Topotecan Hcl Powder CAS 119413-54-6

Topotecan Hcl Powder is a water-soluble camptothecin derivative, which is the hydrochloride form of topotecan. It was successfully developed by SmithKline Beecham company of the United States. In 1996, FDA approved it to be listed in the United States. which is a second-line therapeutic drug for the treatment of ovarian cancer (OVC).

In 1999, the US Food and Drug Administration approved topotecan hydrochloride as a therapeutic drug for small cell lung cancer (SCLC), which has been listed in dozens of countries and regions such as Britain, Germany, and France. At present, it has been listed in China, and the market prospect is promising.

What is the mechanism of action of topotecan hydrochloride?

Topotecan Hcl Powder is an inhibitor of topoisomerase ⅰ. Topology isomerase ⅰ can induce DNA single-strand reversible breakage, loosen DNA spiral strand, and topotecan can combine with topoisomerase ⅰ-DNA complex, thus hindering the reconnection of broken DNA single strand. The ternary complex of topotecan, topoisomerase ⅰ, and DNA interacts with replicas, resulting in the damage of double-stranded DNA, but mammalian cells cannot effectively repair the damaged DNA double-stranded. Its cytotoxic effect is in the process of DNA synthesis, and it is an S-phase cell cycle-specific drug. Topotecan hydrochloride has strong anti-tumor activity and an extensive anti-tumor spectrum. Pre-clinical in vivo anti-tumor tests show that it has an obvious anti-tumor effect on various animal transplanted tumor models such as L1210 and P388 leukemia, B16 melanoma, B16/F10 melanoma sub-strain, Lewis lung cancer, ADJ-PC6 plasma cell tumor, colon cancer 38 and 51, M5076 sarcoma, breast cancer 16/C, Madison lung cancer, etc.

What are the studies on this product on pregnant mice?

Topotecan Hcl Powder has strong teratogenic and reproductive toxic effects on fetal rats. The administration of topotecan hydrochloride 0.1mg/kg/day (about equivalent to the basic clinical dose of mg / m2) for use in rabbits from 6 to 20 days of pregnancy can cause a toxic reaction, embryo death, or weight loss in fetal rabbits. The administration of topotecan hydrochloride 0.23mg/kg/day (about equivalent to the basic clinical dose of mg / m2) for use in rats from mating to 6 days of pregnancy for 14 days can lead to embryo absorption, fetal rat small eyes, loss before implantation and the mild toxic reaction of female rats. The basic dose of ofloxacin hydrochloride (0.1mg / m2 / day) and the basic dose of ofloxacin hydrochloride (0.1mg / m2 / day after implantation can increase the mortality of pregnant rats. The most common malformation sites are eyes (small eyes, no eyes, retinal rosette formation, retinal defect, ectopic eye socket), brain (expansion of lateral ventricle and third ventricle), skull, and vertebrae. Therefore, it is forbidden for pregnant women and lactating women.

Is topotecan hydrochloride effective in treating lung cancer?

There are many patients with lung cancer nowadays, most of whom are related to air pollution and the absorption of smoke products. For example, tobacco contains various chemical components, but many of them are harmful to the human body. They can damage the normal replication of DNA in human bronchial epithelial cells, making it easy to compile erroneous cells, which may include activated cancer cells. The factors that normally inhibit cancer cells may be unable to fight due to poor living conditions, leading to cancer. At present, chemotherapy is still the main method for treating lung cancer. Clinical applications have found that the efficacy of chemotherapy for small cell lung cancer can be confirmed in both early and late stages, and even about 1% of early small cell lung cancer patients are cured through chemotherapy. Chemotherapy generally cannot cure non-small cell lung cancer, it can only prolong the patient's survival and improve their quality of life. According to relevant statistical data, the tumor response rate of chemotherapy for non-small cell lung cancer is 40% to 50%. For first-line chemotherapy failures, the use of topotecan hydrochloride and cisplatin as second-line treatment has become the mainstream for patients with extensive stage small cell lung cancer. However, the most common adverse reaction of topotecan hydrochloride powder is bone marrow suppression, mainly neutropenia. Therefore, when using it, it should be used under the guidance and observation of a chemotherapy pharmacist to promptly and effectively handle related adverse events.

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