarrhea, Nausea, and Vomiting : Consider OTEZLA/OTEZLA XR dosage reduction or suspension if patients develop severe diarrhea, nausea, or vomiting ( 5.2 ) Depression : Advise patients, their caregivers, and families to be alert for the emergence or worsening of depression, suicidal thoughts or other mood changes and if such changes occur to contact their healthcare provider. Carefully weigh risks and benefits of treatment with OTEZLA/OTEZLA XR in patients with a history of depression and/or suicidal thoughts or behavior ( 5.3 ) Weight Decrease : Monitor weight regularly. If unexplained or clinically significant weight loss occurs, evaluate weight loss and consider discontinuation of OTEZLA/OTEZLA XR ( 5.4 ) Drug Interactions : Use with strong cytochrome P450 enzyme inducers (e.g., rifampin, phenobarbital, carbamazepine, phenytoin) is not recommended because loss of efficacy may occur ( 5.5 , 7.1 ) 5.1 Hypersensitivity Hypersensitivity reactions, including cases of angioedema and anaphylaxis, have been reported during post marketing surveillance. Avoid the use of OTEZLA/OTEZLA XR in patients with known hypersensitivity to apremilast or to any of the excipients in the formulation.

The following adverse reactions are described elsewhere in the labeling: Hypersensitivity [see Warnings and Precautions (5.1) ] Diarrhea, Nausea, and Vomiting [see Warnings and Precautions (5.2) ] Depression [see Warnings and Precautions (5.3) ] Weight Decrease [see Warnings and Precautions (5.4) ] Drug Interactions [see Warnings and Precautions (5.5) ] Psoriatic Arthritis : The most common adverse reactions (≥ 5%) are diarrhea, nausea, and headache ( 6.1 ) Plaque Psoriasis : The most common adverse reactions (≥ 5%) are diarrhea, nausea, upper respiratory tract infection, and headache, including tension headache ( 6.1 ) Behçet's Disease : The most common adverse reactions (≥ 10%) are diarrhea, nausea, headache, and upper respiratory tract infection ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Amgen Inc. at 1-800-77-AMGEN (1-800-772-6436) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. Psoriatic Arthritis Clinical Trials OTEZLA was evaluated in three multicenter, randomized, double-blind, placebo-controlled trials (PsA-1, PsA-2, and PsA-3) of similar design in adult subjects with active psoriatic arthritis [see Clinical Studies (14.1) ] .

Severe Renal Impairment : Increased systemic exposure of OTEZLA has been observed. For adults and for pediatric patients weighing 50 kg or more, reduce dosage to OTEZLA 30 mg once daily. For pediatric patients weighing 20 kg to less than 50 kg, reduce dosage to OTEZLA 20 mg once daily ( 2.3 , 8.6 ). 8.1 Pregnancy Risk Summary Available data with OTEZLA use in pregnant women have not identified a drug-associated risk of major birth defects or adverse maternal or fetal outcomes (see Data ) . In animal embryo-fetal development studies, the administration of apremilast to pregnant cynomolgus monkeys during organogenesis resulted in dose-related increases in abortion/embryo-fetal death at dose exposures approximately 2-times the maximum recommended human therapeutic dose (MRHD) and no adverse effect at an exposure of 1.4-times the MRHD. When apremilast was administered to pregnant mice during organogenesis, there were no apremilast-induced malformations up to exposures 4-times the MRHD. Based on findings from animal reproduction studies, OTEZLA/OTEZLA XR may increase the risk for fetal loss (see Data ) . Advise pregnant women of the potential risk of fetal loss. The background risk of major birth defects and miscarriage for the indicated populations is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S.

Metabolism

Absorption OTEZLA when taken orally is absorbed with an absolute bioavailability of ~73%, with peak plasma concentrations (C max ) occurring at a median time (t max ) of ~2.5 hours. Co-administration with food does not alter the extent of absorption of OTEZLA.

• Mar 21, 2014NDANDA205437Amgen Inc

1. 1Diarrhoea24,44517%
2. 2Nausea22,01815%
3. 3Psoriasis20,36614%
4. 4Headache17,78412%
5. 5Drug Ineffective15,43911%
6. 6Abdominal Discomfort8,1455.7%
7. 7Psoriatic Arthropathy7,9585.5%
8. 8Pain6,7334.7%
9. 9Rash6,6074.6%
10. 10Vomiting6,4274.5%
11. 11Arthralgia6,3174.4%
12. 12Fatigue6,1124.2%
13. 13Depression5,4883.8%
14. 14Off Label Use5,1483.6%
15. 15Weight Decreased4,9923.5%

The 10 most recently updated of 170 ClinicalTrials.gov registrations naming Apremilast as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Phase 2 Study of Apremilast in Women and Men With Alcohol Use Disorder
  Recruiting · Phase 2 · Interventional · 80 enrolled · Yale University
  NCT07029529updated 2026-06-08
• Utilization of a Microdevice for Psoriasis and Atopic Dermatitis
  Not yet recruiting · Phase 4 · Interventional · 10 enrolled · University of California, San Francisco
  NCT07352566updated 2026-06-03
• Apremilast for Erythema Multiforme
  Completed · Phase 2 · Interventional · 6 enrolled · Robert Micheletti
  NCT05875714updated 2026-06-03
• Methotrexate Versus Apremilast for Pruritus in Psoriasis
  Not yet recruiting · Phase 4 · Interventional · 80 enrolled · Zarmeen Khawar
  NCT07432386updated 2026-05-15
• Human Laboratory Study of Apremilast for Alcohol Use Disorder
  Recruiting · Phase 2 · Interventional · 100 enrolled · National Institute on Alcohol Abuse and Alcoholism (NIAAA)
  NCT07325266updated 2026-05-01
• [18F]PF-06445974 to Image PDE4B in Major Depressive Disorder Using PET
  Recruiting · Phase 1 · Interventional · 108 enrolled · National Institute of Mental Health (NIMH)
  NCT05703685updated 2026-04-24
• EFFICACY OF ROFLUMILAST IN THE TREATMENT OF FLEXURAL AND/OR GENITAL PSORIASIS: A RANDOMIZED CONTROLLED TRIAL.
  Not yet recruiting · Phase 2 · Interventional · 56 enrolled · Eman Raafat Said
  NCT07543640updated 2026-04-22
• Apremilast Pediatric Study in Children With Active Juvenile Psoriatic Arthritis
  Recruiting · Phase 3 · Interventional · 60 enrolled · Amgen
  NCT04804553updated 2026-04-20
• A Study to Evaluate the Efficacy and Safety of ESK-001 in Patients With Moderate to Severe Plaque Psoriasis
  Completed · Phase 3 · Interventional · 912 enrolled · Alumis Inc
  NCT06586112updated 2026-04-13
• A Study in Patients With Moderate to Severe Plaque Psoriasis to Evaluate the Efficacy and Safety of ESK-001
  Completed · Phase 3 · Interventional · 862 enrolled · Alumis Inc
  NCT06588738updated 2026-04-13

Frequently asked questions

How does Apremilast work?

Apremilast is an oral small molecule inhibitor of phosphodiesterase 4 (PDE4) specific for cyclic adenosine monophosphate (cAMP). PDE4 inhibition results in increased intracellular cAMP levels.

What is Apremilast used for?

According to FDA labeling, Apremilast carries indications including: OTEZLA/OTEZLA XR, an inhibitor of phosphodiesterase 4 (PDE4), is indicated for the treatment of: Adult patients with: Active psoriatic arthritis ( 1.1 ) Plaque psoriasis who are candidates for phototherapy or systemic therapy ( 1.2 ) Oral ulcers associated with Behçet's Disease ( 1.3 ) Pediatric patients 6 years of age and older with: Active psoriatic arthritis ( 1.1 ) Moderate to severe plaque psoriasis who are candidates for phototherapy or systemic therapy ( 1.2 ) In the pediatric population, OTEZLA is indicated for patients weighing at least 20 kg, and OTEZLA XR is indicated for patients weighing at least 50 kg. 1.1 Psoriatic Arthritis OTEZLA is indicated for the treatment of adult patients and pediatric patients 6 years of age and older and weighing at least 20 kg with active psoriatic arthritis.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Apremilast?

Apremilast is classified as Selective immunosuppressants, Phosphodiesterase 4 Inhibitor, Phosphodiesterase 4 Inhibitors, Decreased Leukotriene Production.

What are the brand names for Apremilast?

Apremilast is marketed under brand names including Otezla.

What are the contraindications for Apremilast?

Apremilast labeling lists contraindications including: OTEZLA/OTEZLA XR is contraindicated in patients with a known hypersensitivity to apremilast or to any of the excipients in the formulation [see Warnings and Precautions (5.1) , see Adverse Reactions (6.1) ] .. Always consult the full prescribing information and a clinician.