Tofacitinib Citrate API: Global Demand, Manufacturing, and Market Outlook 2026

Tofacitinib Citrate API: 2026 Sourcing Guide & Technical Risk Assessment
Key Summary:

• API Name: Tofacitinib Citrate (JAK Inhibitor)
• CAS Number: 540737-29-9
• Critical Issue 2025: Managing Nitrosamine (NDSRI) risks and Enantiomeric purity.
• Market Outlook: High demand for generic formulations; Global CAGR ~7.5%.
• Primary Sourcing Hub: Hyderabad, India.

As we approach 2026, the global demand for Tofacitinib Citrate API is shifting. Pharmaceutical manufacturers targeting the Rheumatoid Arthritis (RA) and Ulcerative Colitis (UC) markets are no longer just looking for capacity; they are prioritizing regulatory compliance.

With the USFDA and EMA tightening controls on genotoxic impurities, specifically Nitrosamine Drug Substance Related Impurities (NDSRIs), the “check-box” for selecting a supplier has changed. This guide explores the critical technical specifications, manufacturing challenges, and market trends you must know before locking in your supply chain.

 Technical Specifications: The Data R&D Teams Need

For formulation scientists, consistency in the API’s physical and chemical properties is non-negotiable. Below are the critical parameters for Tofacitinib Citrate.

Attribute	Technical Specification
Active Moiety	Tofacitinib
Salt Form	Citrate
CAS Number	540737-29-9
Molecular Formula	$C_{16}H_{20}N_{6}O \cdot C_{6}H_{8}O_{7}$
Molecular Weight	504.49 g/mol
Solubility	Soluble in water; slightly soluble in alcohol
Therapeutic Class	Selective JAK1 / JAK3 Inhibitor

 

Manufacturing Challenges: Why Process Chemistry Matters

Producing high-purity Tofacitinib Citrate is not a simple synthesis. It requires advanced process chemistry to manage three specific risks that can cause batch rejection during regulatory audits.

1. Enantiomeric Purity (Chirality)

Tofacitinib contains chiral centers that determine its efficacy. The synthesis must yield a high enantiomeric excess (>99.5%). Inferior processes often result in racemic mixtures, which are unacceptable for regulated markets.

2. Nitrosamine Control (NDSRIs)

Since 2023, the biggest hurdle for JAK inhibitors has been the risk of nitrosamine formation.

• The Risk: Secondary amines reacting with nitrosating agents during synthesis.
• The Solution: Advanced manufacturers use “Safe by Design” synthetic routes that eliminate these reagents from the final steps.
• Buyer Tip: Always request a Nitrosamine Risk Assessment Declaration before purchasing.

3. Solid State Stability

Controlling the Particle Size Distribution (PSD) is vital for the dissolution rate of your final oral dosage form. Sourcing from a partner who can customize PSD ensures your generic formulation achieves bioequivalence with the innovator brand.

Market Dynamics: The “India Advantage” in 2026

The global market for JAK inhibitors is projected to grow at a CAGR of 7.5%, driven by patent expirations and the rising prevalence of autoimmune diseases.

Why buyers are shifting to Hyderabad:

India currently captures over 20% of the global API export market, with Hyderabad serving as the central hub. The region offers a unique combination of:

• Cost Efficiency: 30-40% lower production costs compared to Western CMOs.
• Cluster Ecosystem: Access to high-quality Key Starting Materials (KSMs) within a 50km radius.
• Regulatory Maturity: High concentration of WHO-GMP and USFDA-approved facilities.

Procurement Checklist: How to Qualify Your Supplier

If you are a procurement manager, use this checklist to filter potential partners. A “Yes” on all four points indicates a mature, reliable supplier like Bio-Synth.

• DMF Readiness: Do they have an active Drug Master File or open Tech Package?
• Capacity Scalability: Can they move from Gram-scale (R&D) to Kilo-scale (Commercial) seamlessly?
• Audit Transparency: Is the facility open to customer quality audits?
• Stability Data: Do they have 6-month accelerated stability data available?

 

Conclusion: Moving from Investigation to Commercial Supply

Securing a reliable supply of Tofacitinib Citrate requires looking beyond the price per kilogram. It requires a partner who guarantees purity, provides robust documentation, and understands the regulatory landscape of 2026.

Bio-Synth stands at the forefront of this shift, offering high-purity, regulatory-compliant APIs from our Hyderabad facilities.

 

Ready for Commercial Steps?

This guide covered the technical and sourcing aspects. If you are ready to view commercial specifications, download the COA, or request a bulk quote, please visit Tofacitinib Citrate API, our dedicated product page.

With over 80 years of manufacturing heritage, Bio-Synth combines scientific precision with global reliability — delivering Tofacitinib Citrate API that meets the highest regulatory and quality benchmarks.

Contact Bio-Synth today for bulk quotations, DMF access, and CDMO collaboration opportunities.

 

Frequently Asked Questions:

Q1. What is the CAS number for Tofacitinib Citrate? The CAS number for Tofacitinib Citrate is 540737-29-9. It is chemically described as 3-[(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile citrate.

Q2. Does Tofacitinib Citrate API carry a Nitrosamine impurity risk? Like many APIs with secondary amine structures, there is a theoretical risk of forming Nitrosamine Drug Substance Related Impurities (NDSRIs). However, reputable manufacturers like Bio-Synth utilize optimized synthetic routes and rigorous solvent controls to ensure nitrosamine levels remain well below internationally accepted daily intake limits (AI).

Q3. What is the shelf life and storage condition for Tofacitinib Citrate? Tofacitinib Citrate is generally stable but sensitive to moisture and light. It should be stored in tightly closed containers at controlled room temperature (20°C to 25°C). When stored correctly under these conditions, the API typically has a retest period of 36 to 60 months, depending on the manufacturer’s stability data.

Q4. Why is Hyderabad considered the primary sourcing hub for Tofacitinib Citrate? Hyderabad, India, hosts a dense cluster of WHO-GMP certified facilities and has established supply chains for key intermediates (KSMs) required for Janus kinase inhibitors. This ecosystem allows manufacturers in the region to offer cost advantages of 20-30% compared to Western suppliers while maintaining strict USFDA and EMA compliance.

Q5. Can Tofacitinib Citrate be used for both Rheumatoid Arthritis and Ulcerative Colitis formulations? Yes. Tofacitinib Citrate is the active pharmaceutical ingredient (API) approved for formulating treatments for Rheumatoid Arthritis (RA), Psoriatic Arthritis, and Ulcerative Colitis (UC). Formulation scientists must ensure the API grade selected meets the specific particle size distribution (PSD) requirements for the intended dosage form (usually oral tablets).