U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C16H20N6O
Molecular Weight 312.3702
Optical Activity ( + )
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TOFACITINIB

SMILES

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

InChI

InChIKey=UJLAWZDWDVHWOW-YPMHNXCESA-N
InChI=1S/C16H20N6O/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/h4,7,10-11,13H,3,5,8-9H2,1-2H3,(H,18,19,20)/t11-,13+/m1/s1

HIDE SMILES / InChI

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
Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.
2011 Jan 13
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
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 21:26:13 UTC 2021
Edited
by admin
on Fri Jun 25 21:26:13 UTC 2021
Record UNII
87LA6FU830
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
TOFACITINIB
INN   MI   USAN   VANDF   WHO-DD  
USAN   INN  
Official Name English
CP-690550
Code English
1-PIPERIDINEPROPANENITRILE, 4-METHYL-3-(METHYL-7H-PYRROLO(2,3-D)PYRIMIDIN-4-YLAMINO)-.BETA.-OXO-, (3R,4R)-
Systematic Name English
CP-690 FREE BASE
Common Name English
CP690,550
Code English
CP690550
Code English
TOFACITINIB [MI]
Common Name English
3-PIPERIDINAMINE, 1-(CYANOACETYL)-4-METHYL-N-METHYL-N-1H-PYRROLO(2,3-D)PYRIMIDIN-4-YL-, (3R,4R)-
Systematic Name English
TOFACITINIB [INN]
Common Name English
TOFACITINIB [WHO-DD]
Common Name English
CP-690550 FREE BASE
Code English
CP-690,550 FREE BASE
Code English
3-((3R,4R)-4-METHYL-3-(METHYL(7H-PYRROLO(2,3-D)PYRIMIDIN-4-YL)AMINO)PIPERIDIN-1-YL)-3-OXOPROPANENITRILE
Systematic Name English
(+)-TOFACITINIB
Common Name English
TASOCITINIB
Common Name English
CP-690,550
Code English
TOFACITINIB [VANDF]
Common Name English
TOFACITINIB [USAN]
Common Name English
CP-690-550
Code English
Classification Tree Code System Code
LIVERTOX 974
Created by admin on Fri Jun 25 21:26:13 UTC 2021 , Edited by admin on Fri Jun 25 21:26:13 UTC 2021
WHO-ATC L04AA29
Created by admin on Fri Jun 25 21:26:13 UTC 2021 , Edited by admin on Fri Jun 25 21:26:13 UTC 2021
NCI_THESAURUS C1967
Created by admin on Fri Jun 25 21:26:13 UTC 2021 , Edited by admin on Fri Jun 25 21:26:13 UTC 2021
NDF-RT N0000190858
Created by admin on Fri Jun 25 21:26:13 UTC 2021 , Edited by admin on Fri Jun 25 21:26:13 UTC 2021
WHO-VATC QL04AA29
Created by admin on Fri Jun 25 21:26:13 UTC 2021 , Edited by admin on Fri Jun 25 21:26:13 UTC 2021
Code System Code Type Description
EPA CompTox
477600-75-2
Created by admin on Fri Jun 25 21:26:13 UTC 2021 , Edited by admin on Fri Jun 25 21:26:13 UTC 2021
PRIMARY
IUPHAR
5677
Created by admin on Fri Jun 25 21:26:13 UTC 2021 , Edited by admin on Fri Jun 25 21:26:13 UTC 2021
PRIMARY
MESH
C479163
Created by admin on Fri Jun 25 21:26:13 UTC 2021 , Edited by admin on Fri Jun 25 21:26:13 UTC 2021
PRIMARY
INN
9298
Created by admin on Fri Jun 25 21:26:13 UTC 2021 , Edited by admin on Fri Jun 25 21:26:13 UTC 2021
PRIMARY
FDA UNII
87LA6FU830
Created by admin on Fri Jun 25 21:26:13 UTC 2021 , Edited by admin on Fri Jun 25 21:26:13 UTC 2021
PRIMARY
PUBCHEM
9926791
Created by admin on Fri Jun 25 21:26:13 UTC 2021 , Edited by admin on Fri Jun 25 21:26:13 UTC 2021
PRIMARY
LACTMED
Tofacitinib
Created by admin on Fri Jun 25 21:26:13 UTC 2021 , Edited by admin on Fri Jun 25 21:26:13 UTC 2021
PRIMARY
CAS
477600-75-2
Created by admin on Fri Jun 25 21:26:13 UTC 2021 , Edited by admin on Fri Jun 25 21:26:13 UTC 2021
PRIMARY
MERCK INDEX
M10931
Created by admin on Fri Jun 25 21:26:13 UTC 2021 , Edited by admin on Fri Jun 25 21:26:13 UTC 2021
PRIMARY Merck Index
NDF-RT
N0000190857
Created by admin on Fri Jun 25 21:26:13 UTC 2021 , Edited by admin on Fri Jun 25 21:26:13 UTC 2021
PRIMARY Janus Kinase Inhibitors [MoA]
HSDB
8311
Created by admin on Fri Jun 25 21:26:13 UTC 2021 , Edited by admin on Fri Jun 25 21:26:13 UTC 2021
PRIMARY
RXCUI
1357536
Created by admin on Fri Jun 25 21:26:13 UTC 2021 , Edited by admin on Fri Jun 25 21:26:13 UTC 2021
PRIMARY RxNorm
NCI_THESAURUS
C95800
Created by admin on Fri Jun 25 21:26:13 UTC 2021 , Edited by admin on Fri Jun 25 21:26:13 UTC 2021
PRIMARY
ChEMBL
CHEMBL221959
Created by admin on Fri Jun 25 21:26:13 UTC 2021 , Edited by admin on Fri Jun 25 21:26:13 UTC 2021
PRIMARY
EVMPD
SUB33104
Created by admin on Fri Jun 25 21:26:13 UTC 2021 , Edited by admin on Fri Jun 25 21:26:13 UTC 2021
PRIMARY
DRUG CENTRAL
4713
Created by admin on Fri Jun 25 21:26:13 UTC 2021 , Edited by admin on Fri Jun 25 21:26:13 UTC 2021
PRIMARY
DRUG BANK
DB08895
Created by admin on Fri Jun 25 21:26:13 UTC 2021 , Edited by admin on Fri Jun 25 21:26:13 UTC 2021
PRIMARY
Related Record Type Details
METABOLIC ENZYME -> NON-INHIBITOR
METABOLIC ENZYME -> SUBSTRATE
MAJOR
TRANSPORTER -> NON-INHIBITOR
IC50
TRANSPORTER -> SUBSTRATE
EXCRETED UNCHANGED
URINE
TARGET -> INHIBITOR
METABOLIC ENZYME -> NON-INHIBITOR
NO INHIBITION AT 160 TIMES CMAX
METABOLIC ENZYME -> SUBSTRATE
MINOR
TARGET -> INHIBITOR
SALT/SOLVATE -> PARENT
TARGET -> INHIBITOR
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METABOLITE -> PARENT
METABOLITE -> PARENT
FECAL; PLASMA; URINE
METABOLITE -> PARENT
PLASMA; URINE
METABOLITE -> PARENT
PLASMA; URINE
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ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC