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Details

Stereochemistry ABSOLUTE
Molecular Formula C16H20N6O.C6H8O7
Molecular Weight 504.494
Optical Activity ( + )
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TOFACITINIB CITRATE

SMILES

C[C@]1([H])CCN(C[C@]1([H])N(C)c2c3cc[nH]c3ncn2)C(=O)CC#N.C(C(=O)O)C(CC(=O)O)(C(=O)O)O

InChI

InChIKey=SYIKUFDOYJFGBQ-YLAFAASESA-N
InChI=1S/C16H20N6O.C6H8O7/c1-11-5-8-22(14(23)3-6-17)9-13(11)21(2)16-12-4-7-18-15(12)19-10-20-16;7-3(8)1-6(13,5(11)12)2-4(9)10/h4,7,10-11,13H,3,5,8-9H2,1-2H3,(H,18,19,20);13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)/t11-,13+;/m1./s1

HIDE SMILES / InChI

Molecular Formula C6H8O7
Molecular Weight 192.1238
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C16H20N6O
Molecular Weight 312.3702
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: https://www.scribd.com/doc/296556203/A-Review-of-Tofacitinib-Drugs-Pros-and-Cons-of-Pharmaceuticals

Tofacitinib is an orally available inhibitor of Janus kinases (JAK), with immunomodulatory and anti-inflammatory activities. Upon administration, tofacitinib binds to JAK and prevents the activation of the JAK-signal transducers and activators of transcription (STAT) signaling pathway. This may decrease the production of pro-inflammatory cytokines, such as interleukin (IL)-6, -7, -15, -21, interferon-alpha and -beta, and may prevent both an inflammatory response and the inflammation-induced damage caused by certain immunological diseases. JAK kinases are intracellular enzymes involved in signaling pathways affecting hematopoiesis, immunity and inflammation. Tofacitinib was discovered and developed by the National Institutes of Health and Pfizer. Besides rheumatoid arthritis, tofacitinib has also been studied in clinical trials for the prevention of organ transplant rejection, and the treatment of psoriasis and ulcerative colitis. Patients treated with tofacitinib (XELJANZ) are at increased risk for developing serious infections that may lead to hospitalization or death and adverse reactions. Most patients who developed these infections were taking concomitant immunosuppressants such as methotrexate or corticosteroids.

CNS Activity

Curator's Comment:: Penetration of blood-brain barrier was observed both in tofacitinib treated mice.

Originator

Curator's Comment:: Tofacitinib (formerly tasocitinib, CP-690,550 is a medicine of the janus kinase (JAK) inhibitor class, discovered and also created by the National Institutes of Health and wellness and also Pfizer. Marketed as Xeljanz and also Jakvinus. # Pfizer and O'Shea's laboratory at the National Institute of Arthritis and Musculoskeletal and Skin Diseases of the National Institutes of Health

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P23458
Gene ID: 3716
Gene Symbol: JAK1
Target Organism: Homo sapiens (Human)
112 nM [IC50]
Target ID: O60674
Gene ID: 3717
Gene Symbol: JAK2
Target Organism: Homo sapiens (Human)
20 nM [IC50]
Target ID: P52333
Gene ID: 3718
Gene Symbol: JAK3
Target Organism: Homo sapiens (Human)
1 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Secondary
XELJANZ

Approved Use

Is indicated for the treatment of adult patients with moderately to severely active rheumatoid arthritis who have had an inadequate response or intolerance to methotrexate. It may be used as monotherapy or in combination with methotrexate or other nonbiologic disease-modifying antirheumatic drugs (DMARDs). XELJANZ should not be used in combination with biologic DMARDs or potent immunosuppressants such as azathioprine and cyclosporine.

Launch Date

1352160000000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
44.1 ng/mL
5 mg 2 times / day steady-state, oral
dose: 5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TOFACITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
38.7 ng/mL
11 mg 1 times / day steady-state, oral
dose: 11 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TOFACITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
41.2 ng/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOFACITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
36.7 ng/mL
11 mg single, oral
dose: 11 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOFACITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
346.9 ng/mL
100 mg single, oral
dose: 100 mg
route of administration: oral
experiment type: single
co-administered:
TOFACITINIB plasma
Homo sapiens
population: healthy
age:
sex:
food status:
565 ng/mL
100 mg single, oral
dose: 100 mg
route of administration: oral
experiment type: single
co-administered:
TOFACITINIB plasma
Homo sapiens
population: healthy
age:
sex:
food status:
647.4 ng/mL
100 mg single, oral
dose: 100 mg
route of administration: oral
experiment type: single
co-administered:
TOFACITINIB plasma
Homo sapiens
population: healthy
age:
sex:
food status:
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
266.1 ng × h/mL
5 mg 2 times / day steady-state, oral
dose: 5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TOFACITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
272.9 ng × h/mL
11 mg 1 times / day steady-state, oral
dose: 11 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TOFACITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
247.9 ng × h/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOFACITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
259.8 ng × h/mL
11 mg single, oral
dose: 11 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOFACITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
1673.1 ng*h/mL
100 mg single, oral
dose: 100 mg
route of administration: oral
experiment type: single
co-administered:
TOFACITINIB plasma
Homo sapiens
population: healthy
age:
sex:
food status:
2669.7 ng*h/mL
100 mg single, oral
dose: 100 mg
route of administration: oral
experiment type: single
co-administered:
TOFACITINIB plasma
Homo sapiens
population: healthy
age:
sex:
food status:
2670.2 ng*h/mL
100 mg single, oral
dose: 100 mg
route of administration: oral
experiment type: single
co-administered:
TOFACITINIB plasma
Homo sapiens
population: healthy
age:
sex:
food status:
3114.3 ng*h/mL
100 mg single, oral
dose: 100 mg
route of administration: oral
experiment type: single
co-administered:
TOFACITINIB plasma
Homo sapiens
population: healthy
age:
sex:
food status:
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
3.2 h
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOFACITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
5.9 h
11 mg single, oral
dose: 11 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOFACITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
3 h
5 mg 2 times / day multiple, oral
dose: 5 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TOFACITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
3.201 h
100 mg single, oral
dose: 100 mg
route of administration: oral
experiment type: single
co-administered:
TOFACITINIB plasma
Homo sapiens
population: healthy
age:
sex:
food status:
3.284 h
100 mg single, oral
dose: 100 mg
route of administration: oral
experiment type: single
co-administered:
TOFACITINIB plasma
Homo sapiens
population: healthy
age:
sex:
food status:
3.32 h
100 mg single, oral
dose: 100 mg
route of administration: oral
experiment type: single
co-administered:
TOFACITINIB plasma
Homo sapiens
population: healthy
age:
sex:
food status:
3.005 h
100 mg single, oral
dose: 100 mg
route of administration: oral
experiment type: single
co-administered:
TOFACITINIB plasma
Homo sapiens
population: healthy
age:
sex:
food status:
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
61%
TOFACITINIB plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
100 mg single, oral
Highest studied dose
Dose: 100 mg
Route: oral
Route: single
Dose: 100 mg
Sources:
healthy, 18–45 years
Health Status: healthy
Age Group: 18–45 years
Sex: M+F
Sources:
Other AEs: Nausea...
Other AEs:
Nausea (3 patients)
Sources:
30 mg 2 times / day steady, oral
Highest studied dose
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy, 54.2 years ( range: 30–71 years)
Health Status: unhealthy
Age Group: 54.2 years ( range: 30–71 years)
Sex: M+F
Sources:
Disc. AE: Herpes simplex skin chronic ulcers...
Other AEs: Viral infection, Dehydration...
AEs leading to
discontinuation/dose reduction:
Herpes simplex skin chronic ulcers (1 patient)
Other AEs:
Viral infection (severe, 1 patient)
Dehydration (severe, 1 patient)
Sources:
5 mg 2 times / day steady, oral
Recommended
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, adult
Other AEs: Infection, Lymphoma...
5 mg 2 times / day steady, oral
Recommended
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, adult
Disc. AE: Pneumonia, Herpes zoster...
AEs leading to
discontinuation/dose reduction:
Pneumonia (2.5%)
Herpes zoster (2.5%)
Aspartate aminotransferase increased (1.5%)
ALT increased (1.5%)
Creatinine increased (1.5%)
Gastrointestinal disorders (1%)
Respiratory disorder (0.4%)
Eye disorders (0.1%)
Skin disorder (1%)
Hepatobiliary disorders (0.3%)
Immune system disorders (0.1%)
Psychiatric disorders (0.1%)
Sources:
10 mg 2 times / day steady, oral
Dose: 10 mg, 2 times / day
Route: oral
Route: steady
Dose: 10 mg, 2 times / day
Sources:
unhealthy, adult
Disc. AE: Pneumonia, Herpes zoster...
AEs leading to
discontinuation/dose reduction:
Pneumonia (2.7%)
Herpes zoster (2.7%)
Aspartate aminotransferase increased (2%)
ALT increased (2%)
Creatinine increased (2%)
Gastrointestinal disorders (1.5%)
Respiratory disorder (0.6%)
Eye disorders (0.2%)
Skin disorder (0.3%)
Vascular disorders (0.3%)
Immune system disorders (0.1%)
Reproductive system and breast disorders (0.1%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Nausea 3 patients
100 mg single, oral
Highest studied dose
Dose: 100 mg
Route: oral
Route: single
Dose: 100 mg
Sources:
healthy, 18–45 years
Health Status: healthy
Age Group: 18–45 years
Sex: M+F
Sources:
Herpes simplex skin chronic ulcers 1 patient
Disc. AE
30 mg 2 times / day steady, oral
Highest studied dose
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy, 54.2 years ( range: 30–71 years)
Health Status: unhealthy
Age Group: 54.2 years ( range: 30–71 years)
Sex: M+F
Sources:
Dehydration severe, 1 patient
30 mg 2 times / day steady, oral
Highest studied dose
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy, 54.2 years ( range: 30–71 years)
Health Status: unhealthy
Age Group: 54.2 years ( range: 30–71 years)
Sex: M+F
Sources:
Viral infection severe, 1 patient
30 mg 2 times / day steady, oral
Highest studied dose
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy, 54.2 years ( range: 30–71 years)
Health Status: unhealthy
Age Group: 54.2 years ( range: 30–71 years)
Sex: M+F
Sources:
Lymphoma
5 mg 2 times / day steady, oral
Recommended
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, adult
Infection serious
5 mg 2 times / day steady, oral
Recommended
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, adult
Eye disorders 0.1%
Disc. AE
5 mg 2 times / day steady, oral
Recommended
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, adult
Immune system disorders 0.1%
Disc. AE
5 mg 2 times / day steady, oral
Recommended
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, adult
Psychiatric disorders 0.1%
Disc. AE
5 mg 2 times / day steady, oral
Recommended
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, adult
Hepatobiliary disorders 0.3%
Disc. AE
5 mg 2 times / day steady, oral
Recommended
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, adult
Respiratory disorder 0.4%
Disc. AE
5 mg 2 times / day steady, oral
Recommended
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, adult
Gastrointestinal disorders 1%
Disc. AE
5 mg 2 times / day steady, oral
Recommended
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, adult
Skin disorder 1%
Disc. AE
5 mg 2 times / day steady, oral
Recommended
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, adult
ALT increased 1.5%
Disc. AE
5 mg 2 times / day steady, oral
Recommended
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, adult
Aspartate aminotransferase increased 1.5%
Disc. AE
5 mg 2 times / day steady, oral
Recommended
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, adult
Creatinine increased 1.5%
Disc. AE
5 mg 2 times / day steady, oral
Recommended
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, adult
Herpes zoster 2.5%
Disc. AE
5 mg 2 times / day steady, oral
Recommended
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, adult
Pneumonia 2.5%
Disc. AE
5 mg 2 times / day steady, oral
Recommended
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, adult
Immune system disorders 0.1%
Disc. AE
10 mg 2 times / day steady, oral
Dose: 10 mg, 2 times / day
Route: oral
Route: steady
Dose: 10 mg, 2 times / day
Sources:
unhealthy, adult
Reproductive system and breast disorders 0.1%
Disc. AE
10 mg 2 times / day steady, oral
Dose: 10 mg, 2 times / day
Route: oral
Route: steady
Dose: 10 mg, 2 times / day
Sources:
unhealthy, adult
Eye disorders 0.2%
Disc. AE
10 mg 2 times / day steady, oral
Dose: 10 mg, 2 times / day
Route: oral
Route: steady
Dose: 10 mg, 2 times / day
Sources:
unhealthy, adult
Skin disorder 0.3%
Disc. AE
10 mg 2 times / day steady, oral
Dose: 10 mg, 2 times / day
Route: oral
Route: steady
Dose: 10 mg, 2 times / day
Sources:
unhealthy, adult
Vascular disorders 0.3%
Disc. AE
10 mg 2 times / day steady, oral
Dose: 10 mg, 2 times / day
Route: oral
Route: steady
Dose: 10 mg, 2 times / day
Sources:
unhealthy, adult
Respiratory disorder 0.6%
Disc. AE
10 mg 2 times / day steady, oral
Dose: 10 mg, 2 times / day
Route: oral
Route: steady
Dose: 10 mg, 2 times / day
Sources:
unhealthy, adult
Gastrointestinal disorders 1.5%
Disc. AE
10 mg 2 times / day steady, oral
Dose: 10 mg, 2 times / day
Route: oral
Route: steady
Dose: 10 mg, 2 times / day
Sources:
unhealthy, adult
ALT increased 2%
Disc. AE
10 mg 2 times / day steady, oral
Dose: 10 mg, 2 times / day
Route: oral
Route: steady
Dose: 10 mg, 2 times / day
Sources:
unhealthy, adult
Aspartate aminotransferase increased 2%
Disc. AE
10 mg 2 times / day steady, oral
Dose: 10 mg, 2 times / day
Route: oral
Route: steady
Dose: 10 mg, 2 times / day
Sources:
unhealthy, adult
Creatinine increased 2%
Disc. AE
10 mg 2 times / day steady, oral
Dose: 10 mg, 2 times / day
Route: oral
Route: steady
Dose: 10 mg, 2 times / day
Sources:
unhealthy, adult
Herpes zoster 2.7%
Disc. AE
10 mg 2 times / day steady, oral
Dose: 10 mg, 2 times / day
Route: oral
Route: steady
Dose: 10 mg, 2 times / day
Sources:
unhealthy, adult
Pneumonia 2.7%
Disc. AE
10 mg 2 times / day steady, oral
Dose: 10 mg, 2 times / day
Route: oral
Route: steady
Dose: 10 mg, 2 times / day
Sources:
unhealthy, adult
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 >30 uM]
no [IC50 >30 uM]
no [IC50 >30 uM]
no [IC50 >30 uM]
no [IC50 >30 uM]
no (co-administration study)
Comment: tofacitinib had no substatial effect on the exposure of midazolam
Page: 7, 9, 33
no
no
no
no
no
no
no
no
no
no
weak [IC50 150 uM]
weak [IC50 311 uM]
weak [IC50 55.3 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
minor
minor
minor
minor
minor
minor
minor
minor
minor
minor
no
yes
yes (co-administration study)
Comment: fluconazole increased tofactinib AUC by 79% and Cmax by 27%;
Page: 6, 8, 32, 89
yes
yes (co-administration study)
Comment: ketoconazole increased tofacitinib AUC by 103% and Cmax by 16%; fluconazole increased tofactinib AUC by 79% and Cmax by 27%; rifampin decreased tofacitinib AUC by 84% and Cmax by 74%
Page: 6, 8, 32, 89
yes
yes (co-administration study)
Comment: cyclosporine increased tofacitinib AUC by 73% and decreased Cmax by 17%; tofacitinib coadministration with cyclosproine is not recommended
Page: 6, 9, 33
PubMed

PubMed

TitleDatePubMed
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.
2003 Oct 31
Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550).
2008 Dec 25
Dissecting specificity in the Janus kinases: the structures of JAK-specific inhibitors complexed to the JAK1 and JAK2 protein tyrosine kinase domains.
2009 Mar 20
Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection.
2010 Dec 23
Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.
2010 Nov 24
Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.
2011 Jan 13
Comprehensive analysis of kinase inhibitor selectivity.
2011 Oct 30
Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity.
2011 Oct 30
EGCG enhances the therapeutic potential of gemcitabine and CP690550 by inhibiting STAT3 signaling pathway in human pancreatic cancer.
2012
Tofacitinib, a janus kinase inhibitor demonstrates efficacy in an IL-15 transgenic mouse model that recapitulates pathologic manifestations of celiac disease.
2013 Apr
A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
2013 Apr 15
Comparative pathophysiology, toxicology, and human cancer risk assessment of pharmaceutical-induced hibernoma.
2013 Dec 15
Clinical utility of the oral JAK inhibitor tofacitinib in the treatment of rheumatoid arthritis.
2013 Nov 15
JAK inhibitors: treatment efficacy and safety profile in patients with psoriasis.
2014
Ruxolitinib and tofacitinib are potent and selective inhibitors of HIV-1 replication and virus reactivation in vitro.
2014
Reversal of CD8 T-cell-mediated mucocutaneous graft-versus-host-like disease by the JAK inhibitor tofacitinib.
2014 Apr
Killing two birds with one stone: oral tofacitinib reverses alopecia universalis in a patient with plaque psoriasis.
2014 Dec
The JAK inhibitor tofacitinib suppresses synovial JAK1-STAT signalling in rheumatoid arthritis.
2015 Jun
Patents

Sample Use Guides

Recommended dose of XELJANZ is 5 mg twice daily. Recommended dose of XELJANZ XR is 11 mg once daily. Recommended dose in patients with moderate and severe renal impairment and moderate hepatic impairment is XELJANZ 5 mg once daily. Use of XELJANZ/XELJANZ XR in patients with severe hepatic impairment is not recommended.
Route of Administration: Oral
0-4000 nM tofacitinib was used in human T blasts cell to measure IL-2-dependent proliferation. CP-690550 (tofacitinib) was added to freshly plated cells and cultured for 4 days.
Substance Class Chemical
Created
by admin
on Fri Jun 25 21:25:38 UTC 2021
Edited
by admin
on Fri Jun 25 21:25:38 UTC 2021
Record UNII
O1FF4DIV0D
Record Status Validated (UNII)
Record Version
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Name Type Language
TOFACITINIB CITRATE
DASH   ORANGE BOOK   USAN   WHO-DD  
USAN  
Official Name English
TASOCITINIB CITRATE
Common Name English
TOFACITINIB CITRATE [USAN]
Common Name English
XELJANZ XR
Brand Name English
1-PIPERIDINEPROPANENITRILE, 4-METHYL-3-(METHYL-7H-PYRROLO(2,3-D)PYRIMIDIN-4-YLAMINO)-.BETA.-OXO-, (3R,4R)-, 2-HYDROXY-1,2,3-PROPANETRICARBOXYLATE (1:1)
Systematic Name English
TASOCITINIB MONOCITRATE
Common Name English
TOFACITINIB MONOCITRATE [MI]
Common Name English
CP-690550 CITRATE
Common Name English
TOFACITINIB CITRATE [WHO-DD]
Common Name English
3-((3R,4R)-4-METHYL-3-(METHYL(7H-PYRROLO(2,3-D)PYRIMIDIN-4-YL)AMINO)PIPERIDIN-1-YL)-3-OXO-PROPANENITRILE2-HYDROXYPROPANE-1,2,3-TRICARBOXYLATE (1:1)
Common Name English
XELJANZ
Brand Name English
TOFACITINIB CITRATE [ORANGE BOOK]
Common Name English
CP-690,550-10
Code English
CP-690550-10
Code English
CP-690
Common Name English
Classification Tree Code System Code
EMA ASSESSMENT REPORTS XELJANZ (REFUSED: ARTHRITIS, RHEUMATOID)
Created by admin on Fri Jun 25 21:25:38 UTC 2021 , Edited by admin on Fri Jun 25 21:25:38 UTC 2021
NCI_THESAURUS C1967
Created by admin on Fri Jun 25 21:25:38 UTC 2021 , Edited by admin on Fri Jun 25 21:25:38 UTC 2021
Code System Code Type Description
PUBCHEM
10174505
Created by admin on Fri Jun 25 21:25:38 UTC 2021 , Edited by admin on Fri Jun 25 21:25:38 UTC 2021
PRIMARY
NCI_THESAURUS
C95801
Created by admin on Fri Jun 25 21:25:38 UTC 2021 , Edited by admin on Fri Jun 25 21:25:38 UTC 2021
PRIMARY
JAPANESE REVIEW
XELJANZ
Created by admin on Fri Jun 25 21:25:38 UTC 2021 , Edited by admin on Fri Jun 25 21:25:38 UTC 2021
PRIMARY APPROVED MARCH 2013
MERCK INDEX
M10931
Created by admin on Fri Jun 25 21:25:38 UTC 2021 , Edited by admin on Fri Jun 25 21:25:38 UTC 2021
PRIMARY Merck Index
EVMPD
SUB33105
Created by admin on Fri Jun 25 21:25:38 UTC 2021 , Edited by admin on Fri Jun 25 21:25:38 UTC 2021
PRIMARY
FDA UNII
O1FF4DIV0D
Created by admin on Fri Jun 25 21:25:38 UTC 2021 , Edited by admin on Fri Jun 25 21:25:38 UTC 2021
PRIMARY
DRUG BANK
DBSALT000180
Created by admin on Fri Jun 25 21:25:38 UTC 2021 , Edited by admin on Fri Jun 25 21:25:38 UTC 2021
PRIMARY
EPA CompTox
540737-29-9
Created by admin on Fri Jun 25 21:25:38 UTC 2021 , Edited by admin on Fri Jun 25 21:25:38 UTC 2021
PRIMARY
RXCUI
1358492
Created by admin on Fri Jun 25 21:25:38 UTC 2021 , Edited by admin on Fri Jun 25 21:25:38 UTC 2021
PRIMARY RxNorm
CAS
540737-29-9
Created by admin on Fri Jun 25 21:25:38 UTC 2021 , Edited by admin on Fri Jun 25 21:25:38 UTC 2021
PRIMARY
ChEMBL
CHEMBL221959
Created by admin on Fri Jun 25 21:25:38 UTC 2021 , Edited by admin on Fri Jun 25 21:25:38 UTC 2021
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
PARENT -> SALT/SOLVATE
Related Record Type Details
ACTIVE MOIETY