Xeljanz (Tofacitinib Citrate)

Pfizer · FDA-approved approved Small molecule Quality 81/100

Xeljanz (generic name: Tofacitinib Citrate) is a JAK inhibitor Small molecule drug developed by Pfizer. It is currently FDA-approved (first approved 2012) for Juvenile idiopathic arthritis, extended oligoarthritis, Juvenile psoriatic arthritis, Polyarticular juvenile idiopathic arthritis.

Tofacitinib inhibits Janus kinase enzymes to prevent STAT phosphorylation and activation.

Xeljanz, also known as tofacitinib citrate, is a small molecule Janus Kinase (JAK) inhibitor used to treat conditions such as rheumatoid arthritis, pain, fatigue, and cognitive decline. It is classified as an INHIBITOR drug class and has been studied in clinical trials for its efficacy in these conditions.

At a glance

Generic name	Tofacitinib Citrate
Sponsor	Pfizer
Drug class	JAK inhibitor
Target	Janus kinase (JAK) enzymes
Modality	Small molecule
Phase	FDA-approved
First approval	2012
Annual revenue	1087

Mechanism of action

Tofacitinib is a Janus kinase (JAK) inhibitor that modulates intracellular signaling pathways. JAKs are intracellular enzymes that transmit signals 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.

Approved indications

• Juvenile idiopathic arthritis, extended oligoarthritis
• Juvenile psoriatic arthritis
• Polyarticular juvenile idiopathic arthritis
• Psoriatic arthritis
• Rheumatoid arthritis
• Ulcerative colitis

Common side effects

• Herpes zoster
• Upper respiratory tract infection
• Bronchitis
• Nasopharyngitis
• Urinary tract infection
• Rheumatoid arthritis
• Hepatic function abnormal
• Hypertension
• Fall
• Upper respiratory tract inflammation
• Back pain
• Arthralgia

Drug interactions

• Strong CYP3A4 inhibitors (e.g., ketoconazole)
• Moderate CYP3A4 inhibitors concomitantly used with strong CYP2C19 inhibitors (e.g., fluconazole)
• Strong CYP3A4 inducers (e.g., rifampin)
• Immunosuppressive drugs (e.g., azathioprine, tacrolimus, cyclosporine)

Patents

Patent	Expiry	Type

Primary sources

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.

Source	Used for
FDA label	Mechanism, indications, dosing, boxed warnings, drug interactions
FDA Orange Book	Patents + exclusivity
SEC EDGAR	Revenue + earnings

Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Xeljanz CI brief — competitive landscape report
• Xeljanz updates RSS · CI watch RSS
• Pfizer portfolio CI

Frequently asked questions about Xeljanz

What is Xeljanz?

Xeljanz (Tofacitinib Citrate) is a JAK inhibitor drug developed by Pfizer, indicated for Juvenile idiopathic arthritis, extended oligoarthritis, Juvenile psoriatic arthritis, Polyarticular juvenile idiopathic arthritis.

How does Xeljanz work?

Tofacitinib inhibits Janus kinase enzymes to prevent STAT phosphorylation and activation.

What is Xeljanz used for?

Xeljanz is indicated for Juvenile idiopathic arthritis, extended oligoarthritis, Juvenile psoriatic arthritis, Polyarticular juvenile idiopathic arthritis, Psoriatic arthritis, Rheumatoid arthritis.

Who makes Xeljanz?

Xeljanz is developed and marketed by Pfizer (see full Pfizer pipeline at /company/pfizer).

What is the generic name of Xeljanz?

Tofacitinib Citrate is the generic (nonproprietary) name of Xeljanz.

What drug class is Xeljanz in?

Xeljanz belongs to the JAK inhibitor class. See all JAK inhibitor drugs at /class/jak-inhibitor.

When was Xeljanz approved?

Xeljanz was first approved on 2012.

What development phase is Xeljanz in?

Xeljanz is FDA-approved (marketed).

What are the side effects of Xeljanz?

Common side effects of Xeljanz include Herpes zoster, Upper respiratory tract infection, Bronchitis, Nasopharyngitis, Urinary tract infection, Rheumatoid arthritis.

What is Xeljanz's annual revenue?

Xeljanz generated approximately $0.0B in annual revenue.

What does Xeljanz target?

Xeljanz targets Janus kinase (JAK) enzymes and is a JAK inhibitor.

Related

• Drug class: All JAK inhibitor drugs
• Target: All drugs targeting Janus kinase (JAK) enzymes
• Manufacturer: Pfizer — full pipeline
• Indication: Drugs for Juvenile idiopathic arthritis, extended oligoarthritis
• Indication: Drugs for Juvenile psoriatic arthritis
• Indication: Drugs for Polyarticular juvenile idiopathic arthritis