76 results about "Topotecan" patented technology

A method of using an MMP inhibitor and optionally radiation therapy, and one or more antineoplastic agents of the topoisomerase class selected from the group consisting of irinotecan and topotecan, as a combination therapy for the treatment of neoplasia is disclosed.

Conjugates of transferrin, albumin and polyethylence glycol consisting of native or thiolated transferrin or albumin or of polyethylene glycol (MW between approximately 5,000 and 20,0000) with at least one HS-, HO- or H2N group and cytostatic compounds derived through maleinimide or N-hydroxysuccinimide ester compounds, such as doxorubicin, daunorubicin, epirubicin, idarubicin, mitoxandrone, chloroambucil, melphalan, 5-fluorouracyl, 5'-desoxy-5-fluorouridine, thioguanine, methotrexate, paclitaxel, docetaxel, topotecan, 9-aminocamptothecin, etoposide, teniposide, mitopodoside, vinblastine, vincristine, vindesine, vinorelbine or a compound of general formula A, B, C or D, where n=0-6, X=-NH2, -OH, -COOH, -O-CO-R-COR*, -NH-CO-R-COR*, where R is an aliphatic carbon chain with 1-6 carbon atoms or a substituted or unsubstituted phenylene group and R* H, phenyl, alkyl with 1-6 carbon atoms.

Provided herein are methods for predicting the responsiveness of a cancer to a chemotherapeutic agent using gene expression profiles. In particular, methods for predicting the responsiveness to 5-fluorouracil, adriamycin, cytotoxan, docetaxol, etoposide, taxol, topotecan, PB kinase inhibitors and Src inhibitors are provided. Methods for developing treatment plans for individuals with cancer are also provided. Kits including gene chips and instructions for predicting responsiveness and computer readable media comprising responsivity information are also provided.

Convection-enhanced delivery (CED) is used as a method to deliver a direct infusion of therapeutic agents to the central nervous centre thus circumventing the blood-blood barrier. A non-PEGylated liposomal composition comprising at least one saturated neutral phospholipid and at least one saturated anionic phospholipid and a therapeutic or diagnostic agent encapsulated therein is used to overcome toxicity associated with high peak drug concentration delivered locally CED as well as to increase tissue distribution volume for an improved sustained drug release. In one embodiment, the liposome composition comprises a molar ratio of DSPC:DSPG:CHOL of 7:2:1 and the therapeutic or diagnostic agent is selected from topotecan, conotoxin, gadodiamide or rhodamine, and is used in the treatment of epilepsy

New processes are disclosed for the preparation of camptothecin derivatives, such as, irinotecan and topotecan, as well as new intermediates and compounds related thereof.

The use of radio-labeled antitumor drugs in the treatment of solid tumors by the method of administering a radio-labeled anticancer drug to a patient and imaging at least a part of the patient using Positron Emission Tomography imaging is described. The method can be used to monitor delivery of antitumor drugs to tumors, to predict the effectiveness of therapy with a particular antitumor drug or combination of antitumor drugs, to assess the effectiveness of modulators of cellular accumulation, to individualize therapy and to evaluate the effectiveness of antitumor drugs with respect to particular cancers. Particularly preferred drugs are labeled taxanes, e.g., 11C-paclitaxel and 11C-docetaxel, labeled anthracyclines, e.g., 11C-doxorubicin and 11C-epirubicin, and other radiolabeled drugs, e.g. 11C-topotecan, 11C-SN-38, and 11C-imatinib. The invention further describes antitumor drugs labeled with the radioactive label 11C and methods of preparing radio-labeled drugs.

The invention relates to a thermal sensitive liposome preparation containing camptothecin antineoplastic agents, which contains the camptothecin antineoplastic agents, common lipoid, a phase-change regulator and an optional long-circulating material, wherein the phase-change regulator accounts for 6-100% of the weight of liposome, the long-circulating material accounts for 0-40% of the weight of the liposome, and the weight ratio of the amptothecin antineoplastic agents to the liposome is 1:0.5-1:100. Since the liposome preparation is characterized by thermal sensitivity, when the tissues of a tumor are heated partially, the liposome is targeted to the position of the tumor and releases a lot of medicine at the position of the tumor, thereby improving the curative effect and reducing the overall toxic and side effect. The camptothecin antineoplastic agents of the inveition can include water-solubility derivatives, such as irinotecan and topotecan, and water-insolubility derivatives, such as hydroxycamptothecine, SN-38, 9-NC, and the like.

The present invention relates to treatment of Trop-2 postive cancers with the combination of anti-Trop-2 ADC and a Rad51 inhibitor. Preferably the drug conjugated to the antibody is SN-38, and the ADCis sacituzumab govitecan. The ADC may be administered at a dosage of between 4 mg / kg and 16 mg / kg, preferably 4, 6, 8, 9, 10, 12, or 16 mg / kg. When administered at specified dosages and schedules, the combination of ADC and Rad51 inhibitor can reduce solid tumors in size, reduce or eliminate metastases and is effective to treat cancers resistant to standard therapies, such as radiation therapy, chemotherapy or immunotherapy. Surprisingly, the combination is effective to treat cancers that are refractory to or relapsed from irinotecan or topotecan.

New processes are disclosed for the preparation of camptothecin derivatives, such as, irinotecan and topotecan, as well as new intermediates and compositions thereof.

A process for preparing topotecan.

The present invention generally relates to the fields of cancer therapy and cancer prevention. More particularly, the present invention generally relates to a diagnostic marker for predicting the efficacy of topoisomerase I (topo I) inhibitors in the treatment of cancers. More specifically, the present invention relates to methods, machines, computer systems, computable readable media and kits which can be used to identify and determine the effectiveness of topoisomerase I (topo I) inhibitors in the treatment of cancers, and in some embodiments, the level of sensitivity or resistance of a tumor cell to a topoisomerase I inhibitor, such as camptothecin (CPT), or CTP analogues such as topotecan and irinotecan and derivatives thereof. More specifically, the present invention related to methods, machines, computer systems, computable readable media and kits which can be used to determine the presence of phosphorylation of topoisomerase I polypeptide, in some embodiments phosphorylation at residue serine 10 (S10) of a topoisomerase I polypeptide, wherein the presence of phosphorylation, in particular the phosphorylation at serine 10 of a topoI polypeptide indicates a cancer is likely to be unresponsive to a topo I inhibitor, whereas the absence of phosphorylation, in particular, the absence of phosphorylation at residue serine 10 (S10) identifies a cancer is likely to be responsive to a topo I inhibitor. Other aspect of the present invention relate to phospho-serine 10 topoisomerase I antibodies and other protein binding moieties, and uses thereof.

The invention relates to polymer nano-particles for loading alkaline antitumor drugs. A polymer material forming the nanoparticles has biological compatibility and biodegradability, and the polymer material loads the alkaline antitumor drugs; and the polymer material comprises liposome, polylactic acid, polylactic acid-glycolic acid copolymer, polycaprolactone, chitosan, albumin and cyclodextrin; and the alkaline antitumor drug is a micromolecule antitumor drug with pKa being more than 7.4 and comprises adriamycin, pharmorubicin, taxol, docetaxel, vinblastine, vincristine, topotecan and alkaloid Chinese medicine monomers. The polymer nano-particles solve the defects that the pH dependence and physiological drug fastness cannot be reversed. The polymer nano-particles are free from introducing additional drugs, so that the influence on the internal environment of an organism is small, the pH dependence physiological drug fastness is reversed through the polymer nano-particles, not only is the effect realized, but also since no influence is caused for the internal environment of the organism, the polymer nano-particles are safe to use, little in side effect, and wide in application range.

Conjugates of transferrin, albumin and polyethylence glycol consisting of native or thiolated transferrin or albumin or of polyethylene glycol (MW between approximately 5,000 and 20,0000) with at least one HS-, HO- or H2N group and cytostatic compounds derived through maleinimide or N-hydroxysuccinimide ester compounds, such as doxorubicin, daunorubicin, epirubicin, idarubicin, mitoxandrone, chloroambucil, melphalan, 5-fluorouracyl, 5'-desoxy-5-fluorouridine, thioguanine, methotrexate, paclitaxel, docetaxel, topotecan, 9-aminocamptothecin, etoposide, teniposide, mitopodoside, vinblastine, vincristine, vindesine, vinorelbine or a compound of general formula A, B, C or D, where n=0-6, X=-NH2, -OH, -COOH, -O-CO-R-COR*, -NH-CO-R-COR*, where R is an aliphatic carbon chain with 1-6 carbon atoms or a substituted or unsubstituted phenylene group and R*H, phenyl, alkyl with 1-6 carbon atoms.