Taxotere

A drug based on docetaxel, one of the many antitumor agents, the alkaloid Taxotere is a concentrated liquid for intravenous infusions. This drug is often used for second-line chemotherapy, for various cancer processes in the body.

Taxotere is available in pharmacies only with a doctor's prescription.

Indications Taxotere

Taxotere may be prescribed in the following situations:

• as an adjuvant treatment for cancer in the mammary gland, with involvement of the nearest lymph nodes. The treatment is supplemented with Doxorubicin and Cyclophosphamide;
• in localized breast cancer, in metastasis, in combination with Doxorubicin and as the initial chemotherapy regimen. Both first-line and second-line chemotherapy are possible. A unilateral treatment regimen can be carried out in combination with Capecitabine if the initial therapy consisted of anthracyclines and alkylating drugs and was found to be ineffective;
• as an initial chemotherapeutic regimen for breast cancer with metastases and HER2 oncoexpression in combination with Trastuzumab;
• in localized or metastatic non-small cell lung cancer (in combination with Cisplatin and Carboplatin), as an initial chemotherapy regimen or as a re-treatment in the absence of an effect from the previous regimen, including platinum-based drugs;
• in case of metastatic cancer in the ovaries, if the previous type of chemotherapy was considered ineffective;
• for inoperable localized squamous cell carcinoma of the head and neck, in combination with Cisplatin and 5-fluorouracil as initial treatment;
• in metastatic squamous cell carcinoma in the head and neck region as a second-line chemotherapeutic regimen;
• in case of metastatic hormone-dependent malignant process in combination with the medications Prednisolone and Prednisone;
• in metastatic malignant tumor processes in the stomach (including the cardiac region), as an initial treatment in combination with the medications Cisplatin and 5-fluorouracil.

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Release form

Taxotere is a concentrated substance intended for the preparation of infusion fluid.

Taxotere consists of the active ingredient docetaxel and the additional ingredient polysorbate 80. The package includes a solvent liquid in the form of 13% ethyl alcohol diluted with water for injection.

The drug is a colorless oily liquid, the color of which varies from yellowish to brownish. The concentrated medicine is poured into bottles:

• 20 mg/0.5 ml;
• 80 mg/2 ml.

Glass bottles, transparent. Rubber stopper with aluminum protection and plastic cap of green or red color.

One package contains 1 bottle with concentrated medicine and 1 bottle with dissolving liquid. Cell packaging, sealed with polyethylene. Additionally, the pack contains an information leaflet for the medicine.

Names of analogues of the drug Taxotere

The following analogs of the drug Taxotere have been selected based on the active ingredient docetaxel:

• Visdoc is an infusion drug;
• Docemed is a concentrated medicine for the preparation of an infusion solution;
• Docet is a concentrated medicine;
• Docetax is a concentrated medication for the preparation of an infusion solution;
• Docetaxel (Ebeve, Amaxa, Vista, Pharmstandard-Biolek, Teva, Pharmex);
• Docetactin is an infusion concentrated preparation;
• Docetera is a concentrated medicinal product;
• Docet-Health – infusion solution;
• Taxolic is a concentrated medicinal product.

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Pharmacodynamics

Taxotere is a natural antitumor chemotherapeutic agent (taxoid group). The drug's action is due to stimulation of tubulin accumulation in stable microtubules, as well as prevention of their decomposition, which leads to a decrease in the amount of freely existing tubulin. The connection between the active component and microtubules does not affect the number of protofilaments.

Laboratory tests indicate that Taxotere alters the microtubule network, which is important in the cellular phases of mitosis and interphase.

The drug exhibits toxicity towards various malignant cells. However, the effect of Taxotere may not depend on the frequency of use of the drug and may manifest itself in a broad spectrum of anticancer activity.

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Pharmacokinetics

The kinetic properties of Taxotere depend on the amount of drug administered. Plasma protein binding is more than 95%.

Within a week, the active metabolite is excreted with urine and feces (approximately 6% and 75%, respectively). Most of the drug that is excreted with feces can be detected within 2 days as an inactive product.

In case of minor functional disorders of the liver, the total clearance values decrease by 27%, compared to the average value.

The clearance rates of the active ingredient of the drug do not change with a small accumulation of fluid in the body.

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Dosing and administration

To prevent allergic processes and fluid accumulation in tissues, all patients (except for patients with prostate adenocarcinoma) undergo premedication with glucocorticosteroid drugs before chemotherapy. An example of a premedication regimen:

• Dexamethasone orally in the amount of 8 mg twice a day, for 3 days;
• The initial dose of the drug should be taken one day before the start of chemotherapy.

In case of prostate adenocarcinoma, against the background of therapy with prednisolone (or prednisone), premedication is carried out with the drug Dexamethasone at a dosage of 8 mg 12 hours, three hours and 60 minutes before the start of chemotherapy.

To reduce the risk of blood complications, a preventive administration of G-CSF may be prescribed.

Taxotere is administered intravenously by drip over the course of one hour, once every 21 days.

• In the adjuvant treatment of breast cancer, the standard dosage of Taxotere may be 75 mg/m² 60 minutes after Doxorubicin (50 mg/m²) and Cyclophosphamide (500 mg/m²), once every 21 days. The treatment includes 6 injections.

As a stand-alone treatment, Taxotere is administered at a dose of 100 mg/m² once every 21 days. In combination with Doxorubicin (50 mg/m²) and Capecitabine (1250 mg/m²), Taxotere is administered at a dose of 75 mg/m² once every 21 days.

In combination with Trastuzumab, the dose of Taxotere is 100 mg/m² once every 21 days.

• For non-small cell lung cancer, Taxotere is used in a dose of 75 mg/m², either as a single therapy or in combination with platinum-based medications, once every 21 days.
• For metastatic ovarian cancer, Taxotere is used at a dosage of 100 mg/m² once every 21 days.
• For locally localized squamous cell tumor of the head and neck region, Taxotere is administered in an amount of 75 mg/m². On the same day as the drug, Cisplatin is administered in an amount of 75 mg/m² over 60 minutes, followed by drip administration of 5-fluorouracil 750 mg/m² per day for five days. This regimen is used once every 21 days and can be repeated up to 4 times.
• For metastatic squamous cell carcinoma of the head and neck region, Taxotere is administered at a dose of 100 mg/m² once every 21 days.
• In the case of metastatic hormone-independent prostate cancer, Taxotere is administered at a dose of 75 mg/m² once every 21 days. Prednisolone is taken orally at 5 mg twice daily throughout the course of chemotherapy.
• In metastatic cancer in the stomach (including the cardiac region), Taxotere is administered in the amount of 75 mg/m² once every 21 days. On the same day, Cisplatin should be administered by drip in the amount of 75 mg/m², over a 1-3 hour infusion, followed by the administration of 5-fluorouracil in the amount of 750 mg/m² (daily infusion for 5 days).

The concentrated substance is pre-diluted in a dissolving liquid, which is supplied with the drug.

Before diluting the preparation, it must be brought to room temperature. When stirring, do not shake the bottle, but turn it over and hold it for 45 seconds, then leave it for 5 minutes until it is completely dissolved.

Before starting the infusion, it is necessary to ensure that the drug is clean and does not contain turbidity or sediment.

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Use Taxotere during pregnancy

The antitumor drug Taxotere is prohibited for use in pregnant and lactating patients.

Before and during treatment with the drug, contraceptives should be used, which are also used 3 months after the end of the chemotherapy course.

If a woman becomes pregnant during chemotherapy, she must immediately notify her treating doctor.

Clinical trials have shown that Taxotere has a genotoxic effect and can even worsen the quality of male sperm. Therefore, both women and men, during treatment with the drug and for six months after the therapeutic course, must take measures to prevent possible conception of a child. Sometimes, if a couple plans to have children in the future, it is advisable to cryopreserve sperm before starting a course of chemotherapy.

Contraindications

In some diseases and conditions, treatment with Taxotere may not be possible:

• when the level of neutrophils in the peripheral bloodstream is less than 1500 per μl;
• in case of significant functional disorders of the liver;
• during pregnancy and breastfeeding;
• in childhood and adolescence up to 18 years of age;
• if there is a high probability of an allergic reaction to the ingredients of the medication.

When conducting combination treatment with the use of additional drugs, it is also necessary to take into account other contraindications that relate to auxiliary drugs.

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Side effects Taxotere

Like all chemotherapy drugs, Taxotere has a long list of side effects:

• severe transient neutropenia occurring against the background of fever, septic complications and pneumonia;
• thrombocytopenia with the possibility of bleeding, anemia;
• allergic reactions (skin redness, itching, shortness of breath, bronchospasm, rash);
• hair loss, skin rashes, pigmentation of the nail plates, onycholysis;
• swelling of the extremities, accumulation of fluid in the abdominal cavity, generalized edema;
• dyspepsia, changes in taste, inflammation of the mucous membrane of the esophagus, stomach, intestines;
• gastrointestinal ulcers, bleeding;
• numbness of the extremities, peripheral neuropathy, convulsive syndrome;
• arrhythmia, changes in blood pressure, increased thrombus formation, pre-infarction and infarction conditions;
• hepatitis, pneumonia, development of pulmonary fibrosis;
• joint and muscle pain, myasthenia;
• conjunctivitis, lacrimation, transient visual disturbances;
• deterioration of the skin condition, increased pigmentation, pinpoint hemorrhages on the skin, inflammatory lesions of the veins;
• chest pain, redness of the palms and feet, signs of dehydration.

Overdose

The phenomenon of overdose is considered unlikely, since such cases are isolated, since the dosage is calculated individually for each patient.

Signs of using an excessive dose for the body can be considered:

• depressed hematopoietic function;
• generalized inflammation of the mucous tissues;
• peripheral neuropathy.

At present, there is no drug that can reverse the action of Taxotere. If an overdose is suspected, the patient is referred for inpatient treatment with symptomatic medications and constant monitoring of vital functions. The use of colony-stimulating factors (G-CSF) is indicated.

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Interactions with other drugs

According to the conducted studies, it was found that the biological transformation of Taxotere may change with the combined use of drugs that affect the cytochrome P450-3A system (cyclosporines, ketoconazole, oleandomycin, erythromycin). Given this, caution should be exercised with the simultaneous administration of such medications.

Use of Taxotere and Doxorubicin: Taxotere clearance rates may increase, which does not affect the efficacy of the drug.

No other clinically significant drug interactions with Taxotere have been identified.

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Storage conditions

Taxotere is recommended to be stored at a temperature range from +2°C to +25°C, in a dark place, out of reach of children. The shelf life is indicated on the packaging of the drug.

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Shelf life

Taxotere in a dosage of 20 mg is stored for up to 2 years.

Taxotere 80 mg can be stored for up to 3 years.

The prepared solution can be stored in a temperature range from +2°C to +8°C for 8 hours.

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