29 results about "Irinotecan" patented technology

The invention discloses an irinotecan and afatinib maleate co-loaded liposome preparation as well as a preparation method and application thereof, irinotecan and afatinib maleate are taken as effective components of the liposome, and the liposome comprises a liposome carrier, an inner water phase positioned in a liposome membrane and an outer water phase positioned outside the liposome membrane; the irinotecan and the afatinib maleate are encapsulated in the inner water phase; the inner water phase comprises an ammonium salt aqueous solution, and an ammonium salt gradient exists between the inner water phase in the liposome membrane and the outer water phase outside the liposome membrane; the outer water phase is a physiological isotonic solution. According to the present invention, the research results show that the irinotecan and afatinib maleate co-carrying liposome can simultaneously deliver the two drugs with the synergistic ratio into the same tumor cell compared to the irinotecan single drug liposome and the afatinib maleate single drug liposome so as to maximize the synergistic effect of the drugs, and significantly improve the anti-tumor effect;

The invention discloses an application of pegylated irinotecan in preparation of a medicine for preventing and / or treating triple-negative breast cancer brain metastasis diseases, which is shown by in-vivo imaging observation and lifetime observation of high, medium and low dose groups of pegylated irinotecan with a specific structure. The high-dose group, the medium-dose group and the low-dose group all have a definite anti-tumor effect, bioluminescence signal values are inhibited to different degrees, the lifetime is prolonged, and the lifetime of the high-dose group and the lifetime of the medium-dose group are remarkably longer than that of the NKTR-102 group.

This disclosure particularly relates to combination therapy of oncolytic adenoviruses with topoisomerase I inhibitors or their prodrugs (such as topotecan or SN-38) or prodrugs of topoisomerase inhibitors (such as irinotecan) for the treatment or prevention of ovarian cancer, cervical cancer, lung cancer, colon or colorectal cancer and / or pancreatic cancer.

The application relates to the technical field of aspirin pharmaceutical chemistry, in particular to an aspirin-sulfonamide hybrid, a preparation method and application thereof. The preparation method can synthesize a plurality of novel aspirin-sulfonamide hybrids by taking piperazine as a bridge, and by a three-step continuous method of "acyl chlorination, sulfonamidation and N-acylation" according to a "molecular hybridization principle". In the process, only one separation and purification is performed, and the preparation steps are simple. The aspirin-sulfonamide hybrid prepared by the method is most effective on human non-small cell lung cancer cells A549, and the activity is more than 33 times higher than that of a parent aspirin, and is similar to the activity of an anticancer drug irinotecan. The aspirin-sulfonamide hybrid 3k prepared by the method has a certain inhibitory effect on various cancer cells. The hybrid can induce human non-small cell lung cancer A549 cell apoptosis in a concentration-dependent manner, and can induce human non-small cell lung cancer A549 cell cycle arrest in the G0 / G1 phase, and inhibit cell growth.

This invention provides an irinotecan-conjugated polypeptide compound, its preparation method, and its application, belonging to the field of biomedical technology. Irinotecan (Dxd) is the active pharmaceutical ingredient. Irinotecan belongs to the topoisomerase I inhibitor class—camptothecin derivatives—and is a semi-synthetic small molecule chemotherapeutic drug capable of directly killing cancer cells in the active division phase and inhibiting tumor growth. TYLCTACDYTHH is a highly effective PDPN-targeting peptide that can effectively target the PDPN site in human glioblastoma. In vitro and in vivo experimental results show that the conjugated compound of this invention can significantly inhibit the proliferation of primary glioblastoma cells and effectively inhibit the growth of intracranial orthotopic xenografts in NOD-SCID mice, demonstrating good anti-tumor activity. This compound shows promise for targeted therapy of glioblastoma and has the potential to prolong patient survival.

The application discloses a kind of endoplasmic reticulum of tumor cell can be targeted N -(2-hydroxypropyl) methacrylamide (HPMA) polymer-drug conjugate. The chemotherapeutic drug carried by the HPMA polymer is at least one of doxorubicin, epirubicin, pirarubicin, cisplatin, oxaliplatin, camptothecin, paclitaxel, gemcitabine, methotrexate, vinblastine, mitoxantrone, irinotecan, and the linker for connecting the drug and the HPMA polymer is at least one of hydrazone bond, amide bond, ester bond, disulfide bond, and ketosulfenyl bond. The HPMA polymer-drug conjugate targets the drug to the endoplasmic reticulum through receptor-ligand interaction, can cause severe endoplasmic reticulum stress, thereby transporting a large amount of calnexin to the tumor cell membrane surface, greatly improving the immunogenicity of tumor cells, and promoting tumor immunotherapy.

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.

This invention describes methods for treating or ameliorating the symptoms of cancer in a subject with agents, compositions and regimens designed to promote anti-tumor effects and avoid drug resistance effects. Combinations of active agents can be used including agents for inhibiting or suppressing expression of TGF-β2 in combination with an irinotecan-containing agent, regimen or formulation, for example, a FOLFIRINOX agent, a NALIRIFOX agent, an IRIFOX agent, or an IRINOX agent. Biomarkers can be used to select subjects who benefit from such therapeutics.

The present invention relates inter alia to aptamers that specifically bind to Irinotecan and methods of using the same.

The application relates to the field of medicine, in particular to the application of 4-hydroxyphenylacetic acid and irinotecan as cancer chemotherapy drugs. In view of the technical defects that the existing irinotecan chemotherapy hepatoprotective drugs have single action and may interfere with the chemotherapy effect, the application provides the application of 4-hydroxyphenylacetic acid and irinotecan in the preparation of cancer chemotherapy drugs. The application has the following advantages: 1. clear hepatoprotective effect: 4HPAA can significantly alleviate the liver fatty degeneration induced by irinotecan; 2. significant synergistic anti-tumor effect: the tumor inhibition effect of the combination of 4HPAA and irinotecan is significantly better than that of the single-drug group; 3. high safety; and 4. great clinical transformation potential.

This invention describes methods for treating or ameliorating the symptoms of cancer in a subject with agents, compositions and regimens designed to promote anti-tumor effects and avoid drug resistance effects. Combinations of active agents can be used including agents for inhibiting or suppressing expression of TGF-β2 in combination with an irinotecan-containing agent, regimen or formulation, for example, a FOLFIRINOX agent, a NALIRIFOX agent, an IRIFOX agent, or an IRINOX agent. Biomarkers can be used to select subjects who benefit from such therapeutics.

The application discloses application of a pharmaceutical composition with GL-V9 and a chemotherapeutic drug as active ingredients in treatment of tumors, and the GL-V9 can obviously achieve a drug synergistic effect when the GL-V9 is combined with a classical chemotherapeutic drug to treat tumors, and the effect is obviously superior to combination of similar drugs and the chemotherapeutic drug. The chemotherapeutic drugs include PARP1 inhibitors, capecitabine, irinotecan, sorafenib, cisplatin or 5-fluorouracil; and the tumor types include leukemia, colorectal cancer and lung cancer.

The present invention describes a method for treating or improving the symptoms of cancer in subjects with agents, compositions, and regimens designed to promote anti-tumor effects and avoid drug resistance.A combination of active agents can be used, including agents, regimens, or preparations containing irinotecan, such as FOLFIRINOX, NALIRIFOX, IRIFOX, or IRINOX, and agents for inhibiting or suppressing the expression of TGF-β2.Biomarkers can be used to select subjects who will benefit from such therapeutic agents. TIFF2026507184000026.tif117156

Methods of treating, suppressing, or reducing the severity of a liver cancer in a subject are described herein. The disclosed methods include administering to the subject a first amount of safranal or a pharmaceutically acceptable pro-drug thereof and administering to the subject a second amount of a TOP1 inhibitor. In some embodiments, the TOP1 inhibitor is irinotecan, topotecan, camptothecin, lamellarin D, and / or combinations thereof.

The present application belongs to the technical field of biomedical materials and nano drugs, and discloses a polypeptide nano drug capable of inducing necrosis and autophagy related synergistic apoptosis and a preparation method and application thereof. X-DDP1 and DDP1 are self-assembled to form a responsive polypeptide nano drug, which provides a delivery platform for broad-spectrum chemotherapy drugs such as buforin RBG, irinotecan CPT11 or camptothecin CPT, realizes a Caspase-3 / GSH double-response mechanism, improves drug release specificity and spatial controllability, can promote RIPK3 aggregation and activate necrotic apoptosis in cells, can effectively inhibit the growth of cancer, and has potential clinical application value.

This invention discloses an alkaloid, its preparation method, and its application in the preparation of human carboxylesterase 2 inhibitors. The residue of Paeonia lactiflora after ultrasonic extraction was extracted with 95% ethanol and then with ethyl acetate to obtain ethyl acetate extract CS-5. Separation was performed by silica gel column chromatography, using a gradient elution with petroleum ether-acetone mixed solvent and dichloromethane-methanol mixed solvent to obtain six eluent fractions, named A-F. Compound D was separated by silica gel column chromatography, Sephadex LH-20 column chromatography, and semi-preparative HPLC to obtain compound I-2. Compound F was separated by Sephadex LH-20 column chromatography and semi-preparative HPLC to obtain compounds I-1 and I-3. Compound I-1 was separated by a chiral HPLC column to obtain enantiomers I-(+)-1 and I-(–)-1. The four alkaloids of this invention have a pH range of 13.65–14.16. m At concentrations of M, it can significantly inhibit the activity of human carboxylesterase 2. Therefore, it can be applied to the preparation of attenuated and protective agents for anticancer drugs such as irinotecan.

This invention belongs to the field of nanoprodrug technology, specifically relating to an NQO1-activated prodrug, its preparation method, and its applications. The prodrug molecule of this invention can self-assemble into a stable nanodrug in an aqueous phase without the use of excipients. This nanodrug exhibits good structural stability, possesses both active and passive targeting capabilities, and achieves specific recognition of tumor cells, resulting in precise chemotherapy, improved treatment efficiency, and reduced toxic side effects on normal cells. Furthermore, the release of irinotecan can be monitored in real time using changes in its fluorescence. The preparation method is simple and holds promise for widespread application in the specific treatment of cancers with NQO1 overexpression.

The invention belongs to the technical field of medicinal chemistry, and discloses a human carboxylesterase 2A (hCES2A) self-activated covalent inhibitor as well as a preparation method and application thereof. The inhibitor is a novel benzamide-O-carbamate derivative (I) with a structure as shown in a formula (I) and pharmaceutically acceptable salts thereof, and the compound can powerfully and highly selectively inactivate the activity of human intestinal tract hCES2A. Further, the oral bioavailability of the oral prodrug is improved or the intestinal toxicity caused by the carboxylesterase 2A activated prodrug (such as irinotecan) is relieved. The IC50 value of the compound for inhibiting human carboxylesterase 2A can reach a nanomole level and is dose-dependent and time-dependent. The compound provided by the invention also has good safety, and has the advantages of simple preparation process, high yield and the like, which indicates that the compound has good application prospects.

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 invention discloses an oligosaccharide compound preparation capable of remarkably relieving irinotecan chemotherapy-induced intestinal injury, which is prepared by compounding alginic acid oligosaccharide, fructo-oligosaccharide and stachyose according to the mass ratio of (40-60): (20-30): (20-30), the alginic acid oligosaccharide, the fructo-oligosaccharide and the stachyose are high in safety and free of side effects, and can be applied to relieving irinotecan-induced chemotherapy-induced intestinal injury, and the three components cooperate to effectively promote proliferation of beneficial bacteria, so that the curative effect of irinotecan on the chemotherapy-induced intestinal injury is improved. The micro-ecological environment of the intestinal tract is improved from the source; intestinal inflammation caused by chemotherapy is rapidly inhibited, and release of inflammatory factors is reduced; the damaged intestinal mucosa is repaired, and the intestinal barrier function is enhanced; the technical effect of the irinotecan preparation is obviously better than that of a single oligosaccharide preparation or a pairwise compounded preparation, and the irinotecan preparation can effectively solve the clinical pain point of intestinal discomfort in the irinotecan chemotherapy process, so that smooth chemotherapy is guaranteed. Meanwhile, the preparation process disclosed by the invention does not need complex equipment, is simple and convenient to operate, has strong controllability, is suitable for industrial large-scale production, and has a good industrial prospect.

The invention discloses a Tibetan angelica homogeneous polysaccharide, which is composed of Rha, Ara, Gal, Glc and GalA in a molar ratio of 7.5: 38.9: 4.6: 31.5: 7.8. The molecular weight of the Tibetan angelica homogeneous polysaccharide is 2.9 * 10 < 4 > Da. According to the method, polysaccharide components of angelica sinensis are extracted, separated and purified, the monosaccharide composition and molar ratio are determined, and specific connection structures of specific main chain and branch chain structures are analyzed in combination with GC-MS and NMR. Cell experiments and animal experiments show that the prepared Tibetan angelica homogeneous polysaccharide can synergistically enhance the anti-colorectal cancer effect of irinotecan, can reduce the intestinal toxic and side effects of irinotecan, and has important application value.

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.

The present disclosure relates to a method for treating a cancer and / or cancer metastasis in a subject comprising administering to the subject irinotecan loaded in a mesoporous silica nanoparticle. The present disclosure also provides a conjugate comprising an agent loaded in a mesoporous silica nanoparticle (MSN) defining at least one pore and having at least one functional group on a sidewall of the at least one pore.

This invention relates to the field of aspirin medicinal chemistry, and particularly to an aspirin-dithiocarbamate hybrid, its preparation method, and its applications. The preparation method uses aspirin (ASP) as the parent compound and involves a three-step reaction: acylation, dithiocarbamate formation, and N-acylation. During this reaction, several novel aspirin-dithiocarbamate hybrids (3a–l) can be efficiently synthesized through a single silica gel column chromatography separation and purification step, making the preparation process simple. The prepared aspirin-dithiocarbamate hybrids significantly enhance the toxicity of human lung cancer cells A549, approximately eight times that of the parent compound ASP, and are comparable to the anticancer drug irinotecan. The prepared aspirin-dithiocarbamate hybrid 3f exhibits inhibitory effects on various cancer cells and can inhibit the growth of human lung cancer A549 cells by inducing cell cycle arrest in the G0 / G1 phase.

Disclosed in the present application is a heterofunctional four-arm polyethylene glycol derivative as shown in formula (1), containing at least two different terminal reactive groups or protected forms thereof. Also disclosed in the present application is a conjugate formed by coupling the four-arm polyethylene glycol derivative with a targeting moiety (e.g., folic acid) and a bio-related substance (e.g., irinotecan). The modified bio-related substance can be located not only at the ends of the polyethylene glycol chains but also in a portion between two two-arm structures. The heterofunctional four-arm structure is obtained on the basis of pairing and combining two-arm polyethylene glycol derivatives, possessing multiple functional group combinations, and allowing coupling with targeting groups and drug molecules at different ratios, thereby achieving precise, flexible, and controllable targeting and pharmacological effects.

Provided herein are methods of treating cancer by administering a combination therapy comprising a KRAS G12D inhibitor, folinic acid, 5-fluorouracil, irinotecan, and oxaliplatin.

Methods of treating or ameliorating cancer symptoms in a subject using agents, compositions, and therapies designed to promote anti-tumor effects and avoid drug resistance effects are described. In some embodiments, a combination of active agents may be used, including a combination of an agent for inhibiting or suppressing TGF-beta 2 expression with an irinotecan-containing agent, a therapy, or an agent, such as a FOLFIRIOX agent, a NALIRIFOX agent, an IRIFOX agent, or an IRIOX agent. Biomarkers can be used to select subjects that benefit from such treatments.

The invention discloses application of flavonoid glycoside in tea trees in preparation of drugs for inhibiting gastric cancer cell spread in the technical field of medicines, and the flavonoid glycoside in the tea trees is prepared by the following steps: taking fresh leaves of tea trees as raw materials, firstly performing alcohol extraction to obtain an alcohol extract, then performing extraction and vacuum concentration to obtain a concentrated solution, and finally performing vacuum concentration to obtain the flavonoid glycoside in the tea trees. And adsorbing by using macroporous adsorption resin, small-pore adsorption resin and size exclusion chromatographic resin in sequence to obtain the tea extract rich in flavonoid glycoside. The tea leaf extract rich in flavonoid glycoside has the activity of inhibiting growth of gastric cancer cells, the effect of resisting proliferation activity of the gastric cancer cells is improved to a certain extent by compounding the tea leaf extract rich in flavonoid glycoside with irinotecan, and the synergistic effect is achieved; therefore, the tea leaf extract rich in flavonoid glycoside can be used as an auxiliary synergistic component to be applied to preparation of drugs for inhibiting gastric cancer cell diffusion.