Disease-modifying Antirheumatic Agents

DrugDrug NameDrug Indication
DB00005EtanerceptEtanercept is indicated for the treatment of moderately to severely active rheumatoid arthritis in adults and chronic moderate to severe plaque psoriasis in adults. It is also used to manage signs and symptoms of polyarticular idiopathic arthritis in those aged 4 to 17 after insufficient response to one or more disease-modifying anti-rheumatic drugs. Etanercept is also used to improve psoriatic arthritis and ankylosing spondylitis.
DB00026AnakinraFor the treatment of adult rheumatoid arthritis and treatment of Neonatal-Onset Multisystem Inflammatory Disease (NOMID).
DB00051AdalimumabThe following are conditions for which adalimumab has been indicated [F2118], [FDA label], [L4805], [A40001], [A40002], [L4806]. Rheumatoid Arthritis (Moderate to Severe) Juvenile Idiopathic Arthritis (Moderately to Severely Active) Psoriatic Arthritis (Active) Ankylosing Spondylitis (Active) Crohn’s Disease (Moderately to Severely Active) Ulcerative Colitis (Moderately to Severely Active) Plaque Psoriasis (Moderate to Severe Chronic) Non-infectious Intermediate, Posterior and Panuveitis Hidradenitis Suppurativa (Moderate to Severe) Pyoderma Gangrenosum (off-label)
DB00065Infliximab* Indicated for reducing signs and symptoms and inducing and maintaining clinical remission in adult or pediatric (≥ 6 years of age) patients with moderately to severely active **Crohn’s disease** who have had an inadequate response to conventional therapy * Indicated for reducing the number of draining enterocutaneous and rectovaginal fistulas and maintaining fistula closure in adult patients with fistulizing **Crohn’s disease**. * Indicated for reducing signs and symptoms, inducing and maintaining clinical remission and mucosal healing, and eliminating corticosteroid use in adult or pediatric (≥ 6 years of age) patients with moderately to severely active **ulcerative colitis** who have had an inadequate response to conventional therapy. * Indicated for, in combination with methotrexate, reducing signs and symptoms, inhibiting the progression of structural damage, and improving physical function in patients with moderately to severely active **rheumatoid arthritis**. * Indicated for reducing signs and symptoms in patients with active **ankylosing spondylitis**. * Indicated for reducing signs and symptoms of active arthritis, inhibiting the progression of structural damage, and improving physical function in patients with **psoriatic arthritis**. * Indicated for the treatment of adult patients with chronic severe (i.e., extensive and/or disabling) **plaque psoriasis** who are candidates for systemic therapy and when other systemic therapies are medically less appropriate.
DB01097LeflunomideFor the management of the signs and symptoms of active rheumatoid arthritis (RA) to improve physical function and to slow the progression of structural damage associated with the disease. Has also been used for the prevention of acute and chronic rejection in recipients of solid organ trasnplants and is designated by the FDA as an orphan drug for this use.
DB01281AbataceptFor the management of the signs and symptoms of moderate-to-severe active rheumatoid arthritis, inducing major clinical response, slowing the progression of structural damage, and improving physical function in adult patients. It is indicated both as a monotherapy and for use in combination with a continued regimen of DMARDs (not including TNF antagonists). Also used for the management of the signs and symptoms of moderately to severely active polyarticular juvenile idiopathic arthritis in children.
DB05676ApremilastApremilast is indicated for the treating of active psoriatic arthritis in adults, for the treating of active moderate to severe psoriatic arthritis in patients who are eligible for phototherapy and systemic treatment. In addition, apremilast is now indicated for the treatment of oral ulcers associated with Behcet's disease in adults.[L7501]
DB06273TocilizumabIndicated for the treatment of adult patients with moderately to severely active rheumatoid arthritis (RA) who have had an inadequate response to one or more Disease-Modifying Anti-Rheumatic Drugs (DMARDs). It is also indicated for the treatment of active polyarticular juvenile idiopathic arthritis (PJIA) and active systemic juvenile idiopathic arthritis (SJIA) in patients 2 years of age and older.
DB06674GolimumabUsed in adults (i) as an adjunct to methotrexate treatment in patients with moderate to severe active rheumatoid arthritis (RA), (ii) alone or as an adjunct to methotrexate treatment in patients with active psoriatic arthritis (PsA), (iii) as a single agent in patients with active ankylosing spondylitis (AS), and (iv) as a single agent in patients with moderate to severe ulcerative colitis (UC) who require chronic steroids or have experienced intolerance or only a partial response to previous medications.
DB08895TofacitinibFor the treatment of moderate to severe rheumatoid arthritis which is resistant or intolerant to methotrexate therapy. It may also be used as an adjunct to methotrexate therapy, or other non-biologic disease-modifying antirheumatic drugs (DMARDS), when methotrexate alone is not sufficient. Tofacitinib has also been investigated as a preventative therapy for kidney transplant rejections, and as a treatment for psoriasis, ulcerative colitis, and ankylosing spondylitis. It is not to be initiated in patients with a history of chronic or recurrent infections, or in the presence of active infection, even if localized, due to reports of serious and sometimes fatal infections (commonly pneumonia, herpes zoster and urinary tract infections). Use of tofacitinib is also discouraged in those who have been, or are likely to be, exposed to TB. An increased likelihood of exposure may be encountered by traveling to certain areas. In addition, tofacitinib is not to be used in patients with severe hepatic impairment, or low hemoglobin (less than 9g/dL). Cautioned is advised when using tofacitinib in patients at risk of gastrointestinal perforation, and in the elderly who are more susceptible to infection.
DB08904Certolizumab pegolCertolizumab pegol has been approved for several different conditions listed below: - Symptomatic management of Chron's disease patients and for the maintenance of clinical response in patients with moderate to severe disease with inadequate response to conventional therapy. - Treatment of adult patients with moderate to severely active rheumatoid arthritis. - Treatment of adult patients with active psoriatic arthritis. - Treatment of adult patients with active ankylosing spondylitis. - Treatment of adult patients with moderate-to-severe plaque psoriasis that are candidates for systemic therapy or phototherapy.[FDA label] - Treatment of adult patients with active non-radiographic axial spondyloarthritis with objective signs of inflammation.[L5819] In Canada, certolizumab pegol is additionally approved in combination with [methotrexate] for the symptomatic treatment, including major clinical response, and for the reduction of joint damage in adult patients with moderately to severely active rheumatoid arthritis and psoriatic arthritis.[L5825] Inflammation is a biological response against a potential threat. This response can be normal but in certain conditions, the immune system can attack the body's normal cells or tissues which causes an abnormal inflammation.[L5840] TNF-alpha has been identified as a key regulator of the inflammatory response. The signaling cascades of this inflammatory mediator can produce a wide range of reactions including cell death, survival, differentiation, proliferation and migration.[A176660]
DB11767SarilumabIndicated for modere to severe reactive RA in adult patients who are irresponsive, respond inadequately or present intolerance to disease-modifying anti-rheumatic drugs (DMARDs) or tumor necrosis factor (TNF) antagonists. It is indicated to be used in combination with methotrexate (MTX) or as a monotherapy when there is intolerance to MTX or MTX administration is inappropriate.
DrugDrug NameTargetType
DB00005EtanerceptTumor necrosis factortarget
DB00005EtanerceptLymphotoxin-alphatarget
DB00005EtanerceptLow affinity immunoglobulin gamma Fc region receptor III-Btarget
DB00005EtanerceptComplement C1r subcomponenttarget
DB00005EtanerceptComplement C1q subcomponent subunit Atarget
DB00005EtanerceptComplement C1q subcomponent subunit Btarget
DB00005EtanerceptComplement C1q subcomponent subunit Ctarget
DB00005EtanerceptLow affinity immunoglobulin gamma Fc region receptor III-Atarget
DB00005EtanerceptComplement C1s subcomponenttarget
DB00005EtanerceptHigh affinity immunoglobulin gamma Fc receptor Itarget
DB00005EtanerceptLow affinity immunoglobulin gamma Fc region receptor II-atarget
DB00005EtanerceptLow affinity immunoglobulin gamma Fc region receptor II-btarget
DB00005EtanerceptLow affinity immunoglobulin gamma Fc region receptor II-ctarget
DB00005EtanerceptTumor necrosis factor receptor superfamily member 1Btarget
DB00026AnakinraInterleukin-1 receptor type 1target
DB00051AdalimumabTumor necrosis factortarget
DB00065InfliximabTumor necrosis factortarget
DB01097LeflunomideDihydroorotate dehydrogenase (quinone), mitochondrialtarget
DB01097LeflunomideCytochrome P450 1A2enzyme
DB01097LeflunomideCytochrome P450 2C9enzyme
DB01097LeflunomideAryl hydrocarbon receptortarget
DB01097LeflunomideProtein-tyrosine kinase 2-betatarget
DB01097LeflunomideATP-binding cassette sub-family G member 2transporter
DB01281AbataceptT-lymphocyte activation antigen CD80target
DB01281AbataceptT-lymphocyte activation antigen CD86target
DB05676ApremilastPhosphodiesterase isozyme 4target
DB05676ApremilastCytochrome P450 3A4enzyme
DB05676ApremilastCytochrome P450 2A6enzyme
DB05676ApremilastCytochrome P450 1A2enzyme
DB06273TocilizumabInterleukin-6 receptor subunit alphatarget
DB06273TocilizumabCytochrome P450 3A4enzyme
DB06674GolimumabTumor necrosis factortarget
DB08895TofacitinibNon-receptor tyrosine-protein kinase TYK2target
DB08895TofacitinibCytochrome P450 3A4enzyme
DB08895TofacitinibCytochrome P450 2C19enzyme
DB08895TofacitinibTyrosine-protein kinase JAK2target
DB08895TofacitinibTyrosine-protein kinase JAK1target
DB08895TofacitinibTyrosine-protein kinase JAK3target
DB08895TofacitinibSerum albumincarrier
DB08904Certolizumab pegolTumor necrosis factortarget
DB08904Certolizumab pegolAlcohol dehydrogenase [NADP(+)]enzyme
DB11767SarilumabAlanine aminotransferase 1enzyme
DB11767SarilumabAlanine aminotransferase 2enzyme
DB11767SarilumabAspartate aminotransferaseenzyme
DB11767SarilumabCytochrome P450 3A4enzyme
DB11767SarilumabInterleukin-6 receptor subunit alphatarget
DB11767SarilumabHigh affinity immunoglobulin gamma Fc receptor Itarget
DB11767SarilumabLow affinity immunoglobulin gamma Fc region receptor II-atarget
DB11767SarilumabLow affinity immunoglobulin gamma Fc region receptor II-btarget
DB11767SarilumabLow affinity immunoglobulin gamma Fc region receptor III-Atarget
DB11767SarilumabLow affinity immunoglobulin gamma Fc region receptor III-Btarget