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Paclitaxel

Paclitaxel

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Paclitaxel is a mitotic inhibitor used in cancer chemotherapy. It was discovered in a National Cancer Institute program at the Research Triangle Institute in 1967 when Monroe E. Wall and Mansukh C. Wani isolated it from the bark of the Pacific yew tree, Taxus brevifolia and named it ‘taxol’. When it was developed commercially by Bristol-Myers Squibb (BMS) the generic name was changed to ‘paclitaxel’ and the BMS compound is sold under the trademark ‘TAXOL’. In this formulation, paclitaxel is dissolved in Cremophor EL and ethanol, as a delivery agent. A newer formulation, in which paclitaxel is bound to albumin, is sold under the trademark Abraxane.
Paclitaxel is now used to treat patients with lung, ovarian, breast cancer, head and neck cancer, and advanced forms of Kaposi’s sarcoma. Paclitaxel is also used for the prevention of restenosis.
Paclitaxel stabilizes microtubules and as a result, interferes with the normal breakdown of microtubules during cell division. Together with docetaxel, it forms the drug category of the taxanes.

MP 213 °C (dec.)(lit.)
refractive index -49 ° (C=1, MeOH)
storage temp.
2-8°C
Solubility methanol: 50 mg/mL, clear, colorless
Stability Stable. Incompatible with strong oxidizing agents. Combustible.
Outline Paclitaxel is a monomer diterpenoid compound extracted from bark of the natural plant, taxus. It is a kind of complex secondary metabolites and is currently known as the only kind drug that can promote microtubule polymerization and stabilize polymerized microtubules. Isotopic tracing has showed that paclitaxel only binds to polymerized microtubules without reacting with the non-polymerized tubulin dimer. Cells will accumulate large amount of microtubules inside cells after exposure to paclitaxel with the accumulation of these microtubules being able to interfere with various kinds of cellular functions, in particular, being able to stop cell division in the mitosis phase, blocking the normal cell division. ThroughⅡ-Ⅲ clinical study, paclitaxel is mainly applied to the treatment of ovarian and breast cancer and also has certain efficacy in the treatment of lung cancer, colorectal cancer, melanoma, head and neck cancer, lymphoma and brain tumors.
Indications It has good efficacy in the treatment of ovarian cancer and refractory ovarian cancer already being resistant to existing platinum and breast cancer. It also has good prospect on the treatment of prostate cancer, head and neck cancer, esophageal cancer, germ cell tumors, endometrial carcinoma, lymphoma, bladder cancer, upper gastrointestinal cancer, small cell and non-small cell lung cancer.
Small history In 1963, American chemist MC Wani and Monre E. Wall had isolated for the first time of the paclitaxel crude extract from the bark and wood of the pacific yew growing in the western forest of United States. During the screening experiments of taxus, Wani and Wall have discovered that crude extracts of paclitaxel are of great activity to the in vitro culture of mouse tumor cells and began to separate this active ingredient. Owing to the very low levels of the active ingredient in the plant, it was not until 1971 that they, through the cooperation with Professor Andre T. McPhail in Duke University, used x-ray analysis and successfully determined the chemical structure of the active ingredient – a kind of tetracylicditerpene and named it as paclitaxel (Paclitaxel).
In 1971, it had been found of paclitaxel in taxus and found a unique anticancer mechanism.
In 1992 the US government assigned the patent to Bristol-Myers Squibb and the paclitaxel emerged.
In 1994, Paclitaxel ranks first in the global sales of world anti-cancer drugs.
In 2000, the Paclitaxel sales had reached ten billion (after that, due to the supply limit of raw materials, the sales amount got no further rise).
In 2002, the central government had forbidden the cutting of wild yew and had encouraged artificial cultivation.
In 2004, the patent of Bristol-Myers Squibb has expired. More and more global pharmaceutical companies have been involved in Paclitaxel production.
In 2004, Huayuan started to conduct the taxus project and build direct paclitaxel-specific extraction factory with the aims of becoming the largest yew base in China and Asia.
In 2005, the Central government again issued a document for the national census of yew resources to encourage planting.
In 2005, this project received investment from individual investors.
High efficient method for separation and purification of paclitaxel It includes a, extraction: take yew as a raw material to obtain the extract containing paclitaxel; B, remove the gum: remove the gum impurities in the extract; C, separation and purification. Wherein: Paclitaxel production process is as follows: pulverize the bark of yew (the thinner the better), 85% to 95% alcohol ( what’s the ratio between material over liquid) heat reflux at 35-55 ℃ for extraction for three times (how long does it take each time?), 50-70 ℃ vacuum evaporated to heat measurement with the proportion of 1.1 ~ 1.2g / ml; extract with chloroform and the extract was concentrated into paste-like to obtain the chloroform paste with paclitaxel content being 1%. Add chloroform to the chloroform paste containing 1% paclitaxel to dissolve it completely. Add silicone gel the stir uniformly, dry, sieve and pack into a chromatography column; apply chloroform – methanol gradient elution, TLC detection, segmentation, mergence and concentration to give semi-finished product containing 5 to 8% Paclitaxel. Add acetone to the semi-finished content containing 5 to 8% Paclitaxel to dissolve completely; Add silicone gel the stir uniformly, dry, sieve and pack into a chromatography column; apply chloroform – methanol gradient elution, TLC detection, segmentation, mergence and concentration to give semi-finished product containing 20 to 25% Paclitaxel. Use acetone – petroleum ether system for crystallization of 3 to 4 times, apply filtration, 50 ℃ vacuum drying under reduced pressure to give semi-finished product with Paclitaxel content being 75 to 80%. apply 16Mpa pressure chromatography, TLC detection, segmentation, mergence and concentration; the target segment concentrates are subject to acetone – petroleum ether crystallization, filtration, drying to obtain finished product with paclitaxel content ≥99.5%; gum removal process: apply high-pressure silica column chromatography to remove gum while separating the taxane compound to three parts including paclitaxel, cephalomannine, 7-epi Paclitaxel.
Docetaxel Docetaxel is a kind of highly strong bone marrow activity inhibitor drug extracted from yew trees. During the treatment, the patients should be subject to monitoring of blood cell and platelet counts. The mechanism of action for the drug is similar to paclitaxel, namely inhibiting the depolymerization of microtubules and inhibiting cell division. Through intravenous infusion of this drug for administration, it can be used for the treatment of advanced or metastatic breast cancer as well as non-small cell lung cancer.
International market analysis So far, there are only two kinds of paclitaxel API in the international market with one derived from a variety of yew bark; the other being derived from the “10-baccatin” extracted from ornamental yew branches in Europe and further semi-synthesis, namely docetaxel with its structure being highly similar as natural extracts paclitaxel. These two kinds of APIs are both best-selling drug products on the international pharmaceutical market and are in long-term short supply, according to the estimate, the sales ratio of drug paclitaxel and docetaxel API is about 10: 1.
In the United States, the paclitaxel injection (trade name: Paclitaxel) is mainly subject to exclusive manufacturing by Bristol-Myers Squibb. There is now about two to three pharmaceutical companies which produce paclitaxel bulk drugs and formulations. But the market is mostly subject to monopoly by Bristol-Myers Squibb while total sales of the paclitaxel formulation in other few companies only can account for only a small fraction of that in Bristol-Myers Squibb. The docetaxel bulk drugs and formulations are mainly from the co-production of France Poulenc Company and several companies in the United Kingdom and Italy with Planck having the maximal yield.
Paclitaxel is always the first-choice anticancer drugs in hospitals around the world. In the past few years, the cancer incidence around the world has nearly doubled compared to that at 10 years ago with lung, breast and ovarian cancer and other malignancies also showing high-incidence trend. These cancer patients are the major users of paclitaxel. From the overall perspective, before the emergence of a new plant anticancer drug being able to take its place, the sales of paclitaxel will only rise rather than fall.
According to the latest number released by the World Health Organization, the United States has become the country of the world’s first national high incidence of cancer with the annual newly cancer cases increasing by 1.4 million, accounting for 14% of the cases of cancer patients worldwide in that year. The United States has remained the largest consumer of paclitaxel. With the increasing of US cancer incidence, the toxal is used as the major anti-advanced malignancy drug. It is believed that its sales will continue to maintain a rapid upward trend. The United States and other developed countries, during the process of 10 years of clinical use, have already summarized a set of optimal compatibility program for paclitaxel and other anti-cancer drugs. Paclitaxel has become the “backbone” for the related health sector and therefore, the demand for paclitaxel drug will still in the potential of keeping rise.
Precaution for the use of injections 1. Hematological toxicity: The major factor for limiting the increase of the dose. Generally, at WBC less than 1500 / mm3, it should be combined with adjuvant application of G-CSF. At platelets less than 30,000 / mm3, it should be subject to transfusion of blood components.
2. Allergies: In addition to pre-treatment, in case of only mild symptoms such as facial flushing, skin reactions, slightly faster heart rate and slightly lower blood pressure, there is no need for withdrawal and instead we can just slow down the drip rate. However, upon severe reactions such as low blood pressure, angioedema, dyspnea, body hives, the drug should be discontinued and subject to appropriate treatment. Patients with severe allergies should not be applied again of paclitaxel treatment.
3. Nervous System: The most common adverse reaction is numbed fingers and toes. About 4% of the patients, in particular upon high dosage, may exhibit obvious sensory and motor deficits and reduced tendon reflexes. There have been isolated reports of grand mal seizures occur during infusion.
4. Cardiovascular: tachycardia and hypotension are relatively common and generally do not need treatment. In the first hour of infusion, it should be closely monitored. Later there is no need for monitoring once per hour unless in cases of patients with serious conduction blockage.
5. Joints and muscles: about half of the patients will fee joint and muscle pain at 2 to 3 days after drug treatment and are associated with the dose. This usually can recover within a few days. Patients subject to administration of G-CSF will have more severe muscle pain.
6. Hepatobiliary system: Since most paclitaxel is excreted from the bile, patients with hepatobiliary disease should be carefully monitored. In thousands of cases, there are about 8% cases in which the patients had elevated bilirubin, 23% cases of patients got elevated alkaline phosphatase while 18% had elevated aspartate aminotransferase. But there is no information showing that paclitaxel can cause severe liver impairment.
7. Other: gastrointestinal reactions, although uncommon but are generally not heavy with a few cases in which patients may have diarrhea and mucositis. Mild hair loss is also common.
Chemical Properties It is needle-like crystal or amorphous powder precipitated from methanol. Melting point 213 ~ 216 ℃ (decomposition). [α]D20: 49°(methanol). UV absorption maximum (methanol): 227,273nm (ε29800,1700).
General Description Needles (from aqueous methanol) or fine white powder. An anti-cancer drug.
Air & Water Reactions May be sensitive to prolonged exposure to moisture.
Health Hazard TOXIC; inhalation, ingestion or skin contact with material may cause severe injury or death. Contact with molten substance may cause severe burns to skin and eyes. Avoid any skin contact. Effects of contact or inhalation may be delayed. Fire may produce irritating, corrosive and/or toxic gases. Runoff from fire control or dilution water may be corrosive and/or toxic and cause pollution.
Fire Hazard Flash point data for Paclitaxel are not available. Paclitaxel is probably combustible.
Biological Activity Antitumor agent; promotes and stabilizes tubulin polymerization, causing cell cycle arrest. Induces autocatalytic activation of caspase-10 in CCRF-HSB-2 cells, triggering apoptosis.
Usage An antineoplastic. Used in the study of structure and function of microtubles into tubulin. Paclitaxel is now used to treat patients with lung, ovarian, breast cancer, head and neck cancer, and advanc ed forms of Kaposi’s sarcoma. Paclitaxel is a mitotic inhibitor used in cancer chemotherapy.

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