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Tofacitinib XR 11 mg Tablet, Film Coated, Extended Release, 30-count — NDC 70377-057-11 (Billing 70377-0057-11)

by Biocon Pharma Inc · 30 TABLET, FILM COATED, EXTENDED RELEASE in 1 BOTTLE

This is a package of 30 tablets of Tofacitinib XR 11 mg Tablet, Film Coated, Extended Release from Biocon Pharma Inc, marketed since Jun 2026 and currently FDA-listed; retail pharmacies pay about $2.19 per tablet (NADAC). It is this product's only package size.

NDC 70377-0057-11
🏷️ FDA NDC (as labeled) 70377-057-11 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 Jul 24, 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 70377-057-11 alone.

Record
FDA NDC Directory package listing · Human prescription drug
Code segments
70377 labeler · 057 product · 11 package
Package marketed since
Jun 3, 2026
Sample package
No — commercial package
Listing certified through
Dec 31, 2027
Billing quantity
30 EA per package
Barcode (UPC)
0370377057113
FDA record last changed
Jul 24, 2026

Identity & classification

Regulatory identifiers FDA, NLM and CMS codes for this package

FDA NDC (as labeled) 70377-057-11
Product NDC 70377-057
11-digit billing NDC 70377005711
NCPDP billing unit EA — each (per item)
RxCUI 1741046
UNII O1FF4DIV0D
UPC 0370377057113
Application # ANDA219442
SPL Set ID f0160e3d-63ea-75fb-4b88-fe3d6a6ce030
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 TABLET, FILM COATED, EXTENDED RELEASE
Substance TOFACITINIB CITRATE
TE code (Orange Book) AB · RLD · RS

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

GPI-14 66603065107530
GCN Seq No 075641
GCN 38086
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 ER 11 MG TABLET
FDB brand name Tofacitinib Citrate Er
Legend status F — Federal legend — prescription drug or device
Quick answers
  • GSN (GCN sequence number): 075641
  • GCN: 38086
  • GPI-14 (Medi-Span): 66603065107530
  • HICL (First Databank): 039768
  • AHFS class code: 90:24.12.92
  • RxCUI (RxNorm): 1741046
Why two NDCs? The FDA registers this code as 70377-057-11 — 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 → 70377-0057-11. 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 ER 11 MG TABLET 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 eaPer package
Retail pharmacies payNADAC · weekly $2.193 $65.78 / 30 tablets
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.
NADAC price history (per ea) — tap or hover for the price & month
Sep 2026 $2.193 $2.193
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
70377-0057-11 You're viewing this Main listing 30 TABLET, FILM COATED, EXTENDED RELEASE in 1 BOTTLE 2026-06-03 — Active

Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
Tofacitinib Citrate 11 mg 00574-1811-30 Padagis 30 tablets $2.193 AB Availability likely —
Tofacitinib 11 mg 27241-0270-30 Ajanta 30 tablets $2.193 AB Availability likely —
Tofacitinib 11 mg 42799-0970-30 Edenbridge 30 tablets $2.193 AB Availability likely —
Tofacitinib 11 mg 59651-0685-30 Aurobindo 30 tablets $2.193 AB Availability likely —
Tofacitinib 11 mg 60505-4858-03 Apotex 30 tablets $2.193 AB Availability likely —
Tofacitinib XR 11 mgthis 70377-0057-11 Biocon 30 tablets $2.193 AB Availability likely —
tofacitinib 11 mg 70710-1353-03 Zydus 30 tablets $2.193 AB Availability likely —
Tofacitinib 11 mg 76282-0816-30 Exelan 30 tablets $2.193 AB Availability likely —
Xeljanz Xr 11 mg 00069-0501-30 Pfizer 30 tablets $207.896 AB Availability likely +9382%
Xeljanz Xr 11 mg 63539-0501-14 U.S. 14 tablets — AB Discontinued —
tofacitinib 11 mg 70771-1627-03 Zydus 30 tablets — AB FDA listed —
Tofacitinib 11 mg 73190-0102-30 AvKARE 30 tablets — AB FDA listed —
Tofacitinib 11 mg 76333-0111-15 Orient 30 tablets — AB FDA listed —
Tofacitinib 11 mg 84677-0048-30 Golden 30 tablets — AB Discontinued —
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.

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.

Loading inactive ingredients from the official FDA label in the background. No external source is being called by this page request.
Where does this data come from?
Source: official FDA Structured Product Labeling (SPL) via DailyMed and the openFDA label index. Structured IACT rows and label-wide narrative are kept separate; availability and product-level specificity depend on the submitted label.

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

LabelerBiocon Pharma Inc
Application holderBIOCON PHARMA LTD
FDA applicationANDA219442 (ANDA)
Labeler code70377
First marketedJun 2026
Product typeHuman Prescription Drug
Portfolio6 products on file

More NDCs from Biocon Pharma Inc labeler code 70377

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 📦 Storage and Handling 📋 Description 💬 Information for Patients 💬 Medication Guide 🧬 Pharmacokinetics 🔬 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 extended-release tablets 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 ) 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 extended-release tablets use and during therapy. Treatment for latent infection should be initiated prior to tofacitinib extended-release tablets 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 extended-release tablets 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 extended-release tablets 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 extended-release tablets 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), or ankylosing spondylitis (AS) [see Dosage and Administration (2.3)].

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 extended-release tablets 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 resu… [Excerpted — this section continues on DailyMed.]

🎯 Indications and Usage ~1 min read ▾

1 INDICATIONS AND USAGE Tofacitinib extended-release tablets are Janus kinase (JAK) inhibitors. Tofacitinib extended-release tablets are indicated for the treatment of adult patients with: Moderately to severely active rheumatoid arthritis (RA), who have had an inadequate response or intolerance to one or more TNF blockers. Active psoriatic arthritis (PsA), who have had an inadequate response or intolerance to one or more TNF blockers.

Active ankylosing spondylitis (AS), who have had an inadequate response or intolerance to one or more TNF blockers. Limitations of Use : Use of tofacitinib extended-release tablets for RA, AS, or PsA in combination with biologic DMARDs or potent immunosuppressants such as azathioprine and cyclosporine is not recommended. ( 1.1 , 1.2 , 1.3 )

1.1Rheumatoid Arthritis Tofacitinib extended-release tablets are indicated for the treatment of adult patients with moderately to severely active rheumatoid arthritis (RA), who have had an inadequate response or intolerance to one or more TNF blockers. Limitations of Use Use of tofacitinib extended-release tablets in combination with biologic disease-modifying antirheumatic drugs (DMARDs) or with potent immunosuppressants such as azathioprine and cyclosporine is not recommended.

1.2Psoriatic Arthritis Tofacitinib extended-release tablets are indicated for the treatment of adults with active PsA who have had an inadequate response or intolerance to one or more TNF blockers. Limitations of Use Use of tofacitinib extended-release tablets in combination with biologic DMARDs or with potent immunosuppressants such as azathioprine and cyclosporine is not recommended.

1.3Ankylosing Spondylitis Tofacitinib extended-release tablets are indicated for the treatment of adult patients with active ankylosing spondylitis (AS), who have had an inadequate response or intolerance to one or more TNF blockers. Limitations of Use Use of tofacitinib extended-release tablets in combination with biologic DMARDs or 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 extended-release tablets, consider performing an active and latent TB evaluation, viral hepatitis screening, a complete blood count, and updating immunizations. Avoid tofacitinib extended-release tablets 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 Tofacitinib extended-release tablets are not substitutable with tofacitinib (tablets and oral solution).

( 2.2 ) Switching between tofacitinib tablets and tofacitinib extended-release tablets should be made by the healthcare provider. ( 2.2 ) Recommended Dosage Adult Patients with RA, PsA or AS • Tofacitinib extended-release tablets 11 mg once daily. ( 2.3 ) Dosage in Patients with Renal Impairment or Hepatic Impairment Use of tofacitinib extended-release tablets in patients with severe HI is not recommended.

( 2.3 , 8.7 ) See full prescribing information (FPI) for recommended dosage in patients with moderate or severe RI or moderate HI. ( 2.3 , 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. ( 2.3 , 7 )

2.1Recommended Evaluations and Immunization Prior to Treatment Initiation Prior to initiating tofacitinib extended-release tablets, consider performing the following: Active and latent tuberculosis (TB) infection evaluation: If the patient has latent TB, treat for TB prior to tofacitinib extended-release tablets 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 extended-release tablets treatment in patients with a lymphocyte count less than 500 cells/mm 3 , absolute neutrophil count less than 1000 cells/mm 3 , or hemoglobin level less than 9 g/dL [see Warnings and Precautions ( 5.8 )].

Baseline hepatic function evaluation: Tofacitinib extended-release tablets are 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 extended-release tablets should be in accordance with current vaccination guidelines regarding immunosuppressive agents [see Warnings and Precautions ( 5.9 )].

2.2Important Administration Instructions Tofacitinib extended-release tablets are not substitutable with tofacitinib (tablets and oral solution). Switching between tofacitinib 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 ( 5.8 ) and Adverse Reactions ( 6.1 )] .

Interrupt use of tofacitinib extended-release tablets if a patient develops a serious infection until the infection is controlled [see Warnings and Precautions ( 5.1 )] . Take tofacitinib extended-release tablets with or without food [see Clinical Pharmacology ( 12.3 )] . Swallow tofacitinib extended-release tablets whole and intact.

Do not crush, split, or chew the extended-release tablets [see Clinical Pharmacology ( 12.3 )] .

2.3Recommended Dosage in Adults with Rheumatoid Arthritis, Psoriatic Arthritis, and Ankylosing Spondylitis Table 1 displays the recommended dosage of tofacitinib extended-release tablets for adults with RA, PsA, and AS [see Indication and Usage ( 1.1 , 1.2 , 1.3 )] 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 displays the recommended dosage… [Excerpted — this section continues on DailyMed.]

💊 Dosage Forms and Strengths 39 words ▾

3 DOSAGE FORMS AND STRENGTHS Tofacitinib Extended-Release Tablets: Ο 11 mg tofacitinib: Pink colored oval shaped, film coated tablets debossed with T1 on one side and plain on other side. Tofacitinib Extended-Release Tablets: 11 mg tofacitinib ( 3 )

⛔ Contraindications 7 words ▾

4 CONTRAINDICATIONS None. None. ( 4 )

⚠️ Warnings and Cautions ~2 min read ▾

5 WARNINGS AND PRECAUTIONS Serious Infections : Avoid use of tofacitinib extended-release tablets 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 ) Laboratory Monitoring : Recommended due to potential changes in lymphocytes, neutrophils, hemoglobin, liver enzymes and lipids.

( 5.8 ) Vaccinations : Avoid use of live vaccines concurrently with tofacitinib extended-release tablets. ( 5.9 )

5.1Serious Infections Serious and sometimes fatal infections may occur with tofacitinib extended-release tablets. 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 extended-release tablets in patients with an active, serious infection, including localized infections. The risks and benefits of treatment should be considered prior to initiating tofacitinib extended-release tablets 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 extended-release tablets. Interrupt tofacitinib extended-release tablets if a patient develops a serious infection, an opportunistic infection, or sepsis. In patients who develop a new infection during treatment with tofacitinib extended-release tablets, 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 ( 2.3 )].

Tuberculosis Evaluate and test patients for latent or active tuberculosis (TB) infection prior to and per applicable guidelines during administration of tofacitinib extended-release tablets. Consider anti-TB therapy prior to administration of tofacitinib extended-release tablets 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 patients closely for the development of signs and symptoms of TB, including patients who tested negati… [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 )] Laboratory Abnormalities [see Warnings and Precautions ( 5.8 )] 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 ) To report SUSPECTED ADVERSE REACTIONS, contact Biocon Pharma Inc., at 1-866-924-6266 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. 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 Dosage and Administration ( 2.3 ) and Warnings and Precautions ( 5 )]. For the treatment of adults with moderately to severely active RA [see Indications and Usage ( 1.1 )], the recommended dosage of tofacitinib tablets are 5 mg twice daily and the recommended dosage for tofacitinib extended-release tablets are 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 (1044 patients) or 10 mg twice daily (1043 patients) and Placebo (809 patients). All seven trials included provisions for patients taking placebo to receive treatment with tofacitinib 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 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 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 tofacitinib 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 ex… [Excerpted — this section continues on DailyMed.]

🔄 Drug Interactions ~1 min read ▾

7 DRUG INTERACTIONS Table 7 includes drugs with clinically significant drug interactions when concomitantly used with tofacitinib extended-release tablets and instructions for preventing or managing them. Table 7: Clinically Significant Interactions Affecting Tofacitinib Extended-Release Tablets When Concomitantly Used with Other Drugs Strong CYP3A4 Inhibitors (e.g., ketoconazole) Clinical Impact Increased exposure to tofacitinib Intervention Dosage modification of tofacitinib extended-release tablets 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 extended-release tablets 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 extended-release tablets 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 extended-release tablets with biologic DMARDs or potent immunosuppressants has not been studied in patients with RA, PsA, or AS.

Intervention Concomitant use with tofacitinib extended-release tablets 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 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 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 post­natal study in rats, tofacitinib resulted in reductions in live litter size, post-natal 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. 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 appro… [Excerpted — this section continues on DailyMed.]

🤰 Pregnancy ~3 min read ▾

8.1Pregnancy Risk Summary The available data with tofacitinib 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 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 post­natal study in rats, tofacitinib resulted in reductions in live litter size, post-natal 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. 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 times the maximum recommended dose of 10 mg twice daily (on an… [Excerpted — this section continues on DailyMed.]

🧒 Pediatric Use 18 words ▾

8.4Pediatric Use The safety and effectiveness of tofacitinib extended-release tablets in pediatric patients have not been established.

🧓 Geriatric Use 186 words ▾

8.5Geriatric Use Of the 3315 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 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 124 words ▾

10 OVERDOSAGE There is no specific antidote for overdose with tofacitinib extended-release tablets. 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 extended-release tablets. 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 IC 50 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, 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 a (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 14.0 b ) 0.8 (0.5 to 14.0 b ) 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. a Values represent the geometric mean, except T ma… [Excerpted — this section continues on DailyMed.]

🧬 Mechanism of Action 127 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 IC 50 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 100 words ▾

16 HOW SUPPLIED/STORAGE AND HANDLING How Supplied Information for tofacitinib extended-release tablets are shown in Table 23. Table 23: How Supplied Information for Tofacitinib Extended-Release Tablets Bottle Size (number of tablets) NDC Number 11 mg tofacitinib extended-release tablets Pink colored oval shaped, film coated tablets debossed with T1 on one side and plain on other side. 30 NDC 70377-057-11 The 30’s count HDPE bottle comes in child-resistant package.

Tofacitinib extended-release tablets Store tofacitinib extended-release tablets 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.] Do not repackage.

📦 Storage and Handling 32 words ▾

Tofacitinib extended-release tablets Store tofacitinib extended-release tablets 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.] Do not repackage.

📋 Description 183 words ▾

11 DESCRIPTION Tofacitinib extended-release tablets are formulated with the citrate salt of tofacitinib, a JAK inhibitor. Tofacitinib citrate is a white to off-white powder with the following chemical name: 3-[4( R )-methyl-3( R )-[ N -methyl- N -(7 H -pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-l-yl]-3- oxopropanenitrile citrate. Tofacitinib citrate is slightly soluble in

0.1N hydrochloric acid, insoluble or very slightly soluble in water and in methanol. 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 extended-release tablet is supplied for oral administration as a 11 mg pink colored oval shaped, film coated tablets debossed with T1 on one side and plain on other side.

Each 11 mg tablet of tofacitinib extended-release contains 11 mg tofacitinib (equivalent to 17.764 mg tofacitinib citrate) and the following inactive ingredients: hydroxypropyl methylcellulose, lactose monohydrate, magnesium stearate, sodium lauryl sulphate. The film coating contains iron oxide red, polyethylene glycol, polyvinyl alcohol-part. hydrolyzed, talc and titanium dioxide. Chemical Structure

💬 Information for Patients ~2 min read ▾

17 PATIENT COUNSELING INFORMATION Advise patients to read the FDA-approved patient labeling ( Medication Guide ). Serious Infections Inform patients that tofacitinib extended-release tablets may lower the ability of their immune system to fight infections. Advise patients not to start taking tofacitinib extended-release tablets 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 tablets/tofacitinib extended-release tablets [see Warnings and Precautions ( 5.1 )]. Malignancies and Lymphoproliferative Disorders Inform patients that tofacitinib extended-release tablets 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 extended-release tablets 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 extended-release tablets 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 extended-release tablets and to call their healthcare provider right away if they experience any symptoms of allergic reactions while taking tofacitinib extended-release tablets [see Warnings and Precautions ( 5.7 )] .

Important Information on Laboratory Abnormalities Inform patients that tofacitinib extended-release tablets may affect certain lab test results, and that blood tests are required before and during tofacitinib extended-release tablets treatment [see Warnings and Precautions ( 5.8 )] . 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 extended-release tablets and for at least 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 extended-release tablets may impair fertility [see Use in Specific Populations ( 8.3 ), Nonclinical Toxicology ( 13.1 )] . It is not known if this effect is reversible.

Manufactured for: Biocon Pharma Inc., Iselin, New Jersey, 08830-3009 USA. Manufactured by: Biocon Pharma Limited, Bengaluru, India – 560 099 Product of India

💬 Medication Guide ~3 min read ▾

MEDICATION GUIDE This Medication Guide has been approved by the U.S. Food and Drug Administration. Revised: April 2026 Tofacitinib (toe" fa sye' ti nib) extended-release tablets, for oral use What is the most important information I should know about tofacitinib extended-release tablets?

Tofacitinib extended-release tablets may cause serious side effects including: 1. Serious infections. Tofacitinib extended-release tablets are medicines that affect your immune system.

Tofacitinib extended-release tablets can lower the ability of your immune system to fight infections. Some people can have serious infections while taking tofacitinib extended-release tablets, 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 extended-release tablets and during treatment. Your healthcare provider should monitor you closely for signs and symptoms of TB infection during treatment with tofacitinib extended-release tablets. You should not start taking tofacitinib extended-release tablets 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). Before starting tofacitinib extended-release tablets, tell your healthcare provider if you: think you have an infection or have symptoms of an infection such as: o fever, sweating, or chills o cough o blood in phlegm o warm, red, or painful skin or sores on your body o burning when you urinate or urinating more often than normal o muscle aches o shortness of breath o weight loss o diarrhea or stomach pain o feeling very tired 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 extended-release tablets. 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 extended-release tablets, call your healthcare provider right away if you have any symptoms of an infection. Tofacitinib extended-release tablets 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 tablets 5 mg or 10 mg twice daily. 3. Cancer and immune system problems.

Tofacitinib extended-release tablets 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 extended-release tablets. People taking tofacitinib tablets 5 mg twice daily or tofacitinib tablets 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.

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 tablets 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 extended-rel… [Excerpted — this section continues on DailyMed.]

🧬 Pharmacokinetics ~3 min read ▾

12.3Pharmacokinetics Following oral administration of tofacitinib tablets, 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 a (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 14.0 b ) 0.8 (0.5 to 14.0 b ) 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. a Values represent the geometric mean, except T max , for which is the median (range) is shown. b Values beyond 12 hours were after the evening dose which was administered 12 hours after the morning dose of twice-daily tofacitinib tablets.

Absorption Tofacitinib Tablets The absolute oral bioavailability of tofacitinib tablets is 74%. Coadministration of tofacitinib tablets with a high-fat meal resulted in no changes in AUC while C max was reduced by 32%. In clinical trials, tofacitinib tablets was administered without regard to meals [see Dosage and Administration ( 2.2 )].

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, and AS Population pharmacokinetic (PK) analyses indicated that PK characteristics were similar between patients with RA, PsA, and ankylosing spondylitis. 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 Tablets Exposure in Patients with RA, PsA, and AS After Administration of Tofacitinib Tablets 5 mg Twice Daily Pharmacokinetic Parameters a Geometric Mean Tofacitinib Tablets 5 mg Twice Daily (CV%) Rheumatoid Arthritis Psoriatic Arthritis Ankylosing Spondylitis AUC 0-24,ss (ng·h/mL) 504 (22.0%)… [Excerpted — this section continues on DailyMed.]

🔬 Clinical Studies ~3 min read ▾

14 CLINICAL STUDIES

14.1Clinical Studies in Rheumatoid Arthritis The rheumatoid arthritis (RA) clinical development program with tofacitinib tablets (referred to as “tofacitinib” in this subsection of labeling) 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… [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 26 words ▾

RECENT MAJOR CHANGES SECTION ­ Boxed Warning 10/2025 Indications and Usage, Psoriatic Arthritis ( 1.2 ) 10/2025 Warnings and Precautions, Serious Infections ( 5.1 ) 03/2026

📄 Package Label / Principal Display Panel 37 words ▾

PRINCIPAL DISPLAY PANEL - 11 mg Tablet Bottle Label NDC 70377-057-11 Tofacitinib Extended-Release Tablets 11 mg* Dispense the accompanying Medication Guide to each patient. Rx only 30 Tablets PRINCIPAL DISPLAY PANEL - 11 mg Tablet Bottle 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 XR (this brand).

Top reported reactions

Rheumatoid Arthritis2,081
Drug Intolerance1,944
Pain1,867
Synovitis1,769
Joint Swelling1,749
Fatigue1,737
Rash1,723

Age at onset

Neonate17
Infant6
Child61
Adolescent42
Adult1,259
Elderly298

Reporter sex

6,955 reports
Male · 19%
Female · 81%
Unknown · 0%

Serious outcomes

Hospitalization2,697
Disabling2,171
Death1,819
Reports over time (by year) — tap or hover for the count & year
2022 2023 2024 2026 1,422 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.
← 70377-0056-11 · Biocon 70377-0060-11 · Biocon →
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.