upadacitinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	5346	1310726-60-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: upadacitinib hydrate upadacitinib ABT-494 rinvoq	Upadacitinib is a Janus kinase (JAK) inhibitor. JAKs are intracellular enzymes which transmit signals arising from cytokine or growth factor-receptor interactions on the cellular membrane to influence cellular processes of hematopoiesis and immune cell function. Within the signaling pathway, JAKs phosphorylate and activate Signal Transducers and Activators of Transcription (STATs) which modulate intracellular activity including gene expression. Upadacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs. Molecular weight: 380.38 Formula: C17H19F3N6O CLOGP: 2.45 LIPINSKI: 0 HAC: 7 HDO: 2 TPSA: 78.32 ALOGS: -3.73 ROTB: 4 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

upadacitinib hydrate
upadacitinib
ABT-494
rinvoq

Upadacitinib is a Janus kinase (JAK) inhibitor. JAKs are intracellular enzymes which transmit signals arising from cytokine or growth factor-receptor interactions on the cellular membrane to influence cellular processes of hematopoiesis and immune cell function. Within the signaling pathway, JAKs phosphorylate and activate Signal Transducers and Activators of Transcription (STATs) which modulate intracellular activity including gene expression. Upadacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs.

Molecular weight: 380.38
Formula: C17H19F3N6O
CLOGP: 2.45
LIPINSKI: 0
HAC: 7
HDO: 2
TPSA: 78.32
ALOGS: -3.73
ROTB: 4

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
15	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company
Dec. 16, 2019	EMA	AbbVie Deutschland GmbH & Co. KG
Aug. 16, 2019	FDA	ABBVIE INC
Jan. 23, 2020	PMDA	AbbVie GK

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Therapy interrupted	2963.71	16.93	785	12669	31670	63443898
COVID-19	909.35	16.93	453	13001	112650	63362918
Illness	430.06	16.93	209	13245	48850	63426718
Urinary tract infection	234.70	16.93	284	13170	264400	63211168
Herpes zoster	197.12	16.93	153	13301	82309	63393259
Intentional dose omission	144.66	16.93	57	13397	8018	63467550
Therapy cessation	123.02	16.93	78	13376	30379	63445189
Infection	90.85	16.93	169	13285	229004	63246564
Sinusitis	73.88	16.93	154	13300	226499	63249069
Acne	73.11	16.93	51	13403	23242	63452326
Bronchitis	56.93	16.93	98	13356	124837	63350731
Influenza	55.84	16.93	90	13364	108632	63366936
Drug ineffective	55.04	16.93	393	13061	1044372	62431196
Surgery	48.07	16.93	48	13406	35864	63439704
Hospitalisation	47.23	16.93	73	13381	85008	63390560
Antibiotic therapy	43.66	16.93	14	13440	1079	63474489
Osteoarthritis	41.08	16.93	73	13381	95270	63380298
Eczema herpeticum	40.78	16.93	9	13445	160	63475408
Fatigue	40.19	16.93	80	13374	887948	62587620
Fracture pain	39.99	16.93	12	13442	742	63474826
Kidney infection	38.68	16.93	35	13419	23141	63452427
SARS-CoV-2 test positive	38.54	16.93	23	13431	8033	63467535
Ophthalmic herpes zoster	38.41	16.93	15	13439	2058	63473510
Spinal operation	37.98	16.93	23	13431	8248	63467320
Osteogenesis imperfecta	37.61	16.93	11	13443	622	63474946
Drug interaction	37.28	16.93	3	13451	229128	63246440
Spinal cord infection	36.76	16.93	11	13443	674	63474894
Thrombosis	36.54	16.93	56	13398	64699	63410869
Disseminated varicella zoster virus infection	36.36	16.93	9	13445	268	63475300
Pelvic floor muscle weakness	36.32	16.93	7	13447	61	63475507
Infusion related reaction	35.40	16.93	5	13449	245516	63230052
Rheumatoid factor	34.47	16.93	9	13445	333	63475235
Oral lichen planus	32.46	16.93	10	13444	676	63474892
Hypotension	32.12	16.93	9	13445	272595	63202973
Cataract	31.71	16.93	49	13405	57004	63418564
Coronavirus infection	30.85	16.93	16	13438	4262	63471306
Contraindicated product administered	30.08	16.93	5	13449	217643	63257925
Diverticulitis	29.38	16.93	39	13415	39518	63436050
Localised infection	29.20	16.93	34	13420	30176	63445392
Nasopharyngitis	28.54	16.93	118	13336	254139	63221429
Knee operation	28.33	16.93	17	13437	5996	63469572
Arthralgia	27.84	16.93	211	13243	569499	62906069
Glossodynia	27.34	16.93	3	13451	178873	63296695
Pneumonia	26.87	16.93	177	13277	456590	63018978
Cystitis	26.15	16.93	44	13410	54947	63420621
Toxicity to various agents	25.90	16.93	10	13444	247240	63228328
Unevaluable event	25.62	16.93	42	13412	51344	63424224
Aphthous ulcer	25.14	16.93	22	13432	13916	63461652
Malignant syphilis	25.13	16.93	4	13450	9	63475559
Rash vesicular	24.99	16.93	14	13440	4344	63471224
Interstitial lung disease	24.87	16.93	46	13408	61862	63413706
Asthenia	24.64	16.93	27	13427	383577	63091991
Subcutaneous drug absorption impaired	24.46	16.93	6	13448	172	63475396
Ear infection	24.36	16.93	35	13419	38178	63437390
Thoracic vertebral fracture	24.31	16.93	14	13440	4578	63470990
Mouth ulceration	23.70	16.93	32	13422	32952	63442616
Pulmonary embolism	23.59	16.93	66	13388	116618	63358950
Intervertebral disc degeneration	22.86	16.93	22	13432	15710	63459858
COVID-19 pneumonia	22.81	16.93	21	13433	14188	63461380
Immunodeficiency common variable	22.63	16.93	6	13448	236	63475332
Basal cell carcinoma	21.40	16.93	28	13426	27963	63447605
Post procedural complication	21.34	16.93	22	13432	17052	63458516
Upper respiratory tract infection	21.31	16.93	51	13403	81996	63393572
Lichen planus	20.55	16.93	10	13444	2328	63473240
Tooth infection	20.46	16.93	22	13432	17898	63457670
Ostomy bag placement	20.30	16.93	3	13451	3	63475565
Knee arthroplasty	20.19	16.93	39	13415	54167	63421401
Intra-abdominal fluid collection	20.19	16.93	10	13444	2419	63473149
Oesophageal stenosis	20.12	16.93	11	13443	3255	63472313
Abscess	19.98	16.93	21	13433	16647	63458921
Pneumocystis jirovecii pneumonia	19.72	16.93	21	13433	16893	63458675
Gastrointestinal infection	19.51	16.93	16	13438	9265	63466303
Vulval cancer	19.33	16.93	7	13447	780	63474788
Tongue ulceration	19.22	16.93	11	13443	3555	63472013
Postoperative wound infection	19.22	16.93	17	13437	10908	63464660
Herpes zoster cutaneous disseminated	18.95	16.93	5	13449	193	63475375
Infected lymphocele	18.20	16.93	5	13449	225	63475343
Product residue present	18.10	16.93	11	13443	3968	63471600
Systemic lupus erythematosus	18.00	16.93	11	13443	208907	63266661
Rheumatic disorder	17.97	16.93	10	13444	3062	63472506
Somnolence	17.46	16.93	8	13446	178677	63296891
Sinusitis aspergillus	17.23	16.93	4	13450	90	63475478
Discomfort	17.14	16.93	7	13447	167367	63308201
Confusional state	17.05	16.93	15	13439	236365	63239203

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Therapy interrupted	391.53	24.53	116	3715	13581	34939519
COVID-19	134.15	24.53	91	3740	77459	34875641
Illness	93.48	24.53	40	3791	13489	34939611
Herpes zoster	91.18	24.53	53	3778	34346	34918754
Acne	84.05	24.53	35	3796	11031	34942069
Drug ineffective	83.63	24.53	165	3666	456586	34496514
Eczema herpeticum	58.54	24.53	11	3820	170	34952930
Musculoskeletal stiffness	39.48	24.53	36	3795	46644	34906456
Therapeutic product effect incomplete	35.18	24.53	35	3796	50506	34902594
Dermatitis atopic	34.25	24.53	15	3816	5332	34947768
Skin cancer	33.02	24.53	18	3813	10279	34942821
Arthralgia	32.63	24.53	63	3768	169978	34783122
Squamous cell carcinoma of lung	28.79	24.53	10	3821	1919	34951181
Myelomalacia	25.68	24.53	5	3826	94	34953006

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Therapy interrupted	3630.90	17.74	878	12785	30463	79700262
COVID-19	979.68	17.74	495	13168	157179	79573546
Illness	583.75	17.74	239	13424	46272	79684453
Herpes zoster	244.37	17.74	168	13495	92915	79637810
Urinary tract infection	241.94	17.74	265	13398	274247	79456478
Intentional dose omission	177.42	17.74	64	13599	8753	79721972
Sinusitis	121.15	17.74	158	13505	195343	79535382
Infection	116.39	17.74	173	13490	241539	79489186
Therapy cessation	91.88	17.74	65	13598	37497	79693228
Eczema herpeticum	87.04	17.74	18	13645	290	79730435
Influenza	80.59	17.74	105	13558	129501	79601224
Bronchitis	66.36	17.74	96	13567	130548	79600177
Acne	59.52	17.74	44	13619	27146	79703579
Kidney infection	58.54	17.74	40	13623	21811	79708914
Surgery	56.43	17.74	46	13617	32720	79698005
Osteoarthritis	56.22	17.74	72	13591	87237	79643488
Antibiotic therapy	54.52	17.74	15	13648	844	79729881
Hospitalisation	51.90	17.74	72	13591	94164	79636561
Drug interaction	50.45	17.74	6	13657	415177	79315548
SARS-CoV-2 test positive	47.82	17.74	28	13635	11688	79719037
Nasopharyngitis	47.54	17.74	122	13541	253759	79476966
Toxicity to various agents	44.63	17.74	9	13654	421531	79309194
Knee operation	43.85	17.74	21	13642	5845	79724880
Spinal operation	43.48	17.74	23	13640	7894	79722831
Diverticulitis	43.14	17.74	46	13617	45890	79684835
Osteogenesis imperfecta	42.05	17.74	11	13652	510	79730215
Ophthalmic herpes zoster	41.26	17.74	16	13647	2668	79728057
Pneumonia	39.21	17.74	219	13444	660027	79070698
Coronavirus infection	38.98	17.74	21	13642	7476	79723249
Fracture pain	38.29	17.74	11	13652	725	79730000
Herpes zoster cutaneous disseminated	38.28	17.74	10	13653	461	79730264
Fatigue	38.20	17.74	63	13600	929664	78801061
Hypotension	36.35	17.74	15	13648	440302	79290423
Therapeutic product effect incomplete	36.28	17.74	77	13586	141568	79589157
Rheumatoid factor	35.06	17.74	9	13654	387	79730338
Skin cancer	34.40	17.74	25	13638	15015	79715710
Ear infection	33.25	17.74	35	13628	34397	79696328
Unevaluable event	32.91	17.74	44	13619	55541	79675184
COVID-19 pneumonia	32.74	17.74	32	13631	28817	79701908
Rheumatic disorder	32.09	17.74	14	13649	3144	79727581
Aphthous ulcer	31.82	17.74	25	13638	16864	79713861
Thrombosis	31.81	17.74	54	13609	84046	79646679
Knee arthroplasty	31.57	17.74	38	13625	43210	79687515
Pneumocystis jirovecii pneumonia	31.31	17.74	33	13630	32475	79698250
Respiratory tract infection	31.08	17.74	40	13623	48649	79682076
Disseminated varicella zoster virus infection	30.88	17.74	9	13654	624	79730101
Tooth infection	29.43	17.74	25	13638	18807	79711918
Basal cell carcinoma	29.19	17.74	34	13629	37341	79693384
Cataract	29.13	17.74	44	13619	62076	79668649
Squamous cell carcinoma of skin	29.12	17.74	22	13641	14011	79716714
Febrile neutropenia	28.89	17.74	3	13660	230996	79499729
Completed suicide	28.75	17.74	4	13659	245763	79484962
Cystitis	28.58	17.74	40	13623	52692	79678033
Oral lichen planus	28.52	17.74	9	13654	817	79729908
Pelvic floor muscle weakness	28.36	17.74	5	13658	32	79730693
Asthenia	27.84	17.74	28	13635	511661	79219064
Upper respiratory tract infection	27.42	17.74	53	13610	91115	79639610
Intervertebral disc protrusion	26.43	17.74	26	13637	23595	79707130
Infusion related reaction	26.34	17.74	4	13659	230233	79500492
Malignant syphilis	25.98	17.74	4	13659	9	79730716
Squamous cell carcinoma of lung	25.95	17.74	11	13652	2303	79728422
Localised infection	25.78	17.74	32	13631	37543	79693182
Pulmonary embolism	25.64	17.74	76	13587	171578	79559147
Somnolence	25.48	17.74	5	13658	238976	79491749
Confusional state	24.39	17.74	12	13651	317985	79412740
Malaise	24.20	17.74	155	13508	489714	79241011
Gastrointestinal infection	23.85	17.74	18	13645	11443	79719282
Vulval cancer	23.35	17.74	7	13656	535	79730190
Eye infection	23.23	17.74	18	13645	11902	79718823
Lung neoplasm malignant	22.91	17.74	26	13637	27766	79702959
Herpes simplex	22.87	17.74	18	13645	12169	79718556
Pseudarthrosis	22.65	17.74	6	13657	292	79730433
Retinal detachment	22.59	17.74	16	13647	9231	79721494
Thrombocytopenia	21.92	17.74	9	13654	265250	79465475
Postoperative wound infection	21.90	17.74	18	13645	12943	79717782
Disease progression	21.56	17.74	3	13660	184359	79546366
Myelomalacia	21.48	17.74	5	13658	142	79730583
Acute kidney injury	21.44	17.74	35	13628	519369	79211356
Dermatitis atopic	21.39	17.74	16	13647	10040	79720685
Interstitial lung disease	20.92	17.74	54	13609	112546	79618179
Inflammatory marker increased	20.45	17.74	16	13647	10724	79720001
Device loosening	20.21	17.74	6	13657	444	79730281
Tongue ulceration	19.74	17.74	11	13652	4182	79726543
Transitional cell cancer of the renal pelvis and ureter	19.08	17.74	4	13659	69	79730656
Fracture	19.01	17.74	21	13642	21780	79708945
Infected lymphocele	18.96	17.74	5	13658	239	79730486
Reactive gastropathy	18.91	17.74	6	13657	554	79730171
Intervertebral disc degeneration	18.83	17.74	18	13645	15767	79714958
Spinal stenosis	18.83	17.74	18	13645	15773	79714952
Axial spondyloarthritis	18.64	17.74	6	13657	580	79730145
Rotator cuff syndrome	18.60	17.74	17	13646	14078	79716647
Gastroenteritis viral	18.41	17.74	22	13641	24809	79705916
Lichen planus	17.90	17.74	9	13654	2782	79727943

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L04AA44	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS IMMUNOSUPPRESSANTS IMMUNOSUPPRESSANTS Selective immunosuppressants
MeSH PA	D018501	Antirheumatic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D000075242	Janus Kinase Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors
FDA MoA	N0000190857	Janus Kinase Inhibitors
FDA EPC	N0000190858	Janus Kinase Inhibitor

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Ankylosing spondylitis	indication	9631008	DOID:7147
Atopic dermatitis	indication	24079001	DOID:3310
Ulcerative colitis	indication	64766004	DOID:8577
Rheumatoid arthritis	indication	69896004	DOID:7148
Psoriatic arthritis	indication	156370009	DOID:9008
Nonradiographic axial spondyloarthritis	indication	713777005

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.85	acidic
pKa2	12.79	acidic
pKa3	3.25	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
15MG	RINVOQ	ABBVIE	N211675	Aug. 16, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	8962629	Jan. 15, 2031	TREATMENT OF ADULTS WITH ACTIVE ANKYLOSING SPONDYLITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
15MG	RINVOQ	ABBVIE	N211675	Aug. 16, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	8962629	Jan. 15, 2031	TREATMENT OF ADULTS WITH ACTIVE PSORIATIC ARTHRITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
15MG	RINVOQ	ABBVIE	N211675	Aug. 16, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	8962629	Jan. 15, 2031	TREATMENT OF ADULTS WITH MODERATELY TO SEVERELY ACTIVE CROHNS DISEASE WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
15MG	RINVOQ	ABBVIE	N211675	Aug. 16, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	8962629	Jan. 15, 2031	TREATMENT OF ADULTS WITH MODERATELY TO SEVERELY ACTIVE RHEUMATOID ARTHRITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
15MG	RINVOQ	ABBVIE	N211675	Aug. 16, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	8962629	Jan. 15, 2031	TREATMENT OF ADULTS WITH MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
30MG	RINVOQ	ABBVIE	N211675	Jan. 14, 2022	RX	TABLET, EXTENDED RELEASE	ORAL	8962629	Jan. 15, 2031	TREATMENT OF ADULTS WITH MODERATELY TO SEVERELY ACTIVE CROHNS DISEASE WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
30MG	RINVOQ	ABBVIE	N211675	Jan. 14, 2022	RX	TABLET, EXTENDED RELEASE	ORAL	8962629	Jan. 15, 2031	TREATMENT OF ADULTS WITH MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
45MG	RINVOQ	ABBVIE	N211675	March 16, 2022	RX	TABLET, EXTENDED RELEASE	ORAL	8962629	Jan. 15, 2031	TREATMENT OF ADULTS WITH MODERATELY TO SEVERELY ACTIVE CROHNS DISEASE WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
45MG	RINVOQ	ABBVIE	N211675	March 16, 2022	RX	TABLET, EXTENDED RELEASE	ORAL	8962629	Jan. 15, 2031	TREATMENT OF ADULTS WITH MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
15MG	RINVOQ	ABBVIE	N211675	Aug. 16, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	10597400	Oct. 17, 2036	TREATMENT OF ADULTS WITH MODERATELY TO SEVERELY ACTIVE RHEUMATOID ARTHRITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
15MG	RINVOQ	ABBVIE	N211675	Aug. 16, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	10995095	Oct. 17, 2036	TREATMENT OF ADULTS AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH REFRACTORY, MODERATE TO SEVERE ATOPIC DERMATITIS WHOSE DISEASE IS NOT ADEQUATELY CONTROLLED WITH OTHER SYSTEMIC DRUG PRODUCTS, OR WHEN USE OF THOSE THERAPIES ARE INADVISABLE
15MG	RINVOQ	ABBVIE	N211675	Aug. 16, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	11365198	Oct. 17, 2036	TREATMENT OF ADULTS WITH ACTIVE PSORIATIC ARTHRITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
15MG	RINVOQ	ABBVIE	N211675	Aug. 16, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	11512092	Oct. 17, 2036	TREATMENT OF ADULTS WITH ACTIVE ANKYLOSING SPONDYLITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
15MG	RINVOQ	ABBVIE	N211675	Aug. 16, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	11512092	Oct. 17, 2036	TREATMENT OF ADULTS WITH ACTIVE NON-RADIOGRAPHIC AXIAL SPONDYLOARTHRITIS WITH OBJECTIVE SIGNS OF INFLAMMATION WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
15MG	RINVOQ	ABBVIE	N211675	Aug. 16, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	11512092	Oct. 17, 2036	TREATMENT OF ADULTS WITH ACTIVE PSORIATIC ARTHRITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
15MG	RINVOQ	ABBVIE	N211675	Aug. 16, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	11524964	Oct. 17, 2036	TREATMENT OF ADULTS WITH ACTIVE ANKYLOSING SPONDYLITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
15MG	RINVOQ	ABBVIE	N211675	Aug. 16, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	11535624	Oct. 17, 2036	TREATMENT OF ADULTS WITH MODERATELY TO SEVERELY ACTIVE RHEUMATOID ARTHRITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
15MG	RINVOQ	ABBVIE	N211675	Aug. 16, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	11535625	Oct. 17, 2036	TREATMENT OF ADULTS AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH REFRACTORY, MODERATE TO SEVERE ATOPIC DERMATITIS WHOSE DISEASE IS NOT ADEQUATELY CONTROLLED WITH OTHER SYSTEMIC DRUG PRODUCTS, OR WHEN USE OF THOSE THERAPIES ARE INADVISABLE
30MG	RINVOQ	ABBVIE	N211675	Jan. 14, 2022	RX	TABLET, EXTENDED RELEASE	ORAL	10550126	Oct. 17, 2036	TREATMENT OF ADULTS AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH REFRACTORY, MODERATE TO SEVERE ATOPIC DERMATITIS WHOSE DISEASE IS NOT ADEQUATELY CONTROLLED WITH OTHER SYSTEMIC DRUG PRODUCTS, OR WHEN USE OF THOSE THERAPIES ARE INADVISABLE
30MG	RINVOQ	ABBVIE	N211675	Jan. 14, 2022	RX	TABLET, EXTENDED RELEASE	ORAL	11535626	Oct. 17, 2036	TREATMENT OF ADULTS AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH REFRACTORY, MODERATE TO SEVERE ATOPIC DERMATITIS WHOSE DISEASE IS NOT ADEQUATELY CONTROLLED WITH OTHER SYSTEMIC DRUG PRODUCTS, OR WHEN USE OF THOSE THERAPIES ARE INADVISABLE
15MG	RINVOQ	ABBVIE	N211675	Aug. 16, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	11564922	March 9, 2038	TREATMENT OF ADULTS WITH MODERATELY TO SEVERELY ACTIVE CROHNS DISEASE WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
15MG	RINVOQ	ABBVIE	N211675	Aug. 16, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	11607411	March 9, 2038	TREATMENT OF ADULTS WITH MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
45MG	RINVOQ	ABBVIE	N211675	March 16, 2022	RX	TABLET, EXTENDED RELEASE	ORAL	11564922	March 9, 2038	TREATMENT OF ADULTS WITH MODERATELY TO SEVERELY ACTIVE CROHNS DISEASE WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
45MG	RINVOQ	ABBVIE	N211675	March 16, 2022	RX	TABLET, EXTENDED RELEASE	ORAL	11607411	March 9, 2038	TREATMENT OF ADULTS WITH MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
15MG	RINVOQ	ABBVIE	N211675	Aug. 16, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	Aug. 16, 2024	NEW CHEMICAL ENTITY
30MG	RINVOQ	ABBVIE	N211675	Jan. 14, 2022	RX	TABLET, EXTENDED RELEASE	ORAL	Aug. 16, 2024	NEW CHEMICAL ENTITY
45MG	RINVOQ	ABBVIE	N211675	March 16, 2022	RX	TABLET, EXTENDED RELEASE	ORAL	Aug. 16, 2024	NEW CHEMICAL ENTITY
15MG	RINVOQ	ABBVIE	N211675	Aug. 16, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	Dec. 14, 2024	TREATMENT OF ADULTS WITH ACTIVE PSORIATIC ARTHRITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
15MG	RINVOQ	ABBVIE	N211675	Aug. 16, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	Jan. 14, 2025	TREATMENT OF ADULTS AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH REFRACTORY, MODERATE-TO-SEVERE ATOPIC DERMATITIS WHOSE DISEASE IS NOT ADEQUATELY CONTROLLED WITH OTHER SYSTEMIC DRUG PRODUCTS, INCLUDING BIOLOGICS, OR WHEN USE OF THOSE THERAPIES ARE INADVISABLE
30MG	RINVOQ	ABBVIE	N211675	Jan. 14, 2022	RX	TABLET, EXTENDED RELEASE	ORAL	Jan. 14, 2025	TREATMENT OF ADULTS AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH REFRACTORY, MODERATE-TO-SEVERE ATOPIC DERMATITIS WHOSE DISEASE IS NOT ADEQUATELY CONTROLLED WITH OTHER SYSTEMIC DRUG PRODUCTS, INCLUDING BIOLOGICS, OR WHEN USE OF THOSE THERAPIES ARE INADVISABLE
15MG	RINVOQ	ABBVIE	N211675	Aug. 16, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	March 16, 2025	TREATMENT OF ADULT PATIENTS WITH MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
30MG	RINVOQ	ABBVIE	N211675	Jan. 14, 2022	RX	TABLET, EXTENDED RELEASE	ORAL	March 16, 2025	TREATMENT OF ADULT PATIENTS WITH MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
45MG	RINVOQ	ABBVIE	N211675	March 16, 2022	RX	TABLET, EXTENDED RELEASE	ORAL	March 16, 2025	TREATMENT OF ADULT PATIENTS WITH MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
15MG	RINVOQ	ABBVIE	N211675	Aug. 16, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	April 29, 2025	TREATMENT OF ADULTS WITH ACTIVE ANKYLOSING SPONDYLITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
15MG	RINVOQ	ABBVIE	N211675	Aug. 16, 2019	RX	TABLET, EXTENDED RELEASE	ORAL	May 18, 2026	TREATMENT OF ADULT PATIENTS WITH MODERATELY TO SEVERELY ACTIVE CROHNS DISEASE WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
30MG	RINVOQ	ABBVIE	N211675	Jan. 14, 2022	RX	TABLET, EXTENDED RELEASE	ORAL	May 18, 2026	TREATMENT OF ADULT PATIENTS WITH MODERATELY TO SEVERELY ACTIVE CROHNS DISEASE WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS
45MG	RINVOQ	ABBVIE	N211675	March 16, 2022	RX	TABLET, EXTENDED RELEASE	ORAL	May 18, 2026	TREATMENT OF ADULT PATIENTS WITH MODERATELY TO SEVERELY ACTIVE CROHNS DISEASE WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO ONE OR MORE TNF BLOCKERS

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Tyrosine-protein kinase JAK3	Kinase	P52333	JAK3_HUMAN	INHIBITOR	IC50	5.63	SCIENTIFIC LITERATURE	DRUG LABEL
Tyrosine-protein kinase JAK1	Kinase	P23458	JAK1_HUMAN	INHIBITOR	IC50	7.33	SCIENTIFIC LITERATURE	DRUG LABEL
Tyrosine-protein kinase JAK2	Kinase	O60674	JAK2_HUMAN	INHIBITOR	IC50	6.92	SCIENTIFIC LITERATURE	DRUG LABEL
AP2-associated protein kinase 1	Kinase	Q2M2I8	AAK1_HUMAN		Kd	5	CHEMBL
Cyclin-G-associated kinase	Kinase	O14976	GAK_HUMAN		Kd	5.66	CHEMBL
Non-receptor tyrosine-protein kinase TYK2	Kinase	P29597	TYK2_HUMAN	INHIBITOR	IC50	5.33	IUPHAR

External reference:

ID	Source
4RA0KN46E0	UNII
C4726929	UMLSCUI
CHEMBL3622821	ChEMBL_ID
58557659	PUBCHEM_CID
DB15091	DRUGBANK_ID
CHEMBL3707269	ChEMBL_ID
D10994	KEGG_DRUG
10209	INN_ID
9246	IUPHAR_LIGAND_ID
018092	NDDF
789397000	SNOMEDCT_US
789416006	SNOMEDCT_US
4038662	VANDF
2196092	RXNORM
321410	MMSL
37314	MMSL
d09350	MMSL
C000613732	MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Rinvoq	HUMAN PRESCRIPTION DRUG LABEL	1	0074-1043	TABLET, EXTENDED RELEASE	45 mg	ORAL	NDA	31 sections
Rinvoq	HUMAN PRESCRIPTION DRUG LABEL	1	0074-1043	TABLET, EXTENDED RELEASE	45 mg	ORAL	NDA	31 sections
Rinvoq	HUMAN PRESCRIPTION DRUG LABEL	1	0074-1043	TABLET, EXTENDED RELEASE	45 mg	ORAL	NDA	31 sections
Rinvoq	HUMAN PRESCRIPTION DRUG LABEL	1	0074-2306	TABLET, EXTENDED RELEASE	15 mg	ORAL	NDA	31 sections
Rinvoq	HUMAN PRESCRIPTION DRUG LABEL	1	0074-2306	TABLET, EXTENDED RELEASE	15 mg	ORAL	NDA	31 sections
Rinvoq	HUMAN PRESCRIPTION DRUG LABEL	1	0074-2306	TABLET, EXTENDED RELEASE	15 mg	ORAL	NDA	31 sections
Rinvoq	HUMAN PRESCRIPTION DRUG LABEL	1	0074-2306	TABLET, EXTENDED RELEASE	15 mg	ORAL	NDA	31 sections
Rinvoq	HUMAN PRESCRIPTION DRUG LABEL	1	0074-2310	TABLET, EXTENDED RELEASE	30 mg	ORAL	NDA	31 sections
Rinvoq	HUMAN PRESCRIPTION DRUG LABEL	1	0074-2310	TABLET, EXTENDED RELEASE	30 mg	ORAL	NDA	31 sections
Rinvoq	HUMAN PRESCRIPTION DRUG LABEL	1	0074-2310	TABLET, EXTENDED RELEASE	30 mg	ORAL	NDA	31 sections
Rinvoq	HUMAN PRESCRIPTION DRUG LABEL	1	0074-2310	TABLET, EXTENDED RELEASE	30 mg	ORAL	NDA	31 sections