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Lapatinib | CAS No: 231277-92-2 | GMP-certified suppliers
A medication that treats HER2-positive advanced or metastatic breast cancer by targeting tumor growth in patients previously treated with multiple therapies, supporting oncology use in major markets.
Therapeutic categories
Primary indications
- Indicated in combination with capecitabine for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress the human epidermal receptor type 2 (HER2) protein and who have received prior therapy including an anthracycline, a taxane, and trastuzumab
Product Snapshot
- Lapatinib is an oral small molecule available in film-coated tablet form
- It is primarily used in the treatment of advanced or metastatic HER2-positive breast cancer
- The product is approved and marketed in regulatory regions including the US, Canada, and the EU
Clinical Overview
Pharmacologically, lapatinib belongs to the 4-anilinoquinazoline class of kinase inhibitors. It exerts its antineoplastic activity by selectively targeting the intracellular tyrosine kinase domains of both HER2 (ERBB2) and epidermal growth factor receptor (EGFR/HER1/ERBB1). Lapatinib binds with high affinity to the ATP-binding site within these receptor kinases, preventing receptor autophosphorylation and subsequent activation of downstream signaling pathways that promote tumor cell proliferation and survival. This dual inhibition contributes to its effectiveness against HER2-driven malignancies.
Key absorption, distribution, metabolism, and excretion (ADME) parameters include hepatic metabolism predominantly via cytochrome P450 enzymes CYP3A4/5 and CYP2C19. Lapatinib acts as both a substrate and inhibitor of several CYP450 isoforms, notably CYP3A4 and CYP2C8, which has implications for potential drug-drug interactions. It also shows inhibitory activity against P-glycoprotein, which may affect its disposition and that of co-administered drugs. Due to its enzyme inhibition profile, lapatinib may prolong QTc interval, necessitating monitoring in susceptible patients.
Safety considerations include hepatotoxicity and cardiac effects. Liver function tests and electrocardiographic monitoring are recommended during treatment. Common adverse events relate to gastrointestinal disturbances, rash, and fatigue. Importantly, lapatinib displays non-cross-resistance with trastuzumab, making it an option following trastuzumab therapy failure.
Among marketed formulations, lapatinib is available under brand names such as Tykerb (US) and Tyverb (EU). Its use extends primarily within oncology settings focusing on HER2-positive breast cancer, although investigational applications include other solid tumors expressing relevant receptor targets.
From an API sourcing perspective, quality control must emphasize the compound’s structural integrity as a quinazolinamine derivative and consistent assay of purity to meet pharmacopeial standards. Given its complex metabolism and the importance of minimizing impurities that could exacerbate toxicity, manufacturers should ensure robust control of residual solvents, polymorphic form, and stability. Compatibility with formulation excipients and thorough documentation of synthetic routes support regulatory compliance and reliable supply.
Identification & chemistry
| Generic name | Lapatinib |
|---|---|
| Molecule type | Small molecule |
| CAS | 231277-92-2 |
| UNII | 0VUA21238F |
| DrugBank ID | DB01259 |
Pharmacology
| Summary | Lapatinib is a small molecule kinase inhibitor targeting the intracellular tyrosine kinase domains of both EGFR (HER1/ERBB1) and HER2 (ERBB2). It inhibits ERBB-driven tumor cell proliferation by blocking receptor phosphorylation and downstream signaling pathways. Lapatinib demonstrates activity against HER2-overexpressing tumors, including those resistant to trastuzumab, and is used in combination with capecitabine for advanced breast cancer. |
|---|---|
| Mechanism of action | Lapatinib is a 4-anilinoquinazoline kinase inhibitor of the intracellular tyrosine kinase domains of both epidermal growth factor receptor (HER1/EGFR/ERBB1) and human epidermal growth factor receptor type 2 (HER2/ERBB2)with a dissociation half-life of ≥300 minutes. Lapatinib inhibits ERBB-driven tumor cell growth in vitro and in various animal models. An additive effect was demonstrated in an in vitro study when lapatinib and 5-florouracil (the active metabolite of capecitabine) were used in combination in the 4 tumor cell lines tested. The growth inhibitory effects of lapatinib were evaluated in trastuzumab-conditioned cell lines. Lapatinib retained significant activity against breast cancer cell lines selected for long-term growth in trastuzumab-containing medium in vitro. These in vitro findings suggest non-cross-resistance between these two agents. |
| Pharmacodynamics | Lapatinib is a small molecule and a member of the 4-anilinoquinazoline class of kinase inhibitors. An anti-cancer drug, lapatinib was developed by GlaxoSmithKline (GSK) as a treatment for solid tumours such as breast and lung cancer. It was approved by the FDA on March 13, 2007, for use in patients with advanced metastatic breast cancer in conjunction with the chemotherapy drug capecitabine. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Epidermal growth factor receptor | Humans | antagonist |
| Receptor tyrosine-protein kinase erbB-2 | Humans | antagonist |
ADME / PK
| Absorption | Absorption following oral administration of lapatinib is incomplete and variable. |
|---|---|
| Half-life | Single-dose terminal half life: 14.2 hours Effective multiple-dose half life: 24 hours |
| Protein binding | Highly bound (>99%) to albumin and alpha-1 acid glycoprotein |
| Metabolism | Lapatinib undergoes extensive metabolism, primarily by CYP3A4 and CYP3A5, with minor contributions from CYP2C19 and CYP2C8 to a variety of oxidated metabolites, none of which accounts for more than 14% of the dose recovered in the feces or 10% of lapatinib concentration in plasma. |
| Route of elimination | Lapatinib undergoes extensive metabolism, primarily by CYP3A4 and CYP3A5, with minor contributions from CYP2C19 and CYP2C8 to a variety of oxidated metabolites, none of which accounts for more than 14% of the dose recovered in the feces or 10% of lapatinib concentration in plasma. |
Formulation & handling
- Lapatinib is a small molecule API formulated exclusively for oral administration in tablet form.
- Due to its low water solubility and high lipophilicity (LogP 4.64), formulation strategies should address dissolution enhancement for bioavailability.
- Avoid co-administration with grapefruit products and advise dosing at least 1 hour before or after meals to minimize food effects on metabolism and absorption.
Regulatory status
| Lifecycle | The API's primary patents have expired between 2017 and 2021 in the US and Canada, indicating a mature market with potential generic competition in these regions; patent status in the EU suggests similar market conditions. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Lapatinib is originally manufactured by a single originator company with branded products available in the US, Canada, and EU markets under multiple brand names. Several patents have expired between 2017 and 2021 across these regions, indicating the presence of or potential for generic competition in these markets. |
|---|
Safety
| Toxicity | There has been a report of one patient who took 3,000 mg of lapatinib for 10 days. This patient had grade 3 diarrhea and vomiting on day 10. |
|---|
- Exposure to lapatinib may cause gastrointestinal irritation, evidenced by reports of grade 3 diarrhea and vomiting at high dosages
- Handle with appropriate protective measures to minimize risk of mucosal or dermal irritation
- Use under controlled conditions to prevent inadvertent overexposure due to its potential toxicity at elevated doses
Lapatinib 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.
Lapatinib (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.
Lapatinib API manufacturers & distributors
Compare qualified Lapatinib API suppliers worldwide. We currently have 7 companies offering Lapatinib 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 |
| ALP PHARM | Producer | China | China | CoA, USDMF | 33 products |
| Formosa Labs | Producer | Taiwan | Taiwan | CoA, USDMF | 36 products |
| Hetero Labs | Producer | India | India | CoA, USDMF | 90 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Minakem | Producer | France | Canada | BSE/TSE, CoA, FDA, GMP, MSDS, USDMF | 31 products |
| Senova Technology Co., Lt... | Producer | China | China | CoA, GMP, ISO9001, USDMF | 157 products |
When sending a request, specify which Lapatinib 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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