TOFACITINIB CITRATE - Generic Drug Details

What are the generic sources for tofacitinib citrate and what is the scope of freedom to operate?

Tofacitinib citrate is the generic ingredient in three branded drugs marketed by Hikma, Pfizer, Ajanta Pharma Ltd, Aurobindo Pharma Ltd, Dexcel, Sinotherapeutics Inc, Zydus Pharms, Micro Labs, and Pf Prism Cv, and is included in twelve NDAs. There are four patents protecting this compound and two Paragraph IV challenges. Additional information is available in the individual branded drug profile pages.

Tofacitinib citrate has one hundred and twenty-four patent family members in fifty-five countries.

There are twelve drug master file entries for tofacitinib citrate. Two suppliers are listed for this compound. There are seven tentative approvals for this compound.

Summary for TOFACITINIB CITRATE

International Patents:	124
US Patents:	4
Tradenames:	3
Applicants:	9
NDAs:	12
Drug Master File Entries:	12
Finished Product Suppliers / Packagers:	2
Raw Ingredient (Bulk) Api Vendors:	79
Clinical Trials:	12
Patent Applications:	1,792
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for TOFACITINIB CITRATE
DailyMed Link:	TOFACITINIB CITRATE at DailyMed

Recent Clinical Trials for TOFACITINIB CITRATE

Identify potential brand extensions & 505(b)(2) entrants

Sponsor	Phase
Army Medical University, China	PHASE4
Jinnah Hospital	PHASE3
China-Japan Friendship Hospital	Phase 4

See all TOFACITINIB CITRATE clinical trials

Generic filers with tentative approvals for TOFACITINIB CITRATE

Applicant	Application No.	Strength	Dosage Form
		EQ 5MG BASE	TABLET;ORAL
		EQ 10MG BASE	TABLET;ORAL
		EQ 11MG BASE	TABLET, EXTENDED RELEASE;ORAL

The 'tentative' approval signifies that the product meets all FDA standards for marketing, and, but for the patents / regulatory protections, it would approved.

Pharmacology for TOFACITINIB CITRATE

Drug Class	Janus Kinase Inhibitor
Mechanism of Action	Janus Kinase Inhibitors

Anatomical Therapeutic Chemical (ATC) Classes for TOFACITINIB CITRATE

L04AA	Selective immunosuppressants
L04A	IMMUNOSUPPRESSANTS
L04	IMMUNOSUPPRESSANTS
L	Antineoplastic and immunomodulating agents

L04AF	Janus-associated kinase (JAK) inhibitors
L04A	IMMUNOSUPPRESSANTS
L04	IMMUNOSUPPRESSANTS
L	Antineoplastic and immunomodulating agents

Paragraph IV (Patent) Challenges for TOFACITINIB CITRATE

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
XELJANZ	Oral Solution	tofacitinib citrate	1 mg/mL	213082	1	2021-11-12
XELJANZ XR	Extended-release Tablets	tofacitinib citrate	22 mg	208246	1	2020-12-28
XELJANZ	Tablets	tofacitinib citrate	10 mg	203214	1	2019-07-24
XELJANZ	Tablets	tofacitinib citrate	5 mg	203214	3	2016-11-07
XELJANZ XR	Extended-release Tablets	tofacitinib citrate	11 mg	208246	1	2016-11-07

US Patents and Regulatory Information for TOFACITINIB CITRATE

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Pfizer	XELJANZ XR	tofacitinib citrate	TABLET, EXTENDED RELEASE;ORAL	208246-001	Feb 23, 2016	AB	RX	Yes	No	11,253,523*PED				Y
Pfizer	XELJANZ XR	tofacitinib citrate	TABLET, EXTENDED RELEASE;ORAL	208246-002	Dec 12, 2019		RX	Yes	Yes	10,639,309*PED				Y
Pfizer	XELJANZ XR	tofacitinib citrate	TABLET, EXTENDED RELEASE;ORAL	208246-001	Feb 23, 2016	AB	RX	Yes	No	RE41783*PED				Y
Sinotherapeutics Inc	TOFACITINIB CITRATE	tofacitinib citrate	TABLET, EXTENDED RELEASE;ORAL	216001-001	Sep 30, 2025	AB	RX	No	No
Hikma	TOFACITINIB CITRATE	tofacitinib citrate	SOLUTION;ORAL	216878-001	Sep 25, 2023		DISCN	No	No
Micro Labs	TOFACITINIB CITRATE	tofacitinib citrate	TABLET;ORAL	209738-001	Mar 13, 2023		DISCN	No	No

Expired US Patents for TOFACITINIB CITRATE

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Pf Prism Cv	XELJANZ	tofacitinib citrate	TABLET;ORAL	203214-001	Nov 6, 2012	6,956,041
Pf Prism Cv	XELJANZ	tofacitinib citrate	TABLET;ORAL	203214-001	Nov 6, 2012	7,301,023
Pfizer	XELJANZ XR	tofacitinib citrate	TABLET, EXTENDED RELEASE;ORAL	208246-001	Feb 23, 2016	6,956,027
Pfizer	XELJANZ XR	tofacitinib citrate	TABLET, EXTENDED RELEASE;ORAL	208246-002	Dec 12, 2019	7,265,221
Pf Prism Cv	XELJANZ	tofacitinib citrate	TABLET;ORAL	203214-001	Nov 6, 2012	6,965,027
Pfizer	XELJANZ XR	tofacitinib citrate	TABLET, EXTENDED RELEASE;ORAL	208246-001	Feb 23, 2016	7,265,221

International Patents for TOFACITINIB CITRATE

Country	Patent Number	Title	Estimated Expiration
South Africa	201905100	TOFACITINIB ORAL SUSTAINED RELEASE DOSAGE FORMS
Taiwan	I619516
Slovenia	2968155
Peru	10962001
Taiwan	I619516
China	1409712

Supplementary Protection Certificates for TOFACITINIB CITRATE

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1666481	2017/036	Ireland		PRODUCT NAME: TOFACITINIB, OPTIONALLY IN THE FORM OF A PHARMACEUTICALLY ACCEPTABLE SALT, INCLUDING THE CITRATE SALT; REGISTRATION NO/DATE: EU/1/17/1178/001 EU/1/17/1178/004 20170322
1666481	132017000095300	Italy		PRODUCT NAME: TOFACITINIB, OPZIONALMENTE NELLA FORMA DI UN SALE FARMACEUTICAMENTE ACCETTABILE, COMPRENDENTE IL SALE CITRATO(XELJANZ); AUTHORISATION NUMBER(S) AND DATE(S): EU/1/17/1178/001-004, 20170324
1666481	PA2017025,C1666481	Lithuania		PRODUCT NAME: TOFACITINIBAS, PASIRINKTINAI FARMACINIU POZIURIU PRIIMTINOS DRUSKOS PAVIDALE, ISKAITANT CITRATO DRUSKAAA; REGISTRATION NO/DATE: EU/1/17/1178 20170322
1666481	37/2017	Austria		PRODUCT NAME: TOFACITINIB, GEGEBENENFALLS IN FORM EINES PHARMAZEUTISCH VERTRAEGLICHEN SALZES, EINSCHLIESSLICH DES CITRATS; REGISTRATION NO/DATE: EU/1/17/1178 (MITTEILUNG) 20170324
1235830	C01235830/01	Switzerland		PRODUCT NAME: TOFACITINIB; REGISTRATION NO/DATE: SWISSMEDIC 62630 12.07.2013
1666481	CR 2017 00035	Denmark		PRODUCT NAME: TOFACITINIB, EVENTUELT I FORM AF ET FARMACEUTISK ACCEPTABELT SALT, HERUNDER CITRAT-SALTET; REG. NO/DATE: EU/1/17/1178/001-003 20170324

Market Dynamics and Financial Trajectory for Tofacitinib Citrate

Last updated: August 31, 2025

Introduction

Tofacitinib citrate is an oral Janus kinase (JAK) inhibitor developed initially by Pfizer and later marketed under brand names like Xeljanz. Approved primarily for rheumatoid arthritis (RA), ulcerative colitis (UC), and psoriatic arthritis, its market competitiveness hinges on evolving clinical data, regulatory approvals, and the broader shift in autoimmune disease management. Its financial trajectory, shaped by patent protections, market penetration, and competitive dynamics, reflects both its therapeutic promise and challenges.

Market Overview

The global autoimmune disorder treatments market, valued at approximately $40 billion in 2022, is poised for sustained growth driven by unmet medical needs and novel therapies. Tofacitinib's segment, particularly for RA and UC, commands a significant share, thanks to its oral administration advantage over biologics. The drug’s efficacy in multiple indications, combined with ease of use, bolsters its market standing.

Regulatory Landscape and Approvals

Initially approved by the U.S. Food and Drug Administration (FDA) in 2012 for RA, Tofacitinib has subsequently gained approvals for UC (2018) and psoriatic arthritis (2017). Regulatory bodies have periodically expanded its indications, broadening its market footprint. However, safety concerns linked to serious infections and thrombosis have prompted label updates, influencing prescriber confidence and reimbursement policies.

Market Drivers

• Convenience and Efficacy: As an oral JAK inhibitor, Tofacitinib offers a non-injection alternative to biologics, appealing to patients seeking convenience.
• Broad Indication Portfolio: Its approval for multiple autoimmune diseases enhances revenue across segments.
• Unmet Medical Needs: For patients unresponsive to conventional therapies, Tofacitinib provides a valuable alternative.

Market Challenges

• Safety Profile and Regulatory Scrutiny: Post-marketing safety concerns (e.g., increased risk of blood clots and infections) have led to boxed warnings, constraining utilization.
• Market Competition: The JAK inhibitor class has expanded with drugs like baricitinib (Eli Lilly) and upadacitinib (AbbVie), intensifying competitive pressure.
• Patent Expiry and Biosimilar Competition: Patent challenges and upcoming generic/biosimilar entries threaten revenue streams.

Competitive Landscape

The JAK inhibitor class is crowded, with key competitors:

• Baricitinib (Eli Lilly): Approved for RA and UC, with strong clinical data and aggressive marketing.
• Upadacitinib (AbbVie): Positioned as a next-generation JAK inhibitor, with promising efficacy profiles.
• Filgotinib (Gilead): Pending approval in the U.S., but facing regulatory hurdles in other regions.

The competitive edge of Tofacitinib is eroding, although its early market entry provides a strong brand presence.

Financial Trajectory

Revenue Trends
Initial peak sales for Tofacitinib reached approximately $2.6 billion in 2019[1], driven predominantly by RA treatment. Since then, sales have plateaued and declined modestly, influenced by safety concerns and intensified competition. Pfizer reported global sales near $1.2 billion in 2022, indicating a slowdown compared to peak periods.

Patent Protection and Generics
Patent protections in key markets like the U.S. extend into the mid-2020s. However, patent litigation and biosimilar challenges are anticipated to erode exclusivity, risking revenue decline post-patent expiry[2].

Pipeline and Label Expansion
Efforts to expand indications, such as Crohn's disease and alopecia areata, are underway. Successful label extensions could buoy future revenues, but clinical setbacks or regulatory delays pose risks.

Pricing and Reimbursement Dynamics
Pricing strategies have varied by region, with high wholesale costs offset by negotiated discounts and rebates. Reimbursement hurdles are encountered in markets with strict cost-control measures, impacting sales volume.

Market Outlook

Projected revenues suggest a declining trend over the next five years absent significant breakthroughs. Analysts predict a compound annual growth rate (CAGR) of -2% to -4% from 2022 to 2027, considering patent cliff effects and competitive pressures[3].

However, strategic initiatives—such as developing fixed-dose combinations, expansion into new indications, and optimizing dosing regimens—could mitigate decline. Adoption of biosimilars and generics will further influence pricing and market share.

Strategic Implications

Pfizer's aggressive pipelines and potential new formulations are critical for sustaining profitability. Partnerships or licensing deals for combination therapies may also enhance the product’s durability. Regulatory decisions in regions like Europe and emerging markets (e.g., Asia-Pacific) will significantly influence overall financial trajectories.

Conclusion

Tofacitinib citrate's market dynamics are characterized by initial rapid growth, followed by plateauing due to safety concerns, competitive pressures, and patent expiries. While current revenues are stabilizing at moderate levels, significant growth potential exists through pipeline expansion and indications beyond autoimmune disorders. However, the financial outlook necessitates strategic agility to navigate adverse safety signals and market saturation.

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Key Takeaways

• Tofacitinib citrate remains a valuable asset in autoimmune therapy but faces stiffening competition from newer JAK inhibitors.
• Patent expiries and biosimilar entries predict potential revenue erosion starting mid-2020s.
• Safety concerns and regulatory actions will influence prescribing patterns and reimbursement.
• Market expansion hinges on successful label extensions and geographic penetration.
• Long-term profitability requires strategic diversification, pipeline development, and market adaptation.

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FAQs

1. What are the primary indications for Tofacitinib citrate?
   Tofacitinib is approved for rheumatoid arthritis, ulcerative colitis, and psoriatic arthritis, with ongoing research into additional autoimmune conditions.

2. How do safety concerns impact Tofacitinib's market performance?
   Elevated risks of infections, thrombosis, and malignancies have led to stricter labeling and cautious prescribing, potentially limiting sales growth.

3. What competitors pose the biggest threat to Tofacitinib?
   Newer JAK inhibitors like baricitinib and upadacitinib, with comparable efficacy and safety profiles, are the primary competitors.

4. When will patent expiry likely affect Tofacitinib sales?
   Patent protection in key regions is expected to end around 2024–2025, opening the door for biosimilar competition.

5. What strategic moves could extend Tofacitinib’s market life?
   Expanding indications, enhancing safety profiles, optimizing dosing, and entering emerging markets are vital strategies.

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References

[1] Pfizer Annual Reports (2019–2022).
[2] U.S. Patent Office and Court Filings.
[3] MarketResearch.com, "JAK Inhibitors Market Outlook," 2023.