Peringatan Keamanan

The oral LD50 in mice was greater than 2000 mg/kg in mice. In rats, oral LD50 was 2000 mg/kg males and 300 mg/kg in females.L7505

Overdose information

In healthy subjects receiving a maximum dose of 100 mg (given as 50 mg twice daily) for about 5 days, no significant toxicity was observed. In cases of an overdose, supportive and symptomatic treatment should be administered. Contact the local poison control center for the most recent overdose management for apremilast.L7502

Apremilast

DB05676

small molecule approved investigational

Deskripsi

Apremilast, also known as Otezla, is a phosphodiesterase 4 (PDE4) inhibitor used to treat various types of symptoms resulting from certain inflammatory autoimmune diseases. It belongs to the same drug class as Roflumilast and Crisaborole.A181244,L7495 Initially approved in 2014, it is marketed by Celgene.L7501 In July 2019, apremilast was granted a new FDA approval for the treatment of oral ulcers associated with Behcet's disease, an autoimmune condition that causes recurrent skin, blood vessel, and central nervous system inflammation.A181216

Struktur Molekul 2D

Berat 460.5
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The average elimination half-life of this drug ranges from 6-9 hours.[A181226,L7501]
Volume Distribusi The average apparent volume of distribution (Vd) is about 87 L, suggesting that apremilast is distributed in the extravascular compartment.[L7498]
Klirens (Clearance) In healthy patients, the plasma clearance of apremilast is about 10 L/hour.[L7498]

Absorpsi

An oral dose of apremilast is well-absorbed and the absolute bioavailability is approximately 73%. Tmax is approximately 2.5 hoursL7501 and Cmax has been reported to be approximately 584 ng/mL in one pharmacokinetic study.A181229 Food intake does not appear to affect apremilast absorption.L7501

Metabolisme

Apremilast is heavily metabolized by various pathways, which include oxidation, hydrolysis, in addition to conjugation. About 23 metabolites are produced from its metabolism.A3737 The CYP3A4 primarily mediates the oxidative metabolism of this drug, with smaller contributions from CYP1A2 and CYP2A6 enzymes.L7498 The main metabolite of apremilast, M12, is an inactive glucuronide conjugate form of the O-demethylated drug.L7498 Some other major metabolites, M14 and M16, are significantly less active in the inhibition of PDE4 and inflammatory mediators than their parent drug, apremilast. After an oral dose, unchanged apremilast (45%) and the inactive metabolite, O-desmethyl apremilast glucuronide (39%) are found in the plasma. A181235 Minor metabolites M7 and M17 are active, but are only present in about 2% or less of apremilast concentrations, and likely not significant contributors to the actions of apremilast.A181235

Rute Eliminasi

Only 3% and 7% of an apremilast dose are detected in the urine and feces as unchanged drug, respectively, indicating extensive metabolism and high absorption.L7498

Interaksi Makanan

2 Data
  • 1. Avoid St. John's Wort. Apremilast is a CYP3A substrate; therefore, co-administration with St. John's wort, a CYP3A inducer, may reduce the serum level of apremilast.
  • 2. Take with or without food.

Interaksi Obat

1632 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Apremilast.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Apremilast.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Apremilast.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Apremilast.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Apremilast.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Apremilast.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Apremilast.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Apremilast.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Apremilast.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Apremilast.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Apremilast.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Apremilast.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Apremilast.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Apremilast.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Apremilast.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Apremilast.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Apremilast.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Apremilast.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Apremilast.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Apremilast.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Apremilast.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Apremilast.
Cladribine Apremilast may increase the immunosuppressive activities of Cladribine.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Apremilast.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Apremilast.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Apremilast.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Apremilast.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Apremilast.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Apremilast.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Apremilast.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Apremilast.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Apremilast.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Apremilast.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Apremilast.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Apremilast.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Apremilast.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Apremilast.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Apremilast.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Apremilast.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Apremilast.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Apremilast.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Apremilast.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Apremilast.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Apremilast.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Apremilast.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Apremilast.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Apremilast.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Apremilast.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Apremilast.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Apremilast.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Apremilast.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Apremilast.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Apremilast.
Topotecan The risk or severity of adverse effects can be increased when Topotecan is combined with Apremilast.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Apremilast.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Apremilast.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Apremilast.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Apremilast.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Apremilast.
Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Apremilast.
Mitoxantrone The risk or severity of adverse effects can be increased when Mitoxantrone is combined with Apremilast.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Apremilast.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Apremilast.
Decitabine The risk or severity of adverse effects can be increased when Decitabine is combined with Apremilast.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with Apremilast.
Stepronin The risk or severity of adverse effects can be increased when Stepronin is combined with Apremilast.
Castanospermine The risk or severity of adverse effects can be increased when Castanospermine is combined with Apremilast.
Vorinostat The risk or severity of adverse effects can be increased when Vorinostat is combined with Apremilast.
2-Methoxyethanol The risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Apremilast.
Brequinar The risk or severity of adverse effects can be increased when Brequinar is combined with Apremilast.
Interferon alfa The risk or severity of adverse effects can be increased when Interferon alfa is combined with Apremilast.
Glatiramer The risk or severity of adverse effects can be increased when Glatiramer is combined with Apremilast.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Apremilast.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Human interferon omega-1 is combined with Apremilast.
Mepolizumab The risk or severity of adverse effects can be increased when Apremilast is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Apremilast is combined with Abetimus.
Belatacept The risk or severity of adverse effects can be increased when Apremilast is combined with Belatacept.
Pralatrexate The risk or severity of adverse effects can be increased when Apremilast is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Apremilast is combined with Wortmannin.
Eribulin The risk or severity of adverse effects can be increased when Apremilast is combined with Eribulin.
Belimumab The risk or severity of adverse effects can be increased when Apremilast is combined with Belimumab.
Carfilzomib The risk or severity of adverse effects can be increased when Apremilast is combined with Carfilzomib.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Apremilast is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Apremilast is combined with Obinutuzumab.
Vedolizumab The risk or severity of adverse effects can be increased when Apremilast is combined with Vedolizumab.
Blinatumomab The risk or severity of adverse effects can be increased when Apremilast is combined with Blinatumomab.
Dinutuximab The risk or severity of adverse effects can be increased when Apremilast is combined with Dinutuximab.
Tixocortol The risk or severity of adverse effects can be increased when Apremilast is combined with Tixocortol.
Peginterferon beta-1a The risk or severity of adverse effects can be increased when Apremilast is combined with Peginterferon beta-1a.
Antilymphocyte immunoglobulin (horse) The risk or severity of adverse effects can be increased when Apremilast is combined with Antilymphocyte immunoglobulin (horse).
Tepoxalin The risk or severity of adverse effects can be increased when Apremilast is combined with Tepoxalin.
Ixekizumab The risk or severity of adverse effects can be increased when Apremilast is combined with Ixekizumab.
Ravulizumab The risk or severity of adverse effects can be increased when Apremilast is combined with Ravulizumab.
Pirarubicin The risk or severity of adverse effects can be increased when Apremilast is combined with Pirarubicin.
Voclosporin The risk or severity of adverse effects can be increased when Apremilast is combined with Voclosporin.
Peficitinib The risk or severity of adverse effects can be increased when Apremilast is combined with Peficitinib.
Brodalumab The risk or severity of adverse effects can be increased when Apremilast is combined with Brodalumab.
Sirukumab The risk or severity of adverse effects can be increased when Apremilast is combined with Sirukumab.
Guselkumab The risk or severity of adverse effects can be increased when Apremilast is combined with Guselkumab.
Ocrelizumab The risk or severity of adverse effects can be increased when Apremilast is combined with Ocrelizumab.

Target Protein

Phosphodiesterase isozyme 4 PDE4
Cyclin-dependent kinase 4 CDK4
Cyclin-dependent kinase 6 CDK6

Referensi & Sumber

Artikel (PubMed)
  • PMID: 14717786
    Molostvov G, Morris A, Rose P, Basu S, Muller G: The effects of selective cytokine inhibitory drugs (CC-10004 and CC-1088) on VEGF and IL-6 expression and apoptosis in myeloma and endothelial cell co-cultures. Br J Haematol. 2004 Feb;124(3):366-75.
  • PMID: 25864487
    Abdulrahim H, Thistleton S, Adebajo AO, Shaw T, Edwards C, Wells A: Apremilast: a PDE4 inhibitor for the treatment of psoriatic arthritis. Expert Opin Pharmacother. 2015 May;16(7):1099-108. doi: 10.1517/14656566.2015.1034107. Epub 2015 Apr 11.
  • PMID: 21859393
    Hoffmann M, Kumar G, Schafer P, Cedzik D, Capone L, Fong KL, Gu Z, Heller D, Feng H, Surapaneni S, Laskin O, Wu A: Disposition, metabolism and mass balance of (14)Capremilast following oral administration. Xenobiotica. 2011 Dec;41(12):1063-75. doi: 10.3109/00498254.2011.604745. Epub 2011 Aug 23.
  • PMID: 15598081
    Suzuki Kurokawa M, Suzuki N: Behcet's disease. Clin Exp Med. 2004 Sep;4(1):10-20.
  • PMID: 29385021
    Fertig BA, Baillie GS: PDE4-Mediated cAMP Signalling. J Cardiovasc Dev Dis. 2018 Jan 31;5(1). pii: jcdd5010008. doi: 10.3390/jcdd5010008.
  • PMID: 30984205
    Tong B, Liu X, Xiao J, Su G: Immunopathogenesis of Behcet's Disease. Front Immunol. 2019 Mar 29;10:665. doi: 10.3389/fimmu.2019.00665. eCollection 2019.
  • PMID: 27869356
    Young M, Roebuck HL: Apremilast, an oral phosphodiesterase 4 (PDE4) inhibitor: A novel treatment option for nurse practitioners treating patients with psoriatic disease. J Am Assoc Nurse Pract. 2016 Dec;28(12):683-695. doi: 10.1002/2327-6924.12428. Epub 2016 Nov 21.
  • PMID: 26097790
    Liu Y, Zhou S, Nissel J, Wu A, Lau H, Palmisano M: The pharmacokinetic effect of coadministration of apremilast and methotrexate in individuals with rheumatoid arthritis and psoriatic arthritis. Clin Pharmacol Drug Dev. 2014 Nov;3(6):456-465. doi: 10.1002/cpdd.109. Epub 2014 May 8.
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