Taxotere Docetaxel Injection

1. Indications and Usage
Docetaxel Injection is a microtubule inhibitor indicated for the treatment of:
Breast Cancer: Locally advanced or metastatic breast cancer after failure of prior chemotherapy; in combination with doxorubicin and cyclophosphamide for adjuvant treatment of operable node-positive breast cancer.
Non-Small Cell Lung Cancer (NSCLC): Locally advanced or metastatic NSCLC after failure of prior platinum-based chemotherapy; in combination with cisplatin for unresectable, locally advanced or metastatic NSCLC not previously treated with chemotherapy.
Prostate Cancer: Metastatic castration-resistant prostate cancer, in combination with prednisone.
Gastric Adenocarcinoma: Advanced gastric adenocarcinoma, including gastroesophageal junction, in combination with cisplatin and fluorouracil, without prior chemotherapy for advanced disease.
Head and Neck Cancer: Locally advanced squamous cell carcinoma of the head and neck (SCCHN), in combination with cisplatin and fluorouracil, for induction treatment.
2. Dosage and Administration
Premedication: All patients must be premedicated with oral corticosteroids (e.g., dexamethasone 16 mg/day in divided doses for 3 days, starting 1 day before docetaxel) to reduce the incidence and severity of fluid retention and hypersensitivity reactions.
Recommended Dose: 60–100 mg/m² administered as a 1-hour intravenous infusion every 3 weeks, depending on indication and regimen.
Breast cancer (single agent): 60–100 mg/m² every 3 weeks.
Adjuvant breast cancer: 75 mg/m² every 3 weeks after doxorubicin and cyclophosphamide.
NSCLC (single agent or with cisplatin): 75 mg/m² every 3 weeks.
Prostate cancer: 75 mg/m² every 3 weeks with prednisone 5 mg twice daily.
Gastric adenocarcinoma: 75 mg/m² on Day 1, with cisplatin and fluorouracil.
Head and neck cancer: 75 mg/m² on Day 1, with cisplatin and fluorouracil.
Dose Modifications: Reduce dose or withhold treatment for severe neutropenia, febrile neutropenia, severe cutaneous reactions, severe peripheral neuropathy, or hepatic impairment. Discontinue for Grade 3 or higher peripheral neuropathy.
Administration: Dilute in 0.9% Sodium Chloride or 5% Dextrose Injection to a final concentration not exceeding 0.9 mg/mL. Administer via IV infusion over 1 hour. Do not administer as an IV bolus.
3. Mechanism of Action
Docetaxel is a taxane antineoplastic agent that binds to free tubulin and promotes the assembly of stable microtubules while inhibiting their depolymerization. This stabilizes microtubules, disrupts normal microtubule dynamics, and arrests cell division at the G2/M phase of the cell cycle, leading to cell death.
4. Safety and Warnings
Boxed Warning: Toxic deaths, hepatotoxicity, neutropenia, hypersensitivity reactions, and fluid retention.
Toxic Deaths: Treatment-related mortality is increased in patients with abnormal liver function, at higher doses, and in NSCLC patients previously treated with platinum-based chemotherapy receiving 100 mg/m².
Hepatotoxicity: Avoid use in patients with bilirubin > ULN, or AST/ALT >1.5 × ULN with alkaline phosphatase >2.5 × ULN. Obtain liver function tests prior to each cycle.
Neutropenia: Do not administer to patients with neutrophil counts <1,500 cells/mm³. Monitor blood counts frequently.
Hypersensitivity Reactions: Severe reactions, including fatal anaphylaxis, may occur despite premedication. Contraindicated in patients with a history of severe hypersensitivity to docetaxel or polysorbate 80.
Fluid Retention: Severe fluid retention (e.g., pleural effusion, ascites, peripheral edema) may occur. Premedication with corticosteroids is mandatory.
Embryo-Fetal Toxicity: Can cause fetal harm. Advise females and males with female partners of reproductive potential to use effective contraception during treatment and for at least 6 months after the last dose.
5. Adverse Reactions and Clinical Research
Common Adverse Reactions (≥20%): Infections, neutropenia, anemia, febrile neutropenia, hypersensitivity reactions, thrombocytopenia, neuropathy, dysgeusia, dyspnea, constipation, anorexia, nail disorders, fluid retention, asthenia, pain, nausea, diarrhea, vomiting, mucositis, alopecia, skin reactions, and myalgia.
Clinical Research: Efficacy was established in randomized controlled trials across breast cancer, NSCLC, prostate cancer, gastric cancer, and head and neck cancer, demonstrating improvements in response rates, progression-free survival, and/or overall survival compared to control regimens.
6. Drug Interactions
CYP3A4 Inhibitors: Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir) may increase docetaxel exposure. Consider dose reduction or avoid concomitant use.
CYP3A4 Inducers: Concomitant use with strong CYP3A4 inducers (e.g., rifampin, carbamazepine, St. John’s wort) may decrease docetaxel exposure.
Live Vaccines: Avoid administration of live vaccines during treatment.
7. Pharmaceutical Information
Active Ingredient: Docetaxel (anhydrous).
Chemical Name: (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-1,11-Dihydroxy-12b-(benzoyloxy)-6,12b-bis(acetyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-4,6,11-trihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclodeca[3,4]benz[1,2-b]oxet-9-yl (2R,3S)-3-(tert-butoxycarbonyl)amino-2-hydroxy-3-phenylpropanoate.
Molecular Formula: C43H53NO14.
Molecular Weight: 807.88.
Strengths: 20 mg/2 mL (10 mg/mL) and 80 mg/8 mL (10 mg/mL) single-dose vials.
Description: Sterile solution containing polysorbate 80 and dehydrated alcohol. Some formulations are alcohol-free.
Storage: Store unreconstituted vials at 2°C to 25°C (36°F to 77°F). Retain in the original carton to protect from bright light. Do not freeze.