Tofacitinib Citrate API has become one of the most sought-after molecules among global B2B buyers. This guide explores its pharmacology, formulation, regulatory considerations, and why Bio-Synth a Hyderabad-based WHO-GMP-certified organisation, stands among the top Tofacitinib Citrate API Manufacturers in India.
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Tofacitinib API: Mechanism, Clinical Uses, and Formulation Insights

Tofacitinib API: Mechanism, Clinical Uses, and Formulation Insights

 

Tofacitinib Citrate API is a Janus kinase (JAK) inhibitor used to manage autoimmune diseases such as rheumatoid arthritis, psoriasis, and ulcerative colitis. As a small-molecule immunomodulator, it interrupts cytokine signalling by inhibiting the JAK-STAT pathway.
 With the rising demand for oral biologic alternatives, Tofacitinib Citrate API has become one of the most sought-after molecules among global B2B buyers. This guide explores its pharmacology, formulation, regulatory considerations, and why Bio-Synth  a Hyderabad-based WHO-GMP-certified organisation, stands among the top Tofacitinib Citrate API Manufacturers in India.

 

Understanding Tofacitinib: A Potent Kinase Inhibitor API

What is Tofacitinib?

Tofacitinib Citrate API is a synthetic small molecule classified under Janus kinase (JAK) inhibitors. It modulates immune responses by targeting intracellular signaling enzymes that regulate cytokine activity.

Quick Facts:

  • API Category: Kinase inhibitor (JAK family) 
  • Molecular Formula: C₁₆H₂₀N₆O 
  • Therapeutic Class: Immunomodulator 
  • Regulatory Status: Approved by FDA, EMA, and DCGI 
  • Supplied As: High-purity crystalline API powder 

 

How It Works: JAK-STAT Pathway Inhibition

Tofacitinib Citrate API inhibits JAK enzymes, disrupting cytokine signalling via the JAK-STAT pathway — a key driver of inflammation.

Component Function Role of Tofacitinib
Cytokines Trigger immune response Reduces cytokine sensitivity
JAK enzymes Transmit immune signals Direct enzyme inhibition
STAT proteins Activate inflammatory genes Blocks gene activation
Immune response Maintains inflammation balance Downregulated

By preventing cytokine activation, Tofacitinib Citrate API effectively reduces chronic inflammation in autoimmune conditions.

 

Clinical Applications of Tofacitinib API

Approved Therapeutic Indications:

  • Rheumatoid Arthritis (RA) – as monotherapy or with methotrexate 
  • Psoriatic Arthritis – for patients unresponsive to biologics 
  • Ulcerative Colitis – oral alternative to injectable biologics 

Investigational/Off-label Uses: Alopecia areata, lupus, and chronic plaque psoriasis

Formulation Routes:

  • Oral Tablets: 5 mg and 10 mg 
  • Extended-Release Tablets: 11 mg once daily 
  • Combination Formulations: Under research with methotrexate and biologics 

Its pharmacokinetics support once- or twice-daily dosing for improved patient adherence.

 

Why Tofacitinib Matters for Pharma Buyers and CDMOs

Rising Global Demand

The autoimmune therapeutics market is projected to exceed $153 billion by 2030, driven by demand for oral biologics such as Tofacitinib Citrate API.

Key Benefits:

  • Convenient oral administration 
  • Long shelf life suited for export markets 
  • Fast-acting with visible clinical improvement in weeks 

Importance of High-Purity API

Pharma formulators require:

  • ≥ 99% purity (USP / Ph.Eur compliant) 
  • Minimal residual solvents 
  • ICH-zone stability data 
  • WHO-GMP and regulatory documentation 

The synthesis complexity of Tofacitinib Citrate API demands precision in impurity profiling and crystallization control.

🔍 Explore Bio-Synth’s Tofacitinib Citrate API Manufacturers and Suppliers in India for GMP-compliant kinase inhibitors and high-purity actives.

 

Manufacturing Insights: Indian Advantage in API Production

India’s API Leadership

India ranks among the top three API exporters globally, offering:

  • Cost-efficient CDMO capabilities 
  • WHO-GMP-certified facilities 
  • Regulatory expertise with USFDA, EMA, PMDA 

Why Hyderabad is the API Hub

Hyderabad’s Balanagar Industrial Area is home to advanced pharmaceutical manufacturers supported by:

  • Skilled process chemists and engineers 
  • Regulatory filing expertise (DMF, CEP, ANDA) 
  • Strong logistics and export infrastructure 

 

Bio-Synth’s Manufacturing Excellence

Founded in 1943, Bio-Synth has decades of experience in API synthesis and contract manufacturing.

Key Capabilities:

  • Over 50+ APIs and intermediates developed 
  • Partnerships with leading global pharmaceutical companies 
  • Advanced purification and crystallization technologies 
  • APIs compliant with ICH Q7 and WHO-GMP standards 

 

Regulatory and Supply Chain Excellence

Comprehensive Documentation

Each Tofacitinib Citrate API batch includes:

  • Drug Master File (DMF) – US & EU 
  • Certificate of Analysis (CoA) 
  • Batch Manufacturing Record (BMR) 
  • Stability Data (ICH Zone I–IV) 

These streamline regulatory submissions for ANDA or CTD filings.

Global Export Capabilities

Bio-Synth operates from Hyderabad SEZs with:

  • Ambient and cold-chain logistics 
  • Flexible pack sizes (10 g – 50 kg) 
  • Fast air and sea dispatches to North America, MENA, CIS, and Southeast Asia 

 

Process Flow: From Lab to Dispatch

Synthesis → Purification → QC Testing → Regulatory Filing → Packaging → Export Dispatch

Stage Focus Area
Synthesis Multi-step organic process
QC Testing HPLC, NMR, residual solvent analysis
Regulatory DMF, CoA, stability reports
Packaging Triple LDPE liners in HDPE drums
Export WHO-GMP-certified batch dispatch

 

B2B Buyer’s Sourcing Checklist

When sourcing Tofacitinib Citrate API Suppliers in India, verify:

  • WHO-GMP / USFDA audit status 
  • DMF availability 
  • Three-batch analytical data 
  • ICH impurity profiling 
  • Market-specific regulatory support 

A supplier like Bio-Synth provides full technical transparency and documentation, making it one of the most reliable Tofacitinib Citrate API Manufacturers and Suppliers globally.

 

Smart Formulation Insights

R&D and formulation teams should evaluate:

  • Solubility: Moderate; requires excipient optimisation 
  • pKa: ~5, affecting absorption kinetics 
  • Stability: Requires photostability testing 
  • Polymorph Control: Ensures bioequivalence consistency 

These parameters make a reliable Tofacitinib Citrate API Manufacturer essential for formulation success.

 

FAQs: Buyer & Scientist Quick Answers

Q1: Why do global buyers prefer Indian API suppliers for kinase inhibitors?
 India offers cost-efficient synthesis, WHO-GMP compliance, and complete regulatory documentation. Hyderabad’s industrial ecosystem supports rapid, export-grade production.

Q2: How does Tofacitinib differ from biologics?
 Unlike injectable biologics, Tofacitinib Citrate API is a small molecule oral drug that targets intracellular JAK enzymes, offering similar efficacy with higher patient convenience.

Q3: Can Indian CDMOs manufacture Tofacitinib for regulated markets?
 Yes. CDMOs like Bio-Synth follow cGMP protocols, provide DMF support, and ensure flexible batch sizes for both regulated and semi-regulated markets.

 

Conclusion: 

Partner with a Trusted Indian API Manufacturer

Tofacitinib Citrate API is revolutionising immunology by offering an oral, cost-efficient alternative to injectable biologics. For B2B buyers and formulation partners, sourcing from WHO-GMP-certified Tofacitinib Citrate API Manufacturers in India ensures reliability and regulatory readiness.
 With over 80 years of heritage, Bio-Synth continues to deliver high-purity Tofacitinib Citrate API with global quality standards and efficient export logistics.

📩 Contact Bio-Synth for quotes, DMF access, or CDMO collaboration opportunities.

Tofacitinib Citrate API Manufacturers & Suppliers in India

Tofacitinib Citrate API Manufacturers & Suppliers in India

Tofacitinib Citrate API is an inhibitor of Janus kinases, a group of intracellular enzymes involved in signalling pathways that affect hematopoiesis and immune cell function. It is approved by the FDA for the treatment of moderate to severe rheumatoid arthritis that responds inadequately to methotrexate or in those who are intolerant to methotrexate. Tofacitinib has also been studied in clinical trials for the prevention of organ transplant rejection, and is currently under investigation for the treatment of psoriasis.

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Product Description

Product Description

Generic Name: Tofacitinib Citrate API

Chemical Name : ·
3-[(3R,4R)-4-Methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile

CAS Number: 540737-29-9

Molecular weight: 509.49 g/mol

Molecular formula: C22H28N6O8

Category: Janus kinase (JAK) inhibitors

Therapeutic use: Used to treat rheumatoid arthritis and ulcerative colitis

Form: Powder

Color: White to off-white

Size of package: As per requirement

Synonyms: Tasocitinib monocitrate, Tofacitinib monocitrate

Solubility: Freely soluble in N, N-Dimethylacetamide, slightly soluble in water, and very slightly soluble in ethanol (99.5% ethanol)

Tofacitinib Citrate API Specification

  • ☐ Total impurities: Not more than 1.0%
  • ☐ Any unspecified impurity: Not more than 0.1%

Quality Standards and Manufacturing Excellence of Bio-Synth

Bio-Synth operates with an unwavering commitment to quality. Our manufacturing processes integrate

  • ☐ WHO-GMP (Good Manufacturing Practices) compliance
  • ☐ ISO 9000:2015 certification
  • ☐ Adherence to ICH guidelines and pharmacopeia standards

Our facilities are equipped with cutting-edge technology and maintain strict adherence to GLP (Good Laboratory Practices), GDP (Good Documentation Practices), and cGMP (Current Good Manufacturing Practices). This results in consistent product quality, reinforcing Bio-Synth’s reputation for excellence.

Applications of Tofacitinib Citrate API

Tofacitinib is used alone or together with other medicines (eg, DMARDs) to treat moderate to severely active rheumatoid arthritis, active psoriatic arthritis, ulcerative colitis, ankylosing spondylitis, and polyarticular course juvenile idiopathic arthritis (pcJIA) in patients who have taken other medicines that did not work well

Therapeutic Uses and Indications of Tofacitinib Citrate

Tofacitinib is indicated for the treatment of adult patients with moderately-to-severely active rheumatoid arthritis (RA), active psoriatic arthritis, active ankylosing spondylitis, or moderately-to-severely active ulcerative colitis who have had an inadequate response or intolerance to one or more TNF blockers. It is also indicated as an oral solution in patients ≥2 years of age for the treatment of polyarticular course juvenile idiopathic arthritis who have had an inadequate response or intolerance to one or more TNF blockers.

How Tofacitinib Citrate API Works (Mechanism of Action)

Rheumatoid arthritis is an autoimmune disease characterized by a dysregulation of pro-inflammatory cytokines. Cytokines signalling results in tissue inflammation and joint damage by stimulating the recruitment and activation of immune cells via the Janus Kinase signalling pathway.

Tofacitinib is a partial and reversible Janus Kinase (JAK) inhibitor that will prevent the body from responding to cytokine signals. By inhibiting JAKs, tofacitinib prevents the phosphorylation and activation of STATs. The JAK-STAT signalling pathway is involved in the transcription of cells involved in hematopoiesis and immune cell function. Tofacitinib works therapeutically by inhibiting the JAK-STAT pathway to decrease the inflammatory response.

Why Choose Bio-Synth for Tofacitinib Citrate API

Bio-Synth adheres to stringent quality protocols to ensure that each batch of Tofacitinib citrate API meets comprehensive global quality standards. Our robust quality control practices confirm the purity, potency, and safety of our products, ensuring reliable therapeutic results. We manufacture Tofacitinib citrate API in our 60kL WHO-GMP, ISO certified facility with a capacity of 500 kg/month

Bio Synth: Tofacitinib Citrate API Suppliers in India

Bio-synth is one of the leading API manufacturers in India that has included Tofacitinib citrate API in its product portfolio. Bio-synth manufactures all intermediates of Tofacitinib citrate API in-house, thereby offering the best quality, price and lead time.

Tofacitinib Citrate API Price in India

Bio Synth is a reputable supplier of pharmaceutical APIs and intermediates, includingTofacitinib citrate API, used to treat rheumatoid arthritis and ulcerative colitis. Bio-Synth offers Tofacitinib citrate API at highly competitive prices tailored to your specific requirements. We ensure the best value while maintaining the highest quality standards. For detailed pricing and further inquiries, please reach out to us directly, and our team will be happy to assist you.

Frequently Asked Questions

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    Tofacitinib citrate API is a Janus Kinase (JAK) inhibitor used to treat rheumatoid arthritis and ulcerative colitis

    Tofacitinib citrate API is used alone or together with other medicines (eg, DMARDs) to treat moderate to severely active rheumatoid arthritis, active psoriatic arthritis, ulcerative colitis, ankylosing spondylitis, and polyarticular course juvenile idiopathic arthritis (pcJIA) in patients who have taken other medicines that did not work well

    Bio-Synth offers premium-quality Tofacitinib citrate API at competitive prices, tailored to meet your specific requirements. By handling all production stages internally, we maintain strict control over quality while optimizing pricing. For accurate pricing and to discuss your specific needs, we encourage you to reach out with your inquiry. Our team is dedicated to providing timely responses and ensuring your complete satisfaction.

    Bio-synth is one of the top manufacturers of APIs in India. We also manufacture Tofacitinib citrate API, offering top quality, competitive prices, and short lead time.

    The chemical composition of Tofacitinib citrate API is C22H28N6O8, which stands for 3-[(3R,4R)-4-Methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile

    Yes, Tofacitinib Citrate API is available for purchase in India. Bio-synth is one of the leading manufacturers and suppliers of API products. Please reach out via the enquiry form with your requirement, and we will be happy to assist you.

    Bio-Synth has almost 8 decades of experience manufacturing high-quality APIs, with Tofacitinib citrate API as one of the key products in its product portfolio, making Bio-Synth one of the trusted manufacturers in India.

    Bio-Synth offers high-quality Tofacitinib citrate API that meets global standards like WHO-GMP and ISO 9000:2015 certification. Our rigorous quality control ensures a consistent and reliable Tofacitinib citrate API supply, making us a top choice for Tofacitinib citrate API suppliers in India.

    Our facilities are equipped with cutting-edge technology and maintain strict adherence to GLP (Good Laboratory Practices), GDP (Good Documentation Practices), and cGMP (Current Good Manufacturing Practices). This results in consistent product quality, reinforcing Bio-Synth’s reputation for excellence.

    To place an order for Tofacitinib citrate API, contact Bio-Synth through our customer service team or by filling out the contact form on our website. We provide comprehensive support to guide you through the order process and ensure timely delivery to meet your specific needs.