Herceptin - pharmacological anticancer drug used for the treatment of breast cancer and stomach cancer.
Structure and Composition
According to the instructions Herceptin contains the active substance - trastuzumab (150 mg) and auxiliary components.
Available drug in vials as a lyophilisate for infusion 150 mg. The lyophilizate is a transparent liquid, slightly opalescent.
Mode of action of Herceptin
This drug has a selective antitumor activity against tumors which have overexpressed HER2 (certain types of breast cancer and advanced gastric cancer). Herceptin blocks dividing tumor cells overexpressing HER2 both in vivo (in the organism) in vitro (in vitro). Moreover, the cytotoxicity of the drug mainly directed to the affected tumor cells.
The half-life of Herceptin - 28-38 days after the end of therapy with this drug it is completely eliminated from the body through 190 days (5 half-lives).
Clinical studies on the use of the drug in patients with renal and hepatic failure, as well as for the elderly and senile age was conducted.
According to the instructions recommended Herceptin for the treatment of metastatic breast cancer with a tumor overexpressing HER2. The drug can be used alone (if treated preceded by one or more chemotherapy regimens). Also, treatment with Herceptin can be used in combination with other agents (paelitakselom or docetaxel) if the patient before chemotherapy was not carried out (the so-called first line treatment). This drug can be used in combination with an aromatase inhibitor for positive hormone receptor (progesterone and / or estrogen) in postmenopausal women.
At the early stages of breast cancer (a tumor overexpressing HER2) Herceptin is administered as adjuvant therapy after surgery, completion of chemotherapy or radiation therapy. Also, the preparation may be combined with paclitaxel or docetaxel (after adjuvant chemotherapy with doxorubicin and cyclophosphamide).
Treatment with Herceptin also recommended for advanced gastric cancer (or cancer of the gastro-) with a tumor overexpressing HER2.
- hypersensitivity to the active substance (trastuzumab) or other components of the formulation;
- pregnancy and lactation;
- Children's age (studies on the use of Herceptin in children has not been done);
- severe respiratory failure, which is caused by metastatic lesions of the lungs, or who require maintenance treatment with oxygen.
According to the instructions of Herceptin should be used with caution in patients with coronary artery disease, hypertension, heart failure, pulmonary comorbidity (or metastases in the lungs). Also, with particular attention the drug should be used for treatment of patients with prior therapy cardiotoxic agents (eg anthracyclines and cyclophosphamide).
Herceptin Instructions: Dosage and administration
Before starting treatment with Herceptin necessarily testing for the expression of tumor HER2. According to the instructions of Herceptin is administered only intravenously. Inkjet or bolus unacceptable!
The drug is not compatible with a 5% dextrose solution (due to possible loss of protein in the sediment). Herceptin should not be mixed with other drugs.
Please do concentrate solution. For this purpose the contents of the vial with 150 mg of Herceptin dilute 7, 2 ml of sterile water for injection. After production of the concentrate can be diluted for infusion immediately or stored for 24 hours at 2-8 ° C.
The required dose of Herceptin is calculated by the doctor individually for each patient, based on its weight and other factors.
During infusion, the need for monitoring the patient's condition for occurrence of chills, fever and other reactions (after the first infusion for 6 hours, after subsequent - 2 hours). In the case of reactions to the infusion is discontinued. After the disappearance of the symptoms of drug administration can be resumed.
In metastatic breast cancer shows weekly administration of Herceptin. Wherein the loading dose of 4 mg / kg body weight (infusion should last 90 minutes). Maintenance dose - 2mg / kg body weight, once per week. The maintenance dose is administered after a loading after 1 week.
An alternative embodiment of the injection - 3 weeks. This dose administered is calculated separately physician.
With advanced gastric cancer with Herceptin treatment is carried out by the scheme - 3 weeks. Wherein the loading dose of 8 mg / kg body weight, and supporting - 6 mg / kg body weight.
Duration of treatment Herceptin in patients with early-stage breast cancer is 1 year (18 cycles mode after 3 weeks) or until disease recurrence.
Side effects of Herceptin
The most serious side effects of this drug are expressed in cardiotoxicity, infusion reactions occur, gematotoksichnosti (neutropenia) and pulmonary adverse events occur. In the opinion of Herceptin in the long-term administration of 1% causes anemia, neftropeniyu, leukopenia. Also in 1% of cases marked the emergence of infectious and parasitic processes (pneumonia, cystitis, sinusitis, and others.).
Also, according to reviews, Herceptin 1% of cases the cause of anxiety, insomnia, weight loss, dizziness, tremors, paresthesias, dry eye, reduced / increased blood pressure, heart rate, heart rhythm disorders. This drug is very common (10%) may account for violations of the gastrointestinal tract (diarrhea, nausea, swelling of the lips, stomach pain).
In addition, reviews, Herceptin often (10%) causes pain in the joints, muscle stiffness, myalgia, asthenia, fatigue, flu-like phenomenon.
In clinical studies with Herceptin overdoses were not. Introduction of the drug at a dose higher than 10 mg / kg was not investigated. In the opinion of Herceptin doses of less than 10 mg / kg was well tolerated by patients.
Herceptin interaction with other drugs
Special studies on the interaction of the drug with other drugs have been conducted. When administered Herceptin concurrently with the use the drug (doxorubicin, paclitaxel, docetaxel, cisplatin), clinically significant interactions were observed.
According to the instructions of Herceptin is not compatible with 5% dextrose.
Herceptin treatment is carried out only under the supervision of an oncologist after testing the expression of tumor HER2.