Clinical data | |
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Trade names | Daxas, Daliresp, Zoryve, others |
AHFS/Drugs.com | Monograph |
MedlinePlus | a611034 |
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Routes of administration | By mouth, topical |
Drug class | PDE4 inhibitor |
ATC code | |
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Pharmacokinetic data | |
Bioavailability | 79% [4] [3] [8] [9] |
Protein binding | 99% [4] [3] [8] [9] |
Metabolism | Hepatic via CYP1A2 & CYP3A4 [4] [3] [8] [9] |
Elimination half-life | 17 hours (30 hours [active metabolite]) [4] [3] [8] [9] |
Excretion | Urine (70%) [4] [3] [8] [9] |
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PDB ligand | |
CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.210.960 |
Chemical and physical data | |
Formula | C17H14Cl2F2N2O3 |
Molar mass | 403.21 g·mol−1 |
3D model (JSmol) | |
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Roflumilast, sold under the brand name Daxas among others, is a medication used for the treatment of chronic obstructive pulmonary disease, [4] plaque psoriasis, [5] seborrheic dermatitis, [6] and atopic dermatitis. [5] It acts as a selective, long-acting inhibitor of the enzyme phosphodiesterase-4 (PDE-4). [10] It has anti-inflammatory effects. [10] [11] [12]
It was approved for medical use in the European Union in 2010, [7] in the United States in 2011, [4] and in Canada in 2017. [1] It is available as a generic medication. [13]
Roflumilast is indicated for the treatment of severe chronic obstructive pulmonary disease (COPD), [4] plaque psoriasis, [5] [14] seborrheic dermatitis, [6] and atopic dermatitis, [5] [15]
It is used in the prevention of exacerbations (lung attacks) in severe chronic obstructive pulmonary disease (COPD). [3] [4] [7] [8] [9]
Common (1–10% incidence) adverse effects include diarrhea, weight loss, nausea, headache, insomnia, decreased appetite, abdominal pain, rhinitis, sinusitis, urinary tract infection, and depression. [4] [3] [8] [9] [16]
In June 2010, it was approved in the European Union for severe COPD associated with chronic bronchitis. [7] [17] In February 2011, it gained FDA approval in the United States for reducing COPD exacerbations. [18] [19]
Infliximab, a chimeric monoclonal antibody, sold under the brand name Remicade among others, is a medication used to treat a number of autoimmune diseases. This includes Crohn's disease, ulcerative colitis, rheumatoid arthritis, ankylosing spondylitis, psoriasis, psoriatic arthritis, and Behçet's disease. It is given by slow injection into a vein, typically at six- to eight-week intervals.
Pimecrolimus is an immunosuppressant drug of the calcineurin inhibitor class used in the treatment of atopic dermatitis (eczema).
Desonide (INN) is a low-potency topical corticosteroid anti-inflammatory that has been available since the 1970s. It is primarily used to treat atopic dermatitis (eczema), seborrheic dermatitis, contact dermatitis and psoriasis in both adults and children. It has a fairly good safety profile and is available as a cream, ointment, lotion, and as a foam under the tradename Verdeso Foam. Other trade names for creams, lotions, and ointments include Tridesilon, DesOwen, Desonate. It is a group VI corticosteroid under US classification, the second least potent group.
Long-acting β adrenoceptor agonists (LABAs) are beta-adrenergic agonists usually prescribed for moderate-to-severe persistent asthma and chronic obstructive pulmonary disease (COPD).
Cilomilast is a drug which was developed for the treatment of respiratory disorders such as asthma and chronic obstructive pulmonary disease (COPD). It is orally active and acts as a selective phosphodiesterase-4 inhibitor.
Arformoterol, sold under the brand name Brovana among others, is a medication used for the treatment of chronic obstructive pulmonary disease (COPD).
Indacaterol is an ultra-long-acting beta-adrenoceptor agonist developed by Novartis. It needs to be taken only once a day, unlike the related drugs formoterol and salmeterol. It is licensed only for the treatment of chronic obstructive pulmonary disease (COPD). It is delivered as an aerosol formulation through a dry powder inhaler.
A phosphodiesterase-4 inhibitor, commonly referred to as a PDE4 inhibitor, is a drug used to block the degradative action of phosphodiesterase 4 (PDE4) on cyclic adenosine monophosphate (cAMP). It is a member of the larger family of PDE inhibitors. The PDE4 family of enzymes are the most prevalent PDE in immune cells. They are predominantly responsible for hydrolyzing cAMP within both immune cells and cells in the central nervous system.
Piclamilast, is a selective PDE4 inhibitor. It is comparable to other PDE4 inhibitors for its anti-inflammatory effects. It has been investigated for its applications to the treatment of conditions such as chronic obstructive pulmonary disease, bronchopulmonary dysplasia and asthma. It is a second generation compound that exhibits structural functionalities of the PDE4 inhibitors cilomilast and roflumilast. The structure for piclamilast was first elucidated in a 1995 European patent application. The earliest mention of the name "piclamilast" was used in a 1997 publication.
Filaminast was a drug candidate developed by Wyeth-Ayerst. It is a phosphodiesterase 4 inhibitor and an analog of rolipram, which served as a prototype molecule for several development efforts. It was discontinued after a Phase II trial showed that its therapeutic window was too narrow; it could not be dosed high enough without causing significant side effects, which was a problem with the rolipram class of molecules.
Tofacitinib, sold under the brand Xeljanz among others, is a medication used to treat rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, polyarticular course juvenile idiopathic arthritis, and ulcerative colitis. It is a janus kinase (JAK) inhibitor, discovered and developed by the National Institutes of Health and Pfizer.
Ruxolitinib, sold under the brand name Jakafi among others, is a medication used for the treatment of intermediate or high-risk myelofibrosis, a type of myeloproliferative neoplasm that affects the bone marrow; polycythemia vera, when there has been an inadequate response to or intolerance of hydroxyurea; and steroid-refractory acute graft-versus-host disease. Ruxolitinib is a Janus kinase inhibitor. It was developed and marketed by Incyte Corp in the US under the brand name Jakafi, and by Novartis elsewhere in the world, under the brand name Jakavi.
Olodaterol is an ultra-long-acting β adrenoreceptor agonist (ultra-LABA) used as an inhalation for treating people with chronic obstructive pulmonary disease (COPD). It is manufactured by Boehringer Ingelheim.
Apremilast, sold under the brand name Otezla among others, is a medication for the treatment of certain types of psoriasis and psoriatic arthritis. The drug acts as a selective inhibitor of the enzyme phosphodiesterase 4 (PDE4) and inhibits spontaneous production of TNF-alpha from human rheumatoid synovial cells. It is taken by mouth.
Dupilumab, sold under the brand name Dupixent, is a monoclonal antibody blocking interleukin 4 and interleukin 13, used for allergic diseases such as atopic dermatitis (eczema), asthma and nasal polyps which result in chronic sinusitis. It is also used for the treatment of eosinophilic esophagitis and prurigo nodularis.
Fluticasone furoate/vilanterol, sold under the brand name Breo Ellipta among others, is a combination medication for the treatment of chronic obstructive pulmonary disease (COPD) and asthma. It contains fluticasone furoate, an inhaled corticosteroid, and vilanterol, an ultra-long-acting β2 agonist (ultra-LABA).
Umeclidinium bromide/vilanterol, sold under the brand name Anoro Ellipta, among others, is a fixed-dose combination medication for the treatment of chronic obstructive pulmonary disease (COPD). It is administered by inhalation.
Crisaborole, sold under the brand name Eucrisa among others, is a nonsteroidal topical medication used for the treatment of mild-to-moderate atopic dermatitis (eczema) in adults and children.
Revefenacin, sold under the brand name Yupelri, is a medication for the treatment of chronic obstructive pulmonary disease (COPD). It was approved for use in the United States in 2018. It was developed by Theravance Biopharma and is marketed by Mylan. Revefenacin is formulated as a solution that is nebulized and inhaled.
Fluticasone furoate/umeclidinium bromide/vilanterol, sold under the brand name Trelegy Ellipta among others, is a fixed-dose combination inhaled medication that is used for the maintenance treatment of chronic obstructive pulmonary disease (COPD). The medications work in different ways: fluticasone furoate is an inhaled corticosteroid (ICS), umeclidinium is a long-acting muscarinic antagonist (LAMA), and vilanterol is a long-acting beta-agonist (LABA).