The four types of "paclitaxel" each have their own characteristics. In order to facilitate clinical selection and rational use, they are summarized as follows, hoping to be of some clinical help.
In 1963, American chemists isolated a crude extract of paclitaxel from the bark of Pacific yew for the first time.
The emergence of chemotherapy has changed the fate of many patients. For some cancer types, chemotherapy works extremely well! From 1970 to the present, the survival rate of testicular cancer has increased from 67% to 98%, that of leukemia has increased from 12% to 62%, and that of non-Hodgkin lymphoma has increased from 40% to about 75%. The main factors behind these improvements are Widespread use and optimization of chemotherapy. Among them, paclitaxel is the most widely used and one of the most important chemotherapy drugs. It can be used as a first-line drug for three major indications: advanced ovarian cancer, non-small cell lung cancer, and breast cancer.
In 1963, American chemists isolated a crude extract of paclitaxel from the bark of Pacific yew for the first time.
In 1971, scientists determined the chemical structure of this active substance for the first time and named it Paclitaxel. Soon, scientists discovered that paclitaxel could kill cancer cells.
After further research, the first clinical trial of paclitaxel began in 1984. After 10 years of research, paclitaxel was approved for the treatment of advanced breast cancer in 1994. In 1996, another chemotherapy drug of the same type was approved. Cetaxel is also approved for breast cancer treatment.
Initially, paclitaxel could not be synthesized effectively and could only be extracted from the bark of trees. Extracting the bark would directly kill the trees. On the one hand, this resulted in severe restrictions on output. On the other hand, it also attracted a large number of environmentalists. protests, thus seriously affecting its development and clinical trials. Later, new technologies allowed paclitaxel to be obtained from other sources, including cultured cells, solving this thorny problem.
Taxoid drugs have good anti-cancer effects, but they also have shortcomings. The biggest problem is that taxanes are poorly soluble in water, so special solvents are needed, but these solvents themselves can cause trouble. For example, polyoxyethylene castor oil (CrEL) is commonly used to dissolve paclitaxel. This solvent itself can cause severe allergic reactions in the body, directly bringing various restrictions to clinical use. However, after entering the 21st century, the preparation methods and research of paclitaxel have made progress. There are currently four types of paclitaxel. Let us learn about all aspects of the chemotherapy wonder drug paclitaxel.
1
What are the differences in basic characteristics?
Paclitaxel: Stabilizes microtubules by promoting the assembly of tubulin dimers and preventing their depolymerization, thereby inhibiting microtubules that are critical for cell function during interphase and mitosis. The normal dynamic reorganization of the cell cycle blocks the cell cycle in the G2/M phase, causing abnormal or stopped mitosis, hindering the replication of tumor cells, making the cancer cells unable to continue dividing and die. In addition, paclitaxel also has a radiosensitizing effect and can promote cell damage caused by ion irradiation.
Docetaxel: a semi-synthetic paclitaxel analogue synthesized from 10-desacetyl baccatine III from European yew leaf extract. It has the same mechanism of action as paclitaxel and has a higher affinity for binding to microtubules. , has high anti-cancer activity and broad anti-tumor spectrum. Animal experiments suggest that docetaxel is effective in transplanting human tumors in mice such as lung cancer, breast cancer, ovarian cancer, colon cancer, and melanoma.
Abbott India · Highly cost-effective albumin-bound paclitaxel
Albumin-bound paclitaxel: Nanoparticles made of paclitaxel and human albumin through high-pressure vibration technology, a white The protein molecule binds to 7 paclitaxel molecules and uses the albumin receptor Gp60 on the cell membrane and the secretory acidic protein rich in cysteine ??(SPARC) in tumor tissue to promote the drug into the tumor cells and increase the efficacy of chemotherapy.
Paclitaxel liposomes: a new formulation that encapsulates paclitaxel in lipid particles. Liposome is a targeted drug carrier, which is a new dosage form of targeted drug system. It uses special technology to encapsulate drugs in lipid particles with diameters ranging from microns to nanometers, which can make the drugs mainly in the liver and spleen. It accumulates in tissues and organs such as lungs, lungs and bone marrow, thereby improving the therapeutic index of the drug, reducing the therapeutic dose and reducing the toxicity of the drug, and has shown unique advantages in improving patient tolerance.
2
What are the differences in drug safety?
Paclitaxel injection · Italy (Italy) | Corden
Paclitaxel: It is highly lipophilic and insoluble in water, so paclitaxel injection must add polyoxyethylated castor oil and free Water ethanol helps dissolve. Polyoxyethyl-substituted castor oil can cause varying degrees of allergic reactions, aggravate the peripheral neurotoxicity of paclitaxel, affect the diffusion of drug molecules into tissues, and affect the anti-tumor effect. Studies have found that polyoxyethyl-substituted castor oil can dissolve diethylene ethyl phthalate in PVC infusion sets, causing serious adverse reactions.
Docetaxel: It has low water solubility, so polysorbate 80 and absolute ethanol must be added to help dissolve it, both of which can increase the occurrence of adverse reactions. Ethanol can inhibit the central nervous system and penetrate the human red blood cell membrane to cause degeneration or hemolysis of red blood cells; polysorbate 80 is a non-ionic surfactant that can cause allergic reactions and hemolytic reactions.