Adverse Drug Reaction Classification System

Pharmaceutical Information
Drug Name Tofacitinib citrate
Drug ID BADD_D02237
Description Tofacitinib is an inhibitor of Janus kinases, a group of intracellular enzymes involved in signalling pathways that affect hematopoiesis and immune cell function. It is approved by the FDA for treatment of moderate to severe rheumatoid arthritis that responds inadequately to methotrexate or in those who are intolerant to methotrexate. Besides rheumatoid arthritis, tofacitinib has also been studied in clinical trials for the prevention of organ transplant rejection, and is currently under investigation for the treatment of psoriasis. Known adverse effects include nausea and headache as well as more serious immunologic and hematological adverse effects. Tofacitinib is marketed under the brand name Xeljanz by Pfizer.
Indications and Usage For the treatment of moderate to severe rheumatoid arthritis which is resistant or intolerant to methotrexate therapy. It may also be used as an adjunct to methotrexate therapy, or other non-biologic disease-modifying antirheumatic drugs (DMARDS), when methotrexate alone is not sufficient. Tofacitinib has also been investigated as a preventative therapy for kidney transplant rejections, and as a treatment for psoriasis, ulcerative colitis, and ankylosing spondylitis. It is not to be initiated in patients with a history of chronic or recurrent infections, or in the presence of active infection, even if localized, due to reports of serious and sometimes fatal infections (commonly pneumonia, herpes zoster and urinary tract infections). Use of tofacitinib is also discouraged in those who have been, or are likely to be, exposed to TB. An increased likelihood of exposure may be encountered by traveling to certain areas. In addition, tofacitinib is not to be used in patients with severe hepatic impairment, or low hemoglobin (less than 9g/dL). Cautioned is advised when using tofacitinib in patients at risk of gastrointestinal perforation, and in the elderly who are more susceptible to infection.
Marketing Status approved; investigational
ATC Code L04AA29
DrugBank ID DB08895
KEGG ID D09783
MeSH ID C479163
PubChem ID 10174505
TTD Drug ID D0EG1I
NDC Product Code 14501-0083; 42571-289; 60715-1000; 69037-0072; 42765-036; 76397-026; 76397-027; 66039-915; 73377-084; 17337-0079; 53747-053; 52076-6267; 69218-0700; 76397-028; 49574-523; 11712-895; 71052-554
UNII O1FF4DIV0D
Synonyms tofacitinib | tasocitinib | tofacitinib citrate | Xeljanz | CP 690,550 | CP690550 | CP-690550 | CP 690550 | CP-690,550
Chemical Information
Molecular Formula C22H28N6O8
CAS Registry Number 540737-29-9
SMILES CC1CCN(CC1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N.C(C(=O)O)C(CC(=O)O)(C(=O)O)O
Chemical Structure
ADRs Induced by Drug
*The priority for ADR severity classification is based on FAERS assessment, followed by the most severe level in CTCAE rating. If neither is available, it will be displayed as 'Not available'.
**The 'Not Available' level is hidden by default and can be restored by clicking on the legend twice.
ADR Term ADReCS ID ADR Frequency (FAERS) ADR Severity Grade (FAERS) ADR Severity Grade (CTCAE)
Abdominal pain07.01.05.002--
Alanine aminotransferase increased13.03.04.005--
Anaemia01.03.02.001--
Arthralgia15.01.02.001--
Aspartate aminotransferase increased13.03.04.011--
Blood bilirubin increased13.03.04.018--
Blood creatinine13.13.01.020---
Breast cancer16.10.01.001; 21.05.01.003---
Cellulitis11.02.01.001; 23.11.02.004---
Cough22.02.03.001--
Dehydration14.05.05.001--
Diarrhoea07.02.01.001--
Disseminated tuberculosis11.04.01.001---
Diverticulitis07.10.02.001; 11.01.07.003---
Dyspepsia07.01.02.001--
Dyspnoea02.11.05.003; 22.02.01.004--
Erythema23.03.06.001---
Fatigue08.01.01.002--
Gastric cancer07.21.02.001; 16.13.03.001---
Gastritis07.08.02.001--
Headache17.14.01.001--
Hepatic steatosis09.01.07.003; 14.08.04.005---
Herpes zoster11.05.02.003; 17.09.03.026; 23.11.05.005--
High density lipoprotein increased13.12.01.004---
Hypertension24.08.02.001--
Infection11.01.08.002---
Insomnia17.15.03.002; 19.02.01.002--
Joint swelling15.01.02.004---
Low density lipoprotein increased13.12.01.005---
Lymphocyte count decreased13.01.06.006--
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