药品详细
Gemcitabine (吉西他滨 )
化学结构式图
中文名
吉西他滨
英文名
Gemcitabine
分子式
Not Available
化学名
4-amino-1-[(2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-1,2-dihydropyrimidin-2-one
分子量
Average: 263.1981
Monoisotopic: 263.071762265
Monoisotopic: 263.071762265
CAS号
95058-81-4
ATC分类
L01B 抗代谢药
药物类型
small molecule
阶段
商品名
DDFC;DFDC;Gemcin;Gemcitabina [INN-Spanish];Gemcitabine HCl;Gemcitabine hydrochloride;Gemcitabinum [INN-Latin];Gemtro;Gemzar;GEO;
同义名
基本介绍
Gemcitabine is a nucleoside analog used as chemotherapy. It is marketed as Gemzar® by Eli Lilly and Company. As with fluorouracil and other analogues of pyrimidines, the drug replaces one of the building blocks of nucleic acids, in this case cytidine, during DNA replication. The process arrests tumor growth, as new nucleosides cannot be attached to the “faulty” nucleoside, resulting in apoptosis (cellular “suicide”).
Gemcitabine is used in various carcinomas: non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer. It is being investigated for use in oesophageal cancer, and is used experimentally in lymphomas and various other tumor types.
生产厂家
- Eli lilly and co
- Teva parenteral medicines inc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference |
剂型
| Form | Route | Strength |
|---|---|---|
| Powder, for solution | Intravenous |
规格
| Unit description | Cost | Unit |
|---|---|---|
| Gemzar 1 gm Solution Vial | 903.93 USD | vial |
| Gemzar 1 gram vial | 869.16 USD | vial |
| Gemzar 200 mg Solution Vial | 180.78 USD | vial |
化合物类型
| Type | small molecule |
| Classes |
|
| Substructures |
|
适应症
Cancer 癌症;
药理
| Indication | For the first-line treatment of patients with metastatic breast cancer, locally advanced (Stage IIIA or IIIB), or metastatic (Stage IV) non-small cell lung cancer and as first-line treatment for patients with adenocarcinoma of the pancreas. | ||||||
| Pharmacodynamics | Gemcitabine is an antineoplastic anti-metabolite. Anti-metabolites masquerade as purine or pyrimidine - which become the building blocks of DNA. They prevent these substances becoming incorporated in to DNA during the "S" phase (or DNA synthesis phase of the cell cycle), stopping normal development and division. Gemcitabine blocks an enzyme which converts the cytosine nucleotide into the deoxy derivative. In addition, DNA synthesis is further inhibited because Gemcitabine blocks the incorporation of the thymidine nucleotide into the DNA strand. | ||||||
| Mechanism of action | Gemcitabine inhibits thymidylate synthetase, leading to inhibition of DNA synthesis and cell death. Gemcitabine is a prodrug so activity occurs as a result of intracellular conversion to two active metabolites, gemcitabine diphosphate and gemcitabine triphosphate by deoxycitidine kinase. Gemcitabine diphosphate also inhibits ribonucleotide reductase, the enzyme responsible for catalyzing synthesis of deoxynucleoside triphosphates required for DNA synthesis. Finally, Gemcitabine triphosphate (diflurorodeoxycytidine triphosphate) competes with endogenous deoxynucleoside triphosphates for incorporation into DNA. | ||||||
| Absorption | 100% | ||||||
| Volume of distribution |
|
||||||
| Protein binding | Plasma protein binding is negligible (<10%) | ||||||
| Metabolism |
Transformed via nucleoside kinases to two active metabolites, gemcitabine diphosphate and gemcitabine triphosphate. Can also undergo deamination via cytidine deaminase to an inactive uracil metabolite (dFdU). |
||||||
| Route of elimination | Not Available | ||||||
| Half life | Short infusions ranged from 32 to 94 minutes, and the value for long infusions vary from 245 to 638 minutes, depending on age and gender. | ||||||
| Clearance |
|
||||||
| Toxicity | Myelosuppression, paresthesias, and severe rash were the principal toxicities, LD50=500 mg/kg (orally in mice and rats) | ||||||
| Affected organisms |
|
||||||
| Pathways |
|
理化性质
| Properties | |||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| State | solid | ||||||||||||||||||||||||||||||||||||
| Melting point | 168.64oC | ||||||||||||||||||||||||||||||||||||
| Experimental Properties |
|
||||||||||||||||||||||||||||||||||||
| Predicted Properties |
|
||||||||||||||||||||||||||||||||||||
药物相互作用
| Drug | Interaction |
|---|---|
| Acenocoumarol | Gemcitabine may increase the anticoagulant effect of acenocoumarol. |
| Anisindione | Gemcitabine may increase the anticoagulant effect of anisindione. |
| Dicumarol | Gemcitabine may increase the anticoagulant effect of dicumarol. |
| Paclitaxel | Paclitaxel increases the effect/toxicity of gemcitabine |
| Temsirolimus | Co-administration of Temsirolimus and Gemcitabine may result in serious adverse drug reactions. |
| Trastuzumab | Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events. |
| Warfarin | Gemcitabine may increase the anticoagulant effect of warfarin. |
食物相互作用
Not Available
收藏