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TOFACITINIB 1 mg/mL Solution, 240 mL — NDC 72205-0121-81 package photo
Label image from the product's FDA listing (DailyMed) — may show a different pack size or an older label revision.

TOFACITINIB 1 mg/mL Solution, 240 mL — NDC 72205-121-81 (Billing 72205-0121-81)

by Novadoz Pharmaceuticals LLC · 240 mL in 1 BOTTLE

This is a package of 240 mL of TOFACITINIB 1 mg/mL Solution from Novadoz Pharmaceuticals LLC, marketed since Jun 2026 and currently FDA-listed. It is this product's only package size.

NDC 72205-0121-81
🏷️ FDA NDC (as labeled) 72205-121-81 billing pads the product 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 Sep 17, 2026 · sources: openFDA · FDA label (DailyMed) · FDA Orange & Purple Book · First Databank · CMS NADAC, ASP, Medicare & Medicaid · RxNorm
📋 All sources & update times →

This page is curated, coded, and maintained by

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 72205-121-81 alone.

Record
FDA NDC Directory package listing · Human prescription drug
Code segments
72205 labeler · 121 product · 81 package
Package marketed since
Jun 3, 2026
Sample package
No — commercial package
Listing certified through
Dec 31, 2027
Billing quantity
240 mL per package
Barcode (UPC)
0372205121812
FDA record last changed
Sep 17, 2026

Identity & classification

Regulatory identifiers FDA, NLM and CMS codes for this package

FDA NDC (as labeled) 72205-121-81
Product NDC 72205-121
11-digit billing NDC 72205012181
NCPDP billing unit ML — per mL (volume)
RxCUI 2478433
UNII O1FF4DIV0D
UPC 0372205121812
Application # ANDA217298
SPL Set ID 327f6b60-1a5d-49e6-acff-18603d0ee9d0
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 72205-121-81 — a 5-3-2 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 product segment → 72205-0121-81. 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
📖 What it is MedlinePlus · NLM

Tofacitinib is used to treat rheumatoid arthritis (condition in which the body attacks its own joints causing pain, swelling, and loss of function), psoriatic arthritis (a condition that causes joint pain and swelling and scales on the skin), ulcerative colitis (a condition which causes swelling and sores in the lining of the colon [large intestine] and rectum), and polyarticular juvenile idiopathic arthritis (PJIA; a type of childhood arthritis that affects five or more joints during the first six months of the condition, causing pain, swelling, and loss of function). Tofacitinib is in a clas...

Read the full MedlinePlus article ↗
📗 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
72205-0121-81 You're viewing this Main listing 240 mL in 1 BOTTLE 2026-06-03 — Active

Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
tofacitinib solution 1 mg/mL 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/mLthis 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.

🧪 Avoiding an ingredient? See Tofacitinib inactive ingredients by manufacturer: every current product's list side by side, so you can ask your pharmacy for the version that does not list it.

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

  • UNII 6X543N684K
    A natural flavoring derived from grapes that enhances taste appeal. It's used in medicines to improve flavor and make medications more palatable, especially for children or patients who need better taste acceptance.
  • 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 33X04XA5AT
    Lactic acid is a naturally occurring organic acid derived from milk or plant sources. It lowers and maintains pH in formulations, helps preserve the product, and can enhance ingredient stability and absorption.
  • 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 506T60A25R
    Sorbitol is a natural sugar alcohol derived from glucose. It serves as a sweetener, humectant, and bulking agent in medications to improve taste and help maintain moisture in the product.
  • 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 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.

7 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

LabelerNovadoz Pharmaceuticals LLC
Application holderMSN LABORATORIES PRIVATE LTD
FDA applicationANDA217298 (ANDA)
Labeler code72205
First marketedJun 2026
Product typeHuman Prescription Drug
Portfolio249 products on file

More NDCs from Novadoz Pharmaceuticals LLC labeler code 72205

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 🧬 Pharmacokinetics 🧬 Pharmacodynamics 🔬 Clinical Studies 🧪 Nonclinical Toxicology 📄 Carcinogenesis, Mutagenesis, Impairment of Fertility 📄 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 oral solution is 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) and 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 oral solution use and during therapy. Treatment for latent infection should be initiated prior to tofacitinib oral solution 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 oral solution 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 oral solution 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 oral solution 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 XELJANZ 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 XELJANZ tablets 5 mg or 10 mg twice a day [see Warnings and Precautions (5.2 )] . A tofacitinib oral solution 10 mg twice daily dosage is not recommended for the treatment of psoriatic arthritis (PsA) 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 XELJANZ 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 XELJANZ 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 XELJANZ 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 XELJANZ 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 factor treated with XELJANZ tablets 5… [Excerpted — this section continues on DailyMed.]

🎯 Indications and Usage ~1 min read ▾

1 INDICATIONS AND USAGE Tofacitinib oral solution is Janus kinase (JAK) inhibitors. 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 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 oral solution 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 of 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 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 oral solution initiation if absolute lymphocyte count <500 cells/mm 3 , an absolute neutrophil count (ANC) <1000 cells/mm 3 or hemoglobin <9 g/dL. ( 2.1 ) Important Administration Instructions XELJANZ XR (extended-release tablets) are not substitutable with tofacitinib oral solution.

( 2.2 ) Switching between XELJANZ and XELJANZ XR 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 oral solution 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 oral solution 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 oral solution 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 oral solution 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 oral solution should be in accordance with current vaccination guidelines regarding immunosuppressive agents [see Warnings and Precautions (5.10 )].

2.2Important Administration Instructions XELJANZ XR (extended-release tablets) is not substitutable with tofacitinib oral solution. Switching between XELJANZ and XELJANZ XR 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 XELJANZ tablets and 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 (7) and Clinical Pharmacology (12.3) ] , and pediatric patients… [Excerpted — this section continues on DailyMed.]

💊 Dosage Forms and Strengths 24 words ▾

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

⛔ Contraindications 6 words ▾

4 CONTRAINDICATIONS None. None. (4 )

⚠️ Warnings and Cautions ~3 min read ▾

5 WARNINGS AND PRECAUTIONS Serious Infections: Avoid use of tofacitinib oral solution 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 oral solution.

( 5. 10)

5.1Serious Infections Serious and sometimes fatal infections may occur with tofacitinib oral solution. 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. Other serious infections that were not reported in clinical studies may also occur (e.g., coccidioidomycosis).

Avoid use of tofacitinib oral solution in patients with an active, serious infection, including localized infections. The risks and benefits of treatment should be considered prior to initiating tofacitinib oral solution 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 oral solution.

Interrupt tofacitinib oral solution if a patient develops a serious infection, an opportunistic infection, or sepsis. In patients who develop a new infection during treatment with tofacitinib oral solution, 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 oral solution.

Consider anti-TB therapy prior to administration of tofacitinib oral solution 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 for latent TB but who have risk factors for TB infection. Consultation with a physician with expertise in the treatment of TB is recommended to aid in the decision about whether initiating anti-TB therapy is appropriate for an individual patient. Monitor pati… [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: PsA: Reported in ≥2% of adult patients treated with XELJANZ tablets monotherapy or in combination with DMARDs: upper respiratory tract infection (UR-I), nasopharyngitis, diarrhea, and headache.

( 6.1 ) PcJIA: Consistent with common adverse reactions reported in adult patients with RA. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Novadoz Pharmaceuticals LLC at 1-855-668-2369 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 XELJANZ tablets and/or tofacitinib oral solution. Adverse Reactions in Adults with Rheumatoid Arthritis In RA Safety Study 1, 1,455 adults were treated with XELJANZ 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 )].

The safety of XELJANZ tablets 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: • XELJANZ tablets (monotherapy) 5 mg twice daily (292 patients) or 10 mg twice daily (306 patients), • In combination with DMARDs (including methotrexate), XELJANZ 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 XELJANZ tablets at Month3 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 XELJANZ tablets in both the placebo and XELJANZ tablets group of a given interval. Comparisons between placeboand XELJANZ tablets groups were based on the first 3 months of exposure, and comparisons between XELJANZ tablets 5 mg twice daily and XELJANZ 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 double-blind, placebo-controlled trial (including earlier development phase studies) and then participated in one of two long-term safety studies.

The design of the long-term safety studies allowed for modification of XELJANZ tablets doses according to clinical judgment. This limits the interpretation of the long-term safety data with respect to dose. The most common serious adverse reactions were serious infections [see Warnings and Precautions (5.1 )].

The proportion of patients who discontinued treatment due to any adverse reaction during the 0 to 3 months exposure in the double-blind, placebo-controlled trials was 4% for XELJANZ tablets-treated patients and 3% for placebo-treated patients. Overall Infections In the seven placebo-c… [Excerpted — this section continues on DailyMed.]

🔄 Drug Interactions 218 words ▾

7 DRUG INTERACTIONS Table 7 includes drugs with clinically significant drug interactions when concomitantly used with tofacitinib oral solution and instructions for preventing or managing them. Table 7: Clinically Significant Interactions Affecting Tofacitinib Oral Solution When Concomitantly Used with Other Drugs Strong CYP3A4 Inhibitors (e.g., ketoconazole) Clinical Impact Increased exposure to tofacitinib Intervention Dosage modification of tofacitinib oral solution 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 oral solution 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 oral solution 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 oral solution with biologicDMARDs or potent immunosuppressants has not been studied in patients with PsA or pcJIA.

Intervention Concomitant use with tofacitinib oral solution 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 XELJANZ tablets and tofacitinib oral solution and XELJANZ XR (extended-release tablets) 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 2500 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 approxima… [Excerpted — this section continues on DailyMed.]

🤰 Pregnancy ~3 min read ▾

8.1Pregnancy Risk Summary The available data with XELJANZ tablets and tofacitinib oral solution and XELJANZ XR (extended-release tablets) 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 2500 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.]

🧒 Pediatric Use ~2 min read ▾

8.4Pediatric Use The safety and effectiveness of tofacitinib oral solution in pediatric patients for indications, other than in patients with active pcJIA and PsA, have not been established. The safety and effectiveness of tofacitinib oral solution have not been established in pediatric patients less than 2 years of age. Polyarticular Course Juvenile Idiopathic Arthritis (pcJIA) The safety and effectiveness of 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 XELJANZ tablets 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 pc JIA (Study pcJIA-I) [see Adverse Reactions (6.1 ), Clinical Pharmacology (12.3 ), and Clinical Studies (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 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 XELJANZ 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 oral solution for the treatment of pediatric patients with systemic juvenile idiopathic arthritis (sJIA) have not been established. The results from a two-part study (an open-label, run-in phase, followed by a double-blind, placebo-controlled, randomized event-driven withdrawal phase) in 100 patients 2 years to 17 years of age with sJIA with active systemic features did not demonstrate that tofacitinib (dosed at 5 mg twice daily or body weight-based equivalent twice daily) was efficacious in the treatment of sJIA with active systemic features.

Of the 100 patients enrolled in the open-label run-in phase, 59 (59%) patients achieved a clinical response and were eligible for the double-blind withdrawal phase. There were 28 patients randomized to tofacitinib and 31 patients to placebo. The study data were insufficient to demonstrate efficacy and, therefore, tofacitinib is not recommended for the treatment of sJIA.

Adverse reactions observed in pediatric patients with sJIA receiving tofacitinib/tofacitinib oral solution were consistent with those reported in pcJIA and RA patients [see Adverse Reactions (6.1 )] .

🧓 Geriatric Use 121 words ▾

8.5Geriatric Use Of the 3,315 adults who were enrolled in clinical trials with RA, 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 XELJANZ tablets-treated patients 65 years of age and older was higher than among those adults under the age of 65. 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.

🆘 Overdosage 124 words ▾

10 OVERDOSAGE There is no specific antidote for overdose with tofacitinib oral solution. 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 oral solution. 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 XELJANZ tablets and tofacitinib oral solution, peak plasma concentrations were reached within 0.5 hour - 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. Absorption Tofacitinib 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 [see Dosage and Administration (2.2 )] . 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. Pharmacokineti… [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 161 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 Tofacitinib Oral Solution 1 mg/mL Bottle Fill (volume mL) NDC Number Clear, colorless solution 240 mL NDC 72205-121-81 Tofacitinib Oral Solution 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. 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 remaining oral solution after 60 days.

📋 Description 153 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). Tofacitinib citrate is sparingly soluble in 20% aqueous acetic acid, slightly soluble in methanol, water and insoluble in dichloromethane 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 of tofacitinib oral solution contains 1 mg of tofacitinib (equivalent to 1.62 mg tofacitinib citrate) and the following inactive ingredients: grape flavor (propylene glycol, natural and artificial flavor), hydrochloric acid, lactic acid, purified water, sodium benzoate, sucralose, and sorbitol solution. tofacitinib-structure

💬 Information for Patients ~3 min read ▾

17 PATIENT COUNSELING INFORMATION Advise patients to read the FDA-approved patient labeling (Medication Guide and Instructions for Use). Serious Infections Inform patients that tofacitinib oral solution may lower the ability of their immune system to fight infections. Advise patients not to start taking tofacitinib oral solution 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 oral solution [see Warnings and Precautions (5.1) ]. Malignancies and Lymphoproliferative Disorders Inform patients that tofacitinib oral solution may increase their risk of certain cancers, and that lymphoma and other cancers have been observed in patients taking tofacitinib oral solution.

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 oral solution may increase their risk of major adverse cardiovascular events (MAC-E) 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 oral solution 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 oral solution and to call their healthcare provider right away if they experience any symptoms of allergic reactions while taking tofacitinib oral solution [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 oral solution. 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 oral solution may affect certain lab test results, and that blood tests are required before and during tofacitinib oral solution 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 oral solution and for at least 18 hours after the last dose of tofacitinib oral solution [see Use in Specific Populations (8.2) ].

Infertility Advise females of reproductive potential that tofacitinib oral solution may impair fertility [see Use in Specific Populations (8.3) , Nonclinical Toxicology (13.1) ] . It is not known if this effect is reversible. XELJANZ and XELJANZ XR are registered trademarks of Pfizer Inc.

All trademarks are the property of their respective owners. Manufactured by: MSN Pharmaceuticals Inc. Piscataway, NJ 08854 Distributed by: Novadoz Pharmaceuticals LLC Piscataway, NJ 08854-3714 This product’s labeling may have been updated.

For the most recent prescribing information, please visit www.novadozpharma.com. Revised: 08/2026

🧬 Pharmacokinetics ~3 min read ▾

12.3Pharmacokinetics Following oral administration of XELJANZ tablets and tofacitinib oral solution, peak plasma concentrations were reached within 0.5 hour - 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. Absorption Tofacitinib 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 [see Dosage and Administration (2.2 )] . 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%.

Specific Populations Covariate evaluation as part of population PK analyses in adult patient populations indicated no clinically relevant change in tofacitinib exposure, after accounting for differences in renal function (i.e., creatinine clearance) between patients, based on age, weight, biological sex and race (Figure 1). An approximately linear relationship between body weight and volume of distribution was observed, resulting in higher peak (C max ) and lower trough (C min ) concentrations in lighter patients. However, this difference is not considered to be clinically relevant.

Covariate evaluation as part of population PK analyses in pediatric patients with pcJIA, including PsA, identified body weight significantly impacting tofacitinib exposure, which supports weight-based dosing in this population. There were no identified clinically significant differences in tofacitinib exposure with different age, biological sex, racial, or pcJIA or PsA disease severity groups. The effect of renal and hepatic impairment and other intrinsic factors on the PK of tofacitinib is shown in Figure 1.

Figure 1: Impact of Intrinsic Factors on Tofacitinib Pharmacokinetics Note: Reference values for weight, age, biological sex, and race comparisons are 70 kg, 55 years, male, and white, respectively; reference groups for renal and hepatic impairment data are patients with normal renal and hepatic function. Renal function was estimated using creatinine clearance by Cockcroft-Gault method and hepatic function was estimated using Child-Pugh scoring method. In patients with end-stage renal disease maintained on hemodialysis, mean AUC was approximately 40% higher compared with historical healthy subject data, consistent with approximately 30% contribution of renal clearance to the total clearance of tofacitinib [see Dosage and Administration (2.4) and Use in Specific Populations (8.6) ] .

Drug Interaction Studies Potential for Tofacitinib Oral Solution to Influence the PK of Other Drugs In vitro studies indicate that tofacitinib does n… [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

14.2Clinical Studies in Psoriatic Arthritis The psoriatic arthritis (PsA) clinical development program with XELJANZ tablets included 2 multicenter, randomized, double-blind, placebo-controlled trials in 816 adults with active PsA (Studies PsA-I and PsA-II). Trial Designs and Population All patients had active PsA for at least 6 months based upon the Classification Criteria for Psoriatic Arthritis (CASPAR), at least 3 tender/painful joints and at least 3 swollen joints, and active plaque psoriasis. Patients randomized and treated across the 2 clinical trials represented different PsA subtypes at screening, including <5 joints or asymmetric involvement (21%), ≥5 joints involved (90%), distal interphalangeal (DIP) joint involvement (61%), arthritis mutilans (8%), and spondylitis (19%).

Patients in these clinical trials had a diagnosis of PsA for a mean (SD) of 7.7 (7.2) years. At baseline, 80% and 53% of patients had enthesitis and dactylitis, respectively. At baseline, all patients were required to receive treatment with a stable dose of a nonbiologic DMARD (79% received methotrexate, 13% received sulfasalazine, 7% received leflunomide, 1% received other nonbiologic DMARDs).

In both clinical trials, the primary endpoints were the ACR20 response and the change from baseline in HAQ-DI at Month 3. Study PsA-I was a 12-month clinical trial in 422 patients who had an inadequate response to a nonbiologic DMARD (67% and 33% were inadequate responders to 1 nonbiologic DMARD and ≥2 nonbiologic DMARDs, respectively) and who were naïve to treatment with a TNF blocker. Although Study PsA-1 included patients who are TNF blocker-naïve, tofacitinib oral solution is not approved for use in TNF blocker-naïve patients [see Indications and Usage (1.2 )] .

Patients were randomized in a 2:2:2:1:1 ratio to receive XELJANZ tablets 5 mg twice daily, XELJANZ tablets 10mg twice daily, adalimumab 40 mg subcutaneously once every 2 weeks, placebo to XELJANZ tablets 5 mg twice daily treatment sequence, or placebo to XELJANZ tablets 10 mg twice daily treatment sequence, respectively; study drug was added to background nonbiologic DMARD treatment. At the Month 3 visit, all patients randomized to placebo treatment were switched in a blinded fashion to a predetermined XELJANZ tablets dosage of 5 mg or 10 mg twice daily.

Study PsA-I was not designed to demonstrate non-inferiority or superiority to adalimumab. Study PsA-II was a 6-month clinical trial in 394 patients who had an inadequate response to at least 1 approved TNF blocker (66%, 19%, and 15% were inadequate responders to 1 TNF blocker, 2 TNF blockers and ≥3 TNF blockers, respectively). Patients were randomized in a 2:2:1:1 ratio to receive XELJANZ tablets 5 mg twice daily, XELJANZ tablets 10 mg twice daily, placebo to XELJANZ tablets 5 mg twice daily treatment sequence, or placebo to XELJANZ tablets 10 mg twice daily treatment sequence, respectively; study drug was added to background nonbiologic DMARD treatment.

At the Month 3 visit, placebo patients were switched in a blinded fashion to a predetermined XELJANZ tablets dosage of 5 mg or 10 mg twice daily as in Study PsA-I. Although other dosages have been studied, the recommended dosage of tofacitinib oral solution is 5 mg twice daily. A tofacitinib oral solution 10 mg twice daily dosage is not recommended for treatment of PsA.

Clinical Response At Month 3, patients treated with XELJANZ tablets 5 mg twice daily had higher (p≤0.05) response rates versus placebo for ACR20, ACR50, and ACR70 in Study PsA-I and for ACR20 and ACR50 in Study PsA-II; ACR70 response rates were also higher for XELJANZ tablets 5 mg twice daily versus placebo in Study PsA-II, although the differences versus placebo were not statistically significant (p>0.05) (Tables 14 and 15). Table 14: Proportion of Adults with Active PsA with an ACR Response at Month 3 in Study PsA-I* [Nonbiologic DMARD Inadequate Responders (TNF Blocker-Naïve)]** Treatment Group Placebo XELJ… [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.

📄 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 ) 6/2026

📄 Package Label / Principal Display Panel 20 words ▾

PACKAGE LABEL.PRINCIPAL DISPLAY PANEL Tofacitinib Oral Solution 1 mg/mL container label Tofacitinib Oral Solution 1 mg/mL carton label tofacitinib-cntr-label tofacitinib-carton-label

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

Reported adverse events (FAERS)

Read carefully: FAERS reports are voluntary and unverified. Counts are not incidence, do not establish causation, are subject to reporting bias, and cannot be used to compare one drug to another. Shown for signal context only. Reports for Tofacitinib — the ingredient across all brands.

Top reported reactions

Pain26,333
Arthralgia20,097
Condition Aggravated19,917
Rheumatoid Arthritis19,517
Fatigue17,161
Joint Swelling14,867
Headache13,747

Age at onset

Neonate104
Infant20
Child111
Adolescent121
Adult11,960
Elderly3,197

Reporter sex

186,746 reports
Male · 20%
Female · 80%
Unknown · 0%

Serious outcomes

Hospitalization26,629
Death9,652
Disabling8,901
Life-threatening6,475
Reports over time (by year) — tap or hover for the count & year
2019 2021 2023 2026 27,718 0
Most recent year is provisional (FAERS lags ~3 months).
Where does this data come from?
Adverse-event reports from the FDA Adverse Event Reporting System (FAERS) via openFDA. FAERS reports are voluntary and unverified — counts are not incidence and don’t establish causation.

About this NDC listing & data coverage

Finished prescription product
What data is (and isn’t) available for this NDC — tap to expand
NDC identity (package / product / labeler codes) ✓ Available
Labeler ✓ Available
Product & package description ✓ Available
Marketing category & status ✓ Available
Active ingredient / dosage form / route ✓ Available
FDA label (SPL via DailyMed) ✓ Available
Package photos ✓ Available
Inactive ingredients (structured) ✓ Available
NADAC pharmacy acquisition price (CMS) — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey.
Orange Book / therapeutic-equivalence data ✓ Available
HCPCS J-code billing crosswalk — Not published for this NDC Most self-administered / retail products have no J-code — that is normal.
Medicaid utilization (CMS SDUD) — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold.
“Not published” reflects what the public FDA / CMS / NLM sources provide for this exact package code — it is a property of the data feeds, not a judgment about the product.

Questions about this listing

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.
Is the NDC printed on the package the same as the 11-digit billing NDC?
Yes, they identify this exact package in different formats. The form printed on the packaging and shown on DailyMed is the one the FDA registered. Insurance claims use a fixed 11-digit 5-4-2 format, so the short segment is padded with a leading zero and the dashes are dropped. The Identity section at the top of this page lists each form of this code.
Is this package still being marketed?
Yes, per the latest FDA NDC Directory data on this page: this package is listed as actively marketed, with no marketing end date reported by Novadoz Pharmaceuticals LLC. Listing status can change — the directory data on this page refreshes weekly.
Who lists this product with the FDA?
Novadoz Pharmaceuticals LLC is the labeler of record for this NDC — the company under whose FDA-assigned code the package is listed. The labeler may be the manufacturer itself or a distributor marketing the product under its own code.
Do I need a prescription for this product?
This NDC is listed with FDA as a prescription product, so it is dispensed under a prescriber's order. Your pharmacist can tell you whether any over-the-counter forms of the same medication exist.
This page identifies an FDA-listed package (the NDC) and reports public regulatory and pricing data about the listing. It is reference information, not a medical recommendation — talk to your pharmacist or prescriber about your own medication.
Where does this data come from?
Listing facts (marketing category, packager status, marketing dates) from the FDA openFDA NDC Directory; label availability from DailyMed; pricing coverage from CMS NADAC; equivalence scope from the FDA Orange Book.
← 72205-0120-07 · Novadoz 72205-0130-11 · Novadoz →
For educational and professional reference only — not medical advice. Pricing reflects published NADAC and CMS ASP (free public data) and may differ from your acquisition cost; always verify before billing or dispensing.