For whom is docetaxel indicated and what are the adverse effects?

(4s,5r)-3-tert-butoxycarbony-2-(4-anisyl)-4- phenyl-5- oxazolidine carboxylic acid is used as the intermediate of Docetaxel.
　　Docetaxel is suitable for the treatment of locally advanced or metastatic breast cancer. Docetaxel is suitable for the treatment of locally advanced or metastatic non-small cell lung cancer, even after the failure of cisplatin based chemotherapy.
　　Docetaxel, also known as doxorubicin, belongs to the paclitaxel family as well as paclitaxel (solvent-based paclitaxel, liposomal paclitaxel, albumin-bound paclitaxel).
　　Paclitaxel is a substance with antitumor activity extracted directly from the bark of the redbud tree, while docetaxel is an antitumor drug with better hydrophilicity obtained from European redbud with artificial structural modification, so docetaxel is a semi-synthetic paclitaxel antitumor drug.
　　As a mainstream antitumor drug in clinical practice, it is necessary to learn about docetaxel together with you!
　　Who are the patients for whom docetaxel is indicated?
　　Docetaxel has the same efficacy as paclitaxel, exerting anti-tumor effects by binding to microtubule proteins and causing cell division arrest.
　　In vitro studies have found that docetaxel and paclitaxel compete for the same binding site at the same concentration, while docetaxel has a stronger affinity for microtubulin than paclitaxel, and its activity of inhibiting microtubulin is about twice as strong as that of paclitaxel.
　　Moreover, docetaxel has better hydrophilicity and increased solubility in water, making the tumor-inhibiting activity higher than that of paclitaxel. In vitro tests have demonstrated that the antitumor activity of docetaxel is 1.3-12 times higher than that of paclitaxel.
　　Docetaxel is playing an increasing role in antitumor therapy and currently has good clinical efficacy in breast cancer, ovarian cancer, non-small cell lung cancer, head and neck squamous cell carcinoma, cervical cancer, esophageal cancer, gastric cancer and other tumors.
　　In clinical practice, docetaxel is most commonly used in breast cancer patients and is the cornerstone of breast cancer chemotherapy.
　　It can be used in combination with adriamycin and cyclophosphamide for post-operative lymph node positive breast cancer adjuvant chemotherapy, or alone or in combination with adriamycin for locally advanced or metastatic breast cancer patients; it can also be used in combination with trastuzumab for HER2-positive metastatic breast cancer treatment.
　　In addition, docetaxel is by far the most effective drug in the second-line treatment of anthracycline-resistant breast cancer.
　　What are the adverse reactions of docetaxel?
　　The most important adverse reactions - bone marrow suppression
　　Neutropenia is the most common and is usually severe, and it can get worse with the dose. Therefore, regular blood monitoring and active use of leukocyte-raising drugs as necessary are required for docetaxel use.
　　The most serious adverse reactions - acute hypersensitivity reactions
　　The incidence of acute hypersensitivity reactions can be as high as 40% and can occur within about 10 minutes of dosing.
　　In severe cases, hypotension and bronchospasm may be present, and treatment may be interrupted. In mild cases, there may be flushing, skin itching, chest tightness, dyspnea, and chills.
　　Therefore, oral dexamethasone pretreatment with 16 mg daily for at least 3 days is usually required prior to clinical use of docetaxel to effectively prevent allergic reactions and fluid retention.
　　Some patients - may have skin reactions
　　It is mainly seen in the hands and feet, but can also occur on the buttocks, face and chest. It manifests as a rash, which may be accompanied by pruritus, usually within one week after titration, and usually requires only symptomatic treatment such as antipruritus.
　　The most specific adverse reaction - fluid retention
　　It manifests as pleural effusion, peritoneal effusion, and pericardial effusion, with an incidence of about 35%.
　　Usually, to reduce fluid retention, corticosteroids can be used prophylactically prior to drug administration. Fluid retention mostly disappears after discontinuation of treatment.
　　Other adverse effects - nausea, vomiting, hair loss, weakness, arthralgia, etc.
　　It should be noted that since docetaxel is mostly used for breast cancer treatment, mostly for female patients, it is necessary to take precautions before drug use to avoid serious psychological disorders due to hair loss in some patients.
　　Most chemotherapy treatments do not harm the hair follicle stem cells, which are the most important for hair growth, and hair will grow back 3-6 months after chemotherapy is finished.
　　Before chemotherapy, you can cut your hair short or shave it to avoid anxiety when you see hair loss during chemotherapy; you can wear a hat or wig through the hair loss period to reduce the psychological disorder.
　　Docetaxel vs. albumin paclitaxel Who can win in a match between the same family?
　　Both albumin paclitaxel and docetaxel belong to the same class of paclitaxel chemotherapy drugs, and their anti-tumor principles are similar, both belong to anti-microtubulin drugs.
　　However, paclitaxel is a combination of paclitaxel and human albumin through technology, and nano-particles are used as carriers, so that the drug can reach cancer tissues quickly and stay in cancer tissues longer, so the concentration of the drug is higher at the tumor site, and the drug concentrates its fire to kill cancer cells, so theoretically the efficacy is better.
　　In practice, there are fewer studies comparing the two.
　　A clinical study in Japan in 2020 showed that the use of albumin paclitaxel in second-line chemotherapy for advanced non-small cell lung cancer significantly increased the objective remission rate (the proportion of tumor volume reduction), prolonged median progression-free survival and median overall survival compared with docetaxel, and the effect was better in squamous cancer, suggesting that the efficacy of albumin paclitaxel may be better than that of docetaxel in the second-line treatment of squamous lung cancer.
　　Regarding side effects.
　　Allergenicity: Albumin paclitaxel has no added polyoxyethylene-substituted castor oil, which makes it safer compared to docetaxel and does not require antiallergic pretreatment.
　　Hematologic toxicity: The hematologic toxicity of albumin paclitaxel is low, with less effect on leukocytes and neutrophils than docetaxel, while the incidence of peripheral neurotoxicity is higher than that of docetaxel.

PRODUCT TAGS

(4R,5R)-3-(2,2-Dimethylpropanoyl)-2-(4-methoxyphenyl)-4-phenyl-1,3-oxazolidine-5-carboxylicacid;(4S,5R)-3-tert-butoxycarbony-2-(4-anisyl)--phenyl-5-oxazolidinecarboxylicacid;(4S,5R)-2-(4-methoxyphenyl)-4-phenyl-3,5-Oxazolidinedicarboxylicacid3-(1,1-dimethylethyl)ester;sidechainofdocetaxel;(4S,5R)-3-tertChemicalbook-butoxycarbony-2-(4-anisy)-4-phenyl-5-oxazolidinecarboxylicacid;(4S,5R)-2-(4-Methoxyphenyl)-4-phenyl-3,5-oxazolidinedicarboxylicacid3-tert-butylester;(4S,5R)-3-tert-Butoxycarbony-2-(4-anisyl)-4-phenyl-5-oxazolidinecarboxylicacid;(4S,5R)-2-(4-Methoxy-phenyl)-3-N-Boc-4-phenyl-3,5-oxazolidinecarboxylicacid