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Docetaxel

Indications and Usage Mechanisms of Action Pharmacokinetics Clinical Research Drug Interactions Adverse Reactions Contradictions Precautions
Docetaxel
Docetaxel
CAS No.
114977-28-5
Chemical Name:
Docetaxel
Synonyms
rp56976;TAXOTERE;Docetere;BIND-014;Decetaxel;Docetaxel;NSC_628503;Taxotere(R);DOCETAXEL(P);Docetaxel9.5%
CBNumber:
CB1163212
Molecular Formula:
C43H53NO14
Formula Weight:
807.88
MOL File:
114977-28-5.mol

Docetaxel Properties

Melting point:
186-192 °C (dec.)
alpha 
-36 º (c=0.74,EtOH)
Density 
1.38
storage temp. 
Store at +4°C
Water Solubility 
Soluble in dimethyl sulfoxide and ethanol. Insoluble in water.
Merck 
14,3397
InChIKey
BEDLLNJKXXVTSX-LWWLJZAUSA-N
CAS DataBase Reference
114977-28-5(CAS DataBase Reference)
SAFETY
  • Risk and Safety Statements
  • Hazard and Precautionary Statements (GHS)
Hazard Codes  Xi
Risk Statements  36/37/38-61
Safety Statements  26-36/37-53-45
RIDADR  1544
RTECS  DA4172750
HazardClass  6.1(b)
PackingGroup  III
HS Code  29322090
Hazardous Substances Data 114977-28-5(Hazardous Substances Data)
Symbol(GHS):
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H361 Suspected of damaging fertility or the unborn child Reproductive toxicity Category 2 Warning P201, P202, P281, P308+P313, P405,P501
Precautionary statements:
P201 Obtain special instructions before use.
P202 Do not handle until all safety precautions have been read and understood.
P280 Wear protective gloves/protective clothing/eye protection/face protection.
P308+P313 IF exposed or concerned: Get medical advice/attention.
P405 Store locked up.
P501 Dispose of contents/container to..…

Docetaxel price More Price(12)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich 01885 Docetaxel purum, ≥97.0% (HPLC) 114977-28-5 5mg-f $191.5 2017-11-08 Buy
Sigma-Aldrich 01885 Docetaxel purum, ≥97.0% (HPLC) 114977-28-5 25mg-f $659 2017-11-08 Buy
TCI Chemical D4102 Docetaxel >98.0%(HPLC) 114977-28-5 1g $635 2017-11-08 Buy
TCI Chemical D4102 Docetaxel >98.0%(HPLC) 114977-28-5 100mg $127 2017-11-08 Buy
Alfa Aesar J60174 Docetaxel, 99% 114977-28-5 100mg $153 2017-11-08 Buy

Docetaxel Chemical Properties,Uses,Production

Indications and Usage

Docetaxel is a taxane, antineoplastic, and anticancer drug used to treat locally advanced or metastatic breast cancer, even after the failure of cisplatin therapy. Its anti-tumor efficacy has been proven in in vitro tests to be 1.3-12 times that of paclitaxel. Clinical studies have shown that it is more effective than paclitaxel against anthracycline resistant breast cancer. Docetaxel is currently the most effective for the second-line treatment of anthracycline resistant breast cancer. In single cell therapy and combined chemotherapy for non-small cell lung cancer, it is one of the most effective drugs. It can be used for cancer of the uterus, and to study antibiotics, cell biology, cell signaling, neuroscience, apoptosis, and cell cycles. It is also used to study hair loss caused by docetaxel chemotherapy, and to prevent and treat small-cell lung cancer in patients contraindicated for chemotherapy. It is also used to investigate the roles of hypoxia-inducible factors-1α and 2α in androgen-insensitive prostate cancer cells.

Mechanisms of Action

Docetaxel promotes microtubule stabilization by promoting the assembly of microtubule dimers into microtubules, and preventing depolymerization, thus blocking cells in the G2 and M stages, and inhibiting the mitosis and proliferation of cancer cells. Its pharmacological effects are stronger than those of paclitaxel, with 3 times the intracellular concentration and long retention time within the cell, and twice the microtubule affinity; As a microtubule stabilizer and assembly promoter, its activity is twice that of paclitaxel; as a microtubule depolymerization inhibitor, its activity is also twice that of paclitaxel.

Pharmacokinetics

In a pharmacokinetic study in which cancer patients took 20-115 mg/m2, when the dose was 75-115 mg/m2 over a 1-2 hour intravenous drip, AUC was correlated with dose. Its pharmacokinetic characteristics conform to a three-compartmental pharmacokinetic model, with α, β, and γ half-lives of 4, 36, and 11.1 hours respectively. The concentration of the initial phase decreased rapidly, indicating that the drug was distributed to the peripheral compartment. The latter phase is partly due to the relatively slow elimination of the drug from the compartment. Within an hour of intravenous infusion of 100 mg/m2 of paclitaxel, the average peak was 3.7 ug/ml, AUC was 4.6 ug/ml•h, and total clearance and steady-state distribution were 21 L/h/m2 and 113 L. In vitro studies have shown that it has a plasma protein binding rate of more than 94-97%, and dexamethasone does not affect its protein binding. Docetaxel and its metabolites are mainly excreted from feces. Fecal and urinary excretion accounted for 75% and 6% of the dose, and only a small part is excreted in original form. In vitro studies have shown that docetaxel is metabolized by CYP3A4 isoenzymes, which can be inhibited by CYP3A4 inhibitors.

Clinical Research

Genotoxicity: docetaxel induced fractures in CHO-K1 cellular chromosome aberration tests and mouse bone marrow micronucleus tests, but no mutagenicity was observed in Ames tests and CHO/HGPRT gene mutation tests. Reproductive toxicity: no damage to fertility upon intravenous injection 0.3 mg/kg in mice (calculated by body surface area, about 1/50 of the recommended clinical dosage), but could cause reduction in testicular weight. This result is correlated with the results of repeatedly administering it to rats and dogs for 10 cycles (administered once every 21 days, for 6 months); when the intravenous doses were 5 mg/kg and 0.375 mg/kg respectively (converted by surface area, 1/3 and 1/15 of the recommended clinical dose, respectively), testicular atrophy and degeneration were observed. Similar effects were also observed in rats when given low doses more frequently. When rats and rabbits were given ≥0.3 mg/kg/day and 0.03 mg/kg/day (converted from surface area, respectively equivalent to 1/50 and 1/300 of the clinically recommended dose) during organogenesis), embryonic and fetal toxicity was observed (manifesting as intrauterine death, absorbed fetus, and fetal weight loss and delayed ossification). The above dose may case maternal toxicity.

Drug Interactions

In vitro studies have found that CYP3A4 inhibitors may interfere with the metabolism of docetaxel, so it should be used with caution in combination with such drugs (such as ketoconazole, erythromycin, cyclosporine, etc.)

Adverse Reactions

1. Bone marrow suppression: neutropenia is the most common adverse reaction is usually severe (under 500/mm3). Reversible and does not accumulate. Fever and infection associated with neutropenia have been reported in the literature. Anemia can be seen in most cases, with rare severe thrombocytopenia. 2. Allergic reactions: some patients experience severe allergic reactions, characterized by hypotension and bronchospasm, requiring interruption of treatment. The patient can return to normal immediately after discontinuing treatment. Mild allergic reactions, such as blush (with or without itchy erythema), chest tightness, back pain, difficulty breathing, drug fever, or chills, occur in some patients. 3. Skin reactions are usually manifest as erythema, mainly local rashes on hands and feet, sometimes also on arms, face, and chest, sometimes accompanied by itching. Rashes usually occur within a week of infusion, but can return before the next infusion. Severe symptoms, such as peeling after skin rash, occur rarely. Fingernail (or toenail) lesions may occur, characterized by hyperpigmentation or thinning, and sometimes pain and nail loss. 4. Fluid retention: edema, and a few reported cases of pleural effusion, ascites, pericardial effusion, increased capillary permeability, and weight gain. Lower limb fluid retention after four cycles of treatment or cumulative dose of 400mg/m2 may develop into systemic edema, and weight gain of 3kg or more. After discontinuing treatment, fluid retention gradually disappears. Corticosteroids should be given to prophylactically reduce fluid retention. 5. Gastrointestinal reactions such as nausea, vomiting, or diarrhea may occur. 6. There have been reports of neurotoxicity in clinical trials. 7. Cardiovascular adverse reactions such as hypotension, sinus tachycardia, palpitations, pulmonary edema, and hypertension may occur. 8. Other adverse reactions may include: hair loss, weakness, mucositis, joint and muscle pain, hypotension, and reaction at injection site. 9. Patients with normal liver function have also experienced elevated transaminase during treatment. For those with elevated bilirubin, the relationship with docetaxel is still unclear.

Contradictions

1 Patients with a history of severe allergic sensitivity to docetaxel or polysorbate-80.
2 Patients with white blood cell count under 1500/mm3.
3 Patients with severe liver damage.

Precautions

At present there is still insufficient strictly controlled clinical data for pregnant women. Patient who are a pregnant woman or become pregnant while using docetaxel should be informed of potential damage to the fetus and risk of miscarriage. Women who may become pregnant during treatment should use birth control. It is not clear whether docetaxel is excreted from human milk. Given that many drugs may be excreted from human milk, and that docetaxel may have serious adverse reactions for breastfeeding infants, mothers should stop breastfeeding before treatment.
The efficacy and safety of docetaxel in children has not yet been determined.

Chemical Properties

Off-white Cryst

Uses

antineoplastic;binds to microtubules

Definition

ChEBI: A tetracyclic diterpenoid that is paclitaxel with the N-benzyloxycarbonyl group replaced by N-tert-butoxycarbonyl, and the acetoxy group at position 10 replaced by a hydroxy group.

Uses

Docetaxel is a semisynthetic analog of taxol that inhibits microtubule disassembly (IC50 = 0.2 μM) and inhibits cell replication (IC50 = 0.13 μM). It has proven more effective than taxol in preventing the proliferation of cancer cells. Docetaxel has applications in breast cancer and hormone-refractory prostate cancer. This product is intended for research applications.

Docetaxel Preparation Products And Raw materials

Raw materials

Preparation Products


Docetaxel Suppliers

Global( 415)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Capot Chemical Co.,Ltd.
+86 (0)571-855 867 18
+86 (0)571-858 647 95 sales@capotchem.com China 19953 60
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 9974 55
Sichuan Tuskwei Import and Export Trade Co., Ltd.
86-311-83306736
86-311-83306736 sales@tuskwei.com CHINA 168 58
Nanjing Gold Pharmaceutical Technology Co. Ltd.
025-84209270 15906146951
025-84209270 wgp@nanjing-pharmaceutical.com CHINA 290 55
Frapp's ChemicalNFTZ Co., Ltd.
+86 (576) 8169-6106
+86 (576) 8169-6105 sales@frappschem.com China 887 50
Beijing Zhongshuo Pharmaceutical Technology Development Co., Ltd 010-64430626/13801208576
010-64215766 maggie@chinazhongshuo.com China 194 65
Nanjing Chemlin Chemical Co., Ltd 025-83697070
+86-25-83453306 sales@chemlin.com.cn China 20013 64
Wuhan Wei Shunda Technology Development Co., Ltd. 86-027-88774375
86-027-88416321 mwmwhot@163.com China 234 65
Nanjing JinruiJiuAn Biotechnology Co., Ltd. 025-58196018 QQ:800028039
025-83453306 sales@fartop.net China 2234 55
Target molecule Corp. 857-239-0968
857-239-8801 market@targetmol.com United States 2567 60

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