Upadacitinib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2019
- First approval year
- 2019
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Upadacitinib
- Molecular weight
- 380.37
- Structure (SMILES)
- CC[C@@H]1CN(C(=O)NCC(F)(F)F)C[C@@H]1c1cnc2cnc3[nH]ccc3n12
- upadacitinib component of abbv 599
- Upadacitinib component of abbv-599
- abbv 599 component upadacitinib
- ABBV-599 COMPONENT UPADACITINIB
- abt 494
- abt 494 12mg
- ABT-494
- upadacitinib
- Upadacitinib
- upadacitinib [INN]
- UPADACITINIB [MI]
- UPADACITINIB [ORANGE BOOK]
- UPADACITINIB [USAN]
- Upadacitinib [WHO-DD]
- upadacitinib anhydrous
- Upadacitinib anhydrous
- upadacitinib inn
- upadacitinib mi
- upadacitinib orange book
- upadacitinib usan
- upadacitinib who dd
- CAS registry numbers
- 1310726-60-3
- ChEMBL ID
- CHEMBL3622821
- InChIKey
- WYQFJHHDOKWSHR-MNOVXSKESA-N
- PubChem compound IDs
- 58557659
- RxNorm IDs (RxCUI)
- 2196092
- FDA ingredient codes (UNII)
- 4RA0KN46E0
- L04AA44
- L04AF03
Sources for recorded values
- Applicant
- ABBVIE
- Approval date
- 16 Aug 2019
- Application number
- NDA211675
- Status
- Authorised
- Status date
- 16 Dec 2019
- Authorisation date
- 16 Dec 2019
- Approved indications
- Rheumatoid arthritis Rinvoq is indicated for the treatment of moderate to severe active rheumatoid arthritis in adult patients who have responded inadequately to, or who are intolerant to one or more disease-modifying anti-rheumatic drugs (DMARDs). Rinvoq may be used as monotherapy or in combination with methotrexate. Psoriatic arthritis Rinvoq is indicated for the treatment of active psoriatic arthritis in adult patients who have responded inadequately to, or who are intolerant to one or more DMARDs. Rinvoq may be used as monotherapy or in combination with methotrexate. Polyarticular juvenile idiopathic arthritis Rinvoq is indicated for the treatment of active polyarticular juvenile idiopathic arthritis (polyarticular rheumatoid factor positive [RF+] or negative [RF-], extended oligoarticular), in patients 2 years of age and older who have responded inadequately to, or who are intolerant to one or more DMARDs. RINVOQ may be used as monotherapy or in combination with methotrexate. Axial spondyloarthritis Non-radiographic axial spondyloarthritis (nr-axSpA) Rinvoq is indicated for the treatment of active non-radiographic axial spondyloarthritis in adult patients with objective signs of inflammation as indicated by elevated C-reactive protein (CRP) and/or magnetic resonance imaging (MRI), who have responded inadequately to nonsteroidal anti-inflammatory drugs (NSAIDs). Ankylosing spondylitis (AS, radiographic axial spondyloarthritis) Rinvoq is indicated for the treatment of active ankylosing spondylitis in adult patients who have responded inadequately to conventional therapy. Giant cell arteritis Rinvoq is indicated for the treatment of giant cell arteritis in adult patients. Atopic dermatitis Rinvoq is indicated for the treatment of moderate to severe atopic dermatitis in adults and adolescents 12 years and older who are candidates for systemic therapy. Alopecia areata Rinvoq is indicated for the treatment of severe alopecia areata in adults and adolescents 12 years and older. Vitiligo Rinvoq is indicated for the treatment of non-segmental vitiligo in adults and adolescents 12 years and older who are candidates for systemic therapy. Ulcerative colitis Rinvoq is indicated for the treatment of adult patients with moderately to severely active ulcerative colitis who have had an inadequate response, lost response or were intolerant to either conventional therapy or a biologic agent. Crohn’s disease Rinvoq is indicated for the treatment of adult patients with moderately to severely active Crohn’s disease who have had an inadequate response, lost response or were intolerant to either conventional therapy or a biologic agent.
- Product number
- EMEA/H/C/004760
- Authorisation holder
- AbbVie Deutschland GmbH & Co. KG
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Alopecia Areata
- Arthritis, Psoriatic
- Arthritis, Rheumatoid
- Axial Spondyloarthritis
- Colitis, Ulcerative
- Crohn Disease
- Dermatitis, Atopic
- Giant Cell Arteritis
- Spondylitis, Ankylosing
- Vitiligo
European medicines record
- Patents
- 56
- Designations
- 3
- Earliest recorded loss of exclusivity
- 9 Mar 2038
- First in class
- No
- Fast track
- No
- Breakthrough designation
- Yes
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Boxed warning
- Yes
- United States (FDA)
- Approved
- European Union (EMA)
- Authorised
- Pharmacology name
- upadacitinib
- Type
- Synthetic organic
- Drug name stem
- -tinib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- Janus kinase 2
- Gene symbol
- JAK2
- Protein identifier
- O60674
- Median affinity
- 6.92
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- Janus kinase 1
- Gene symbol
- JAK1
- Protein identifier
- P23458
- Median affinity
- 7.37
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- Janus kinase 1
- Gene symbol
- JAK1
- Protein identifier
- P23458
- Median affinity
- 8.52
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- tyrosine kinase 2
- Gene symbol
- TYK2
- Protein identifier
- P29597
- Median affinity
- 5.33
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- Janus kinase 3
- Gene symbol
- JAK3
- Protein identifier
- P52333
- Median affinity
- 5.64
- Affinity units
- pIC50
- Mechanism
- Tyrosine-protein kinase JAK1 inhibitor
- Action type
- Inhibitor
- Target
- Tyrosine-protein kinase JAK1
- Mechanism
- Tyrosine-protein kinase JAK2 inhibitor
- Action type
- Inhibitor
- Target
- Tyrosine-protein kinase JAK2
- Mechanism
- Tyrosine-protein kinase JAK3 inhibitor
- Action type
- Inhibitor
- Target
- Tyrosine-protein kinase JAK3
- Mechanism
- Tyrosine-protein kinase TYK2 inhibitor
- Action type
- Inhibitor
- Target
- Non-receptor tyrosine-protein kinase TYK2
- Action type
- Inhibitor
- Gene symbol
- JAK2
- Protein identifier
- O60674
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- JAK1
- Protein identifier
- P23458
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- TYK2
- Protein identifier
- P29597
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- JAK3
- Protein identifier
- P52333
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Dermatitis, Atopic
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000274
- Subject identifier
- D003876
- Condition
- Crohn Disease
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000384
- Subject identifier
- D003424
- Condition
- Arthritis, Rheumatoid
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000685
- Subject identifier
- D001172
- Condition
- Colitis, Ulcerative
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000729
- Subject identifier
- D003093
- Condition
- Arthritis, Juvenile
- Highest recorded phase
- 3
- Condition identifier
- EFO:0002609
- Subject identifier
- D001171
- Condition
- Arthritis, Psoriatic
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003778
- Subject identifier
- D015535
- Condition
- Spondylitis, Ankylosing
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003898
- Subject identifier
- D013167
- Condition
- Alopecia Areata
- Highest recorded phase
- 3
- Condition identifier
- EFO:0004192
- Subject identifier
- D000506
- Condition
- Vitiligo
- Highest recorded phase
- 3
- Condition identifier
- EFO:0004208
- Subject identifier
- D014820
- Condition
- Hidradenitis Suppurativa
- Highest recorded phase
- 3
- Condition identifier
- EFO:1000710
- Subject identifier
- D017497
- Condition
- Giant Cell Arteritis
- Highest recorded phase
- 3
- Condition identifier
- EFO:1001209
- Subject identifier
- D013700
- Condition
- Takayasu Arteritis
- Highest recorded phase
- 3
- Condition identifier
- EFO:1001857
- Subject identifier
- D013625
- Condition
- Lupus Erythematosus, Systemic
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0007915
- Subject identifier
- D008180
- Condition identifier
- EFO_0000274
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000384
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000685
- Condition identifier
- EFO_0000729
- Highest recorded phase
- 3
- Condition identifier
- EFO_0002609
- Highest recorded phase
- 3
- Condition identifier
- EFO_0003767
- Condition identifier
- EFO_0003778
- Highest recorded phase
- 3
- Condition identifier
- EFO_0003780
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003898
- Highest recorded phase
- 3
- Condition identifier
- EFO_0004192
- Highest recorded phase
- 3
- Condition identifier
- EFO_0004208
- Highest recorded phase
- 3
- Condition identifier
- EFO_0009856
- Highest recorded phase
- 2
- Condition identifier
- EFO_1000710
- Highest recorded phase
- 3
- Condition identifier
- EFO_1001209
- Highest recorded phase
- 3
- Condition identifier
- EFO_1001857
- Highest recorded phase
- 3
- Condition identifier
- HP_0002094
- Highest recorded phase
- 3
- Condition identifier
- HP_0002098
- Highest recorded phase
- 3
- Condition identifier
- HP_0002360
- Highest recorded phase
- 3
- Condition identifier
- HP_0010447
- Highest recorded phase
- 1
- Condition identifier
- HP_0012378
- Highest recorded phase
- 3
- Condition identifier
- HP_0100543
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0004980
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005011
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005083
- Condition identifier
- MONDO_0005101
- Highest recorded phase
- 4
And 18 more, listed on the interactive page.
- Warning
- Black Box Warning
- Effect
- carcinogenicity
- Country
- United States
- Warning
- Black Box Warning
- Effect
- vascular toxicity
- Country
- United States
- Event
- antibiotic therapy
- Reports
- 8
- Reporting signal score
- 25.0724
- Event
- covid-19
- Reports
- 110
- Reporting signal score
- 213.131
- Event
- herpes zoster
- Reports
- 66
- Reporting signal score
- 83.0302
- Event
- illness
- Reports
- 50
- Reporting signal score
- 107.335
- Event
- infected lymphocele
- Reports
- 5
- Reporting signal score
- 23.2102
- Event
- infection
- Reports
- 55
- Reporting signal score
- 32.4867
- Event
- localised infection
- Reports
- 24
- Reporting signal score
- 32.8759
- Event
- lumbosacral plexopathy
- Reports
- 6
- Reporting signal score
- 33.3604
- Event
- oral lichen planus
- Reports
- 7
- Reporting signal score
- 24.1819
- Event
- perineal rash
- Reports
- 6
- Reporting signal score
- 32.1336
- Event
- rheumatoid arthritis
- Reports
- 58
- Reporting signal score
- 41.9785
- Event
- sars-cov-2 test positive
- Reports
- 13
- Reporting signal score
- 26.5196
- Event
- sinusitis
- Reports
- 49
- Reporting signal score
- 37.2962
- Event
- therapy interrupted
- Reports
- 204
- Reporting signal score
- 700.465
- Event
- urinary tract infection
- Reports
- 92
- Reporting signal score
- 73.7011
- NCT01741493
- NCT01960855
- NCT02049138
- NCT02066389
- NCT02629159
- NCT02675426
- NCT02706847
- NCT02706873
- NCT02706951
- NCT02720523
- NCT02955212
- NCT03086343
- NCT03682705
- NCT03823378
- NCT05121298
- NCT02365649
- NCT02782663
- NCT03345823
- NCT03345836
- NCT03345849
- NCT06227910
- NCT06332534
- NCT02819635
- NCT03006068
- NCT03653026
And 27 more, listed on the interactive page.
- Dose
- 15 mg
- Route
- Oral
- How often
- Once daily
- Hydrogen bond acceptors
- 4
- Hydrogen bond donors
- 2
- Polar surface area
- 78.32
- Calculated partition coefficient (ALogP)
- 2.91
- Calculated partition coefficient (XLogP)
- 2.7
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 3
- Heavy atoms
- 27
- Molecular formula
- C17H19F3N6O
- Monoisotopic mass
- 380.15724374
- Natural product
- No
- 0074-1043
- 0074-2306
- 0074-2310
- 0074-2320
- Recorded assays
- 456
- Active assays
- 176
- Confirmatory
- Other
- Janus Kinase Inhibitors
- Antirheumatic Agents
Related records
Trials (115)
- A 24-Week Real-World Study of Upadacitinib in Moderate-to-Severe Hidradenitis Suppurativa
- A Maintenance and Long-Term Extension Study of the Efficacy and Safety of Upadacitinib (ABT-494) in Participants With Crohn's Disease Who Completed the Studies M14-431 or M14-433
- A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study of ABT-494 for the Induction of Symptomatic and Endoscopic Remission in Subjects With Moderately to Severely Active Crohn's Disease Who Have Inadequately Responded to or Are Intolerant to Immunomodulators or Anti-TNF Therapy
- A Phase 1 Study of the Safety and How the Body Processes ABBV-722 and Upadacitinib After Multiple Oral Doses in Healthy Adult Participants
- A Phase 3 Study to Compare Upadacitinib to Abatacept in Subjects With Rheumatoid Arthritis on Stable Dose of Conventional Synthetic Disease- Modifying Antirheumatic Drugs (csDMARDs) Who Have an Inadequate Response or Intolerance to Biologic DMARDs
- A Pragmatic Trial of Interleukin-17 Inhibition Versus Janus Kinase Inhibition After Tumor Necrosis Factor-alpha Inhibitor Failure in Axial Spondyloarthritis
- A Study Comparing Upadacitinib (ABT-494) Monotherapy to Methotrexate (MTX) Monotherapy in Adults With Rheumatoid Arthritis (RA) Who Have an Inadequate Response to MTX (SELECT-MONOTHERAPY)
- A Study Comparing Upadacitinib (ABT-494) to Placebo and to Adalimumab in Adults With Rheumatoid Arthritis Who Are on a Stable Dose of Methotrexate and Who Have an Inadequate Response to Methotrexate
- A Study Comparing Upadacitinib (ABT-494) to Placebo and to Adalimumab in Participants With Psoriatic Arthritis Who Have an Inadequate Response to at Least One Non-Biologic Disease Modifying Anti-Rheumatic Drug (DMARD)
- A Study Comparing Upadacitinib (ABT-494) to Placebo in Adults With Rheumatoid Arthritis on a Stable Dose of Conventional Synthetic Disease-Modifying Antirheumatic Drugs (csDMARDs) Who Have an Inadequate Response to csDMARDs Alone
- A Study Comparing Upadacitinib (ABT-494) to Placebo in Participants With Active Psoriatic Arthritis Who Have a History of Inadequate Response to at Least One Biologic Disease Modifying Anti-Rheumatic Drug
- A Study Evaluating the Safety and Efficacy of Upadacitinib in Adults With Active Ankylosing Spondylitis
- A Study in Healthy Adults and Adult Subjects With Rheumatoid Arthritis to Evaluate the Safety, Tolerability and Pharmacokinetics After Multiple Doses of ABT-494
- A Study in Rheumatoid Arthritis Patients Who Have Completed a Preceding Study With ABBV-105 Given Alone or in Combination With Upadacitinib
- A Study Investigating the Efficacy and Safety of ABT-494 Given With Methotrexate in Subjects With Rheumatoid Arthritis Who Failed Anti-Tumor Necrosis Factor (TNF) Biologic Therapy
- A Study Investigating the Efficacy and Safety of Upadacitinib (ABT-494) Given With Methotrexate (MTX) in Adults With Rheumatoid Arthritis Who Have Had an Inadequate Response to MTX Alone
- A Study of Oral Upadacitinib Tablet Compared to Placebo in Adult Participants With Moderate to Severe Hidradenitis Suppurativa to Assess Change in Disease Symptoms
- A Study of Oral Upadacitinib Tablets to Assess Change in Disease State in Participants Aged 12-75 Years With Moderate to Severe Atopic Dermatitis in Brazil
- A Study of the Efficacy and Safety of Upadacitinib (ABT-494) in Participants With Moderately to Severely Active Crohn's Disease Who Have Inadequately Responded to or Are Intolerant to Biologic Therapy
- A Study of the Efficacy and Safety of Upadacitinib (ABT-494) in Participants With Moderately to Severely Active Ulcerative Colitis
In development for (20)
- Alopecia areata Phase 3
- Anal fistula Phase 1
- Ankylosing spondylitis Phase 3
- Atopic eczema Phase 3
- Autoimmune thrombocytopenic purpura Phase 2
- Behcet disease Phase 2
- Crohn disease Phase 3
- Eosinophilic esophagitis Phase 2
- Hidradenitis suppurativa Phase 3
- Juvenile idiopathic arthritis Phase 3
- Psoriatic arthritis Phase 3
- Relapsing polychondritis Phase 1
- Rheumatoid arthritis Phase 3
- Sjogren syndrome Phase 2
- Systemic lupus erythematosus Phase 2
- Systemic-onset juvenile idiopathic arthritis Phase 3
- Takayasu arteritis Phase 3
- Temporal arteritis Phase 3
- Ulcerative colitis Phase 3
- Vitiligo Phase 3