19 results about "Topotecan" patented technology

The invention relates to preparation of a novel indole camptothecin derivative and an application of the novel indole camptothecin derivative in an anti-tumor aspect. The structural general formula of the compound is shown in the specification. In-vitro cytotoxic activity screening results show that the novel indole camptothecin derivative has broad-spectrum antitumor activity, and shows relatively strong inhibitory activity on human liver cancer cells (HepG2), human non-small cell lung cancer cells (A549), human colon cancer cells (SW480), human intrahepatic bile duct cancer cells (RBE), human breast cancer cells (MCF-7), human pancreatic cancer cells (BxPC3), human bladder cancer cells (T24) and human bladder cancer cells (umuc3). Wherein the anti-tumor activity of the compound D-18 is the most prominent, the compound D-18 shows a relatively strong inhibition effect on the tested 8 tumor cell lines, the IC50 range is 0.2585-10.69 mu M, the compound D-18 is obviously superior to that of a contrast drug irinotecan, and the activity of the compound D-18 is equivalent to that of topotecan. Therefore, the indole camptothecin derivative is expected to be developed into a novel antitumor drug. # imgabs0 #

Topotecan for use in the treatment of COVID-19 and / or its associated symptoms. Also disclosed is a method of treating an individual infected with a coronavirus, wherein said method comprises the steps of: providing Topotecan: and administering said Topotecan to said individual in a dosage amount sufficient to prevent / stabilize / reduce the risks and / or symptoms associated with a coronavirus infection.

The present invention provides a method for manufacturing a drug-coated balloon and a drug-coated balloon obtained by the method. The method for manufacturing a drug-coated balloon is used to apply a drug coating on the surface of a balloon body prepared in advance and in a filled and expanded state, and the anti-proliferative drug component in the drug coating is one or more of nimustine, carmustine, 5-fluorouracil, fluguanosine, gemcitabine, daunorubicin, doxorubicin, paclitaxel, vinblastine, topotecan, aminoglutethimide, sirolimus, everolimus, and zotarolimus. The drug-coated balloon prepared by the method can effectively ensure that when the balloon enters the human body, the thickness of the drug coating on the balloon surface is more uniform and consistent, thereby improving the clinical use effect.

The application discloses a steroid-indole alkaloid hybrid dimer compound, a preparation method thereof and application of the compound in preparation of an antitumor chemotherapy drug sensitizer, and first prepares the steroid-indole diketopiperazine alkaloid hybrid compound from a fungus Aspergillus sp. EGF15-0-3 rice culture medium. The compound is a new skeleton compound first discovered in nature. It is first discovered that the hybrid compound has Tdp1 inhibitory activity and can be applied as a tyrosine-DNA phosphodiesterase 1 (Tdp1) inhibitor. It is first discovered that the hybrid compound has chemotherapy sensitization activity on a tumor chemotherapy drug topotecan TPT, which provides a drug source molecule and data support for development of a new natural antitumor combination inhibitor, and has important significance for development and utilization of marine Aspergillus sp. fungus resources.

The anti-cancer use of a camptothecin derivative which demonstrates a surprising resistance to the degrading effects of Human Serum Albumin ("HSA") in vivo is disclosed. Since HSA represents about half of serum protein in human blood, previous camptothecins generally worked poorly or not at all in vivo due to inactivation by HSA among other factors. Since NSS-01 is similar in mechanism of action to other camptothecins, and as demonstrated herein has both: (i) greater anti-tumor activity against various human cancers and (ii) less toxicity at therapeutic dosing - than topotecan and irinotecan; and without wishing to be bound by theory, NSS-01 demonstrated desirable antitumor activity against adenocarcinomas, it therefore should demonstrate desirable antitumor activity against other cancers that are susceptible to Topoisomerase I inhibitors.

The present invention belongs to the field of biological extraction technology, and particularly relates to a method for extracting topotecan from sycamore leaves. Sycamore leaves are used as raw materials, soaked in a solvent for extraction for a certain period of time, centrifuged, and the supernatant is filtered. The filtrate is filtered using an organic filter membrane to obtain a filtrate; after resin enrichment, column chromatography, evaporation, and purification, topotecan is obtained. The raw materials used are sycamore leaves, and the method provides a method for effectively treating fallen leaf waste, which can effectively alleviate the environmental problems caused by this type of plant waste, realize the transformation of plant waste into valuables, and has broad application prospects. The preparation process is simple, the extract is high in purity, high in safety, strong in availability, and easy to achieve large-scale production.

This invention relates to the preparation of 10-trifluoromethoxycamptothecin compounds and their use in antitumor drugs. The structural formula of these compounds is shown below. In vitro cytotoxicity screening results show that 10-trifluoromethoxycamptothecin compounds possess broad-spectrum antitumor activity, exhibiting strong inhibitory activity against human hepatocellular carcinoma cells (HepG2), human non-small cell lung cancer cells (A549), human colon cancer cells (SW480), human cholangiocarcinoma cells (QBC939), human breast cancer cells (MCF-7), human pancreatic cancer cells (PANC-1), and human pancreatic cancer cells (BxPC-3). Compounds 10-trifluoromethoxycamptothecin I and 7-ethyl-10-trifluoromethoxycamptothecin II showed strong inhibitory effects against all seven tested tumor cell lines, with IC50 values ​​exceeding 100%. 50 The concentrations were 0.913–0.0661 μM and 4.932–0.0578 μM, respectively, both significantly superior to the control drug topotecan. Among them, compounds I and II exhibited the strongest inhibitory activity against the BxPC-3 cell line, with IC50 values ​​of [missing value]. 50 The values ​​were 0.0661±0.0065μM and 0.0578±0.0043μM, respectively. Therefore, 10-trifluoromethoxycamptothecin compounds hold promise for development into a novel antitumor drug.

This invention discloses a non-cationic polymer siRNA and chemical drug co-delivery system, comprising a non-cationic polymer and a complex of siRNA and drug loaded on the polymer; the complex is composed of a target siRNA and a corresponding drug; the non-cationic polymer contains several branches with aromatic rings, the aromatic rings being selected from one or more of 5- to 15-membered aromatic rings or 5- to 15-membered heteroaromatic rings; the drug is selected from one or more of gemcitabine, mitoxantrone, topotecan, beloteccan, irinotecan, doxorubicin, camptothecin, and derivatives of any of the above drugs. This invention enables the synergistic delivery of siRNA and chemical drugs, effectively overcoming the cytotoxicity problems caused by cationic delivery systems, and demonstrates promising application prospects in the field of modern drug delivery.

Disclosed herein is use of a combination of Compound (A), or a pharmaceutically acceptable salt thereof, (also known as azenosertib or ZN-c3) and Compound (B), or a pharmaceutically acceptable salt thereof, or an antibody -drag conjugate comprising Compound (B), or a pharmaceutically acceptable salt thereof, for treating a disease, such as a cancer, wherein Compound (B) can be a topoisomerase I inhibitor (e.g., topotecan, belotecan, irinotecan, SN-38, govitecan, exatecan or deruxtecan).

Disclosed are methods, compositions, and kits for treating pediatric cancers using hydroxyureamethyl acylfulvene (LP-184) or pharmaceutically acceptable salts / solvates thereof. The methods include monotherapy and combination regimens for pediatric sarcoma, medulloblastoma, glioma (including DIPG), hepatoblastoma, Wilms tumor, and related malignancies. Combination therapies include LP-184 with vincristine, topoisomerase I poisons (topotecan or irinotecan), PARP inhibitors (e.g., rucaparib), or spironolactone, yielding additive or greater-than-additive reductions in tumor growth or cell viability.

The present application relates to a kind of preparation of new indole camptothecin derivatives and its use in antitumor, the structure of the compound general formula is shown as follows.In vitro cytotoxic activity screening results show that new indole camptothecin derivatives have broad-spectrum antitumor activity, to human hepatoma cell (HepG2), human non-small cell lung cancer cell (A549), human colon cancer cell (SW480), human intrahepatic cholangiocarcinoma cell (RBE), human breast cancer cell (MCF-7), human pancreatic cancer cell (BxPC3), human bladder cancer cell (T24), human bladder cancer cell (umuc3) show strong inhibitory activity. Among them, the antitumor activity of compound D-18 is most outstanding, and shows strong inhibition to the 8 tumor cell lines measured, IC 50 The range is 0.2585-10.69 μM, significantly better than the control drug irinotecan, and comparable to topotecan activity. Therefore, indole camptothecin derivatives are expected to be developed into a new antitumor drug.

An object of the present invention is to provide a medicinal drug obtained by combining a liposome composition encompassing topotecan or a salt thereof and a DNA damage repair inhibitor. According to the present invention, there is provided a medicinal drug including in combination: (A) a liposome composition that contains a liposome having an inner water phase and contains an aqueous solution which is an outer water phase and disperses the liposome, where the liposome encompasses topotecan or a salt thereof, and a lipid constituting the liposome includes dihydrosphingomyelin; and (B) a DNA damage repair inhibitor. The liposome composition and the DNA damage repair inhibitor are administered at the same time or sequentially.

A method for treating cancer, especially small-cell lung cancer with a compound of formula I, e.g. compound A, the pharmaceutically acceptable salt or the solvate thereof, as a focal adhesion kinase inhibitor. A pharmaceutical combination or a kit comprising the compound and a chemotherapy agent, e.g. topotecan, etoposide, or carboplatin.

The disclosed method rapidly identifies with desired accuracy AML patients, including elderly AML patients, likely to respond to treatment with a combination of a farnesyltransferase inhibitor and one or more of etoposide, teniposide, tamoxifen, sorafenib, paclitaxel, temozolomide, topotecan, trastuzumab and cisplatinum. In an embodiment, the improvements include the use of whole blood rather than the customary bone marrow sample, thus making the assay more accurate, rapid, less intrusive, less expensive as well as less painful. The method includes evaluation of a two-gene expression ratio (RASGRP1:APTX), which with a corresponding threshold, provides sufficient accuracy for predicting the response to the combination treatment. In the preferred embodiment the combination treatment combines tipifarnib (R115777, ZARNESTRA®) with etoposide. Further, the elderly AML patients identified as being likely responsive to the combination treatment with tipinifarb and etoposide have a complete recovery rate comparable to the best therapy available for younger patients.

Pharmaceutical compositions comprising oil as a vehicle, a suspending agent, and a surfactant are disclosed to be used in conjunction with active pharmaceutical ingredients which are water soluble or insoluble, or which are sensitive to water but insoluble in oil. Such active pharmaceutical ingredients may include temozolomide, lenalidomide, Oxaliplatin, Cisplatin, Carboplatin, 5-fluorouracil, irinotecan, topotecan, cyclophosphamide, doxorubicin, vincristine, vinblastine, Melphalan, Chlorambucil, Dacarbazine, Daunorubicin, Epirubicin, Mitoxantrone, Etoposide, Teniposide, Azacitidine, Cytarabine, Gemcitabine, vinoralbine, Pemetrexed, a derivative thereof, or a combination thereof. The pharmaceutical compositions may be administered as an oral suspension. Other embodiments are directed towards methods of using and methods of making such formulations.

This invention relates to a novel *Bletilla striata* alkaloid boric acid compound, its preparation method, and its use in the preparation of antitumor drugs. The general chemical formula of this class of compounds is shown in structural formulas (I) and (II). In vitro antitumor activity screening results showed that compounds of formulas I and II possess broad-spectrum antitumor activity, exhibiting strong inhibitory activity against human liver cancer (HepG2), human pancreatic cancer (SW1990), human ovarian cancer (A2780), human breast cancer (MCF7), and human colon cancer (SW480) cell lines. Compounds N-3 and N-4 showed strong inhibitory effects against all five tested tumor cell lines, with IC50 values ​​exceeding 100%. 50 The values ​​were 0.26–0.89 μM and 0.22–0.91 μM, respectively; compounds N-1, N-3, and N-4 exhibited strong inhibitory effects on the human pancreatic cancer (SW1990) cell line, with IC50 values ​​of 0.26–0.89 μM and 0.22–0.91 μM, respectively. 50 The concentrations were 0.97, 0.45, and 0.63 μM, respectively, significantly superior to the control drug topotecan; simultaneously, compounds N-3 and N-4 also exhibited strong inhibitory effects on the human breast cancer (MCF7) cell line, with IC50 values ​​of 0.97, 0.45, and 0.63 μM. 50 The concentrations were 0.80 and 0.65 μM, respectively, significantly better than the control drug topotecan. Therefore, the new cypermethrin borate compound holds promise for development into a novel antitumor drug.

The present application relates to a kind of preparation of trifluoromethyl camptothecin compound and its use in antitumor drugs, the structural formula of the compound is shown as follows.In vitro cytotoxic activity screening results show that trifluoromethyl camptothecin compound has broad-spectrum antitumor activity, to human hepatocellular carcinoma cell (HepG2), human non-small cell lung cancer cell (A549), human colon cancer cell (SW480), human cholangiocarcinoma cell (QBC939), human breast cancer cell (MCF-7), human pancreatic cancer cell (PANC-1), human pancreatic cancer cell (BxPC-3) shows strong inhibitory activity.4 trifluoromethyl camptothecin compounds I, II, III, IV all show strong inhibition to the 7 tumor cell lines measured, IC 50 Value is 0.503-0.0112 μM, 4.8477-0.6516 μM, 1.825-0.0005 μM and 4.9043-0.4612 μM, all significantly better than control drug topotecan. Among them, the compound shows the strongest inhibitory activity to BxPC-3 cell line, IC 50 Value is in the range of 0.6516-0.0005 μM. Therefore, trifluoromethyl camptothecin compound is expected to be developed into a new antitumor drug.

The invention belongs to the technical field of neuroblastoma, and particularly discloses a prognosis improvement and treatment sensitivity determination method and system for NBL patients, and the method comprises the steps: collecting and preprocessing data, constructing a gene co-expression network, screening immune-related modules in the gene co-expression network, and obtaining immune-related prognosis features. According to the method, neuroblastoma patients are subjected to immunotherapy, a novel immune-related risk stratification model NIRSM is constructed, prognosis, immunotherapy and chemotherapy reactions of the neuroblastoma patients are predicted, the novel immune-related risk stratification model NIRSM shows that the patients in a low-risk group show better immunotherapy reactions, and differences of reactions of the patients in different groups to certain chemotherapy drugs are predicted. Cyclophosphamide and topotecan are more sensitive in a low-risk group, and cis-platinum and docetaxel are more sensitive in a high-risk group. By adopting the technical scheme, the optimal clinical prognosis and treatment strategy are promoted, and the progress of neuroblastoma patients with different risks can be known.

The invention belongs to the technical field of biological extraction, and particularly relates to a method for extracting topotecan from phoenix tree leaves. The method comprises the following steps: soaking phoenix tree leaves serving as a raw material in a solvent, extracting for a certain time, centrifuging, taking supernate, filtering, and filtering by using an organic filter membrane to obtain filtrate; and carrying out resin enrichment, column chromatography, drying by distillation and purification to obtain the topotecan. The used raw material is phoenix tree leaves, a method capable of effectively treating the fallen leaf garbage is provided, the environmental problem caused by the plant garbage can be effectively relieved, the plant garbage is turned into wealth, and the application prospect is wide. The preparation process is simple, the extract is high in purity, high in safety and strong in availability, and large-scale production is easy to realize.