Basic information Description Uses Metabolism and Drug interaction safety information side effects References Safety Related Supplier
ChemicalBook >  Product Catalog >  Biochemical Engineering >  Inhibitors >  Metabolism >  PDE inhibitors >  ApreMilast

ApreMilast

Basic information Description Uses Metabolism and Drug interaction safety information side effects References Safety Related Supplier
ApreMilast Basic information
ApreMilast Chemical Properties
  • Boiling point:741.3±60.0 °C(Predicted)
  • Density 1.381
  • pka14.01±0.20(Predicted)
  • CAS DataBase Reference608141-41-9
ApreMilast Usage And Synthesis
  • DescriptionApremilast (Otezla) was approved by the FDA on March 21, 2014 for the treatment of adult patients with active psoriatic arthritis. Apremilast is a member of a new class of oral small molecule inhibitors of the phosphosphodiesterase 4 (PDE4) enzyme. When PDE4 is inhibited in immune cells, it results in elevation of intracellular cyclic adenosine monophosphate (cAMP) levels, which can regulate inflammatory mediators. The current clinical data indicate that apremilast is an effective and well tolerated option for the management of psoriasis and PsA in adults.
  • UsesTreating active psoriatic arthritis. It is also used to treat moderate to severe plaque psoriasis in certain patients.
  • Metabolism and Drug interactionOral administration of apremilast has an absolute biovailability of 73% with peak concentration at 2.5 hours (Tmax). The half-life of apremilast is 6-9 hours. Apremilast is metabolized by the both cytochrome (CYP) and non-CYP pathways. In vitro studies have demonstrated that apremilast metabolism is primarily mediated by the CYP3A4 pathway. Thus, concomitant use of apremilast with CYP450 enzyme inducers (such as rifampin, phenobarbital, carbamazepine, phenytoin) is not recommended. There are no significant drug-drug interactions with oral contraceptives, ketoconazole, or methotrexate.
  • safety information1.Apremilast may cause depression. The risk may be greater in patients who have a history of depression or suicidal thoughts or actions. Families and caregivers must closely watch patients who take apremilast. It is important to keep in close contact with the patient's doctor. Tell the doctor right away if the patient has new, worsened, or sudden symptoms, such as depression; anxiety, restlessness, or irritability; panic attacks; or any changes in behavior. Contact the doctor right away if any signs of suicidal thoughts or actions occur.
    2.Apremilast may cause weight loss. You will need to have regular weight checks while you are taking apremilast.
  • side effectsDiarrhea; headache; nausea; weight loss.
  • References1. http://www.rheumatology.org/Learning-Center/Publications-Communications/Drug-Safety/Hotline-Apremilast-for-the-Treatment-of-Psoriatic-Arthritis
    2. https://www.ncbi.nlm.nih.gov/pubmed/26220911
    3. https://www.drugs.com/cdi/apremilast.html
    4. http://reference.medscape.com/drug/otezla-apremilast-999915
  • DefinitionChEBI: A member of the class of isoindoles that is isoindole-1,3-dione substituted at position 4 by an acetamido group and at position 1 by a 1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl group. Used for treatment of psoriatic arthritis.
  • Enzyme inhibitorThis thalidomide-like psoriasis drug (FW = 460.50 g/mol; CAS 608141-41-9; Solubility: 90 mg/mL DMSO; <1 mg/mL H2O), also known as CC-10004, Otezla? and N-[2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methyl-sulfonyl)ethyl]-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]acetamide, is a potent, orally active phosphodiesterase inhibitor that targets phosphodiesterase PDE4 (IC50 = 74 nM), itself a proinflammatory mediator, and TNF-α, IC50 = 77 nM. Apremilast inhibits PBMC production of the chemokines CXCL9 and CXCL10, cytokines interferon-γ and tumor necrosis factor-α (TNF-α), and interleukins IL-2, IL-12 and IL- 23 from human rheumatoid synovial membrane cultures. Apremilast significantly reduces clinical scores in both murine models of arthritis over a ten-day treatment period and maintains healthy joint architecture in a dose-dependent manner. Unlike rolipram, however, apremilast demonstrated no adverse behavioral effects in na?ve mice. Otezla is specifically indicated by the Food & Drug Administration for the treatment of patients with moderate to severe plaque psoriasis who are typically candidates for phototherapy or systemic therapy. That said, the specific mechanism(s) for therapeutic action in psoriatic arthritis patients and psoriasis patients is unclear.
ApreMilast(608141-41-9)Related Product Information
ApreMilastSupplierMore
  • Company Name:CGeneTech (Suzhou, China) Co., Ltd. Gold
  • Tel:18151113715 0512-62956963
  • Email:sales@cgenetech.com.cn
  • Products Intro:Product Name:Apremilast
    CAS:608141-41-9
    Purity:99% HPLC%
  •  
  • Company Name:Suzhou Huihe Pharmaceutical Co. Ltd. Gold
  • Tel:86-0512-88819360/88985990
  • Email:asynderm@163.com
  • Products Intro:Product Name:Apremilast
    CAS:608141-41-9
    Purity:≥99% Package:1kg,5kg,10kg
  •  
  • Company Name:Sichuan Welltzpharm Inc. Gold
  • Tel:028-84249321
  • Email:info@welltzpharm.com;info@welltzpharm.com
  • Products Intro:Product Name:ApreMilast
    CAS:608141-41-9
    Purity:99.8%HPLC Package:25g;100g;500g;1kg;5kg;25kg
  •  
  • Company Name:Heta Pharm & Chem CO.,Ltd. Gold
  • Tel:+86-571-88298691 89905385
  • Email:sales@hetapharm.com;sales2@hetapharm.com
  • Products Intro:Product Name:Apremilast
    CAS:608141-41-9
    Purity:99%
  •  
  • Company Name:Zhuhai Yourun Co., Ltd. Gold
  • Tel:13923369215
  • Email:zhuhaiyourun@126.com;
  • Products Intro:Product Name:Apremilast (CC-10004)
    CAS:608141-41-9
    Purity:>99% HPLC Package:25KG.5KG;1KG
  •