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Osimertinib | CAS No: 1421373-65-0 | GMP-certified suppliers
A medication that supports treatment of resected or metastatic EGFR‑mutated non‑small cell lung cancer, including cases progressing after earlier targeted therapies.
Therapeutic categories
Primary indications
- Osimertinib is indicated as adjuvant therapy after tumor resection in adult patients with non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R mutations (as detected by an FDA-approved test), and as the first-line treatment of adult patients with metastatic NSCLC whose tumors have EGFR exon 19 deletions or exon 21 L858R mutations (as detected by an FDA-approved test)
- Osimertinib is also indicated for the treatment of adult patients with metastatic EGFR T790M mutation-positive NSCLC, as detected by an FDA-approved test, whose disease has progressed on or after EGFR TKI therapy
Product Snapshot
- Osimertinib is an oral small‑molecule tablet formulation
- Its primary use is for EGFR‑mutation–positive non‑small cell lung cancer across adjuvant, first‑line metastatic, and T790M‑positive post‑TKI settings
- It is approved in major regulatory markets including the US, EU, and Canada
Clinical Overview
The compound belongs to the n‑alkylindole class and was developed to address resistance arising during treatment with earlier EGFR TKIs. First‑generation agents frequently encounter the T790M gatekeeper mutation, while second‑generation agents demonstrate broader EGFR inhibition with increased toxicity. Osimertinib selectively targets mutant EGFR variants including T790M, L858R, and exon 19 deletions, while sparing wild‑type EGFR. In vitro data show substantially higher affinity for L858R/T790M double‑mutant receptors compared with wild type.
Pharmacologically, osimertinib covalently binds mutant EGFR, suppressing downstream signaling pathways that regulate cellular proliferation and survival in NSCLC. A pharmacokinetic and pharmacodynamic analysis indicates a concentration‑dependent QTc prolongation of approximately 14 msec at the approved 80 mg dose, which informs clinical monitoring practices.
Absorption, distribution, metabolism, and elimination characteristics are defined by its role as both a substrate and modulator of CYP3A pathways and transporter systems such as BCRP and P‑glycoprotein. These properties create potential for clinically relevant drug interactions and support its classification as a narrow‑therapeutic‑index kinase inhibitor.
Commonly recognized brand use includes contexts where osimertinib is supplied as an oral targeted therapy for EGFR‑mutated NSCLC.
For API procurement, suppliers should document impurity profiles, control of stereochemistry and covalent‑binding related intermediates, and full compliance with ICH quality standards to ensure consistent performance in formulation and regulatory submissions.
Identification & chemistry
| Generic name | Osimertinib |
|---|---|
| Molecule type | Small molecule |
| CAS | 1421373-65-0 |
| UNII | 3C06JJ0Z2O |
| DrugBank ID | DB09330 |
Pharmacology
| Summary | Osimertinib is a third‑generation EGFR tyrosine kinase inhibitor that targets mutant EGFR variants, including T790M, L858R, and exon 19 deletions, which drive a subset of non‑small cell lung cancers. It exhibits high selectivity for these mutant receptors while sparing wild‑type EGFR, supporting mutation‑directed inhibition of signaling pathways involved in tumor growth. At therapeutic concentrations, it is associated with a measurable, concentration‑dependent QTc prolongation. |
|---|---|
| Mechanism of action | Osimertinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that binds to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletion) that predominate in non-small cell lung cancer (NSCLC) tumours following treatment with first-line EGFR-TKIs.As a third-generation tyrosine kinase inhibitor, osimertinib is specific for the gate-keeper T790M mutation which increases ATP binding activity to EGFR and results in poor prognosis for late-stage disease. Furthermore, osimertinib has been shown to spare wild-type EGFR during therapy, thereby reducing non-specific binding and limiting toxicity.Compared to wild-type EGFR, osimertinib has 200 times higher affinity for EGFR molecules with the L858R/T790M mutation _in vitro_. |
| Pharmacodynamics | A pharmacokinetic/pharmacodynamic analysis suggested a concentration-dependent QTc interval prolongation of 14 msec (upper bound of two-sided 90% CI: 16 msec) at a dose of osimertinib 80 mg. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Epidermal growth factor receptor | Humans | inhibitor, regulator |
ADME / PK
| Absorption | The median time to Cmax was found to be 6 hours. |
|---|---|
| Half-life | The population estimated mean half-life is 48 hours. |
| Protein binding | Plasma protein binding of osimertinib is 95%. |
| Metabolism | Osimertinib is metabolized to at least two pharmacologically active metabolites, AZ7550 and AZ5104, that circulate at approximately 10% of the concentration of the parent compound. Biochemical assays have shown that AZ7550 has similar potency and efficacy to osimertinib, while AZ5104 is more potent against mutant and wild-type EGFR. The main metabolic pathways are oxidation (predominantly by CYP3A) and dealkylation. |
| Route of elimination | Osimertinib is primarily eliminated through excretion in the feces (68%), to a lesser extent through urine (14%), while only 2% is excreted unchanged. |
| Volume of distribution | The mean volume of distribution at steady state is 918 L. |
| Clearance | Oral clearance is 14.3 L/hr. |
Formulation & handling
- Solid, poorly water‑soluble small molecule formulated as oral tablets; high LogP may require solubilization or dispersion strategies for consistent absorption.
- Oral administration is not food‑dependent, but excipient selection should support dissolution across fed and fasted states.
- Metabolism is CYP3A‑mediated; formulations and handling should avoid co‑exposure to strong CYP3A inducers such as St. John’s wort during evaluation.
Regulatory status
| Lifecycle | US patents extending from 2032 to 2035 indicate that the API remains in a protected phase of its lifecycle, with limited generic competition expected in the near term. Current availability across Canada, the US, and the EU reflects a mature, actively marketed product in major regulated markets. |
|---|
| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | Osimertinib is supplied primarily by a single originator, reflected by the consistent branding of Tagrisso across available markets. The product has established global availability in the US, EU, and Canada. US patents extending into 2032–2035 indicate that generic competition is unlikely until the next decade. |
|---|
Safety
| Toxicity | Across clinical trials, interstitial lung disease (ILD)/pneumonitis occurred in 3.7% of treated patients with 0.3% of these being fatal. There is also a change of QTc interval prolongation; electrocardiogram and electrolytes should be monitored in patients with a history or predisposition for QTc prolongation. Cardiomyopathy occurred in 3% of patients, therefore left ventricular ejection fraction (LVEF) should be measured at baseline and during treatment. Osimertinib can cause embryo-fetal toxicity, requiring female patients to take effective birth control during therapy and for 6 weeks after final dose. |
|---|
- Associated with interstitial lung disease/pneumonitis in clinical settings
- Handle with controls that limit inhalation exposure to mitigate respiratory hazard potential
- Demonstrates QTc‑prolonging and cardiotoxic liabilities, indicating relevance for workflows sensitive to compounds with electrophysiologic or myocardial risk profiles
Osimertinib 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.
Osimertinib (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.
Osimertinib API manufacturers & distributors
Compare qualified Osimertinib API suppliers worldwide. We currently have 6 companies offering Osimertinib 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 |
|---|---|---|---|---|---|
| Apino Pharma Co., Ltd. | Producer | China | China | BSE/TSE, CoA, ISO9001, MSDS | 229 products |
| MSN Labs. | Producer | India | India | CoA, USDMF | 119 products |
| R&S Chemicals | Producer | United States | United States | CoA | 2 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Shandong Boyuan | Producer | China | China | BSE/TSE, CoA, MSDS | 55 products |
| Tianjin Pharmacn Medical ... | Producer | China | China | BSE/TSE, CoA, GMP, MSDS | 66 products |
When sending a request, specify which Osimertinib 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 Osimertinib 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.
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Technical
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Regulatory
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