Osi-774 (Erlotinib) API Manufacturers & Suppliers
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Erlotinib | CAS No: 183321-74-6 | GMP-certified suppliers
A medication that treats metastatic non-small cell lung cancer with specific EGFR mutations and is used with first-line therapy for advanced pancreatic cancer.
Therapeutic categories
Primary indications
- Erlotinib is indicated for:
- The treatment of metastatic non-small cell lung cancer (NSCLC) with tumors showing epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations
- In combination with first-line treatment for patients diagnosed with locally advanced, unresectable or metastatic pancreatic cancer
- The safety and efficacy of erlotinib have not been established for patients with NSCLC whose tumors show other EGFR mutations
Product Snapshot
- Erlotinib is an oral small molecule formulated as film-coated tablets
- It is primarily used in the treatment of metastatic non-small cell lung cancer with specific EGFR mutations and in combination therapy for locally advanced or metastatic pancreatic cancer
- Erlotinib is approved in key regulatory markets including the US, Canada, and the European Union
Clinical Overview
Pharmacologically, erlotinib competitively and reversibly binds to the ATP-binding site of EGFR tyrosine kinase, inhibiting intracellular phosphorylation events critical for signal transduction pathways involved in tumor cell proliferation and survival. Although the precise mechanisms underlying its antitumor activity are not fully elucidated, it selectively targets EGFR expressed on both normal and cancerous cells. Recent findings also identify erlotinib as a potent inhibitor of the mutant JAK2V617F kinase, suggesting potential investigative applications in myeloproliferative disorders such as polycythemia vera.
Erlotinib belongs to quinazolinamine derivatives, a class of heterocyclic aromatic compounds. Its metabolism is primarily hepatic, involving cytochrome P450 enzymes—especially CYP3A4 and CYP1A2 isoforms—with known interactions affecting these metabolic pathways. Erlotinib exhibits a narrow therapeutic index and is classified as a substrate and inhibitor of multiple cytochrome P450 enzymes and drug transporters including P-glycoprotein and organic anion transporting polypeptide 2B1. These characteristics necessitate careful consideration of potential drug-drug interactions.
Safety considerations include risks associated with QTc prolongation, hepatic toxicity, interstitial lung disease, and dermatologic adverse effects. Close monitoring of cardiac and hepatic function is recommended during therapy.
Erlotinib is predominantly marketed under the trade name Tarceva. Quality considerations for API procurement focus on stringent adherence to regulatory standards for identity, purity, polymorphic form, and impurity profiles due to the narrow therapeutic index and complex metabolism. Suppliers must ensure comprehensive documentation and compliance with current Good Manufacturing Practices to support global regulatory submissions.
Identification & chemistry
| Generic name | Erlotinib |
|---|---|
| Molecule type | Small molecule |
| CAS | 183321-74-6 |
| UNII | J4T82NDH7E |
| DrugBank ID | DB00530 |
Pharmacology
| Summary | Erlotinib is a tyrosine kinase inhibitor that targets the intracellular phosphorylation of the epidermal growth factor receptor (EGFR), a receptor expressed on both normal and cancerous cells. It is primarily used to inhibit EGFR-driven signaling pathways involved in tumor cell proliferation and survival in certain non-small cell lung cancers and pancreatic cancers. Its inhibitory specificity for other tyrosine kinase receptors remains incompletely characterized. |
|---|---|
| Mechanism of action | The mechanism of clinical antitumor action of erlotinib is not fully characterized. Erlotinib inhibits the intracellular phosphorylation of tyrosine kinase associated with the epidermal growth factor receptor (EGFR). Specificity of inhibition with regard to other tyrosine kinase receptors has not been fully characterized. EGFR is expressed on the cell surface of normal cells and cancer cells. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Nuclear receptor subfamily 1 group I member 2 | Humans | agonist |
| Epidermal growth factor receptor | Humans | antagonist |
ADME / PK
| Absorption | Erlotinib is about 60% absorbed after oral administration and its bioavailability is substantially increased by food to almost 100%. Peak plasma levels occur 4 hours after dosing. The solubility of erlotinib is pH dependent. Solubility decreases pH increases. Smoking also decrease the exposure of erlotinib. |
|---|---|
| Half-life | Median half-life of 36.2 hours. |
| Protein binding | 93% protein bound to albumin and alpha-1 acid glycoprotein (AAG) |
| Metabolism | Metabolism occurs in the liver. In vitro assays of cytochrome P450 metabolism showed that erlotinib is metabolized primarily by CYP3A4 and to a lesser extent by CYP1A2, and the extrahepatic isoform CYP1A1. |
| Route of elimination | Following a 100 mg oral dose, 91% of the dose was recovered in which 83% was in feces (1% of the dose as unchanged parent compound) and 8% in urine (0.3% of the dose as unchanged parent compound). |
| Volume of distribution | Apparent volume of distribution = 232 L |
| Clearance | Smokers have a 24% higher rate of erlotinib clearance. |
Formulation & handling
- Erlotinib is a small molecule API formulated for oral administration as film-coated tablets.
- Administer erlotinib on an empty stomach to avoid increased bioavailability and potential variability in drug exposure.
- Handle with consideration of CYP3A4 interactions, notably with grapefruit products and St. John's Wort, which can alter metabolism and serum levels.
Regulatory status
| Lifecycle | The API's key patents in Canada and the United States expired between 2015 and 2024, indicating that the product is in a mature market phase with established availability in Canada, the US, and the EU. Generic or alternative versions may be present in these regions. |
|---|
| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | Erlotinib is originally manufactured by a limited number of companies, with several packagers involved in its supply chain. The branded products have a significant presence across major markets including the US, EU, and Canada. Patent expirations, notably between 2019 and 2024 in the US and Canada, indicate that generic competition is either present or imminent in these regions. |
|---|
Safety
| Toxicity | Symptoms of overdose include diarrhea, rash, and liver transaminase elevation. The most common adverse reactions (>50%) in NSCLC are rash, diarrhea, anorexia and fatigue. The most common adverse reactions (>50%) in pancreatic cancer are fatigue, rash, nausea and anorexia. |
|---|
- Overdose may result in gastrointestinal disturbances, dermatologic reactions, and elevated hepatic transaminases
- Adverse effects with high incidence include rash, diarrhea, fatigue, anorexia, and nausea, varying by cancer indication
- Monitor for potential hepatotoxicity indicated by transaminase elevations during handling and formulation
Erlotinib 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.
Erlotinib (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.
Erlotinib API manufacturers & distributors
Compare qualified Erlotinib API suppliers worldwide. We currently have 21 companies offering Erlotinib API, with manufacturing taking place in 5 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 |
| Asymchem | Producer | China | China | CoA, USDMF | 10 products |
| Cipla | Producer | India | India | CoA, USDMF | 164 products |
| Fujian South Pharma | Producer | China | China | CoA, WC | 7 products |
| Gonane Pharma | Producer | India | India | BSE/TSE, CoA, GMP, MSDS | 166 products |
| Hetero Labs | Producer | India | India | CoA, GMP, USDMF, WC | 90 products |
| Intas Pharma | Producer | United Kingdom | Unknown | CoA, USDMF | 30 products |
| Kolon Life Science | Producer | South Korea | South Korea | CoA | 32 products |
| Laurus Labs | Producer | India | India | CoA, GMP, WC | 50 products |
| Mac Chem Products | Producer | India | India | CoA, GMP, WC | 25 products |
| MSN Labs. | Producer | India | India | CoA, USDMF | 119 products |
| Mylan | Producer | India | India | CoA, USDMF | 201 products |
| Natco Pharma | Producer | India | India | CoA, FDA, GMP, KDMF, USDMF, WC | 40 products |
| Qilu Antibiotics | Producer | China | China | CoA, USDMF, WC | 33 products |
| Reliance Life Sciences | Producer | India | India | CoA, USDMF, WC | 11 products |
| Rochem International, Inc... | Distributor | United States | United States | BSE/TSE, CoA, GMP, ISO9001, MSDS | 144 products |
| Senova Technology Co., Lt... | Producer | China | China | CoA, GMP, ISO9001, USDMF | 157 products |
| Shaoxing Hantai Pharma | Distributor | China | China | CoA | 162 products |
| Shilpa Medicare Ltd | Producer | India | India | BSE/TSE, CoA, EDMF/ASMF, GMP, ISO9001, MSDS, USDMF, WC | 54 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, ISO9001, USDMF | 757 products |
| Sun Pharma | Producer | India | India | CoA, USDMF | 219 products |
When sending a request, specify which Erlotinib 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 Erlotinib 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.
