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Icotinib | CAS No: 610798-31-7 | GMP-certified suppliers
A medication that provides targeted treatment for advanced non-small-cell lung cancer patients with EGFR mutations after chemotherapy failure, demonstrating efficacy and tolerability.
Therapeutic categories
Primary indications
- Icotinib hydrochloride is a novel epidermal growth factor receptor (EGFR)–tyrosine kinase inhibitor, exhibits encouraging efficacy and tolerability in patients with advanced non-small-cell lung cancer (NSCLC) who failed previous chemotherapy
Product Snapshot
- Icotinib is an oral small molecule tyrosine kinase inhibitor targeting EGFR
- It is primarily indicated for advanced non-small-cell lung cancer (NSCLC) after chemotherapy failure
- Icotinib is currently classified as an experimental and investigational agent with no finalized regulatory approvals
Clinical Overview
Pharmacodynamically, icotinib exhibits dose-dependent inhibition of EGFR kinase activity with an IC50 around 5 nanomolar, achieving complete inhibition at approximately 62.5 nanomolar concentrations in vitro. The compound selectively inhibits both wild-type and mutant EGFR variants with inhibition efficacies ranging from 61% to 99%. It disrupts EGFR-mediated intracellular tyrosine phosphorylation and demonstrates antiproliferative effects in multiple cancer cell lines, with pronounced sensitivity in EGFR-overexpressing cells such as A431. In vivo studies using xenograft mouse models have confirmed dose-dependent antitumor activity at doses up to 120 mg/kg/day, which were well tolerated without significant toxicity or weight loss.
Mechanistically, icotinib reversibly binds to the ATP-binding site of the EGFR tyrosine kinase domain, inhibiting receptor autophosphorylation and downstream signaling pathways that control cell proliferation and survival. This action is particularly effective in tumors harboring activating mutations such as exon 19 deletions or exon 21 L858R substitutions.
Icotinib underwent regulatory approval in China in 2011 and has been evaluated in clinical trials including a phase III, randomized, controlled study comparing it to gefitinib in advanced NSCLC. It is classified as a substrate and inducer of various cytochrome P450 enzymes including CYP1A2, CYP3A4, and CYP3A5, indicating a potential for drug–drug interactions that require careful consideration during formulation and clinical use.
From an API sourcing perspective, ensuring pharmaceutical-grade purity with consistent potency is essential due to the molecule’s specific binding requirements and narrow therapeutic index. Compliance with current good manufacturing practices (cGMP) and robust analytical characterization, including impurity profiling within regulatory limits, are critical for supporting downstream pharmaceutical development and regulatory submissions.
Identification & chemistry
| Generic name | Icotinib |
|---|---|
| Molecule type | Small molecule |
| CAS | 610798-31-7 |
| UNII | 9G6U5L461Q |
| DrugBank ID | DB11737 |
Pharmacology
| Summary | Icotinib is a selective first-generation tyrosine kinase inhibitor targeting the epidermal growth factor receptor (EGFR), including wild-type and activating mutations commonly found in non-small-cell lung cancer (NSCLC). It reversibly binds to the ATP binding site of EGFR, inhibiting receptor autophosphorylation and downstream signal transduction, thereby reducing tumor cell proliferation. Preclinical studies demonstrate dose-dependent inhibition of EGFR activity and antitumor effects across multiple cancer cell lines and xenograft models. |
|---|---|
| Mechanism of action | Icotinib is a highly selective, first generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) which binds reversibly to the ATP binding site of the EGFR protein, preventing completion of the signal transduction cascade. EGFR is an oncogenic receptor and patients with activating somatic mutations, such as an exon 19 deletion or exon 21 L858R mutation, within the tyrosine kinase domain display unchecked cell proliferation. |
| Pharmacodynamics | In vitro: Icotinib inhibits EGFR activity in a dose-dependent manner, with an IC50 value of 5 nM and complete inhibition at 62.5 nM. Icotinib selectively solely inhibits the EGFR members including the wild type and mutants with inhibition efficacies of 61-99%. Icotinib blocks EGFR-mediated intracellular tyrosine phosphorylation in human epidermoid carcinoma A431 cells in a dose-dependent manner. Meanwhile, in the proliferation assay performed on A431, BGC-823, A549, H460, HCT8, KB and Bel-7402 cell lines, it was found that the relative sensitivity of cell lines to Icotinib is A431 > BGC-823 > A549 > H460 > KB > HCT8 and Bel-7402. Icotinib exhibits a broad spectrum of antitumor activity and it is especially effective against tumors expressing higher levels of EGFR. In vivo: In vivo studies demonstrated that Icotinib exhibited potent dose-dependent antitumor effects in nude mice carrying a variety of human tumor-derived xenografts. The drug was well tolerated at doses up to 120 mg/kg/day in mice without mortality or significant body weight loss during the treatment. A head to head randomized, double blind phase III trial using Gefitinib as an active control for patients with advanced non-small cell lung cancer (NSCLC) was finished recently (Trial registration ID: NCT01040780). |
Targets
| Target | Organism | Actions |
|---|---|---|
| Epidermal growth factor receptor | Humans | antagonist |
ADME / PK
| Absorption | Bioavailability = 52% |
|---|---|
| Half-life | 5.5 hrs |
| Protein binding | Icotinib binds to Sudlow's site I in subdomain IIA of Human Serum Albumin (HSA) molecule, resulting in the formation of icotinib-HSA complexes. |
| Metabolism | Hepatic (mainly CYP3A4, less CYP1A2) |
| Route of elimination | >90% via faeces, 9% via urine |
| Volume of distribution | the volume of distribution was calculated as Vz/F = 115.00 ± 63.26 l |
| Clearance | the clearance was calculated as CL/F = 13.30 ± 4.78 l/h |
Formulation & handling
- Icotinib is a small molecule with low water solubility, suitable primarily for oral administration.
- Its moderate lipophilicity (LogP 3.03) suggests formulation strategies should address bioavailability and solubility enhancement.
- Stability and handling must consider its quinazolinamine structure, avoiding conditions that promote degradation or amine group modification.
Regulatory status
Safety
| Toxicity | The most common toxicities reported are skin-related events and diarrhea. |
|---|
- Handle with appropriate personal protective equipment to minimize skin exposure due to reported dermal toxicity
- Use in well-ventilated areas to reduce risk of gastrointestinal irritation associated with incidental inhalation or ingestion
- Avoid prolonged or repeated exposure to prevent potential cumulative adverse skin effects
Clopamide is a type of Diuretics
Diuretics, a subcategory of pharmaceutical active pharmaceutical ingredients (APIs), are compounds commonly used in the treatment of conditions such as hypertension, congestive heart failure, and edema. Diuretics, also known as water pills, function by increasing the production of urine, thereby promoting the excretion of excess water and electrolytes from the body.
There are several types of diuretics, including thiazide diuretics, loop diuretics, and potassium-sparing diuretics. Thiazide diuretics, such as hydrochlorothiazide, work by inhibiting the reabsorption of sodium and chloride in the kidneys, leading to increased urine production. Loop diuretics, such as furosemide, act on the loop of Henle in the kidneys to block the reabsorption of sodium and chloride, resulting in a more potent diuretic effect. Potassium-sparing diuretics, like spironolactone, help retain potassium in the body while still promoting diuresis.
These diuretic APIs are widely used in the pharmaceutical industry to formulate medications that effectively manage fluid retention and related conditions. They are available in various forms, including tablets, capsules, and intravenous formulations. Diuretics are often prescribed as part of combination therapies to enhance their effectiveness and minimize adverse effects.
It is important to note that the use of diuretics should be closely monitored by healthcare professionals due to potential side effects such as electrolyte imbalances, dehydration, and hypotension. Proper dosage and patient-specific considerations are crucial to ensure optimal therapeutic outcomes.
In conclusion, diuretics are a vital subcategory of pharmaceutical APIs used to treat conditions characterized by fluid retention. Their mechanisms of action vary, but they all facilitate increased urine production, assisting the body in eliminating excess fluids. The proper use of diuretics, in combination with medical supervision, can effectively manage various cardiovascular and renal conditions.
Clopamide (Diuretics), classified under Antihypertensive agents
Antihypertensive agents are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) used to treat high blood pressure, also known as hypertension. These medications are designed to lower blood pressure and reduce the risk of associated cardiovascular complications.
Antihypertensive agents function by targeting various mechanisms involved in blood pressure regulation. Some common classes of antihypertensive agents include angiotensin-converting enzyme (ACE) inhibitors, angiotensin II receptor blockers (ARBs), beta-blockers, calcium channel blockers (CCBs), and diuretics.
ACE inhibitors work by inhibiting the enzyme responsible for converting angiotensin I to angiotensin II, a hormone that constricts blood vessels. ARBs, on the other hand, block the receptors to which angiotensin II binds, thereby preventing its vasoconstrictive effects.
Beta-blockers reduce blood pressure by blocking the effects of adrenaline and noradrenaline, which are responsible for increasing heart rate and constricting blood vessels. CCBs inhibit calcium from entering the smooth muscles of blood vessels, resulting in relaxation and vasodilation. Diuretics promote the elimination of excess fluid and sodium from the body, reducing blood volume and thereby lowering blood pressure.
Antihypertensive agents are typically prescribed based on the individual patient's condition and specific needs. They can be used alone or in combination to achieve optimal blood pressure control. It is important to note that antihypertensive agents should be taken regularly as prescribed by a healthcare professional and may require periodic monitoring to ensure their effectiveness and manage any potential side effects.
In summary, antihypertensive agents play a vital role in the management of hypertension by targeting various mechanisms involved in blood pressure regulation. These medications offer significant benefits in reducing the risk of cardiovascular complications associated with high blood pressure.
Clopamide API manufacturers & distributors
Compare qualified Clopamide API suppliers worldwide. We currently have 1 companies offering Clopamide API, with manufacturing taking place in 1 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 |
|---|---|---|---|---|---|
| Polpharma | Producer | Poland | Poland | BSE/TSE, CoA, EDMF/ASMF, FDA, GMP, MSDS | 64 products |
When sending a request, specify which Clopamide 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.).
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