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tofacitinib solution 1 mg/mL Solution — NDC 00054-0821-58 package photo
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tofacitinib solution 1 mg/mL Solution — NDC 0054-0821-58 (Billing 00054-0821-58)

by Hikma Pharmaceuticals USA Inc. · 1 BOTTLE in 1 CARTON / 240 mL in 1 BOTTLE

This is a package of tofacitinib solution 1 mg/mL Solution from Hikma Pharmaceuticals USA Inc., marketed since Jun 2026 and currently FDA-listed. It is this product's only package size.

NDC 00054-0821-58
🏷️ FDA NDC (as labeled) 0054-0821-58 billing pads the labeler segment with a zero
Rx only Generic On market Non-controlled ⇄ Compare with another NDC
🗂️ FDA directory synced Oct 1, 2026 · this listing last changed Aug 20, 2026 · sources: openFDA · FDA label (DailyMed) · FDA Orange & Purple Book · First Databank · CMS NADAC, ASP, Medicare & Medicaid · RxNorm
📋 All sources & update times →

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Compiled from public FDA, CMS, DailyMed, NADAC, and related drug data sources. Editorial policy

NDC database record

One package, one record: these facts belong to NDC 0054-0821-58 alone.

Record
FDA NDC Directory package listing · Human prescription drug
Code segments
0054 labeler · 0821 product · 58 package
Package marketed since
Jun 3, 2026
Sample package
No — commercial package
Listing certified through
Dec 31, 2027
Barcode (UPC)
0300540821586
FDA record last changed
Aug 20, 2026

Identity & classification

Regulatory identifiers FDA, NLM and CMS codes for this package

FDA NDC (as labeled) 0054-0821-58
Product NDC 0054-0821
11-digit billing NDC 00054082158
NCPDP billing unit ML — per mL (volume)
RxCUI 2478433
UNII O1FF4DIV0D
UPC 0300540821586
Application # ANDA216878
SPL Set ID d9cf18a9-e825-49ac-b080-68957c0e79ae
Established class (EPC) Janus Kinase Inhibitor
Mechanism of action Janus Kinase Inhibitors
DEA schedule Non-controlled
Marketing category ANDA
Marketing status On market
FDA listing status Listed (active directory)
Marketing start 2026-06-03
Route ORAL
Dosage form SOLUTION
Substance TOFACITINIB CITRATE
TE code (Orange Book) AA · RLD · RS

Drug-database identifiers Medi-Span GPI and First Databank GCN / HICL / AHFS classification

GCN Seq No 081537
GCN 48684
HICL code 039768
Ingredient (HICL) Tofacitinib Citrate
HIC1 code Z
Therapeutic class — broad (HIC1) Body As A Whole
HIC2 code Z2
Therapeutic class — intermediate (HIC2) Antihistamines, Antiserotonins, Immunosuppressants
HIC3 code Z2Z
Therapeutic class — specific (HIC3) Janus Kinase (Jak) Inhibitors
AHFS code 90:24.12.92
AHFS class Janus Kinase Inhibitors, Miscellaneous
FDB label name TOFACITINIB 1 MG/ML SOLUTION
FDB brand name Tofacitinib Citrate
Legend status F — Federal legend — prescription drug or device
Quick answers
  • GSN (GCN sequence number): 081537
  • GCN: 48684
  • HICL (First Databank): 039768
  • AHFS class code: 90:24.12.92
  • RxCUI (RxNorm): 2478433
Why two NDCs? The FDA registers this code as 0054-0821-58 — a 4-4-2 layout, and that's what's printed on the package and shown on DailyMed. For insurance claims, every NDC is standardized to a uniform 11-digit 5-4-2 format by adding a zero to the labeler segment → 00054-0821-58. Same drug, same package — only the format differs.
Where does this data come from?
Identifiers from the FDA openFDA NDC Directory and Structured Product Labeling; RxCUI from RxNorm (NLM); GPI from Medi-Span; GCN / HIC / AHFS / legend from First Databank.

RxNorm drug class

This medicine belongs to the Janus Kinase Inhibitor class.

Pharmacologic class Janus Kinase Inhibitor
Drug family (ATC) Janus-associated kinase (JAK) inhibitors
How it works Janus Kinase Inhibitors
Where does this data come from?
Therapeutic classes from RxNorm RxClass (U.S. National Library of Medicine) — Established Pharmacologic Class (FDA), ATC drug family (WHO) and mechanism of action, matched by this product’s RxCUI.

Clinical

Label name TOFACITINIB 1 MG/ML SOLUTION Ingredient Tofacitinib Citrate
📗 Our plain-language guide HelloPharmacist
  • It treats rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis and ulcerative colitis in adults, usually after a TNF blocker didn't work or wasn't tolerated. Xeljanz a...
  • You take it by mouth. Tablets and solution are usually taken twice a day, and extended-release tablets once a day. It can be taken with or without food. Follow your prescriber's di...
  • Colds, stuffy or sore nose and throat, diarrhea, and headache are most common. Some people with ulcerative colitis also get rash, shingles, or higher cholesterol. Call your doctor...
  • Get help right away for chest pain, stroke symptoms, sudden shortness of breath, or leg swelling and pain, which can signal a clot or heart problem. Also report new belly pain, sig...
📖 Read our full Tofacitinib guide →
Where does this data come from?
Plain-language summary from MedlinePlus (U.S. National Library of Medicine); supplement & herbal interactions and nutrient depletion data from the Natural Medicines database; our full guide is HelloPharmacist editorial content.

Pricing

A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.

Price systemPer mLPer package
Retail pharmacies payNADAC · weekly Not in the retail survey — common for institutional, discontinued, or low-volume packs.
Medicaid paysCMS SDUD · 12 mo No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data.
Medicare drug plans payPart D · quarterly No Part D plan price is available for this NDC in our data.
ℹ️
No price is published for this exact package yet. CMS surveys NADAC per package size, so a different pack of the same drug often has one.
Where does this data come from?
NADAC (National Average Drug Acquisition Cost) is the CMS weekly pharmacy-acquisition-cost survey — what pharmacies pay. ASP (Average Sales Price) is the CMS Medicare Part B drug-payment file, published quarterly. Medicaid pays is computed by us from CMS State Drug Utilization Data (total reimbursed ÷ units, trailing 12 months) — gross of rebates and inclusive of dispensing fees, so it reflects what Medicaid paid, not an acquisition cost. Medicare drug plans pay is the median negotiated point-of-sale unit cost across plans listing this NDC in the CMS quarterly Prescription Drug Plan pricing files, before rebates. The VA pays is the federal contract price (FSS, and the statutory Big 4 ceiling where listed) from the VA National Acquisition Center pharmaceutical price file. All are free public government data; each measures a different payer, so the figures are not directly comparable.

Packaging — all sizes for this product

Package NDCDescription Marketing startMarketing endStatus
00054-0821-58 You're viewing this Main listing 1 BOTTLE in 1 CARTON / 240 mL in 1 BOTTLE 2026-06-03 — Active

Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
tofacitinib solution 1 mg/mLthis 00054-0821-58 Hikma 1 bottle — AA FDA listed —
Xeljanz 1 mg/mL 00069-1029-02 Pfizer 1 bottle — AA FDA listed —
Xeljanz 1 mg/mL 63539-0029-02 U.S. 1 bottle — AA FDA listed —
Tofacitinib 1 mg/mL 70095-0008-02 Sun 1 bottle — AA FDA listed —
Tofacitinib 1 mg/mL 71085-0099-24 IPG 1 bottle — AA FDA listed —
Tofacitinib 1 mg/mL 72205-0121-81 Novadoz 240 ml — AA FDA listed —
About this product: this is a generic version of the medicine. FDA equivalence ratings are shown when available, and other versions are listed above, least expensive first.
Where does this data come from?
Equivalents are other NDCs of the same ingredient, form and route from the openFDA NDC Directory, ranked least-expensive-first by NADAC. Therapeutic-equivalence (AB) ratings come from the FDA Orange Book; biologics use the FDA Purple Book for biosimilar & interchangeable status.

Availability & generic status

🏛️
2026
On the market since
Jun 2026
📍
2026
Currently FDA-listed
listed with the FDA
🔓
·
Generic on the market
this product is a generic
✅This is a generic drug

This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.

Where does this data come from?
Patents and exclusivity from the FDA Orange Book (small-molecule drugs), refreshed from public FDA data. Generic launch timing is an estimate, not a guarantee.

What it looks like

FlavorGrape
One label can cover several strengths, so colors may be combined — always confirm a loose pill against the dispensed prescription label or a pharmacist.
Where does this data come from?
Physical description (imprint, shape, color, scoring, coating) from this product’s FDA Structured Product Labeling (SPL), mirrored from DailyMed / openFDA.

Inactive Ingredients / Excipients

Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.

💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.

  • UNII QTT17582CB
    A strong acid used to adjust and maintain the proper pH level in liquid medicines, ensuring stability and preventing breakdown of active ingredients.
  • UNII 4550K0SC9B
    Sodium acetate is a salt derived from acetic acid. It acts as a buffer to help maintain the medicine's pH stability and may serve as a preservative or solubilizer in liquid formulations.
  • UNII OJ245FE5EU
    Sodium benzoate is a salt derived from benzoic acid, a preservative. It's added to medicines to prevent growth of bacteria, fungi, and other microorganisms that could spoil the product.
  • UNII 55X04QC32I
    A strong alkaline chemical used to adjust and maintain the pH balance of liquid medicines. It helps keep the medicine stable and ensures it stays effective during storage.
  • UNII 96K6UQ3ZD4
    Sucralose is a synthetic sweetener made from sugar. It's added to medicines to improve taste without adding calories, helping make bitter or unpleasant-tasting drugs easier to take.
  • UNII W4888I119H
    Tartaric acid is a natural organic acid found in grapes and tamarinds. In medicines, it works as a buffer to control acidity, an antioxidant to prevent spoilage, and sometimes a flavoring or binding agent.
  • UNII 059QF0KO0R
    Water is a liquid solvent that dissolves and mixes ingredients together in liquid medicines, syrups, and injections. It helps distribute the active drug evenly throughout the product.
  • UNII 3GOV20705G
    Wine grape is a plant-derived ingredient used as a natural flavoring and color source in medications. It provides taste and appearance while serving as a filler or binding component in the formulation.

8 inactive ingredients listed in the exact product block matched to this NDC.

Where does this data come from?
Data sourced from official FDA Structured Product Labeling (SPL) via DailyMed — ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.

Inactive ingredient FAQ

Are inactive ingredients the same for every manufacturer?
No. Inactive ingredients can differ by manufacturer, dosage form, strength, and package / product version.
Why might an inactive ingredient be missing?
Some SPLs do not provide a complete structured inactive-ingredient list, and older or unusual labels may only include the information in narrative text.
Can inactive ingredients matter?
Yes. They can matter for allergies, intolerances, dyes, gluten / lactose concerns, preservatives, and formulation differences — but confirm with a pharmacist or the manufacturer when it’s clinically important.

Manufacturer & labeler

LabelerHikma Pharmaceuticals USA Inc.
Application holderHIKMA PHARMACEUTICALS USA INC
FDA applicationANDA216878 (ANDA)
Labeler code00054
First marketedJun 2026
Product typeHuman Prescription Drug
Portfolio726 products on file

More NDCs from Hikma Pharmaceuticals USA Inc. labeler code 00054

The labeler markets the product; the application holder owns the FDA approval. They’re often the same company but can differ (e.g. a repackager or an authorized generic). A mailing address / phone appears here when the manufacturer includes it in the product’s FDA label (not all do).
Where does this data come from?
Labeler, application holder and registered establishment from the FDA openFDA NDC Directory and Drugs@FDA; address/contact from the product’s FDA label.

Full prescribing information FDA SPL

The complete FDA label for this product — the official prescribing information, verbatim, section by section. Very long sections are excerpted here and marked; the full text is on DailyMed (linked in the sources below). Jump with a chip, search within the label, or expand everything.
🚨 Boxed Warning 🎯 Indications and Usage ⏱️ Dosage and Administration 💊 Dosage Forms and Strengths ⛔ Contraindications ⚠️ Warnings and Cautions 🤒 Adverse Reactions 🔄 Drug Interactions 👥 Use in Specific Populations 🤰 Pregnancy 🧒 Pediatric Use 🧓 Geriatric Use 🆘 Overdosage 🧬 Clinical Pharmacology 🧬 Mechanism of Action 📦 How Supplied / Storage and Handling 📋 Description 💬 Information for Patients 💬 Medication Guide 🧬 Pharmacokinetics 🧬 Pharmacodynamics 🔬 Clinical Studies 🧪 Nonclinical Toxicology 📄 Carcinogenesis, Mutagenesis, Impairment of Fertility 📖 Instructions for Use 📄 Recent Major Changes 📄 Package Label / Principal Display Panel
🚨 Boxed Warning ~3 min read ▾

WARNING: SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS, and THROMBOSIS SERIOUS INFECTIONS Patients treated with tofacitinib are at increased risk for developing serious bacterial, fungal, viral, and opportunistic infections, including tuberculosis (TB), that may lead to hospitalization or death [see Warnings and Precautions ( 5.1 ), Adverse Reactions ( 6.1 )] . Most patients who developed these infections were taking concomitant immunosuppressants such as methotrexate or corticosteroids.

Reported infections included: • Active TB, which may present with pulmonary or extrapulmonary disease. Patients should be tested for latent TB before tofacitinib use and during therapy. Treatment for latent infection should be initiated prior to tofacitinib use. • Invasive fungal infections, including cryptococcosis and pneumocystosis.

Patients with invasive fungal infections may present with disseminated, rather than localized, disease. • Bacterial, viral, including herpes zoster, and other infections due to opportunistic pathogens. The risks and benefits of tofacitinib treatment should be carefully considered prior to initiating therapy in patients with chronic or recurrent infection. Patients should be closely monitored for the development of signs and symptoms of infection during and after tofacitinib treatment, including the possible development of TB in patients who tested negative for latent TB infection prior to initiating therapy.

If a serious infection develops, interrupt tofacitinib until the infection is controlled [see Warnings and Precautions ( 5.1 )] . MORTALITY In a large, randomized, postmarketing safety study in rheumatoid arthritis (RA) patients 50 years of age and older with at least one cardiovascular (CV) risk factor comparing tofacitinib tablets 5 mg or 10 mg twice a day to tumor necrosis factor (TNF) blockers, a higher rate of all-cause mortality, including sudden CV death, was observed with tofacitinib tablets 5 mg or 10 mg twice a day [see Warnings and Precautions ( 5.2 )] .

Tofacitinib tablets 10 mg twice daily and tofacitinib extended-release tablets 22 mg once daily dosages are not recommended for the treatment of RA, psoriatic arthritis (PsA), ankylosing spondylitis (AS), or polyarticular course juvenile idiopathic arthritis (pcJIA) [see Dosage and Administration ( 2.4 )] . MALIGNANCIES Malignancies, including lymphomas and solid tumors, have occurred in patients treated with tofacitinib and other Janus kinase inhibitors used to treat inflammatory conditions. In RA patients, a higher rate of malignancies (excluding non-melanoma skin cancer (NMSC)) was observed in patients treated with tofacitinib tablets 5 mg or 10 mg twice a day compared with TNF blockers [see Warnings and Precautions ( 5.3 )] .

Lymphomas and lung cancers were observed at a higher rate in patients treated with tofacitinib tablets 5 mg or 10 mg twice a day in RA patients compared to those treated with TNF blockers. Patients who are current or past smokers are at additional increased risk. MAJOR ADVERSE CARDIOVASCULAR EVENTS RA patients 50 years of age and older with at least one cardiovascular risk factor, treated with tofacitinib tablets 5 mg or 10 mg twice daily, had a higher rate of major adverse cardiovascular events (MACE) (defined as cardiovascular death, myocardial infarction, and stroke), compared to those treated with TNF blockers.

Patients who are current or past smokers are at additional increased risk. Discontinue tofacitinib oral solution in patients that have experienced a myocardial infarction or stroke [see Warnings and Precautions ( 5.4 )] . THROMBOSIS Thrombosis, including pulmonary embolism, deep venous thrombosis, and arterial thrombosis have occurred in patients treated with tofacitinib and other Janus kinase inhibitors used to treat inflammatory conditions.

Many of these events were serious and some resulted in death. RA patients 50 years of age and older with at least one cardiovascular risk… [Excerpted — this section continues on DailyMed.]

🎯 Indications and Usage ~1 min read ▾

1 INDICATIONS AND USAGE Tofacitinib is a Janus kinase (JAK) inhibitor. Tofacitinib oral solution is indicated for the treatment of pediatric patients 2 years of age and older with: • Active psoriatic arthritis (PsA), who have had an inadequate response or intolerance to one or more TNF blockers. • Active polyarticular course juvenile idiopathic arthritis (pcJIA), who have had an inadequate response or intolerance to one or more TNF blockers. Limitations of Use : • Use of tofacitinib oral solution for PsA or pcJIA in combination with biologic DMARDs or potent immunosuppressants such as azathioprine and cyclosporine is not recommended ( 1.2 , 1.4 )

1.2Psoriatic Arthritis Tofacitinib oral solution is indicated for the treatment of adult and pediatric patients 2 years of age and older with active psoriatic arthritis (PsA), who have had an inadequate response or intolerance to one or more TNF blockers. Limitations of Use Use of tofacitinib in combination with biologic DMARDs or with potent immunosuppressants such as azathioprine and cyclosporine is not recommended.

1.4Polyarticular Course Juvenile Idiopathic Arthritis Tofacitinib oral solution is indicated for the treatment of pediatric patients 2 years of age and older with active polyarticular course juvenile idiopathic arthritis (pcJIA), who have had an inadequate response or intolerance to one or more TNF blockers. Limitations of Use Use of tofacitinib in combination with biologic DMARDs or with potent immunosuppressants such as azathioprine and cyclosporine is not recommended.

⏱️ Dosage and Administration ~3 min read ▾

2 DOSAGE AND ADMINISTRATION Recommended Evaluations and Immunization Prior to Treatment Initiation • Prior to initiating tofacitinib oral solution, consider performing an active and latent TB evaluation, viral hepatitis screening, a complete blood count, and updating immunizations. Avoid tofacitinib initiation if absolute lymphocyte count <500 cells/mm 3 , an absolute neutrophil count (ANC) <1,000 cells/mm 3 or hemoglobin <9 g/dL. ( 2.1 ) Important Administration Instructions • Tofacitinib extended-release tablets are not substitutable with tofacitinib tablets and tofacitinib oral solution.

( 2.2 ) • Switching between tofacitinib oral solution and tofacitinib extended-release tablets should be made by the healthcare provider. ( 2.2 ) Recommended Dosage Pediatric Patients 2 Years of Age and Older with PsA or pcJIA Who Weigh At Least 10 kg • Tofacitinib oral solution 5 mg twice daily for those ≥40 kg or weight-based equivalent twice daily for those <40 kg. ( 2.4 ) Dosage in Patients with Renal Impairment or Hepatic Impairment • Use of tofacitinib in patients with severe HI is not recommended.

( 2.4 , 8.7 ) • See full prescribing information (FPI) for recommended dosage in patients with moderate or severe RI or moderate HI. ( 2.4 , 8.6 , 8.7 ) Dosage Modification See the full prescribing information for dosage modification by indication for patients who concomitantly use CYP2C19 and/or CYP3A4 inhibitors and patients with lymphopenia, neutropenia, or anemia. ( 2.4 , 7 )

2.1Recommended Evaluations and Immunization Prior to Treatment Initiation Prior to initiating tofacitinib oral solution, consider performing the following: • Active and latent tuberculosis (TB) infection evaluation: If the patient has latent TB, treat for TB prior to tofacitinib treatment [see Warnings and Precautions ( 5.1 )] . • Viral hepatitis screening in accordance with clinical guidelines [see Warnings and Precautions ( 5.1 )] . • A complete blood count: Avoid initiation of tofacitinib treatment in patients with a lymphocyte count less than 500 cells/mm 3 , absolute neutrophil count less than 1,000 cells/mm 3 , or hemoglobin level less than 9 g/dL [see Warnings and Precautions ( 5.9 )] . • Baseline hepatic function evaluation: tofacitinib is not recommended for patients with severe hepatic impairment [see Use in Specific Populations ( 8.7 ) and Clinical Pharmacology ( 12.3 )] . • Update immunizations according to current immunization guidelines.

The interval between live vaccinations and initiation of tofacitinib should be in accordance with current vaccination guidelines regarding immunosuppressive agents [see Warnings and Precautions ( 5.10 )] .

2.2Important Administration Instructions • Tofacitinib extended-release tablets are not substitutable with tofacitinib oral solution. Switching between tofacitinib oral solution and tofacitinib extended-release tablets should be made by the healthcare provider. • Dose interruption is recommended for management of lymphopenia, neutropenia, and anemia [see Warnings and Precautions ( 5.9 ) and Adverse Reactions ( 6.1 )] . • Interrupt use of tofacitinib oral solution if a patient develops a serious infection until the infection is controlled [see Warnings and Precautions ( 5.1 )] . • Take tofacitinib oral solution with or without food [see Clinical Pharmacology ( 12.3 )] .

2.4Recommended Dosage in Pediatric Patients 2 Years of Age and Older with Psoriatic Arthritis or Polyarticular Course Juvenile Idiopathic Arthritis Table 2 displays the recommended body weight-based dosages for tofacitinib oral solution in pediatric patients 2 years of age and older with PsA or pcJIA [see Indication and Usage ( 1.2 , 1.4 )] with and without renal impairment (including those who are undergoing hemodialysis) or hepatic impairment [see Use in Specific Populations ( 8.6 , 8.7 )] . The table also includes recommended dosage modification for pediatric patients concomitantly using CYP2C19 and/or CYP3A4 inhibitors [see Drug Interactions (… [Excerpted — this section continues on DailyMed.]

💊 Dosage Forms and Strengths 25 words ▾

3 DOSAGE FORMS AND STRENGTHS Tofacitinib oral solution: 1 mg/mL of tofacitinib: Clear, colorless oral solution. • Tofacitinib oral solution: 1 mg/mL ( 3 )

⛔ Contraindications 7 words ▾

4 CONTRAINDICATIONS None. None. ( 4 )

⚠️ Warnings and Cautions ~3 min read ▾

5 WARNINGS AND PRECAUTIONS • Serious Infections : Avoid use of tofacitinib during an active serious infection, including localized infections. ( 5.1 ) • Gastrointestinal Perforations : Promptly evaluate patients at increased risk for gastrointestinal perforation who present with new onset abdominal symptoms. ( 5.6 ) • Hypoglycemia in Patients with Diabetes : Consider increased monitoring of blood glucose; advise patients with diabetes to notify their healthcare provider if they develop signs or symptoms of hypoglycemia.

( 5.8 ) • Laboratory Monitoring : Recommended due to potential changes in lymphocytes, neutrophils, hemoglobin, liver enzymes and lipids. ( 5.9 ) • Vaccinations : Avoid use of live vaccines concurrently with tofacitinib. ( 5.10 )

5.1Serious Infections Serious and sometimes fatal infections may occur with tofacitinib. Serious and sometimes fatal infections due to bacterial, mycobacterial, invasive fungal, viral, or other opportunistic pathogens have been reported in patients receiving tofacitinib. The most common serious infections reported with tofacitinib included pneumonia, urinary tract infection, cellulitis, herpes zoster, bronchitis, septic shock, diverticulitis, gastroenteritis, appendicitis, and sepsis.

Among opportunistic infections, tuberculosis and other mycobacterial infections, cryptococcosis, histoplasmosis, esophageal candidiasis, pneumocystosis, multi-dermatomal herpes zoster, cytomegalovirus infections, BK virus infection, and listeriosis were reported with tofacitinib. Some patients have presented with disseminated rather than localized disease, and were often taking concomitant immunomodulating agents such as methotrexate or corticosteroids. In the UC population, treatment with tofacitinib tablets 10 mg twice daily was associated with greater risk of serious infections compared to 5 mg twice daily.

Additionally, opportunistic herpes zoster infections (including meningoencephalitis, ophthalmologic, and disseminated cutaneous) were seen in patients who were treated with tofacitinib tablets 10 mg twice daily. Other serious infections that were not reported in clinical studies may also occur (e.g., coccidioidomycosis). Avoid use of tofacitinib in patients with an active, serious infection, including localized infections.

The risks and benefits of treatment should be considered prior to initiating tofacitinib in patients: • with chronic or recurrent infection • who have been exposed to tuberculosis • with a history of a serious or an opportunistic infection • who have resided or traveled in areas of endemic tuberculosis or endemic mycoses; or • with underlying conditions that may predispose them to infection. Closely monitor patients for the development of signs and symptoms of infection during and after treatment with tofacitinib. Interrupt tofacitinib if a patient develops a serious infection, an opportunistic infection, or sepsis.

In patients who develop a new infection during treatment with tofacitinib, promptly complete diagnostic testing appropriate for an immunocompromised patient; initiate appropriate antimicrobial therapy, and monitor the patients closely. Caution is also recommended in patients with a history of chronic lung disease, or in those who develop interstitial lung disease, as they may be more prone to infections. Risk of infection may be higher with increasing degrees of lymphopenia and consideration should be given to lymphocyte counts when assessing individual patient risk of infection.

Discontinuation and monitoring criteria for lymphopenia are recommended [see Dosage and Administration ( 2.4 )] . Tuberculosis Evaluate and test patients for latent or active tuberculosis (TB) infection prior to and per applicable guidelines during administration of tofacitinib. Consider anti-TB therapy prior to administration of tofacitinib in patients with a past history of latent or active TB in whom an adequate course of treatment cannot be confirmed, and for patients with a negative test… [Excerpted — this section continues on DailyMed.]

🤒 Adverse Reactions ~3 min read ▾

6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: • Serious Infections [see Warnings and Precautions ( 5.1 )] • Increased Risk of Mortality [see Warnings and Precautions ( 5.2 )] • Malignancy and Lymphoproliferative Disorders [see Warnings and Precautions ( 5.3 )] • Major Adverse Cardiovascular Events [see Warnings and Precautions ( 5.4 )] • Thrombosis [see Warnings and Precautions ( 5.5 )] • Gastrointestinal Perforations [see Warnings and Precautions ( 5.6 )] • Hypersensitivity Reactions [see Warnings and Precautions ( 5.7 )] • Hypoglycemia in Patients with Diabetes [see Warnings and Precautions ( 5.8 )] • Laboratory Abnormalities [see Warnings and Precautions ( 5.9 )] Most common adverse reactions are: • RA, PsA, and AS : Reported in ≥2% of adult patients treated with tofacitinib tablets monotherapy or in combination with DMARDs: upper respiratory tract infection (URI), nasopharyngitis, diarrhea, and headache.

( 6.1 ) • PcJIA : Consistent with common adverse reactions reported in adult patients with RA. ( 6.1 ) • UC : Reported in ≥5% of adult patients treated with either tofacitinib tablets and ≥1% greater than reported in patients treated with placebo: nasopharyngitis, elevated cholesterol levels, headache, URI, increased blood creatine phosphokinase, rash, diarrhea, and herpes zoster. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Hikma Pharmaceuticals USA Inc. at 1-800-962-8364 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

6.1Clinical Trials Experience Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not predict the rates observed in a broader patient population in clinical practice. The clinical studies described in this subsection were conducted using tofacitinib tablets and/or tofacitinib oral solution. Adverse Reactions in Adults with Rheumatoid Arthritis In RA Safety Study 1, 1,455 adults were treated with tofacitinib tablets 5 mg twice daily, 1,456 adults were treated with 10 mg twice daily, and 1,451 adults were treated with a TNF blocker for a median of 4 years [see Clinical Studies ( 14.6 )] .

A dosage of tofacitinib tablets 10 mg twice daily is not recommended for the treatment of RA because of increased risks [see Warnings and Precautions ( 5 )] . For the treatment of adults with moderately to severely active RA, the recommended dosage of tofacitinib tablets is 5 mg twice daily and the recommended dosage for tofacitinib extended-release tablets is 11 mg once daily. The safety of tofacitinib was also evaluated in two Phase 2 and five Phase 3 double-blind, placebo-controlled, multicenter trials in patients with RA.

In these trials, adults were randomized to receive: • Tofacitinib tablets (monotherapy) 5 mg twice daily (292 patients) or 10 mg twice daily (306 patients), • In combination with DMARDs (including methotrexate), tofacitinib tablets 5 mg twice daily (1,044 patients) or 10 mg twice daily (1,043 patients and • Placebo (809 patients). All seven trials included provisions for patients taking placebo to receive treatment with tofacitinib tablets at Month 3 or Month 6 either by patient response (based on uncontrolled disease activity) or by design, so that adverse events cannot always be unambiguously attributed to a given treatment.

Therefore, some analyses that follow include patients who changed treatment by design or by patient response from placebo to tofacitinib tablets in both the placebo and tofacitinib group of a given interval. Comparisons between placebo and tofacitinib groups were based on the first 3 months of exposure, and comparisons between tofacitinib tablets 5 mg twice daily and tofacitinib tablets 10 mg twice daily were based on the first 12 months of exposure. The long-term safety population includes all adults with RA who participated in a… [Excerpted — this section continues on DailyMed.]

🔄 Drug Interactions 213 words ▾

7 DRUG INTERACTIONS Table 7 includes drugs with clinically important drug interactions when administered concomitantly with tofacitinib and instructions for preventing or managing them. Table 7: Clinically Significant Interactions Affecting Tofacitinib When Concomitantly Used with Other Drugs Strong CYP3A4 Inhibitors (e.g., ketoconazole) Clinical Impact Increased exposure to tofacitinib Intervention Dosage modification of tofacitinib is recommended [see Dosage and Administration ( 2 ), Clinical Pharmacology, Figure 3 ( 12.3 )] Moderate CYP3A4 Inhibitors Concomitantly Used with Strong CYP2C19 Inhibitors (e.g., fluconazole) Clinical Impact Increased exposure to tofacitinib Intervention Dosage modification of tofacitinib is recommended [see Dosage and Administration ( 2 ), Clinical Pharmacology, Figure 3 ( 12.3 )] Strong CYP3A4 Inducers (e.g., rifampin) Clinical Impact Decreased exposure to tofacitinib and may result in loss of or reduced clinical response Intervention Concomitant use with tofacitinib is not recommended [see Clinical Pharmacology, Figure 3 ( 12.3 )] Immunosuppressive Drugs (e.g., azathioprine, tacrolimus, cyclosporine) Clinical Impact Risk of added immunosuppression; concomitant use of tofacitinib with biologic DMARDs or potent immunosuppressants has not been studied in patients with RA, PsA, AS, UC, or pcJIA.

Intervention Concomitant use with tofacitinib is not recommended [see Indications and Usage ( 1 ), Clinical Pharmacology, Figure 3 ( 12.3 )] See FPI for clinically significant drug interactions. ( 2 , 7 )

👥 Use in Specific Populations ~3 min read ▾

8 USE IN SPECIFIC POPULATIONS Lactation : Advise not to breastfeed. ( 8.2 )

8.1Pregnancy Risk Summary The available data with tofacitinib from a pregnancy exposure registry that enrolled 11 exposed pregnant females, pharmacovigilance, and published literature are insufficient to draw conclusions about a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. There are risks to the mother and the fetus associated with RA and UC in pregnancy (see Clinical Considerations) . In animal reproduction studies, fetocidal and teratogenic effects were noted when pregnant rats and rabbits received tofacitinib during the period of organogenesis at exposures multiples of 73-times and 6.3-times the maximum recommended dose of 10 mg twice daily, respectively.

Further, in a peri- and post-natal study in rats, tofacitinib resulted in reductions in live litter size, postnatal survival, and pup body weights at exposure multiples of approximately 73-times the recommended dosage of 5 mg twice daily and approximately 36 times the maximum recommended dosage of 10 mg twice daily, respectively (see Data) . The background risks of major birth defects and miscarriage for the indicated populations are unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes.

The background risks in the U.S. general population of major birth defects and miscarriages are 2 to 4% and 15 to 20% of clinically recognized pregnancies, respectively. Clinical Considerations Disease-Associated Maternal and/or Embryo/Fetal Risk Published data suggest that increased disease activity is associated with the risk of developing adverse pregnancy outcomes in women with RA or UC. Adverse pregnancy outcomes include preterm delivery (before 37 weeks of gestation), low birth weight (less than 2,500 grams) infants, and small for gestational age at birth.

Data Animal Data In a rat embryofetal developmental study, in which pregnant rats received tofacitinib during organogenesis, tofacitinib was teratogenic at exposure levels approximately 146 times the recommended dose of 5 mg twice daily, and approximately 73 times the maximum recommended dose of 10 mg twice daily (on an AUC basis at oral doses of 100 mg/kg/day in rats). Teratogenic effects consisted of external and soft tissue malformations of anasarca and membranous ventricular septal defects, respectively; and skeletal malformations or variations (absent cervical arch; bent femur, fibula, humerus, radius, scapula, tibia, and ulna; sternoschisis; absent rib; misshapen femur; branched rib; fused rib; fused sternebra; and hemicentric thoracic centrum).

In addition, there was an increase in post-implantation loss, consisting of early and late resorptions, resulting in a reduced number of viable fetuses. Mean fetal body weight was reduced. No developmental toxicity was observed in rats at exposure levels approximately 58 times the recommended dose of 5 mg twice daily, and approximately 29 times the maximum recommended dose of 10 mg twice daily (on an AUC basis at oral doses of 30 mg/kg/day in pregnant rats).

In a rabbit embryofetal developmental study in which pregnant rabbits received tofacitinib during the period of organogenesis, tofacitinib was teratogenic at exposure levels approximately 13 times the recommended dose of 5 mg twice daily, and approximately 6.3 times the maximum recommended dose of 10 mg twice daily (on an AUC basis at oral doses of 30 mg/kg/day in rabbits) in the absence of signs of maternal toxicity. Teratogenic effects included thoracogastroschisis, omphalocele, membranous ventricular septal defects, and cranial/skeletal malformations (microstomia, microphthalmia), mid-line and tail defects.

In addition, there was an increase in post-implantation loss associated with late resorptions. No developmental toxicity was observed in rabbits at exposure levels approximately 3 times the recommended dose of 5 mg twice daily, and approximately 1.5… [Excerpted — this section continues on DailyMed.]

🤰 Pregnancy ~3 min read ▾

8.1Pregnancy Risk Summary The available data with tofacitinib from a pregnancy exposure registry that enrolled 11 exposed pregnant females, pharmacovigilance, and published literature are insufficient to draw conclusions about a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. There are risks to the mother and the fetus associated with RA and UC in pregnancy (see Clinical Considerations) . In animal reproduction studies, fetocidal and teratogenic effects were noted when pregnant rats and rabbits received tofacitinib during the period of organogenesis at exposures multiples of 73-times and 6.3-times the maximum recommended dose of 10 mg twice daily, respectively.

Further, in a peri- and post-natal study in rats, tofacitinib resulted in reductions in live litter size, postnatal survival, and pup body weights at exposure multiples of approximately 73-times the recommended dosage of 5 mg twice daily and approximately 36 times the maximum recommended dosage of 10 mg twice daily, respectively (see Data) . The background risks of major birth defects and miscarriage for the indicated populations are unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes.

The background risks in the U.S. general population of major birth defects and miscarriages are 2 to 4% and 15 to 20% of clinically recognized pregnancies, respectively. Clinical Considerations Disease-Associated Maternal and/or Embryo/Fetal Risk Published data suggest that increased disease activity is associated with the risk of developing adverse pregnancy outcomes in women with RA or UC. Adverse pregnancy outcomes include preterm delivery (before 37 weeks of gestation), low birth weight (less than 2,500 grams) infants, and small for gestational age at birth.

Data Animal Data In a rat embryofetal developmental study, in which pregnant rats received tofacitinib during organogenesis, tofacitinib was teratogenic at exposure levels approximately 146 times the recommended dose of 5 mg twice daily, and approximately 73 times the maximum recommended dose of 10 mg twice daily (on an AUC basis at oral doses of 100 mg/kg/day in rats). Teratogenic effects consisted of external and soft tissue malformations of anasarca and membranous ventricular septal defects, respectively; and skeletal malformations or variations (absent cervical arch; bent femur, fibula, humerus, radius, scapula, tibia, and ulna; sternoschisis; absent rib; misshapen femur; branched rib; fused rib; fused sternebra; and hemicentric thoracic centrum).

In addition, there was an increase in post-implantation loss, consisting of early and late resorptions, resulting in a reduced number of viable fetuses. Mean fetal body weight was reduced. No developmental toxicity was observed in rats at exposure levels approximately 58 times the recommended dose of 5 mg twice daily, and approximately 29 times the maximum recommended dose of 10 mg twice daily (on an AUC basis at oral doses of 30 mg/kg/day in pregnant rats).

In a rabbit embryofetal developmental study in which pregnant rabbits received tofacitinib during the period of organogenesis, tofacitinib was teratogenic at exposure levels approximately 13 times the recommended dose of 5 mg twice daily, and approximately 6.3 times the maximum recommended dose of 10 mg twice daily (on an AUC basis at oral doses of 30 mg/kg/day in rabbits) in the absence of signs of maternal toxicity. Teratogenic effects included thoracogastroschisis, omphalocele, membranous ventricular septal defects, and cranial/skeletal malformations (microstomia, microphthalmia), mid-line and tail defects.

In addition, there was an increase in post-implantation loss associated with late resorptions. No developmental toxicity was observed in rabbits at exposure levels approximately 3 times the recommended dose of 5 mg twice daily, and approximately 1.5 times the maximum recommended dose of 10 mg twice daily (on an AUC basis at… [Excerpted — this section continues on DailyMed.]

🧒 Pediatric Use ~2 min read ▾

8.4Pediatric Use The safety and effectiveness of tofacitinib in pediatric patients for indications other than in patients with active pcJIA and PsA, have not been established. The safety and effectiveness of tofacitinib have not been established in pediatric patients less than 2 years of age. The safety and effectiveness of tofacitinib extended-release tablets in pediatric patients have not been established.

Polyarticular Course Juvenile Idiopathic Arthritis (pcJIA) The safety and effectiveness of tofacitinib tablets/tofacitinib oral solution for the treatment of active pcJIA have been established in pediatric patients 2 years of age and older who have had an inadequate response or intolerance to one or more TNF blockers. Use of tofacitinib for this indication is supported by evidence from adequate and well-controlled studies of tofacitinib in adults with RA, pharmacokinetic (PK) data from adult patients with RA, and with additional safety, efficacy, and PK data from a clinical trial of tofacitinib in pediatric patients 2 years and older with active pcJIA (Study pcJIA-I) [see Adverse Reactions ( 6.1 ), Clinical Pharmacology ( 12.3 ), and Clinical Studies ( 14.1 , 14.4 )] .

Adverse reactions observed in pediatric patients with pcJIA who received tofacitinib were consistent with those reported in adults with RA [see Adverse Reactions ( 6.1 )] . Psoriatic Arthritis The safety and effectiveness of tofacitinib tablets/tofacitinib oral solution for the treatment of active PsA have been established in pediatric patients 2 years of age and older who have had an inadequate response or intolerance to one or more TNF blockers. Use of tofacitinib for this indication is supported by evidence from well-controlled studies of tofacitinib tablets in adults with PsA, PK data from adults with PsA, and PK data from a clinical trial of tofacitinib in 225 pediatric patients with JIA, and safety data from 280 pediatric patients 2 years of age and older with JIA [see Adverse Reactions ( 6.1 ), Clinical Pharmacology ( 12.3 ), and Clinical Studies ( 14.2 )] .

Following administration of the recommended tofacitinib dosage in pediatric patients 2 years of age and older with PsA, tofacitinib plasma exposures are predicted to be comparable to those observed in adults with PsA based on population PK modeling and simulation [see Clinical Pharmacology ( 12.3 )] . Systemic Juvenile Idiopathic Arthritis The safety and effectiveness of tofacitinib for the treatment of pediatric patients with systemic juvenile idiopathic arthritis (sJIA) have not been established. Additional pediatric information describing a clinical study in which efficacy was not demonstrated is approved for Pfizer Inc.’s Xeljanz (tofacitinib) tablets and oral solution.

However, due to Pfizer Inc.’s marketing exclusivity rights, this drug product is not labeled with that information.

🧓 Geriatric Use ~1 min read ▾

8.5Geriatric Use Of the 3,315 adults who were enrolled in clinical trials with RA (Studies RA-I to V), a total of 505 patients were 65 years of age and older, including 71 patients 75 years and older. The frequency of serious infection among tofacitinib tablets-treated patients 65 years of age and older was higher than among those adults under the age of 65. Of the 1,156 tofacitinib tablet-treated patients in clinical trials of patients with UC, a total of 77 patients (7%) were 65 years of age or older.

Clinical studies of tofacitinib tablets in patients with UC did not include sufficient numbers of patients aged 65 years and older to determine whether they respond differently from younger adult patients. Of the 783 tofacitinib tablet-treated patients in clinical trials of patients with PsA, a total of 72 (9.2%) patients were 65 years of age and older, including 2 (0.3%) patients 75 years and older. These clinical studies did not include sufficient numbers of patients aged 65 years and older with PsA to determine if they respond differently from younger adult patients.

Of the 420 tofacitinib tablet-treated patients in clinical trials of patients with AS, a total of 12 (2.9%) patients were 65 years of age and older, including 1 (0.2%) patient 75 years and older. These clinical studies did not include sufficient numbers of patients aged 65 years and older with AS to determine if they respond differently from younger adult patients.

🆘 Overdosage 120 words ▾

10 OVERDOSAGE There is no specific antidote for overdose with tofacitinib. In case of an overdose, it is recommended that the patient be monitored for signs and symptoms of adverse reactions. In a study in patients with end-stage renal disease (ESRD) undergoing hemodialysis, plasma tofacitinib concentrations declined more rapidly during the period of hemodialysis and dialyzer efficiency, calculated as dialyzer clearance/blood flow entering the dialyzer, was high [mean (SD) = 0.73 (0.15)].

However, due to the significant non-renal clearance of tofacitinib, the fraction of total elimination occurring by hemodialysis was small, and thus, limits the value of hemodialysis for treatment of overdose with tofacitinib. Consider contacting the Poison Help line (1-800-222-1222) or a medical toxicologist for additional overdose management recommendations.

🧬 Clinical Pharmacology ~3 min read ▾

12 CLINICAL PHARMACOLOGY

12.1Mechanism of Action Tofacitinib 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.

Tofacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs. JAK enzymes transmit cytokine signaling through pairing of JAKs (e.g., JAK1/JAK3, JAK1/JAK2, JAK1/TyK2, JAK2/JAK2). Tofacitinib inhibited the in vitro activities of JAK1/JAK2, JAK1/JAK3, and JAK2/JAK2 combinations with IC50 of 406, 56, and 1377 nM, respectively.

However, the relevance of specific JAK combinations to therapeutic effectiveness is not known.

12.2Pharmacodynamics Treatment with tofacitinib was associated with dose-dependent reductions of circulating CD16/56+ natural killer cells, with estimated maximum reductions occurring at approximately 8 to 10 weeks after initiation of therapy. These changes generally resolved within 2 to 6 weeks after discontinuation of treatment. Treatment with tofacitinib was associated with dose-dependent increases in B cell counts.

Changes in circulating T-lymphocyte counts and T-lymphocyte subsets (CD3+, CD4+ and CD8+) were small and inconsistent. The clinical significance of these changes is unknown. Total serum IgG, IgM, and IgA levels after 6-month dosing in patients with rheumatoid arthritis (RA) were lower than in patients who received placebo; however, changes were small and not dose-dependent.

After treatment with tofacitinib in patients with RA, rapid decreases in serum C-reactive protein (CRP) were observed and maintained throughout dosing. Changes in CRP observed with tofacitinib treatment do not reverse fully within 2 weeks after discontinuation, indicating a longer duration of pharmacodynamic activity compared to the pharmacokinetic half-life. Similar changes in T cells, B cells, and serum CRP have been observed in patients with active psoriatic arthritis (PsA) although reversibility was not assessed.

Total serum immunoglobulins were not assessed in patients with active PsA.

12.3Pharmacokinetics Following oral administration of tofacitinib tablets/tofacitinib oral solution, peak plasma concentrations were reached within 0.5-hour to 1 hour, elimination half-life was about 3 hours and a dose-proportional increase in systemic exposure was observed in the therapeutic dosage range. Steady state concentrations were achieved in 24 to 48 hours with negligible accumulation after twice daily administration. Following oral administration of tofacitinib extended-release tablets, peak plasma concentrations were reached at 4 hours and half-life was about 6 to 8 hours.

Steady state concentrations were achieved within 48 hours with negligible accumulation after once daily administration. Table 8 describes the pharmacokinetic parameters of tofacitinib tablets and tofacitinib extended-release tablets. Table 8: Pharmacokinetic Parameters of Tofacitinib Tablets/Tofacitinib Extended-Release Tablets Following Multiple Oral Dosing PK Parameters Values represent the geometric mean, except T max , for which is the median (range) is shown.

(CV%) Tofacitinib Tablets Tofacitinib Extended-Release Tablets Dosing Regimen 5 mg Twice Daily 10 mg Twice Daily 11 mg Once Daily 22 mg Once Daily AUC 24 (ng•hr/mL) 263.4 (15) 539.6 (22) 269.0 (18) 596.6 (19) C max (ng/mL) 42.7 (26) 84.7 (18) 38.2 (15) 83.8 (25) C min (ng/mL) 1.41 (40) 3.10 (54) 1.07 (69) 3.11 (43) T max (hours) 1.0 (0.5 to

14.0Values beyond 12 hours were after the evening dose which was administered 12 hours after the morning dose of twice-daily tofacitinib tablets. ) 0.8 (0.5 to 14.0 ) 4.0 (3.0 to 4.0) 4.0 (2.0 to 4.0) Abbreviations: AU… [Excerpted — this section continues on DailyMed.]

🧬 Mechanism of Action 126 words ▾

12.1Mechanism of Action Tofacitinib 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.

Tofacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs. JAK enzymes transmit cytokine signaling through pairing of JAKs (e.g., JAK1/JAK3, JAK1/JAK2, JAK1/TyK2, JAK2/JAK2). Tofacitinib inhibited the in vitro activities of JAK1/JAK2, JAK1/JAK3, and JAK2/JAK2 combinations with IC50 of 406, 56, and 1377 nM, respectively.

However, the relevance of specific JAK combinations to therapeutic effectiveness is not known.

📦 How Supplied / Storage and Handling 166 words ▾

16 HOW SUPPLIED/STORAGE AND HANDLING How supplied information for tofacitinib oral solution is shown in Table 23. Table 23: How Supplied Information for Tofacitinib Oral Solution Bottle Fill (volume mL) NDC Number Tofacitinib Oral Solution 1 mg/mL Clear, colorless solution 240 mL NDC 0054-0821-58 Tofacitinib 1 mg/ mL oral solution is a clear, colorless solution that contains 1 mg of tofacitinib. It is packaged in HDPE bottles as follows: Each bottle is packaged with one press-in bottle adapter and one 5 mL oral dosing syringe with 3.2 mL, 4 mL, and 5 mL gradations.

The press-in bottle adapter and oral dosing syringe are not made with natural rubber latex. Storage and Handling for Tofacitinib Oral Solution Store at 20°C to 25°C (68°F to 77°F), excursions permitted between 15°C and 30°C (between 59°F and 86°F). [See USP Controlled Room Temperature]. Store in the original bottle and carton to protect from light.

Use contents of bottle within 60 days of opening. Discard unused oral solution after 60 days.

📋 Description 142 words ▾

11 DESCRIPTION Tofacitinib oral solution is formulated with the citrate salt of tofacitinib, a JAK inhibitor. Tofacitinib citrate is a white to off-white powder with the following chemical name: (3R,4R)-4-methyl-3-(methyl-7H-pyrrolo [2,3-d]pyrimidin-4-ylamino)-ß-oxo-1- piperidinepropanenitrile, 2-hydroxy-1,2,3-propanetricarboxylate (1:1). The solubility of tofacitinib citrate in water is 2.9 mg/mL.

Tofacitinib citrate has a molecular weight of 504.5 Daltons (or 312.4 Daltons as the tofacitinib free base) and a molecular formula of C 16 H 20 N 6 O•C 6 H 8 O 7 . The chemical structure of tofacitinib citrate is: Tofacitinib oral solution is supplied for oral administration as a 1 mg/mL clear, colorless solution. Each 1 mL contains 1 mg of tofacitinib (equivalent to 1.62 mg of tofacitinib citrate) and the following inactive ingredients: grape flavor (natural & artificial), hydrochloric acid, purified water, sodium acetate trihydrate, sodium benzoate, sodium hydroxide, sucralose and tartaric acid. structure-formula.jpg

💬 Information for Patients ~3 min read ▾

17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Medication Guide and Instructions for Use). Serious Infections Inform patients that tofacitinib may lower the ability of their immune system to fight infections. Advise patients not to start taking tofacitinib if they have an active infection.

Instruct patients to contact their healthcare provider immediately during treatment if symptoms suggesting infection appear to ensure rapid evaluation and appropriate treatment [see Warnings and Precautions ( 5.1 )] . Advise patients that the risk of herpes zoster, some cases of which can be serious, is increased in patients treated with tofacitinib [see Warnings and Precautions ( 5.1 )] . Malignancies and Lymphoproliferative Disorders Inform patients that tofacitinib may increase their risk of certain cancers, and that lymphoma and other cancers have been observed in patients taking tofacitinib.

Instruct patients to inform their healthcare provider if they have ever had any type of cancer [see Warnings and Precautions ( 5.3 )] . Major Adverse Cardiovascular Events Inform patients that tofacitinib may increase their risk of major adverse cardiovascular events (MACE) defined as myocardial infarction, stroke, and cardiovascular death. Instruct all patients, especially current or past smokers or patients with other cardiovascular risk factors, to be alert for the development of signs and symptoms of cardiovascular events [see Warnings and Precautions ( 5.4 )] .

Thrombosis Advise patients to stop taking tofacitinib and to call their healthcare provider right away if they experience any symptoms of thrombosis (sudden shortness of breath, chest pain worsened with breathing, swelling of leg or arm, leg pain or tenderness, red or discolored skin in the affected leg or arm) [see Warnings and Precautions ( 5.5 )] . Hypersensitivity Advise patients to stop taking tofacitinib and to call their healthcare provider right away if they experience any symptoms of allergic reactions while taking tofacitinib [see Warnings and Precautions ( 5.7 )] .

Hypoglycemia in Patients with Diabetes Consider advising patients with diabetes to increase monitoring of blood glucose since hypoglycemia, including severe hypoglycemia, has been reported after starting tofacitinib. Advise patients with diabetes to notify their healthcare provider if they develop signs or symptoms of hypoglycemia [see Warnings and Precautions ( 5.8 )] . Important Information on Laboratory Abnormalities Inform patients that tofacitinib may affect certain lab test results, and that blood tests are required before and during tofacitinib treatment [see Warnings and Precautions ( 5.9 )] .

Pregnancy Advise pregnant females and females of reproductive potential of the potential risk to a fetus. Advise females to inform their prescriber of a known or suspected pregnancy [see Use in Specific Populations ( 8.1 )] . Lactation Advise women not to breastfeed during treatment with tofacitinib and for at least 18 hours after the last dose of tofacitinib or 36 hours after the last dose of tofacitinib extended-release tablets [see Use in Specific Populations ( 8.2 )] .

Infertility Advise females of reproductive potential that tofacitinib may impair fertility [see Use in Specific Populations ( 8.3 ), Nonclinical Toxicology ( 13.1 )] . It is not known if this effect is reversible. Residual Tablet Shell Patients receiving tofacitinib extended-release tablets may notice an inert tablet shell passing in the stool or via colostomy.

Patients should be informed that the active medication has already been absorbed by the time the patient sees the inert tablet shell. Manufactured by: Aphena Pharma Solutions Easton, Maryland (MD) 21601, United States (USA) Distributed by: Hikma Pharmaceuticals USA Inc. Berkeley Heights, NJ 07922 C50001592/02 Revised: July 2026

💬 Medication Guide ~3 min read ▾

MEDICATION GUIDE Tofacitinib (TOE-fa-SYE-ti-nib) Oral Solution What is the most important information I should know about Tofacitinib Oral Solution? Tofacitinib oral solution may cause serious side effects including: 1. Serious infections.

Tofacitinib oral solution is a medicine that affects your immune system. Tofacitinib oral solution can lower the ability of your immune system to fight infections. Some people can have serious infections while taking tofacitinib oral solution, including tuberculosis (TB), and infections caused by bacteria, fungi, or viruses that can spread throughout the body.

Some people have died from these infections. • Your healthcare provider should test you for TB before starting tofacitinib oral solution and during treatment. • Your healthcare provider should monitor you closely for signs and symptoms of TB infection during treatment with tofacitinib oral solution. You should not start taking tofacitinib oral solution if you have any kind of infection unless your healthcare provider tells you it is okay. You may be at a higher risk of developing shingles (herpes zoster).

People with ulcerative colitis taking the higher dose of tofacitinib tablets (10 mg twice daily) or tofacitinib extended-release tablets (22 mg one time each day) have a higher risk of serious infections and shingles. Before starting tofacitinib oral solution, tell your healthcare provider if you: • think you have an infection or have symptoms of an infection such as: • are being treated for an infection. • get a lot of infections or have infections that keep coming back. • have diabetes, chronic lung disease, HIV, or a weak immune system.

People with these conditions have a higher chance for infections. • have TB, or have been in close contact with someone with TB. • live or have lived, or have traveled to certain parts of the country (such as the Ohio and Mississippi River valleys and the Southwest) where there is an increased chance for getting certain kinds of fungal infections (histoplasmosis, coccidioidomycosis, or blastomycosis). These infections may happen or become more severe if you take tofacitinib oral solution. Ask your healthcare provider if you do not know if you have lived in an area where these infections are common. • have or have had hepatitis B or C.

After starting tofacitinib oral solution, call your healthcare provider right away if you have any symptoms of an infection. Tofacitinib oral solution can make you more likely to get infections or make worse any infection that you have. 2.

Increased risk of death in people 50 years of age and older who have at least 1 heart disease (cardiovascular) risk factor and are taking tofacitinib 5 mg or 10 mg twice daily. 3. Cancer and immune system problems.

Tofacitinib oral solution may increase your risk of certain cancers by changing the way your immune system works. • Lymphoma and other cancers including skin cancers can happen in people taking tofacitinib oral solution. People taking tofacitinib oral solution 5 mg twice daily or tofacitinib oral solution 10 mg twice daily have a higher risk of certain cancers including lymphoma and lung cancer, especially if you are a current or past smoker. People with ulcerative colitis taking the higher dose of tofacitinib tablets (10 mg twice daily) or tofacitinib extended-release tablets (22 mg one time each day) have a higher risk of skin cancers.

Tell your healthcare provider if you have ever had any type of cancer. 4. Increased risk of major cardiovascular events such as heart attack, stroke or death in people 50 years of age and older who have at least 1 heart disease (cardiovascular) risk factor and are taking tofacitinib 5 mg or 10 mg twice daily, especially if you are a current or past smoker.

Get emergency help right away if you have any symptoms of a heart attack or stroke while taking tofacitinib, including: • discomfort in the center of your chest that lasts for more than a few minutes, or that goes away and comes back • s… [Excerpted — this section continues on DailyMed.]

🧬 Pharmacokinetics ~3 min read ▾

12.3Pharmacokinetics Following oral administration of tofacitinib tablets/tofacitinib oral solution, peak plasma concentrations were reached within 0.5-hour to 1 hour, elimination half-life was about 3 hours and a dose-proportional increase in systemic exposure was observed in the therapeutic dosage range. Steady state concentrations were achieved in 24 to 48 hours with negligible accumulation after twice daily administration. Following oral administration of tofacitinib extended-release tablets, peak plasma concentrations were reached at 4 hours and half-life was about 6 to 8 hours.

Steady state concentrations were achieved within 48 hours with negligible accumulation after once daily administration. Table 8 describes the pharmacokinetic parameters of tofacitinib tablets and tofacitinib extended-release tablets. Table 8: Pharmacokinetic Parameters of Tofacitinib Tablets/Tofacitinib Extended-Release Tablets Following Multiple Oral Dosing PK Parameters Values represent the geometric mean, except T max , for which is the median (range) is shown.

(CV%) Tofacitinib Tablets Tofacitinib Extended-Release Tablets Dosing Regimen 5 mg Twice Daily 10 mg Twice Daily 11 mg Once Daily 22 mg Once Daily AUC 24 (ng•hr/mL) 263.4 (15) 539.6 (22) 269.0 (18) 596.6 (19) C max (ng/mL) 42.7 (26) 84.7 (18) 38.2 (15) 83.8 (25) C min (ng/mL) 1.41 (40) 3.10 (54) 1.07 (69) 3.11 (43) T max (hours) 1.0 (0.5 to

14.0Values beyond 12 hours were after the evening dose which was administered 12 hours after the morning dose of twice-daily tofacitinib tablets. ) 0.8 (0.5 to 14.0 ) 4.0 (3.0 to 4.0) 4.0 (2.0 to 4.0) Abbreviations: AUC 24 = area under the concentration-time profile from time 0 to 24 hours; C max = maximum plasma concentration; C min = minimum plasma concentration; T max = time to C max ; CV = Coefficient of variation. Absorption Tofacitinib Tablets The absolute oral bioavailability of tofacitinib is 74%. Coadministration of tofacitinib with a high-fat meal resulted in no changes in AUC while C max was reduced by 32%.

In clinical trials, tofacitinib was administered without regard to meals. Tofacitinib Extended-Release Tablets Coadministration of tofacitinib extended-release tablets 11 and 22 mg with a high-fat meal resulted in no changes in AUC while C max was increased by 27% and 19% respectively. T max was extended by approximately 1 hour for both tofacitinib extended-release tablets 11 and 22 mg.

Distribution After intravenous administration, the volume of distribution was 87 L. The protein binding of tofacitinib is approximately 40%. Tofacitinib binds predominantly to albumin and does not appear to bind to α1-acid glycoprotein.

Tofacitinib distributes equally between red blood cells and plasma. Metabolism and Excretion Clearance mechanisms for tofacitinib are approximately 70% hepatic metabolism and 30% renal excretion of the parent drug. The metabolism of tofacitinib is primarily mediated by CYP3A4 with minor contribution from CYP2C19.

In a human radiolabeled study, more than 65% of the total circulating radioactivity was accounted for by unchanged tofacitinib, with the remaining 35% attributed to 8 metabolites, each accounting for less than 8% of total radioactivity. The pharmacologic activity of tofacitinib is attributed to the parent molecule. Pharmacokinetics in Patients with RA, PsA, AS, and UC Population pharmacokinetic (PK) analyses indicated that PK characteristics were similar between patients with RA, PsA, ankylosing spondylitis, and UC.

The coefficient of variation (%) in AUC of tofacitinib were generally similar across different disease patients, ranging from 22% to 34% (Table 9). Table 9: Tofacitinib Exposure in Patients with RA, PsA, AS, and UC After Administration of Tofacitinib Tablets 5 mg Twice Daily or 10 mg Twice Daily Pharmacokinetic Parameters Pharmacokinetic parameters estimated based on population pharmacokinetic analysis. Geometric Mean (CV%) Tofacitinib Tablets 5 mg Twice Daily Tofacitinib Tablets 10 mg Twice Daily Rh… [Excerpted — this section continues on DailyMed.]

🧬 Pharmacodynamics 196 words ▾

12.2Pharmacodynamics Treatment with tofacitinib was associated with dose-dependent reductions of circulating CD16/56+ natural killer cells, with estimated maximum reductions occurring at approximately 8 to 10 weeks after initiation of therapy. These changes generally resolved within 2 to 6 weeks after discontinuation of treatment. Treatment with tofacitinib was associated with dose-dependent increases in B cell counts.

Changes in circulating T-lymphocyte counts and T-lymphocyte subsets (CD3+, CD4+ and CD8+) were small and inconsistent. The clinical significance of these changes is unknown. Total serum IgG, IgM, and IgA levels after 6-month dosing in patients with rheumatoid arthritis (RA) were lower than in patients who received placebo; however, changes were small and not dose-dependent.

After treatment with tofacitinib in patients with RA, rapid decreases in serum C-reactive protein (CRP) were observed and maintained throughout dosing. Changes in CRP observed with tofacitinib treatment do not reverse fully within 2 weeks after discontinuation, indicating a longer duration of pharmacodynamic activity compared to the pharmacokinetic half-life. Similar changes in T cells, B cells, and serum CRP have been observed in patients with active psoriatic arthritis (PsA) although reversibility was not assessed.

Total serum immunoglobulins were not assessed in patients with active PsA.

🔬 Clinical Studies ~3 min read ▾

14 CLINICAL STUDIES

14.1Clinical Studies in Rheumatoid Arthritis The rheumatoid arthritis (RA) clinical development program with tofacitinib tablets included six randomized controlled trials in adults with moderate to severe active RA . Trial Design • Study RA-I (NCT00814307) was a 6-month monotherapy trial in which 610 patients with moderate to severe active RA who had an inadequate response to a DMARD (nonbiologic or biologic) received tofacitinib tablets 5 mg or 10 mg twice daily or placebo added to their background DMARD. At the Month 3 visit, all patients randomized to placebo treatment were switched in a blinded fashion to a second predetermined treatment of tofacitinib tablets 5 mg or 10 mg twice daily.

The primary endpoints at Month 3 were the proportion of patients who achieved an ACR20 response, changes in Health Assessment Questionnaire – Disability Index (HAQ-DI), and rates of Disease Activity Score DAS28-4(ESR) less than 2.6. • Study RA-II (NCT00856544) was a 12-month trial in which 792 patients with moderate to severe active RA who had an inadequate response to a nonbiologic DMARD received tofacitinib tablets 5 mg or 10 mg twice daily or placebo added to background DMARD treatment (excluding potent immunosuppressive treatments such as azathioprine or cyclosporine).

At the Month 3 visit, nonresponding patients were switched in a blinded fashion to a second predetermined treatment of tofacitinib tablets 5 mg or 10 mg twice daily. At the end of Month 6, all patients treated with placebo were switched to their second predetermined tofacitinib treatment in a blinded fashion. The primary endpoints were the proportion of patients who achieved an ACR20 response at Month 6, changes in HAQ-DI at Month 3, and rates of DAS28-4(ESR) less than 2.6 at Month 6. • Study RA-III (NCT00853385) was a 12-month trial in 717 patients with moderate to severe active RA who had an inadequate response to methotrexate (MTX).

Patients received tofacitinib tablets 5 mg or 10 mg orally twice daily, adalimumab 40 mg subcutaneously every other week, or placebo added to background MTX. Patients treated with placebo were switched as in Study RA-II. The primary endpoints were the proportion of patients who achieved an ACR20 response at Month 6, HAQ-DI at Month 3, and DAS28-4(ESR) less than 2.6 at Month 6. • Study RA-IV (NCT00847613) was a 2-year trial with a planned analysis at 1 year in which 797 patients with moderate to severe active RA who had an inadequate response to MTX received tofacitinib tablets 5 mg or 10 mg twice daily or placebo added to background MTX.

Patients treated with placebo were switched as in Study RA-II. The primary endpoints were the proportion of patients who achieved an ACR20 response at Month 6, mean change from baseline in van der Heijde-modified total Sharp Score (mTSS) at Month 6, HAQ-DI at Month 3, and DAS28-4(ESR) less than 2.6 at Month 6. • Study RA-V (NCT00960440) was a 6-month trial in which 399 patients with moderate to severe active RA who had an inadequate response to at least one approved TNF blocking biological product received tofacitinib tablets 5 mg or 10 mg twice daily or placebo added to background MTX.

At the Month 3 visit, all patients randomized to placebo treatment were switched in a blinded fashion to a second predetermined treatment of tofacitinib tablets 5 or 10 mg twice daily. The primary endpoints at Month 3 were the proportion of patients who achieved an ACR20 response, HAQ-DI, and DAS28-4(ESR) less than 2.6. • Study RA-VI (NCT01039688) was a 2-year monotherapy trial with a planned analysis at 1 year in which 952 MTX-naïve patients with moderate to severe active RA received tofacitinib tablets 5 or 10 mg twice daily or MTX dose-titrated over 8 weeks to 20 mg weekly.

The primary endpoints were mean change from baseline in van der Heijde-modified Total Sharp Score (mTSS) at Month 6 and the proportion of patients who achieved an ACR70 response at Month 6. Although other dosages have been studied,… [Excerpted — this section continues on DailyMed.]

🧪 Nonclinical Toxicology ~2 min read ▾

13 NONCLINICAL TOXICOLOGY

13.1Carcinogenesis, Mutagenesis, Impairment of Fertility In a 39-week toxicology study in monkeys, tofacitinib at exposure levels approximately 6 times the recommended dose of 5 mg twice daily, and approximately 3 times the 10 mg twice daily dose (on an AUC basis at oral doses of 5 mg/kg twice daily) produced lymphomas. No lymphomas were observed in this study at exposure levels 1 times the recommended dose of 5 mg twice daily, and approximately 0.5 times the 10 mg twice daily dose (on an AUC basis at oral doses of 1 mg/kg twice daily).

The carcinogenic potential of tofacitinib was assessed in 6-month rasH2 transgenic mouse carcinogenicity and 2-year rat carcinogenicity studies. Tofacitinib, at exposure levels approximately 34 times the recommended dose of 5 mg twice daily, and approximately 17 times the 10 mg twice daily dose (on an AUC basis at oral doses of 200 mg/kg/day) was not carcinogenic in mice. In the 24-month oral carcinogenicity study in Sprague-Dawley rats, tofacitinib caused benign Leydig cell tumors, hibernomas (malignancy of brown adipose tissue), and benign thymomas at doses greater than or equal to 30 mg/kg/day (approximately 42 times the exposure levels at the recommended dose of 5 mg twice daily, and approximately 21 times the 10 mg twice daily dose on an AUC basis).

The relevance of benign Leydig cell tumors to human risk is not known. Tofacitinib was not mutagenic in the bacterial reverse mutation assay. It was positive for clastogenicity in the in vitro chromosome aberration assay with human lymphocytes in the presence of metabolic enzymes, but negative in the absence of metabolic enzymes.

Tofacitinib was negative in the in vivo rat micronucleus assay and in the in vitro CHO-HGPRT assay and the in vivo rat hepatocyte unscheduled DNA synthesis assay. In rats, tofacitinib at exposure levels approximately 17 times the recommended dose of 5 mg twice daily, and approximately 8.3 times the 10 mg twice daily dose (on an AUC basis at oral doses of 10 mg/kg/day) reduced female fertility due to increased post-implantation loss. There was no impairment of female rat fertility at exposure levels of tofacitinib equal to the recommended dose of 5 mg twice daily, and approximately 0.5 times the 10 mg twice daily dose (on an AUC basis at oral doses of 1 mg/kg/day).

Tofacitinib exposure levels at approximately 133 times the recommended dose of 5 mg twice daily, and approximately 67 times the 10 mg twice daily dose (on an AUC basis at oral doses of 100 mg/kg/day) had no effect on male fertility, sperm motility, or sperm concentration.

📄 Carcinogenesis, Mutagenesis, Impairment of Fertility ~2 min read ▾

13.1Carcinogenesis, Mutagenesis, Impairment of Fertility In a 39-week toxicology study in monkeys, tofacitinib at exposure levels approximately 6 times the recommended dose of 5 mg twice daily, and approximately 3 times the 10 mg twice daily dose (on an AUC basis at oral doses of 5 mg/kg twice daily) produced lymphomas. No lymphomas were observed in this study at exposure levels 1 times the recommended dose of 5 mg twice daily, and approximately 0.5 times the 10 mg twice daily dose (on an AUC basis at oral doses of 1 mg/kg twice daily).

The carcinogenic potential of tofacitinib was assessed in 6-month rasH2 transgenic mouse carcinogenicity and 2-year rat carcinogenicity studies. Tofacitinib, at exposure levels approximately 34 times the recommended dose of 5 mg twice daily, and approximately 17 times the 10 mg twice daily dose (on an AUC basis at oral doses of 200 mg/kg/day) was not carcinogenic in mice. In the 24-month oral carcinogenicity study in Sprague-Dawley rats, tofacitinib caused benign Leydig cell tumors, hibernomas (malignancy of brown adipose tissue), and benign thymomas at doses greater than or equal to 30 mg/kg/day (approximately 42 times the exposure levels at the recommended dose of 5 mg twice daily, and approximately 21 times the 10 mg twice daily dose on an AUC basis).

The relevance of benign Leydig cell tumors to human risk is not known. Tofacitinib was not mutagenic in the bacterial reverse mutation assay. It was positive for clastogenicity in the in vitro chromosome aberration assay with human lymphocytes in the presence of metabolic enzymes, but negative in the absence of metabolic enzymes.

Tofacitinib was negative in the in vivo rat micronucleus assay and in the in vitro CHO-HGPRT assay and the in vivo rat hepatocyte unscheduled DNA synthesis assay. In rats, tofacitinib at exposure levels approximately 17 times the recommended dose of 5 mg twice daily, and approximately 8.3 times the 10 mg twice daily dose (on an AUC basis at oral doses of 10 mg/kg/day) reduced female fertility due to increased post-implantation loss. There was no impairment of female rat fertility at exposure levels of tofacitinib equal to the recommended dose of 5 mg twice daily, and approximately 0.5 times the 10 mg twice daily dose (on an AUC basis at oral doses of 1 mg/kg/day).

Tofacitinib exposure levels at approximately 133 times the recommended dose of 5 mg twice daily, and approximately 67 times the 10 mg twice daily dose (on an AUC basis at oral doses of 100 mg/kg/day) had no effect on male fertility, sperm motility, or sperm concentration.

📖 Instructions for Use ~3 min read ▾

INSTRUCTIONS FOR USE Tofacitinib (toe-fa′-sye-ti-nib) Oral Solution Read this Instructions for Use before you start taking Tofacitinib Oral Solution and each time you get a refill. There may be new information. This leaflet does not take the place of talking to your healthcare provider about your medical condition or treatment.

Important information about measuring Tofacitinib Oral Solution: Always use the oral dosing syringe that comes with tofacitinib oral solution to measure and take your prescribed dose. Ask your healthcare provider or pharmacist to show you how to measure your prescribed dose if you are not sure. How should I store Tofacitinib? • Store tofacitinib oral solution at room temperature between 68°F to 77°F (20°C to 25°C). • Always store tofacitinib oral solution in the original bottle and carton to protect from light.

Keep Tofacitinib and all medicines out of the reach of children. Use tofacitinib oral solution within 60 days of opening the bottle. Throw away (discard) remaining tofacitinib oral solution after 60 days.

To help you remember when to throw away your bottle of tofacitinib oral solution, you can write the date when you first start to use it on the carton and below: Date of first use ____ / ____ / ____. Before each use: Wash your hands with soap and water and place the items from the carton on a clean, flat surface. Each carton of tofacitinib oral solution contains: • 1 press-in bottle adapter • 1 bottle of Tofacitinib Oral Solution • 1 oral dosing syringe Step 1.

Remove bottle from carton Open the carton and remove the bottle of Tofacitinib Oral Solution. Step 2. Open bottle Open the bottle by pushing down on the child-resistant cap and turning it to the left (counter-clockwise) as shown.

Remove the seal off the top of the bottle (first time only) . Do not throw away the child-resistant cap. Note: The bottle does not need to be shaken before use.

Step 3. Insert press-in bottle adapter (first time only) Remove the press-in bottle adapter and oral dosing syringe from the carton. With the bottle on a flat surface, push the ribbed end of the press-in bottle adapter all the way into the neck of the bottle with your thumbs while holding the bottle firmly.

Note: Do not remove the press-in bottle adapter from the bottle after it is inserted. Step 4. Remove air from oral dosing syringe Push the oral dosing syringe plunger all the way down to the tip of the syringe barrel to remove excess air.

Step 5. Insert the oral dosing syringe Insert the oral dosing syringe tip into the upright bottle through the opening of the press-in bottle adapter until it is firmly in place. Step 6.

Withdraw dose from bottle With the oral dosing syringe in place, turn the bottle upside down. Pull down on the plunger until the bottom of the plunger is even with the markings on the oral dosing syringe for your prescribed dose of oral solution. If you see air bubbles in the oral dosing syringe, fully push the plunger in so that the oral solution flows back into the bottle.

Then withdraw your prescribed dose of oral solution. Step 7. Remove oral dosing syringe Turn the bottle upright and place the bottle on a flat surface.

Remove the oral dosing syringe from the press-in bottle adapter and bottle by pulling straight up on the oral dosing syringe barrel. Step 8. Check the dose Check that the correct dose was drawn up into the oral dosing syringe.

If the dose is not correct, insert the oral dosing syringe tip firmly into the press-in bottle adapter. Fully push in the plunger so that the oral solution flows back into the bottle. Repeat Step 6 and Step 7.

Step 9. Take the dose of Tofacitinib Place the tip of the oral dosing syringe into the inside of the cheek. Slowly push the plunger all the way down to give all of the medicine in the oral dosing syringe.

Make sure there is time to swallow the medicine. Step 10. Close the bottle Close the bottle tightly by turning the child-resistant cap to the right (clockwise), leaving the press-in bott… [Excerpted — this section continues on DailyMed.]

📄 Recent Major Changes 60 words ▾

Boxed Warning 10/2025 Indications and Usage, Psoriatic Arthritis ( 1.2 ) 10/2025 Dosage and Administration, Recommended Dosage in Pediatric Patients 2 Years of Age and Older with Psoriatic Arthritis or Polyarticular Course Juvenile Idiopathic Arthritis ( 2.4 ) 10/2025 Warnings and Precautions, Serious Infections ( 5.1 ) 03/2026 Warnings and Precautions, Hypoglycemia in Patients with Diabetes ( 5.8 ) 06/2026

📄 Package Label / Principal Display Panel 36 words ▾

PACKAGE/LABEL PRINCIPAL DISPLAY PANEL NDC 0054- 0821 -58 240 mL Tofacitinib Oral Solution 1 mg/mL Rx only tofacitinib-os-bottle-label-image.jpg

PACKAGE/LABEL PRINCIPAL DISPLAY PANEL NDC 0054- 0821 -58 240 mL Tofacitinib Oral Solution 1 mg/mL Rx only tofacitinib-os-folding-carton-image.jpg

Source: FDA Structured Product Labeling, mirrored from DailyMed / openFDA. Prefer the government’s original formatting? View this label on DailyMed ↗

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Why is there no price listed?
The pricing shown on our NDC pages comes from CMS NADAC, a voluntary survey of retail community pharmacy invoices. CMS does not publish a NADAC for every NDC — packages outside the retail survey (institutional and hospital products, bulk packages, discontinued items, and many OTC items) may never receive one. A missing price reflects the survey's scope, not this product's actual cost, and does not mean the product is free or unavailable.
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← 00054-0812-21 · Hikma 00054-0829-25 · Hikma →
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