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Xeljanz
tofacitinib
Black Box Warnings .
Serious Infections
incr. risk of serious infection leading to hospitalization or death; pulmonary and extrapulmonary TB, invasive fungal infections, and other opportunistic infections observed; most infections occur in combo w/ immunosuppressants; screen for latent TB infection before and during tofacitinib tx; initiate anti-TB tx before tofacitinib tx; weigh risk/benefit in patients w/ chronic or recurrent infection; monitor closely for infection signs/symptoms during and after tx, incl. TB development in patients w/ negative TB test; D/C tofacitinib if serious infection develops
Mortality
higher rate of mortality, incl. sudden cardiovascular death, observed in RA patients 50 yo and older w/ at least 1 cardiovascular risk factor treated w/ tofacitinib 5 mg bid or 10 mg bid vs. TNF blockers in a large, randomized, post-marketing study; tofacitinib 10 mg bid or 22 mg ER qd not recommended for tx of RA or psoriatic arthritis
Malignancies
malignancies, incl. lymphoma and solid tumors, occurred in patients treated w/ JAK inhibitors for inflammatory conditions; higher rate of malignancies (excluding non-melanoma skin CA), lymphoma, and lung CA observed in RA patients treated w/ tofacitinib 5 mg bid or 10 mg bid vs. TNF blockers; incr. risk in current or past smokers
Major Adverse Cardiovascular Events
higher rate of major adverse cardiovascular events, incl. cardiovascular death, non-fatal MI, and non-fatal stroke, observed in RA patients 50 yo and older w/ at least 1 cardiovascular risk factor treated w/ tofacitinib 5 mg bid or 10 mg bid vs. TNF blockers; incr. risk in current or past smokers; D/C tofacitinib in patients that experienced MI or stroke
Thrombosis
thrombosis, incl. PE, DVT, and arterial thrombosis occurred in patients treated w/ JAK inhibitors for inflammatory conditions; many adverse events were serious, sometimes fatal; higher rate of thrombosis observed in RA patients 50 yo and older w/ at least 1 cardiovascular risk factor on tofacitinib 5 mg bid or 10 mg bid vs. TNF blockers; avoid tofacitinib in patients w/ thrombosis risk; D/C tofacitinib and promptly evaluate patients w/ thrombosis symptoms
Adult Dosing .
Dosage forms: TAB: 5 mg, 10 mg; SOL: 1 mg per mL
Special Note
- [equivalency or interchangeability info]
- Info: tofacitinib IR products not interchangeable with ER product; do not substitute on a mg to mg basis
rheumatoid arthritis, moderate-severe
- [5 mg PO bid]
- Info: see pkg insert for toxicity-related dose adjustments
psoriatic arthritis
- [5 mg PO bid]
- Info: use w/ non-biologic DMARDs; see pkg insert for toxicity-related dose adjustments
ankylosing spondylitis
- [5 mg PO bid]
- Info: see pkg insert for toxicity-related dose adjustments
ulcerative colitis, moderate-severe
- [induction tx]
- Dose: 10 mg PO bid for at least 8wk; Info: may continue for up to 16wk based on response; D/C if no benefit after 16wk; see pkg insert for toxicity-related dose adjustments
- [maintenance tx]
- Dose: 5 mg PO bid; Start: after at least 8wk induction tx; Info: use lowest effective dose; may consider 10 mg PO bid limited to shortest duration if response lost; see pkg insert for toxicity-related dose adjustments
COVID-19 (off-label)
- [10 mg PO bid for up to 14 days]
- Info: for hospitalized patients w/ severe COVID-19 and elevated systemic inflammatory markers; not 1st-line agent; see pkg insert for toxicity-related dose adjustments
renal dosing
- [if usual dose 5 mg bid]
- CrCl <50: 5 mg qd
- HD: 5 mg qd, on dialysis days admin. after dialysis; no supplement; PD: not defined
- [if usual dose 10 mg bid]
- CrCl <50: 5 mg bid
- HD: 5 mg bid, on dialysis days admin. after dialysis; no supplement; PD: not defined
hepatic dosing
- [if usual dose 5 mg bid]
- Child-Pugh Class B: 5 mg qd; Child-Pugh Class C: avoid use
- [if usual dose 10 mg bid]
- Child-Pugh Class B: 5 mg bid; Child-Pugh Class C: avoid use
Peds Dosing .
- Dosage forms: TAB: 5 mg, 10 mg; SOL: 1 mg per mL
psoriatic arthritis
- [2 yo and older, 10-19 kg]
- Dose: 3.2 mg PO bid; Info: see pkg insert for toxicity-related dose adjustments
- [2 yo and older, 20-39 kg]
- Dose: 4 mg PO bid; Info: see pkg insert for toxicity-related dose adjustments
- [2 yo and older, >40 kg]
- Dose: 5 mg PO bid; Info: see pkg insert for toxicity-related dose adjustments
polyarticular juvenile idiopathic arthritis
- [2 yo and older, 10-19 kg]
- Dose: 3.2 mg PO bid; Info: see pkg insert for toxicity-related dose adjustments
- [2 yo and older, 20-39 kg]
- Dose: 4 mg PO bid; Info: see pkg insert for toxicity-related dose adjustments
- [2 yo and older, >40 kg]
- Dose: 5 mg PO bid; Info: see pkg insert for toxicity-related dose adjustments
renal dosing
- [adjust dose frequency]
- CrCl <50: give usual dose q24h
- HD: give usual dose q24h, on dialysis days admin. after dialysis; no supplement; PD: not defined
hepatic dosing
- [see below]
- Child-Pugh Class B: give usual dose q24h; Child-Pugh Class C: avoid use
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- baseline Hgb <9
- baseline lymphocytes <500
- baseline ANC <1000
- hepatic impairment, Child-Pugh Class C
- infection, active
- GI stricture, severe (ER form)
- thrombosis risk
- avoid: breastfeeding during tx and x18h after D/C (IR form)
- avoid: breastfeeding during tx and x36h after D/C (ER form)
- caution: elderly patients
- caution: patients of childbearing potential
- caution: CrCl <50
- caution: hepatic impairment, Child-Pugh Class B
- caution: opportunistic infection history
- caution: infection, chronic
- caution: infection, recurrent
- caution: infection risk
- caution: TB infection, active
- caution: TB infection, latent
- caution: TB infection risk
- caution: lung disease history, chronic
- caution: interstitial lung disease
- caution: herpes zoster history
- caution: HBV infection
- caution: HBV infection history
- caution: HCV infection
- caution: cardiovascular disease
- caution: cardiovascular disease risk
- caution: smokers
- caution: past smokers
- caution: malignancy
- caution: GI perforation risk
- caution: diabetes mellitus
Drug Interactions .
Overview
tofacitinib
JAK inhibitor
- CYP2C19 substrate
- CYP3A4 substrate
- immunomodulatory effects
- myelosuppressive effects
- thrombogenic effects
Contraindicated
- adenovirus vaccine, live
- BCG live intravesical
- chikungunya vaccine, live
- cholera vaccine, live
- dengue vaccine, live
- influenza nasal vaccine, live
- measles/mumps/rubella vaccine, live
- rotavirus vaccine, live
- smallpox vaccine, live
- talimogene laherparepvec
- typhoid vaccine, live
- varicella vaccine, live
- yellow fever vaccine, live
Avoid/Use Alternative
- abatacept
- abrocitinib
- adalimumab
- anakinra
- anti-thymocyte globulin
- apalutamide
- basiliximab
- belatacept
- belimumab
- bosentan
- butalbital
- canakinumab
- carbamazepine
- cenobamate
- certolizumab pegol
- cladribine oral
- cyclosporine
- dabrafenib
- deferiprone
- delgocitinib topical
- deuruxolitinib
- efavirenz
- encorafenib
- enzalutamide
- etanercept
- etrasimod
- etravirine
- everolimus
- fexinidazole
- fosamprenavir
- fosphenytoin
- ganciclovir
- golimumab
- grapefruit
- guselkumab
- infliximab
- ivosidenib
- ixekizumab
- lopinavir/ritonavir
- lorlatinib
- lumacaftor/ivacaftor
- lymphocyte immune globulin, anti-thymocyte globulin
- mavacamten
- mitapivat
- mitotane
- modafinil
- mycophenolate mofetil
- mycophenolic acid
- nafcillin
- natalizumab
- netupitant
- pacritinib
- penicillamine
- pentobarbital
- pexidartinib
- phenobarbital
- phenytoin
- pimecrolimus topical
- primaquine
- primidone
- rabies vaccine
- radium Ra 223 dichloride
- repotrectinib
- rifabutin
- rifampin
- rifapentine
- rilonacept
- ritlecitinib
- rituximab
- ropeginterferon alfa-2b
- ruxolitinib topical
- sarilumab
- secukinumab
- sipuleucel-T
- sirolimus
- sotorasib
- St. John's wort
- stiripentol
- tacrolimus
- tocilizumab
- tranexamic acid
- upadacitinib
- ustekinumab
- vaccinia immune globulin
- valganciclovir
- voclosporin
Monitor/Modify Tx
- abemaciclib
- acalabrutinib
- adagrasib
- ado-trastuzumab emtansine
- afamitresgene autoleucel
- aflibercept
- albendazole
- aldesleukin
- alemtuzumab
- allopurinol
- aminocaproic acid
- angiotensin II
- anthrax immune globulin
- anthrax vaccine
- anti-inhibitor coagulant complex
- antihemophilic factor (factor VIII)/von Willebrand factor complex
- aprepitant
- arsenic trioxide
- asciminib
- asparaginase
- atazanavir
- atidarsagene autotemcel
- auranofin
- avacopan
- avatrombopag
- axicabtagene ciloleucel
- axitinib
- azacitidine
- azathioprine
- balsalazide
- baricitinib
- bazedoxifene
- belantamab mafodotin
- belinostat
- bendamustine
- benznidazole
- berotralstat
- betibeglogene autotemcel
- bevacizumab
- bexarotene
- binimetinib
- blinatumomab
- bortezomib
- bosutinib
- botulism immune globulin
- brentuximab vedotin
- brexucabtagene autoleucel
- brolucizumab
- busulfan
- C1 esterase inhibitor
- cabazitaxel
- cabozantinib
- calaspargase
- cannabidiol
- cannabis
- capecitabine
- carboplatin
- carfilzomib
- carmustine
- celecoxib
- ceritinib
- chikungunya vaccine
- chlorambucil
- chloramphenicol
- chorionic gonadotropin
- cidofovir
- ciltacabtagene autoleucel
- ciprofloxacin
- cisplatin
- cladribine injection
- clarithromycin
- clofarabine
- clofazimine
- clozapine
- coagulation factor IX
- coagulation factor VIIa
- coagulation factor XIII A-subunit
- cobicistat
- colchicine
- concizumab
- conivaptan
- copanlisib
- COVID-19 vaccine
- crizotinib
- cyclophosphamide
- cytarabine
- cytomegalovirus immune globulin
- dacarbazine
- dactinomycin
- danazol
- dapsone
- daratumumab
- darbepoetin alfa
- darunavir
- dasatinib
- daunorubicin
- decitabine
- deferasirox
- deflazacort
- desogestrel (contraceptive)
- dexamethasone
- dexrazoxane
- diclofenac
- diclofenac topical
- dienogest (contraceptive)
- diflunisal
- diltiazem
- dinutuximab
- diphtheria/tetanus vaccine
- diphtheria/tetanus/pertussis vaccine
- docetaxel
- dostarlimab
- doxorubicin
- dronedarone
- drospirenone (contraceptive)
- drospirenone (hormone replacement)
- duvelisib
- ebola vaccine, live
- eflornithine
- elivaldogene autotemcel
- elranatamab
- eltrombopag
- enfortumab vedotin
- entrectinib
- epcoritamab
- epirubicin
- epoetin alfa
- eribulin
- erythromycin
- estetrol (contraceptive)
- estradiol (contraceptive)
- estradiol (hormone replacement)
- estrogens, conjugated (hormone replacement)
- estrogens, esterified (hormone replacement)
- ethinyl estradiol (contraceptive)
- ethinyl estradiol (hormone replacement)
- ethynodiol (contraceptive)
- etodolac
- etonogestrel (contraceptive)
- etoposide
- exagamglogene autotemcel
- factor XIII concentrate
- fam-trastuzumab deruxtecan
- faricimab
- fedratinib
- fenofibrate
- fenofibric acid
- fenoprofen
- fitusiran
- floxuridine
- fluconazole
- flucytosine
- fludarabine
- fluorouracil
- fluoxetine
- fluphenazine
- flurbiprofen
- fluvoxamine
- follitropin
- foscarnet
- fostamatinib
- fruquintinib
- gemcitabine
- gemtuzumab ozogamicin
- givinostat
- glasdegib
- glofitamab
- Haemophilus b vaccine
- hepatitis A vaccine
- hepatitis B immune globulin
- hepatitis B vaccine
- human papillomavirus vaccine
- hydroxychloroquine
- hydroxyurea
- ibritumomab tiuxetan
- ibrutinib
- ibuprofen
- idarubicin
- idecabtagene vicleucel
- idelalisib
- ifosfamide
- imatinib
- imetelstat
- immune globulin
- indomethacin
- influenza H5N1 vaccine
- influenza vaccine
- inotuzumab ozogamicin
- interferon beta 1a
- interferon beta 1b
- interferon gamma 1b
- iohexol
- iomeprol
- iopamidol
- irinotecan
- isatuximab
- isavuconazonium
- itraconazole
- ixabepilone
- Japanese encephalitis vaccine
- ketoconazole
- ketoprofen
- ketorolac
- lazertinib
- lefamulin
- leflunomide
- lenacapavir
- lenalidomide
- lenvatinib
- letermovir
- levoketoconazole
- levonorgestrel (contraceptive)
- levonorgestrel (hormone replacement)
- lifileucel
- linezolid
- linvoseltamab
- lisocabtagene maraleucel
- lomustine
- lonafarnib
- loncastuximab tesirine
- lovotibeglogene autotemcel
- lurbinectedin
- luspatercept
- lusutrombopag
- lutetium Lu 177 dotatate
- lutetium Lu 177 vipivotide tetraxetan
- meclofenamate
- medroxyprogesterone (contraceptive)
- medroxyprogesterone (hormone replacement)
- mefenamic acid
- megestrol
- meloxicam
- melphalan
- meningococcal vaccine
- menotropins
- mercaptopurine
- mesalamine
- mesalamine rectal
- methotrexate
- methoxy polyethylene glycol-epoetin beta
- methyltestosterone
- midostaurin
- mifepristone
- mitomycin
- mitoxantrone
- mogamulizumab
- momelotinib
- mosunetuzumab
- nabumetone
- naproxen
- necitumumab
- nefazodone
- nelarabine
- nelfinavir
- nilotinib
- nintedanib
- niraparib
- nirogacestat
- norelgestromin (contraceptive)
- norethindrone (contraceptive)
- norethindrone (hormone replacement)
- norgestimate (contraceptive)
- norgestrel (contraceptive)
- obecabtagene autoleucel
- obinutuzumab
- ofatumumab
- olaparib
- olsalazine
- omeprazole
- ospemifene
- oxaliplatin
- oxaprozin
- paclitaxel
- palbociclib
- panobinostat
- pazopanib
- pegaspargase
- peginterferon alfa 2a
- peginterferon beta 1a
- pemetrexed
- pentamidine
- pentostatin
- piroxicam
- pirtobrutinib
- pneumococcal vaccine
- polatuzumab vedotin
- poliovirus vaccine
- pomalidomide
- ponatinib
- porfimer
- posaconazole
- pralatrexate
- procarbazine
- progesterone (hormone replacement)
- progesterone vaginal (hormone replacement)
- proguanil
- prothrombin complex concentrate (human)
- pyrimethamine
- quizartinib
- raloxifene
- ramucirumab
- ranibizumab
- respiratory syncytial virus vaccine
- Rho(D) immune globulin
- ribavirin
- ribociclib
- rilzabrutinib
- ritonavir
- romidepsin
- romiplostim
- rucaparib
- ruxolitinib
- sacituzumab govitecan
- salsalate
- satralizumab
- segesterone (contraceptive)
- selinexor
- sirolimus albumin-bound
- smallpox/mpox vaccine, live
- sodium tetradecyl sulfate
- sotatercept
- streptozocin
- succimer
- sulfasalazine
- sulindac
- tafasitamab
- tagraxofusp
- talazoparib
- talquetamab
- tamoxifen
- tarlatamab
- tazemetostat
- teclistamab
- temozolomide
- temsirolimus
- teplizumab
- teriflunomide
- testosterone
- thalidomide
- thioguanine
- thiotepa
- tick-borne encephalitis vaccine
- tipranavir
- tisagenlecleucel
- tivozanib
- tolmetin
- topotecan
- toremifene
- trabectedin
- trametinib
- trastuzumab
- treosulfan
- tretinoin
- trifluridine
- trimethoprim
- tucatinib
- typhoid vaccine
- vadadustat
- valoctocogene roxaparvovec
- valproic acid
- vamorolone
- vancomycin
- varicella zoster immune globulin
- venetoclax
- verapamil
- vinblastine
- vincristine
- vinorelbine
- von Willebrand factor
- voriconazole
- vorinostat
- zanubrutinib
- zidovudine
- ziv-aflibercept
- zopapogene imadenovec
Caution Advised
- anifrolumab
- armodafinil
- artemether/lumefantrine
- beclomethasone inhaled
- beclomethasone nasal
- belzutifan
- betamethasone
- bimekizumab
- brigatinib
- brodalumab
- budesonide
- budesonide inhaled
- budesonide nasal
- budesonide rectal
- clobazam
- clobetasol ophthalmic
- coccidioides immitis skin test antigen
- corticotropin
- cortisone
- crovalimab
- danicopan
- danshen
- darolutamide
- deucravacitinib
- dexamethasone ophthalmic
- dicloxacillin
- difluprednate ophthalmic
- dimethyl fumarate
- diroximel fumarate
- dupilumab
- echinacea
- eculizumab
- efgartigimod alfa
- elafibranor
- elagolix
- elotuzumab
- emapalumab
- enasidenib
- eslicarbazepine acetate
- felbamate
- fingolimod
- fludrocortisone
- flunisolide nasal
- fluocinolone intravitreal
- fluorometholone ophthalmic
- fluticasone furoate
- fluticasone propionate
- garlic
- ginkgo
- ginseng, Asian
- glycerol phenylbutyrate
- griseofulvin
- hydrocortisone
- hydrocortisone ophthalmic
- inebilizumab
- iptacopan
- lebrikizumab
- loteprednol ophthalmic
- meropenem
- methylprednisolone
- mirikizumab
- mobocertinib
- mometasone implant
- mometasone inhaled
- mometasone nasal
- monomethyl fumarate
- nadofaragene firadenovec intravesical
- nevirapine
- nipocalimab
- ocrelizumab
- odevixibat
- olutasidenib
- omaveloxolone
- oxcarbazepine
- ozanimod
- pegcetacoplan
- perampanel
- pioglitazone
- ponesimod
- pozelimab
- prednisolone
- prednisolone ophthalmic
- prednisone
- ravulizumab
- regorafenib
- risankizumab
- rozanolixizumab
- rufinamide
- siltuximab
- siponimod
- spesolimab
- sunvozertinib
- sutimlimab
- suzetrigine
- tecovirimat
- telotristat ethyl
- tildrakizumab
- topiramate
- tovorafenib
- tralokinumab
- triamcinolone
- tuberculin purified protein derivative
- ublituximab
- vaborbactam
- vedolizumab
- vemurafenib
- vilobelimab
- vorasidenib
- zilucoplan
Adverse Reactions .
Serious Reactions
- mortality incr.
- cardiovascular death
- MI
- stroke
- infection, severe
- opportunistic infection
- viral reactivation
- HBV reactivation
- malignancy
- lymphoma
- lung CA
- non-melanoma skin CA
- pulmonary embolism
- DVT
- arterial thrombosis
- neutropenia
- lymphopenia
- anemia
- hypersensitivity reaction
- GI perforation
- interstitial lung disease
- infertility (animal studies)
Common Reactions
- URI
- cholesterol incr.
- headache
- CPK incr.
- rash
- diarrhea
- herpes zoster
- anemia
- nausea
- UTI
- HTN
- ALT or AST incr.
- lymphocytosis, transient
- Cr incr.
Safety/Monitoring .
Monitoring Parameters
hepatitis panel at baseline; CBC w/ diff at baseline, 4-8wk after tx start, then q3mo; TB test at baseline, then periodically; lipid panel 4-8wk after tx start; LFTs; dermatologic exams if incr. skin CA risk
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy; inadequate human data available; possible risk of embryo-fetal toxicity based on animal data at 6.3x and 73x MRHD
Individuals of Reproductive Potential
weigh risk/benefit in patients of childbearing potential; consider using effective contraception during tx
Lactation
Clinical Summary
avoid breastfeeding during tx and x18h after last IR dose or x36h after last ER dose; no known risk of infant harm based on limited human data, though drug excreted into milk; no human data available to assess effects on milk production
Pharmacology .
Metabolism: liver; CYP450: 2C19, 3A4 (primary) substrate
Excretion: urine (>65% unchanged); Half-life: 3h (IR forms), 6-8h (ER form)
Subclass: DMARDs, JAK Inhibitors ; Inflammatory Bowel Disease (IBD) ; Psoriasis, Systemic Agents ; Spondyloarthropathies
Mechanism of Action
inhibits janus-associated kinases (JAK) 1, 2, and 3, leading to disruption of cytokine and growth factor signaling pathways
Formulary .
No Formulary Selected
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