67 results about "Temozolomida" patented technology

This invention generally relates to novel compositions and methods for the treatment of certain cancers. Additionally, this invention relates to novel compositions and methods to screen drugs for the treatment of certain cancers. Specifically, the invention contemplates that temozolomide and methoxyamine, in combination or in sequence, shall be used as a treatment for certain tumors that are resistant to treatment by temozolomide alone.

The use of dianhydrogalactitol provides a novel therapeutic modality for the treatment of non-small-cell lung carcinoma (NSCLC) and ovarian cancer, as well as other types of malignancy, including brain metastases of NSCLC. Dianhydrogalactitol acts as an alkylating agent on DNA that creates N⁷ methylation. Dianhydrogalactitol is effective in suppressing the growth of cancer stem cells and is active against tumors that are refractory to temozolomide, cisplatin, and tyrosine kinase inhibitors; the drug acts independently of the MGMT repair mechanism. Dianhydrogalactitol can be used together with other anti-neoplastic agents and can possess additive or super-additive effects.

The present invention relates to tetraaza phenalen-3-one compounds which inhibit poly (ADP-ribose) polymerase (PARP) and are useful in the chemosensitization of cancer therapeutics. The induction of peripheral neuropathy is a common side-effect of many of the conventional and newer chemotherapies. The present invention further provides means to reliably prevent or cure chemotherapy-induced neuropathy. The invention also relates to the use of the disclosed PARP inhibitor compounds in enhancing the efficacy of chemotherapeutic agents such as temozolomide. The invention also relates to the use of the disclosed PARP inhibitor compounds to radiosensitize tumor cells to ionizing radiation. The invention also relates to the use of the disclosed PARP inhibitor compounds for treatment of cancers with DNA repair defects.

The invention discloses a binary solution type formulation for intravenous and intracerebral injection, shown as right. The main active component thereof is temozolomide with the binary system and having temozolomide sterile powder and solvent for dissolving medicaments. The operating temozolomide solution agent can be obtained through the combination of the solvent. The invention is characterized in that, 1, the binary formulation is stable at the room temperature for over 2 years; 2, the prepared medicaments liquid is stable at the room temperature at least for 48h to meet the operating requirement of injection administration; 3, the solvent is nontoxic and non-irritant, and the prepared medicaments can be used for the intracerebral injection during the operation and stereotaxic intraturmor injection of local chemotherapy.

This invention relates to unit dosage forms of temozolomide. These unit dosage forms are particularly well-suited for decreasing the pill burden and increasing patient compliance. The invention also relates to methods of treating proliferative disorders in a patient with these unit dosage forms. The invention additionally relates to kits comprising these unit dosage forms.

The invention discloses a modified optimized synthetic method for temozolomide and an intermediate thereof. The synthetic method is characterized in that a new oxidation ring-closing reagent is introduced for a reaction with lithium chloride and sodium nitrite in an aqueous solution, and the synthetic method helps to improve the yield of the reaction, increase the controllability on the reaction and avoid usage of methyl isocyanate with relatively high toxicity.

Disclosed is a slow release injection agent of anticancer composition containing platinum-group compounds and synergistic agent, which comprises slow release microspheres and dissolvent, wherein the slow release microspheres comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being conventional dissolvent or specific dissolvent containing suspension adjuvant. The viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose, the platinum-group compounds are selected from cisplatin, Carboplatin, Nedaplatin or Oxaliplatin, the synergistic agent can be selected from tetrazine drugs such as Mitozolomide or Temozolomide, and / or anticancer antibiotics such as Adriamycin, Aclarubicin, Epirubicin, mitomycin or pidorubicin, the slow release auxiliary materials are selected from polyphosphate ester copolymers such as p(LAEG-EOP), p(DAPG-EOP), copolymer or blend of polyphosphate ester with polylactic acid, Polifeprosan, sebacylic acid and PLGA. The anticancer composition can also be prepared into slow release implanting agent for injection or placement in or around tumor with a period of effective concentration maintenance over 60 days, as well as the treatment effect of appreciably lowering general reaction of the drugs, and improving the treatment effect of the non-operative treatment methods such as chemotherapy.

The invention relates to a pharmaceutical preparation, in particular to a compound pharmaceutical preparation with ginsenoside Rh2 and temozolomide as medicine active ingredients.

Provided are methods and compositions for use in therapy, and in particular for treating cancer, preferably drug-resistant cancer, and/or radiation resistant cancer. The compounds may be used for reducing tumor size in a mammalian subject and for inducing apoptosis in a tumor cell. The methods are effective on tumor cells that are resistant to drugs such as temozolomide, doxorubicin, and geldanamycin, as well as non-resistant tumor cells. Further provided are barbiturate and thiobarbiturates diene compounds for use in treating cancer, and uses, methods and compositions relating to these compounds.

Disclosed herein is a method for the prevention, delay of progression or treatment of cancer in a subject, comprising administering to the subject in need thereof a PARP inhibitor, particularly, (R)-2-fluoro-10a-methyl-7, 8, 9, 10, 10a, 11-hexahydro-5, 6, 7a, 11-tetraazacyclohepta [def] cyclopenta [a] fluoren-4 (5H)-one, a sesqui-hydrate thereof, or a pharmaceutically acceptable salt thereof, in combination with temozolomide and/or radiation therapy. Also, disclosed a pharmaceutical combination comprising a PARP inhibitor, particularly, (R)-2-fluoro-10a-methyl-7, 8, 9, 10, 10a, 11-hexahydro-5, 6, 7a, 11-tetraazacyclohepta [def] cyclopenta [a] fluoren-4 (5H)-one, a sesqui-hydrate thereof, or a pharmaceutically acceptable salt thereof, in combination with temozolomide and the use thereof.

The invention relates to sustained release temozolomide capsules and a preparation method thereof, and belongs to the technical field of medicine. Each sustained release temozolomide capsule comprises2-20 sustained release micro-tablets and a capsule shell, wherein each micro-tablet contains 2-20 mg of temozolomide. The sustained release micro-tablets comprise raw and auxiliary materials in percentage by weight as follows: 5%-50% of temozolomide, 5%-40% of a diluent, 10%-70% of a sustained release agent, 0.5%-2% of an antioxidant, 0-5% of an adhesive and 0.5%-2% of a lubricant. The inventionfurther discloses the preparation method of the sustained release temozolomide capsules. The materials are pelletized or mixed and pressed into the micro-tablets directly, and the micro-tablets are loaded to hollow capsules quantitatively. The sustained release temozolomide capsules have the advantages of being good in dissolution, convenient to use, stable in plasma concentration and long in acting time, compliance of patients is improved, the preparation process is simple and lower in cost, and industrial production is easy.

The present invention discloses general formula I of Temozolomide-8-carboxylate compounds, the process for preparation, pharmaceutical compositions comprising the compounds and the use of the compounds and pharmaceutical compositions for the manufacture of an antitumor medicament. The said pharmaceutical composition comprises one or more general formula I Temozolomide-8-carboxylate compounds as active ingredient, together with conventional pharmaceutical carriers. The composition also comprises one or more pharmaceutically acceptable acidic material, optionally second or tertiary alcohol or ester or ether derivatives thereof. The said pharmaceutical composition can be made into various common formulations, particularly oral formulations as well as topically transdermal patches. The present invention also discloses the application of the compounds and the compositions to treat tumor.

The invention discloses an injectable anticancer drug temozolomide freeze-dried powder injection preparation and its preparation method. The powder injection preparation is stable, controllable in quality, simple in preparation process and strong in operability, and a prepared product has the characteristics of good solubility, convenient clinical use, a long period of storage and the like.

Disclosed is a slow release injection agent of anticancer composition containing nitrosourea drugs and synergistic agent, which comprises slow release microspheres and dissolvent, wherein the slow release microspheres comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being conventional dissolvent or specific dissolvent containing suspension adjuvant. The viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose, the nitrosourea drugs are selected from Carmustine, Nimustine or Fotemustine, the synergistic agent can be selected from tetrazine drugs such as Mitozolomide or temozolomide and / or anticancer antibiotics such as Adriamycin, Aclarubicin, Epirubicin, mitomycin or pidorubicin, the slow release auxiliary materials are selected from polyphosphate ester copolymers such as p(LAEG-EOP), p(DAPG-EOP), copolymer or blend of polyphosphate ester with polylactic acid, Polifeprosan, sebacylic acid and PLGA. The anticancer composition can also be prepared into slow release implanting agent, for injection or placement in or around tumor with a period of effective concentration maintenance over 60 days, as well as the treatment effect of appreciably lowering general reaction of the drugs, and improving the treatment effect of the non-operative treatment methods such as chemotherapy.

The invention relates to eutectic crystal of temozolomide and baicalein as well as a preparation method for the eutectic crystal. Specifically, an X-ray powder diffraction pattern of the eutectic crystal has characteristic peaks with 2 theta value being 7.7 +/-0.2 degree, 8.6+/-0.2 degree, and 12.7+/-0.2 degree. The eutectic crystal provided by the invention has obvious advantages in stability, solubility, pharmacokinetic properties and the like of two pharmaceutical ingredients in comparison with existing temozolomide and baicalein bulk drugs, has an important value in developing drug combination of two drugs.

The invention provides a nano-composite formed by a DNA tetrahedron and temozolomide, and preferably, the nano-composite is also covalently connected with a nucleic acid aptamer AS1411 and/or a nucleic acid aptamer GS24. The invention also provides a preparation method of the composite.The method comprises the following steps of carrying out oscillation incubation on the DNA tetrahedron and the temozolomide, centrifuging, and taking the supernatant to obtain the composite The invention also provides application of the composite in preparation of anti-tumor drugs, especially anti-glioma drugs.Compared with the temozolomide, the composite has higher efficacy, can reverse the drug resistance of tumor cells to temozolomide, and has good application prospects.

The invention provides a biomarker for detecting glioma prognosis or temozolomide drug resistance. The biomarker comprises a first marker for displaying the expression level of a ferritin light chain (FTL) and a second marker for displaying the expression level of a ferritin heavy chain 1 (FTH1). The invention also provides an application of the gene in preparation of a diagnostic reagent. The invention provides a very clear indication index for glioma prognosis, and successfully provides a guiding reference for clinical prognosis prediction and treatment modes of patients.

The invention discloses a temozolomide and hesperetin cocrystal and a preparation method thereof. The molar ratio of temozolomide to hesperetin in the cocrystal is 1:1, and an X-ray powder diffractionpattern of the cocrystal has characteristic peaks when the 2theta values are 11.9+/-0.2 degrees, 25.3+/-0.2 degrees, 26.8+/-0.2 degrees and 27.1+/-0.2 degrees. The cocrystal preparation method provided by the invention is simple in process, the crystallization process is easy to control, the reproducibility is good, and the method is suitable for industrial production. The cocrystal can effectively improve the stability and tabletting property of temozolomide, improve the solubility of hesperetin and slow down the dissolution of temozolomide, and provides a research basis for treatment of cancer by combining temozolomide and hesperetin.