Filters
Custom request?
Type
Production region
Qualifications
Country of origin
Iressa (Gefitinib) API Manufacturers & Suppliers
18 verified results
All Gefitinib data. Full access. Full negotiation power
Commercial-scale Suppliers
Employees: 25+
All certificates
Employees: 50+
All certificates
Employees: 19
All certificates
Employees: 200+
All certificates
Employees: 400+
All certificates
All certificates
All certificates
All certificates
All certificates
All certificates
All certificates
All certificates
All certificates
All certificates
All certificates
All certificates
All certificates
All certificates
Total market transparency
Supplier trade data access
Buyer / supplier flow comparison
Gefitinib | CAS No: 184475-35-2 | GMP-certified suppliers
A medication that supports continued management of locally advanced or metastatic non‑small cell lung cancer in patients whose disease has progressed after prior platinum or docetaxel therapies.
Therapeutic categories
Primary indications
- For the continued treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of either platinum-based or docetaxel chemotherapies
Product Snapshot
- Gefitinib is an oral small‑molecule API supplied in coated and film‑coated tablet formulations
- It is used for management of locally advanced or metastatic non‑small cell lung cancer following prior platinum‑based or docetaxel therapy
- It is approved in major markets including the US, EU, and Canada, with some investigational status in certain regions
Clinical Overview
Gefitinib exhibits selective inhibition of the EGFR tyrosine kinase by binding at the ATP‑binding pocket of the receptor. EGFR overexpression or dysregulated signaling is common in several carcinomas, including subsets of lung cancer. By blocking receptor autophosphorylation, gefitinib reduces downstream activation of proliferative and anti-apoptotic pathways, including Ras-mediated signaling cascades, resulting in attenuation of malignant cell survival and proliferation. Its pharmacodynamic activity also includes inhibition of other intracellular tyrosine kinases associated with transmembrane receptors.
Absorption following oral administration is variable and influenced by gastrointestinal pH. Gefitinib is extensively metabolized hepatically, primarily via CYP3A pathways, and to a lesser extent by CYP2D6. It is both a substrate and inhibitor of several CYP isoforms and transporters, including CYP3A, CYP2D6, BCRP/ABCG2, and P-glycoprotein, creating potential for clinically relevant drug interactions. Elimination occurs mainly through fecal excretion of metabolites.
Safety considerations include dose‑related dermatologic and gastrointestinal adverse effects, as well as risks of interstitial lung disease, hepatotoxicity, and corneal disorders. Exposure may increase in patients with hepatic impairment or when co-administered with potent CYP3A inhibitors. Acid‑suppressive therapies can reduce drug absorption. As with other EGFR inhibitors, monitoring for pulmonary symptoms, liver function changes, and persistent diarrhea is standard practice.
Gefitinib’s clinical use has centered on molecularly characterized NSCLC populations in various global regulatory contexts, with availability differing by region.
For API procurement, sourcing should prioritize manufacturers with demonstrated control of polymorphic form, impurity profile, and residual solvent levels, along with comprehensive stability data and adherence to current Good Manufacturing Practices to support regulatory submissions.
Identification & chemistry
| Generic name | Gefitinib |
|---|---|
| Molecule type | Small molecule |
| CAS | 184475-35-2 |
| UNII | S65743JHBS |
| DrugBank ID | DB00317 |
Pharmacology
| Summary | Gefitinib is a selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that blocks ATP‑dependent receptor activation. By suppressing EGFR signaling, it reduces downstream pathways that support malignant cell survival and proliferation. Its pharmacodynamic activity reflects inhibition of EGFR‑associated intracellular phosphorylation in both normal and cancer cells. |
|---|---|
| Mechanism of action | Gefitinib is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase that binds to the adenosine triphosphate (ATP)-binding site of the enzyme. EGFR is often shown to be overexpressed in certain human carcinoma cells, such as lung and breast cancer cells. Overexpression leads to enhanced activation of the anti-apoptotic Ras signal transduction cascades, subsequently resulting in increased survival of cancer cells and uncontrolled cell proliferation. Gefitinib is the first selective inhibitor of the EGFR tyrosine kinase which is also referred to as Her1 or ErbB-1. By inhibiting EGFR tyrosine kinase, the downstream signaling cascades are also inhibited, resulting in inhibited malignant cell proliferation. |
| Pharmacodynamics | Gefitinib inhibits the intracellular phosphorylation of numerous tyrosine kinases associated with transmembrane cell surface receptors, including the tyrosine kinases associated with the epidermal growth factor receptor (EGFR-TK). EGFR is expressed on the cell surface of many normal cells and cancer cells. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Epidermal growth factor receptor | Humans | antagonist |
ADME / PK
| Absorption | Absorbed slowly after oral administration with a mean bioavailability of 60%. Peak plasma levels occurs 3-7 hours post-administration. Food does not affect the bioavailability of gefitinib. |
|---|---|
| Half-life | 48 hours [IV administration] |
| Protein binding | 90% primarily to serum albumin and alpha 1-acid glycoproteins (independent of drug concentrations). |
| Metabolism | Primarily hepatic via CYP3A4. Three sites of biotransformation have been identified: metabolism of the N-propoxymorpholino-group, demethylation of the methoxy-substituent on the quinazoline, and oxidative defluorination of the halogenated phenyl group. |
| Route of elimination | Elimination is by metabolism (primarily CYP3A4) and excretion in feces. Excretion is predominantly via the feces (86%), with renal elimination of drug and metabolites accounting for less than 4% of the administered dose. |
| Volume of distribution | * 1400 L [IV administration] |
| Clearance | * 595 mL/min [IV administration] |
Formulation & handling
- Oral small‑molecule API with low aqueous solubility, requiring solubility‑enhancing strategies for tablet formulations.
- Moderate lipophilicity (LogP ~3.8) supports conventional oral solid dosage design but may lead to dissolution‑rate‑limited absorption.
- Metabolism via CYP3A4 makes it sensitive to grapefruit products, but no strict food‑dependence for administration.
Regulatory status
| Lifecycle | The API’s foundational U.S. and Canadian patents expired between 2013 and 2017, indicating a well‑established maturity stage. With products marketed in Canada, the US, and the EU, the ingredient is positioned in a fully generic, late‑lifecycle market. |
|---|
| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | Gefitinib is supplied by a single originator manufacturer with additional roles carried out by commercial packagers in North America. Branded products are established across the US, EU, and Canada, indicating broad global distribution. Patent expiries between 2013 and 2017 suggest that generic competition is already present or well‑established in most markets. |
|---|
Safety
| Toxicity | The acute toxicity of gefitinib up to 500 mg in clinical studies has been low. In non-clinical studies, a single dose of 12,000 mg/m<sup>2</sup> (about 80 times the recommended clinical dose on a mg/m<sup>2</sup> basis) was lethal to rats. Half this dose caused no mortality in mice. Symptoms of overdose include diarrhea and skin rash. |
|---|
- Acute toxicity is low in humans up to 500 mg, but non‑clinical data show lethality in rats at single doses around 12,000 mg/m², indicating a wide species‑dependent toxicity margin
- Overexposure in studies has produced dose‑related gastrointestinal and dermatologic reactions such as diarrhea and rash, useful as markers of excessive EGFR inhibition
- High‑dose animal findings suggest the need for controlled handling conditions to prevent accidental high‑level exposure during API manufacturing or processing
Gefitinib is a type of Protein kinase inhibitors
Protein kinase inhibitors are a vital subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a crucial role in targeted cancer therapies. These inhibitors specifically target and block the activity of protein kinases, enzymes that regulate various cellular processes, including cell growth, division, and signal transduction.
Protein kinase inhibitors function by binding to the active site of protein kinases, preventing them from phosphorylating specific proteins and disrupting intracellular signaling pathways. This targeted approach inhibits the uncontrolled growth and proliferation of cancer cells, ultimately leading to their death.
The development of protein kinase inhibitors has revolutionized cancer treatment by providing more effective and less toxic alternatives to traditional chemotherapy. These drugs have demonstrated impressive results in the treatment of various cancers, including lung, breast, and leukemia.
The pharmaceutical industry invests heavily in research and development to discover novel protein kinase inhibitors with improved potency, selectivity, and pharmacokinetic properties. High-throughput screening, computational modeling, and structure-activity relationship studies are employed to identify potential lead compounds.
The success of protein kinase inhibitors in treating cancer has spurred significant interest in this subcategory of APIs. Ongoing research aims to expand their applications to other diseases, such as autoimmune disorders and neurological conditions.
In conclusion, protein kinase inhibitors are a valuable class of pharmaceutical APIs with immense potential for targeted cancer therapies. Continued advancements in this field hold promise for improved treatment outcomes and enhanced patient care.
Gefitinib (Protein kinase inhibitors), classified under Anticancer drugs
Anticancer drugs belong to the pharmaceutical API (Active Pharmaceutical Ingredient) category designed specifically to combat cancer cells. These powerful medications play a crucial role in cancer treatment and are developed to target and destroy cancerous cells, preventing their growth and spread.
Anticancer drugs are classified based on their mode of action and can include various types such as chemotherapy drugs, targeted therapy drugs, immunotherapy drugs, and hormonal therapy drugs. Chemotherapy drugs work by interfering with the cell division process, thereby inhibiting the growth of cancer cells. Targeted therapy drugs, on the other hand, are designed to attack specific molecules or genes involved in cancer growth, minimizing damage to healthy cells. Immunotherapy drugs stimulate the body's immune system to recognize and destroy cancer cells. Hormonal therapy drugs are used in cancers that are hormone-dependent, such as breast or prostate cancer, to block the hormones that fuel cancer cell growth.
These APIs are typically synthesized through complex chemical processes in state-of-the-art manufacturing facilities. Stringent quality control measures ensure the purity, potency, and safety of these drugs. Anticancer APIs undergo rigorous testing and adhere to stringent regulatory guidelines before being approved for clinical use.
Due to their critical role in cancer treatment, anticancer drugs are in high demand worldwide. Researchers and pharmaceutical companies continually strive to develop new and more effective APIs in this category to enhance treatment outcomes and minimize side effects. The ongoing advancements in the field of anticancer drug development offer hope for improved cancer therapies and better patient outcomes.
Gefitinib API manufacturers & distributors
Compare qualified Gefitinib API suppliers worldwide. We currently have 18 companies offering Gefitinib API, with manufacturing taking place in 3 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Adley Formulations | Producer | India | India | CoA, GMP | 14 products |
| BDR Lifesciences | Producer | India | India | CoA, WC | 4 products |
| Cipla | Producer | India | India | CEP, CoA, GMP, USDMF, WC | 164 products |
| Gonane Pharma | Producer | India | India | BSE/TSE, CoA, GMP, MSDS | 166 products |
| Hetero Labs | Producer | India | India | CoA, GMP, JDMF, USDMF, WC | 90 products |
| Kolon Life Science | Producer | South Korea | South Korea | CoA, JDMF | 32 products |
| Mac Chem Products | Producer | India | India | CEP, CoA, GMP | 25 products |
| MSN Labs. | Producer | India | India | CoA, GMP, USDMF, WC | 119 products |
| Natco Pharma | Producer | India | India | CEP, CoA, GMP, JDMF, USDMF, WC | 40 products |
| Qilu Antibiotics | Producer | China | China | CEP, CoA, GMP, USDMF, WC | 33 products |
| Senova Technology Co., Lt... | Producer | China | China | CoA, GMP, ISO9001, USDMF | 157 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Shaoxing Hantai Pharma | Distributor | China | China | CoA | 162 products |
| Sichuan Benepure | Producer | China | China | CoA | 23 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CEP, CoA, GMP, ISO9001, USDMF | 764 products |
| Suzhou Lixin Pharmaceutic... | Producer | China | China | BSE/TSE, CoA, GMP, MSDS | 34 products |
| Yabao Pharma | Producer | China | China | CoA, USDMF | 5 products |
| Zhejiang Hisun Pharma | Producer | China | China | CoA, USDMF | 69 products |
When sending a request, specify which Gefitinib API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Gefitinib API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
Frequently asked questions about Gefitinib API
Sourcing
What matters most when sourcing GMP-grade Gefitinib?
Which documents are typically required when sourcing Gefitinib API?
Which manufacturers are known to produce Gefitinib API?
How can I request quotes for Gefitinib API from GMP suppliers?
Is a GMP audit report available for Gefitinib manufacturers?
How many suppliers offer Gefitinib API on Pharmaoffer?
Which countries are known to manufacture Gefitinib API?
Which certifications do suppliers of Gefitinib usually hold?
Technical
What is Gefitinib (CAS 184475-35-2) used for?
Which therapeutic class does Gefitinib fall into?
What conditions is Gefitinib mainly prescribed for?
How does Gefitinib work?
What should someone know about the safety or toxicity profile of Gefitinib?
What are important formulation and handling considerations for Gefitinib as an API?
Is Gefitinib a small molecule?
Are there special stability concerns for oral Gefitinib?
Regulatory
Where is Gefitinib approved or in use globally?
What’s the regulatory and patent landscape for Gefitinib right now?
Pharmaoffer
How does Pharmaoffer’s Smart Sourcing Service help with Gefitinib procurement?
Is Gefitinib included in the PRO Data Insights coverage?
Where can I access the API market report for Gefitinib?
