| Drug Name |
Upadacitinib |
| Drug ID |
BADD_D02407 |
| Description |
Upadacitinib is an oral Janus kinase (JAK)1-selective inhibitor and a disease-modifying antirheumatic drug (DMARD) used in the treatment of rheumatoid arthritis to slow down disease progression. Rheumatoid arthritis is a chronic autoimmune inflammatory disease affecting the peripheral joints. It is characterized by synovial inflammation and hyperplasia, autoantibody production, cartilage damage and bone destruction, leading to co-morbidities.[A189165] Despite a variety of therapeutic agents available for treatment, up to 40% of the patients do not respond to current therapies, including biological therapies.[A189171] The etiology of the disease is mostly unknown; however, the role of JAK as a driver of immune-mediated conditions was discovered, leading to the use of JAK as therapeutic targets for rheumatoid arthritis.[A189168] To reduce dose-related toxicity (as seen with some pan-JAK inhibitors) without significantly affecting efficacy, more selective JAK1 inhibitors, upadacitinib and [filgotinib], were developed.[A189165]
The FDA approved Upadacitinib in August 2019 for the treatment of adults with moderately to severely active rheumatoid arthritis who have had an inadequate response or intolerance to methotrexate.[L10896] In December 2019, it was additionally approved by the European Commission for the same indication in patients with inadequate response or intolerance to one or more DMARDs and can be used as monotherapy or in combination with methotrexate.[L10899] Upadacitinib is marketed under the brand name RINVOQ™ for oral administration.[L10896] It is currently being investigated in several clinical trials assessing its therapeutic effectiveness in other inflammatory diseases, such as psoriatic arthritis, ankylosing spondylitis, ulcerative colitis, and atopic dermatitis.[A189165] |
| Indications and Usage |
Upadacitinib is indicated for the treatment of moderately to severely active rheumatoid arthritis or active psoriatic arthritis in adult patients who have had an inadequate response or intolerance to one or more disease-modifying anti-rheumatic drugs (DMARDs), such as methotrexate or TNF blockers.[L10896, L39474] For these indications, upadacitinib may be used as monotherapy or in combination with methotrexate.[L39474]
Upadacitinib is also indicated for the treatment of active ankylosing spondylitis in adult patients who have an inadequate response to conventional therapy and for the treatment of moderate to severe atopic dermatitis in patients aged 12 years and older who are candidates for systemic therapy.[L39474]
Combining upadacitinib with other JAK inhibitors, biologic DMARDs, or other potent immunosuppressive agents is not recommended.[L10896] |
| Marketing Status |
approved; investigational |
| ATC Code |
L04AA44 |
| DrugBank ID |
DB15091
|
| KEGG ID |
D10994
|
| MeSH ID |
C000613732
|
| PubChem ID |
58557659
|
| TTD Drug ID |
D07JAG
|
| NDC Product Code |
68513-2310; 0074-1043; 68513-2306; 0074-2310; 68513-1043; 59651-788; 0074-2306 |
| UNII |
4RA0KN46E0
|
| Synonyms |
upadacitinib | (3S,4R)-3-ethyl-4-(3H-imidazo(1,2-a)pyrrolo(2,3-e)pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)-1-pyrrolidinecarboxamide | ABT-494 | Rinvoq |
