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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:

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

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FDA Adverse Event Reporting System (Female)

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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

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FDA Adverse Event Reporting System (Male)

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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

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FDA Adverse Event Reporting System (Geriatric)

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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

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

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

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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

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🐶 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)

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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
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

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Orange Book exclusivity data (new drug applications)

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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
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
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
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	Aug. 16, 2024	NEW CHEMICAL ENTITY
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
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
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

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Bioactivity Summary:

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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

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External reference:

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ID	Source
018092	NDDF
10209	INN_ID
2196092	RXNORM
321410	MMSL
37314	MMSL
4038662	VANDF
4RA0KN46E0	UNII
58557659	PUBCHEM_CID
789397000	SNOMEDCT_US
789416006	SNOMEDCT_US

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Pharmaceutical products:

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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

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