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Docetaxel | CAS No: 114977-28-5 | GMP-certified suppliers
A medication that treats various advanced solid tumors, including breast, non-small cell lung, prostate, gastric, and head and neck cancers, by inhibiting tumor cell growth and proliferation.
Therapeutic categories
Primary indications
- Docetaxel is indicated as a single agent for the treatment of locally advanced or metastatic breast cancer after chemotherapy failure
- And with doxorubicin and cyclophosphamide as adjuvant treatment of operable node-positive BC
- It is also indicated as a single agent for locally advanced or metastatic non-small cell lung cancer (NSCLC) after platinum therapy failure
- And with cisplatin for unresectable, locally advanced or metastatic untreated NSCLC
Product Snapshot
- Docetaxel is formulated primarily as an injectable solution for parenteral administration
- It is used mainly for the treatment of various advanced or metastatic cancers, including breast cancer, non-small cell lung cancer, prostate cancer, gastric adenocarcinoma, and squamous cell carcinoma of the head and neck
- Docetaxel has approved regulatory status in major markets including the United States, Canada, and the European Union
Clinical Overview
Pharmacologically, docetaxel is a semisynthetic analogue of paclitaxel with approximately twice the potency in inhibiting microtubule depolymerization. It exerts its antimitotic effects by reversibly binding with high affinity in a 1:1 ratio to the β-subunit of tubulin within microtubules. This binding stabilizes microtubules by promoting polymerization and preventing depolymerization, disrupting the dynamic instability necessary for mitosis and intracellular transport. The resultant microtubule stabilization leads to mitotic arrest and activation of apoptotic pathways, including inhibition of the anti-apoptotic protein Bcl-2.
Docetaxel is administered intravenously due to poor oral bioavailability. It undergoes hepatic metabolism predominantly via cytochrome P450 3A4/5 isoenzymes, with biliary excretion as the primary clearance route. The drug’s pharmacokinetics necessitate caution in patients with hepatic impairment. Dose adjustments may be required based on hepatic function and hematologic tolerance.
Safety considerations include risks of hematologic toxicity such as neutropenia, fluid retention syndromes, hypersensitivity reactions, hepatotoxicity, enterocolitis, and potential embryo-fetal toxicity. Careful monitoring is warranted to mitigate these risks. Documented treatment-related fatalities have occurred especially in breast cancer and NSCLC populations. Given docetaxel’s narrow therapeutic index and complex pharmacology, it is classified under multiple categories including antimitotic agents, myelosuppressive agents, and cytochrome P450 substrates/inhibitors.
Docetaxel is commercially available as an injectable solution following FDA approval in 1996, marketed under various brand names worldwide.
For API procurement, it is critical to verify quality attributes including purity, residual solvents, enantiomeric composition, and compliance with pharmacopeial standards. Suppliers should provide comprehensive documentation supporting the consistency of the semisynthetic process and stability profile due to the molecule’s complex diterpenoid structure. Monitoring for potential impurities related to taxane derivatives and adherence to regulatory guidelines is essential to ensure suitability for formulation and clinical use.
Identification & chemistry
| Generic name | Docetaxel |
|---|---|
| Molecule type | Small molecule |
| CAS | 114977-28-5 |
| UNII | 699121PHCA |
| DrugBank ID | DB01248 |
Pharmacology
| Summary | Docetaxel is a taxane antineoplastic agent that stabilizes microtubules by binding to the β-subunit of tubulin, preventing their depolymerization and disrupting normal microtubule dynamics essential for mitosis and intracellular transport. This stabilization inhibits cell division and induces apoptosis, partly through inhibition of the anti-apoptotic protein Bcl-2. Its pharmacodynamic effects include the promotion of abnormal microtubule bundling and mitotic spindle formation disruption. |
|---|---|
| Mechanism of action | Docetaxel interferes with the normal function of microtubule growth. Whereas drugs like [colchicine] cause the depolymerization of microtubules in vivo, docetaxel arrests their function by having the opposite effect; it hyper-stabilizes their structure. This destroys the cell's ability to use its cytoskeleton in a flexible manner. Specifically, docetaxel binds to the β-subunit of tubulin. Tubulin is the "building block" of microtubules, and the binding of docetaxel locks these building blocks in place. The resulting microtubule/docetaxel complex does not have the ability to disassemble. This adversely affects cell function because the shortening and lengthening of microtubules (termed dynamic instability) is necessary for their function as a transportation highway for the cell. Chromosomes, for example, rely upon this property of microtubules during mitosis. Further research has indicated that docetaxel induces programmed cell death (apoptosis) in cancer cells by binding to an apoptosis-stopping protein called Bcl-2 (B-cell leukemia 2), thus arresting its function. |
| Pharmacodynamics | Docetaxel is a taxoid antineoplastic agent. It promotes the assembly of microtubules from tubulin dimers and stabilizes microtubules by preventing depolymerization. This stability results in the inhibition of the normal dynamic reorganization of the microtubule network which is essential for vital interphase and mitotic cellular functions. In addition, docetaxel induces abnormal arrays or "bundles" of microtubules throughout the cell cycle and multiple asters of microtubules during mitosis. The use of docetaxel may lead to treatment-related deaths in breast cancer and non-small cell lung cancer patients, hepatic impairment, hematologic effects, enterocolitis and neutropenic colitis, hypersensitivity reactions, fluid retention, second primary malignancies, cutaneous reactions, neurologic reactions, eye disorders, asthenia, embryo-fetal toxicity, and tumor lysis syndrome. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Tubulin beta-1 chain | Humans | |
| Microtubule-associated protein 2 | Humans | |
| Microtubule-associated protein 4 | Humans |
ADME / PK
| Absorption | The pharmacokinetic profile of docetaxel is consistent with a three-compartment model. The initial rapid decline represents the distribution to the peripheral compartments, and the late (terminal) phase is partly due to a relatively slow efflux of docetaxel from the peripheral compartment. The area under the curve (AUC) was dose proportional at doses between 70 mg/m<sup>2</sup> and 115 mg/m<sup>2</sup> with infusion times of 1 to 2 hours. In a group of patients with solid tumors given 100 mg/m<sup>2</sup> of docetaxel intravenously, the Cmax and AUC were 2.41 μg/mL and 5.93 μg⋅h/mL, respectively. |
|---|---|
| Half-life | With plasma sampling up to 8 to 22 days after docetaxel infusion, the terminal elimination half-life was 116 hours. Doses between 70 and 115 mg/m<sup>2</sup> with infusion times of 1 to 2 hours produce a triphasic elimination profile. The half-life of the alpha, beta, and gamma phases are 4 minutes, 36 minutes, and 11.1 hours, respectively. |
| Protein binding | _In vitro_ studies show that 94% of docetaxel is bound to proteins, mainly alpha-1-acid glycoprotein, albumin, and lipoproteins. When measured in cancer patients, docetaxel is 97% bound to plasma protein. Dexamethasone does not affect the protein binding of docetaxel. |
| Metabolism | Docetaxel undergoes hepatic metabolism. _In vitro_ drug interaction studies revealed that docetaxel is metabolized by the CYP3A4 isoenzyme. CYP3A5 also plays a role in the metabolism of this drug. In humans, docetaxel is metabolized by CYP3A4/5 into four metabolites: M1, M2, M3 and M4. Docetaxel undergoes hydroxylation of the synthetic isobutoxy side chain, forming metabolite M2. The oxidation of M2 forms an unstable aldehyde that is immediately cyclised into the stereoisomers M1 and M3. M4 is then formed by the oxidation of M1/M3. |
| Route of elimination | Docetaxel was eliminated in urine and feces following oxidative metabolism of the tert-butyl ester group, but fecal excretion was the main elimination route. Within 7 days, urinary and fecal excretion accounted for approximately 6% and 75% of the administered radioactivity, respectively. In the first 48 hours, approximately 80% of the radioactivity recovered was excreted in feces. One major and three minor metabolites were excreted at this point, with less than 8% as the unchanged drug. |
| Volume of distribution | Docetaxel has a steady-state volume of distribution of 113 L. Its pharmacokinetic profile is consistent with a three-compartment pharmacokinetic model. |
| Clearance | After the administration of 20–115 mg/m<sup>2</sup> of intravenous docetaxel to cancer patients, the total body clearance was 21 L/h/m<sup>2</sup>. In patients aged 1 to 20 years with solid tumors that received 55 mg/m<sup>2</sup> to 235 mg/m<sup>2</sup> of docetaxel in a 1-hour intravenous infusion every 3 weeks, clearance was 17.3 L/h/m<sup>2</sup>. |
Formulation & handling
- Docetaxel is a poorly water-soluble small molecule taxane used primarily via intravenous injection and other parenteral routes.
- Formulations often require lyophilized powder or concentrate solutions due to limited aqueous solubility and stability considerations.
- Avoid concomitant use with grapefruit and St. John's Wort to prevent significant changes in drug metabolism via CYP3A4 interactions.
Regulatory status
| Lifecycle | The API has established presence in Canada, the US, and the EU, with several earlier patents having expired between 2010 and 2014, while a key patent in the US remains in effect until 2033, indicating ongoing market protection and moderate maturity. |
|---|
| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | Docetaxel is supplied by originator manufacturers with branded products available across North American and European markets, including Canada, the US, and the EU. Multiple patents are in place with expiration dates extending to 2033, indicating continued patent protection and limited generic competition at present. |
|---|
Safety
| Toxicity | There is no known antidote for an overdose of docetaxel injection. In case of overdose, patients should be closely monitored in specialized units. Some of the anticipated complications of overdosage include: bone marrow suppression, peripheral neurotoxicity, and mucositis. After an overdose is discovered, patients should receive granulocyte colony-stimulating factor (G-CSF) as soon as possible. Other appropriate symptomatic measures should be taken as needed. In two reports of overdose, one patient received 150 mg/m<sup>2</sup>, and the other received 200 mg/m<sup>2</sup> as 1-hour infusions. Both patients experienced severe neutropenia, mild asthenia, cutaneous reactions, and mild paresthesia, and recovered without incident. In rats, the oral LD<sub>50</sub> of docetaxel is >2000 mg/kg. The intravenous LD<sub>50</sub> in mice is 138 mg/kg. |
|---|
- Overdose of docetaxel may result in severe bone marrow suppression, peripheral neurotoxicity, and mucositis
- No specific antidote is available
- Exposure management requires close monitoring and administration of granulocyte colony-stimulating factor (G-CSF) alongside symptomatic treatment
Docetaxel is a type of Antineoplastics
Antineoplastics are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) primarily used in the treatment of cancer. These powerful substances inhibit or destroy the growth of cancer cells, thus impeding the progression of malignancies.
Antineoplastics exert their therapeutic effects through various mechanisms. Some APIs interfere with DNA replication, inhibiting the division and proliferation of cancer cells. Others target specific proteins or enzymes involved in tumor growth, effectively blocking their function. Additionally, certain antineoplastic agents induce programmed cell death, known as apoptosis, in cancer cells.
These APIs find application in a wide range of cancer treatments, including chemotherapy, targeted therapy, immunotherapy, and hormone therapy. They are often administered in combination with other drugs to optimize therapeutic outcomes and minimize drug resistance.
Antineoplastics are typically synthesized through complex chemical processes, ensuring high purity and potency. Stringent quality control measures are implemented throughout manufacturing to meet regulatory standards and ensure patient safety.
Although antineoplastics offer significant benefits in treating cancer, they can also cause adverse effects due to their cytotoxic nature. Common side effects include bone marrow suppression, gastrointestinal disturbances, hair loss, and immune system suppression. Close monitoring and supportive care are essential to manage these side effects effectively.
In conclusion, antineoplastics are a vital category of pharmaceutical APIs used in the treatment of cancer. Through their diverse mechanisms of action, these compounds play a critical role in combating malignancies and improving patient outcomes.
Docetaxel API manufacturers & distributors
Compare qualified Docetaxel API suppliers worldwide. We currently have 29 companies offering Docetaxel API, with manufacturing taking place in 11 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 |
| Aurora Industry Co., Ltd | Distributor | China | China | BSE/TSE, CEP, CoA, FDA, GMP, ISO9001, MSDS, USDMF, WC | 250 products |
| Chongqing Sintaho Pharmac... | Producer | China | China | BSE/TSE, CEP, CoA, FDA, GMP, ISO9001, MSDS, USDMF, WC | 42 products |
| Chongqing Taihao | Producer | China | China | CoA, GMP, WC | 7 products |
| Dr. Reddy's | Producer | India | India | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, MSDS, USDMF, WC | 170 products |
| Eigenmann & Veronelli | Producer | Italy | Italy | CoA, GMP | 6 products |
| Emcure Pharma | Producer | India | India | CoA, USDMF | 80 products |
| Fujian South Pharma | Producer | China | China | CEP, CoA, GMP, WC | 7 products |
| Hubei Haosun Pharma | Producer | China | China | CEP, CoA, FDA, USDMF | 8 products |
| Indena | Producer | Italy | Unknown | CEP, CoA, GMP, JDMF, USDMF | 15 products |
| Intas Pharma | Producer | United Kingdom | United Kingdom | CEP, CoA, FDA, GMP, USDMF | 30 products |
| Jiangxi Bioman Pharma Lim... | Producer | China | China | CoA | 15 products |
| Kromozome | Distributor | India | India | CoA, GMP | 17 products |
| Laurus Labs | Producer | India | India | CEP, CoA, GMP, USDMF, WC | 50 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Mac Chem Products | Producer | India | India | CoA, GMP, USDMF, WC | 25 products |
| MSN Labs. | Producer | India | India | CEP, CoA, FDA, GMP, USDMF, WC | 119 products |
| Phyton Biotech | Producer | Canada | Canada | CEP, CoA, FDA, JDMF, USDMF | 2 products |
| Polymed Therapeutics | Producer | United States | United States | CEP, CoA, USDMF | 11 products |
| Rochem International, Inc... | Distributor | United States | United States | BSE/TSE, CEP, CoA, GMP, ISO9001, MSDS, USDMF | 144 products |
| Samyang Bio | Producer | South Korea | South Korea | CEP, CoA, USDMF | 2 products |
| Sanofi | Producer | France | Unknown | CEP, CoA, FDA, GMP | 93 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Shanghai Jinhe Bio-Pharma | Producer | China | China | CoA | 12 products |
| Sicor De México | Producer | Mexico | Mexico | CoA, JDMF | 11 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CEP, CoA, GMP, ISO9001, USDMF | 757 products |
| Tenatra Exports Private L... | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, MSDS | 263 products |
| Yung Shin Pharmaceutical | Producer | Taiwan | Taiwan | CoA, USDMF | 7 products |
| Zhejiang Hisun Pharma | Producer | China | China | CoA, USDMF | 69 products |
When sending a request, specify which Docetaxel 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.).
Use the list above to find high-quality Docetaxel API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
