Sorafenat (Sorafenib) is an anticancer drug used in medical practice for treating malignant tumors in the kidneys, liver, and thyroid gland. The drug is used to suppress metastasis and the spread of metastases from these organs throughout the body. The drug is a conservative treatment of tumors.
Release form composition and packaging
The drug is made in the form of tablets that contain 200 mg of sorafenib tosylate.
As auxiliary substances are used:
croscarmellose sodium and lauryl sulfate;
The outer film shell consists of macrogol, a red dye of iron oxide, titanium dioxide, and hypromellose. Tablets have a biconvex round shape and a red tinge. Each blister pack contains 28 units. the drug, in a cardboard bundle – 4 blisters.
Sorafenib price – an anticancer drug. The mechanism of action is based on multi-kinase inhibition – the drug suppresses mitotic division and further infiltration of tumor cells into the tissue.
When oral doses are prescribed, the active substance sorafenibosylate reduces the functional activity of intracellular kinases and phosphotransferases located on the cell surface. The latter include:
Kinases within tumor units are referred to as: c-CRAF, standard and mutant BRAF. Theoretically, membrane and intracellular phosphotransferase are involved in apoptosis, signaling activity and the formation of new blood vessels (angiogenesis).
After oral administration, the bioavailability of sorafenib varies from 38 to 50%, depending on the individual characteristics. The film membrane is destroyed by intestinal esterases.
When absorbed by the microvilli of the small intestine, tosylate sorafenib enters the systemic vascular bed, where it reaches maximum plasma values within 3 hours. Food intake does not affect the speed and completeness of absorption of the drug, but when consumed with fatty foods, bioavailability decreases by 30%.
The active substance is associated with albumin and other proteins in the blood by 99.5%. With the help of such a complex, the drug penetrates into the malignant cells. Tosylate sorafenib is transformed in the liver cells due to oxidative reactions and gluconization. The resulting metabolic products break up in the digestive tract under the action of glucuronidase bacterial flora.
Indications for use Sorafenib
The drug is used to suppress malignant growth in the following cases:
metastatic cancer of the kidney cells;
metastatic differentiated tumor of the thyroid gland, which is resistant to radioactive iodine isotopes (this type of malignant neoplasm can infiltrate into local tissues);
Dosage and administration of Sorafenib
Per day is recommended to take 4 times 0.2 g (800 mg) of the drug. The dosage is divided into 2 doses for use into the intervals between eating food or with food containing a low or medium level of fat. Tablets need to be swallowed without chewing (mechanical grinding reduces absorption and bioavailability), drinking plenty of liquid.
Mode of application
The recommended daily dose of sorafenib is 800 mg in 2 doses, either between meals or with a diet containing low or moderate amounts of fat.
Treatment is continued for as long as clinical efficacy persists or until an unacceptable toxic effect appears.
The development of adverse reactions may require the temporary cessation and / or reduction of the dose of sorafenib. If necessary, the dose of sorafenib can be reduced to 400 mg 1 time / day.
With the development of skin toxicity, a dose reduction of sorafenib is required.