药品详细
Erlotinib (厄洛替尼 )
化学结构式图
中文名
厄洛替尼
英文名
Erlotinib
分子式
Not Available
化学名
N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine
分子量
Average: 393.4357
Monoisotopic: 393.168856239
Monoisotopic: 393.168856239
CAS号
183321-74-6
ATC分类
L01X 其它抗肿瘤药
药物类型
small molecule
阶段
商品名
Tarceva;
同义名
erlotinib;OSI-774;
基本介绍
Erlotinib hydrochloride (trade name Tarceva, Genentech/OSIP, originally coded as OSI-774) is a drug used to treat non-small cell lung cancer, pancreatic cancer and several other types of cancer.
Similar to gefitinib, erlotinib specifically targets the epidermal growth factor receptor (EGFR) tyrosine kinase. It binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor. Erlotinib has recently been shown to be a potent inhibitor of JAK2V617F activity. JAK2V617F is a mutant of tyrosine kinase JAK2, is found in most patients with polycythemia vera (PV) and a substantial proportion of patients with idiopathic myelofibrosis or essential thrombocythemia. The study suggests that erlotinib may be used for treatment of JAK2V617F-positive PV and other myeloproliferative disorders.
生产厂家
- Osi pharmaceuticals inc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference |
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剂型
| Form | Route | Strength |
|---|---|---|
| Tablet | Oral |
规格
| Unit description | Cost | Unit |
|---|---|---|
| Tarceva 150 mg tablet | 163.98 USD | tablet |
| Tarceva 100 mg tablet | 144.98 USD | tablet |
| Tarceva 25 mg tablet | 52.78 USD | tablet |
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
Cancer 癌症;
药理
| Indication | For the treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of at least one prior chemotherapy regimen. Also for use, in combination with gemcitabine, as the first-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer. | ||||||
| Pharmacodynamics | Erlotinib is a Human Epidermal Growth Factor Receptor Type 1/Epidermal Growth Factor Receptor (HER1/EGFR) tyrosine kinase inhibitor. | ||||||
| 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. | ||||||
| Absorption | Erlotinib is about 60% absorbed after oral administration and its bioavailability is substantially increased by food to almost 100%. | ||||||
| Volume of distribution | Not Available | ||||||
| Protein binding | 93% protein bound to albumin and alpha-1 acid glycoprotein (AAG) | ||||||
| Metabolism |
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. |
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| Route of elimination | Not Available | ||||||
| Half life | Median half-life of 36.2 hours. | ||||||
| Clearance | Not Available | ||||||
| Toxicity | Symptoms of overdose include diarrhea, rash, and liver transaminase elevation. | ||||||
| Affected organisms |
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| Pathways |
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理化性质
| Properties | |||||||||||||||||||||||||||||||||||||
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| State | solid | ||||||||||||||||||||||||||||||||||||
| Melting point | Not Available | ||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Atazanavir | This CYP3A4 inhibitor increases levels/toxicity of erlotinib |
| Clarithromycin | This CYP3A4 inhibitor increases levels/toxicity of erlotinib |
| Erythromycin | This CYP3A4 inhibitor increases levels/toxicity of erlotinib |
| Indinavir | This CYP3A4 inhibitor increases levels/toxicity of erlotinib |
| Itraconazole | Itraconazole may decrease the metabolism of erlotinib. Monitor for changes in the therapeutic and adverse effects of erlotinib if itraconazole is initiated, discontinued or dose changed. |
| Ketoconazole | This CYP3A4 inhibitor increases levels/toxicity of erlotinib |
| Nefazodone | This CYP3A4 inhibitor increases levels/toxicity of erlotinib |
| Nelfinavir | This CYP3A4 inhibitor increases levels/toxicity of erlotinib |
| Rifabutin | Decreased levels/effect of erlotinib |
| Rifampin | Decreased levels/effect of erlotinib |
| Rifapentine | Decreased levels/effect of erlotinib |
| Ritonavir | This CYP3A4 inhibitor increases levels/toxicity of erlotinib |
| Saquinavir | This CYP3A4 inhibitor increases levels/toxicity of erlotinib |
| St. John's Wort | Decreased levels/effect of erlotinib |
| Telithromycin | Telithromycin may reduce clearance of Erlotinib. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Erlotinib if Telithromycin is initiated, discontinued or dose changed. |
| Trastuzumab | Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events. |
| Troleandomycin | This CYP3A4 inhibitor increases levels/toxicity of erlotinib |
| Voriconazole | Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of erlotinib by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of erlotinib if voriconazole is initiated, discontinued or dose changed. |
食物相互作用
- Take at least 1 hour before or 2 hours after any food.
- Take with a glass of water.
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