19 results about "Sunitinib" patented technology

The invention relates to a kit for detecting the sensitivity of kidney cancer to a targeted drug, which comprises an RNA (Ribonucleic Acid) nucleic acid probe, and the sequence of the RNA nucleic acid probe is shown as SEQ ID NO: 4. The invention also provides a construction method of the specific annular RNA probe. The construction method comprises the following steps: S1, designing and constructing a recombinant plasmid containing a target gene; s2, constructing a tricRNA (Ribonucleic Acid) vector containing a reverse complementary sequence crossing a backspace junction site and a Broccoli sequence, wherein the reverse complementary sequence crossing the backspace junction site and the Broccoli sequence are subjected to reverse complementary sequence crossing the backspace junction site; s3, carrying out vector transfection on the HEK293T cell to express a tricRNA probe, and extracting the tricRNA probe; and S4, constructing a tricAGAP1 Probe-Broccoli probe. The method comprises the following steps of: constructing a tricAGAP1 probe; the invention provides application of a probe in preparation of a cell imaging probe and in preparation of a kit for detecting sensitivity of kidney cancer to a targeted drug. The invention not only provides a new method and technology for guiding the medication of sunitinib for patients with advanced kidney cancer, but also provides a technical example for the development of other circRNA detection technologies.

The present application provides an application of an RIPK1 O-GlcNAc glycosylation inhibitor in the preparation of a drug for enhancing the sensitivity of sunitinib to renal cell carcinoma. The present application discovers that RIPK1 O-GlcNAc glycosylation, especially the O-GlcNAc glycosylation of serine at positions 331, 440, and 669, reduces the sensitivity of renal cell carcinoma to sunitinib. Therefore, by inhibiting RIPK1 O-GlcNAc glycosylation or knocking down the expression of O-GlcNAc transferase, the sensitivity of renal cell carcinoma to sunitinib can be increased. Therefore, the O-GlcNAc glycosylation level of RIPK1 can be used as a biomarker for predicting the sensitivity of renal cell carcinoma to sunitinib; by using an RIPK1 O-GlcNAc glycosylation inhibitor to reduce the RIPK1 O-GlcNAc glycosylation level, especially the O-GlcNAc glycosylation of serine at positions 331, 440, and 669, the sensitivity of renal cell carcinoma to sunitinib can be increased, and the therapeutic effect of sunitinib can be improved.

The invention discloses an application of sunitinib in preparation of a medicine for treating secondary injury caused by intracranial hemorrhage. It is found for the first time that sunitinib can act on a CSF-1R / PI3K / Akt axis, pathological activation and pro-inflammatory response of microglial cells are effectively inhibited, the normal phagocytic function and lipid metabolism balance of the microglial cells are remarkably recovered, myelin sheath damage around hematoma is effectively relieved, and the neurological function score, the movement coordination ability and the exploration behavior of ICH mice are remarkably improved; the progress of secondary injury caused by intracranial hemorrhage is hindered from multiple dimensions, the curative effect is superior to that of a positive control drug pecetinib (PLX3397), and a brand new molecular target and an interference strategy are provided for comprehensive treatment of ICH.

Methods and materials for treating or preventing cardiotoxicity and / or hypertension induced by one or more anti-cancer agents (e.g., tyrosine kinase inhibitor (TKI) -induced cardiotoxicity (e.g., sunitinib-induced cardiotoxicity) and / or TKI-induced hypertension (e.g., sunitinib-induced hypertension)) are provided herein. For example, provided herein are methods for using polypeptides (e.g., chimeric polypeptides) that include (a) one or more natriuretic peptides and (b) one or more angiotensin 1-7 (ANG1-7) polypeptides to treat or prevent cardiotoxicity and / or hypertension induced by one or more anti-cancer agents.

The invention discloses an intermediate silk protein as a biomarker for predicting the staging, prognosis and drug resistance of renal clear cell carcinoma and application of the intermediate silk protein. By detecting the IFFO1 expression level of a ccRCC patient tissue specimen and analyzing a database, a new insight is provided for taking the expression quantity of the IFFO1 as a ccRCC biomarker. By changing the expression level of IFFO1 in the cell, the increase in proliferation, transfer and clone generation of the ccRCC cell as well as the improvement in genome stability are detected. In addition, after the IFFO1 is expressed in the ccRCC cells, the tolerance degree to sunitinib is increased, and the expression quantity of the IFFO protein family in the constructed ccRCC drug-resistant cells is increased. Researches show that the IFFO protein in ccRCC stabilizes a genome and promotes the tolerance of cells to a DNA damage inducer and a tyrosine kinase inhibitor sunitinib, molecular mechanism research and drug development taking IFFO as a target spot are beneficial to improvement of a treatment effect, and the IFFO protein has clear and beneficial practical application value.

The invention discloses a diagnostic marker for the drug resistance of kidney cancer sunitinib. The diagnostic marker for the drug resistance of kidney cancer sunitinib is selected from a group consisting of histone acetyltransferase KAT2A. The invention further discloses a kit for detecting the sunitinib drug resistance of the kidney cancer. The kit comprises a reagent for detecting the expression quantity of KAT2A. The KAT2A provided by the invention is used as a renal cancer sunitinib drug resistance diagnosis marker, has good specificity and high sensitivity, provides a new diagnosis and treatment means for renal cancer sunitinib drug resistance, is beneficial to drug resistance monitoring and avoids further invalid treatment, and has a good medical conversion prospect.

The invention relates to the technical field of biomedical engineering, and provides a pharmaceutical composition for treating kidney cancer, and the pharmaceutical composition comprises sunitinib, CYT387 and a pharmaceutically acceptable carrier. The invention also provides an application of the combination of sunitinib and CYT387 in preparation of a medicine for treating kidney cancer, and a result shows that the combination of CYT387 and sunitinib can obviously enhance the anti-kidney tumor activity and shows an obvious synergistic effect. Therefore, the invention provides a new exploration for overcoming the drug resistance of sunitinib, is beneficial to improving the drug sensitivity of malignant tumors, and has a certain clinical application prospect.

Selective and potent inhibitors of G protein-coupled receptor kinase 5 (GRK5), a pharmaceutical composition comprising same, and a method of use, such as in the treatment of heart disease or cancer.

The present application belongs to the technical field of biological medicine, and relates to a gene therapy preparation for treating drug-resistant renal cell carcinoma as well as a preparation method and application thereof. It is found for the first time that UBL3 is a key gene for mediating cross-resistance of VEGFR inhibitors of renal cancer, and a lipid nanoparticle composite system integrating specific gene editing and active targeted delivery functions is constructed based on this. The preparation can effectively restore the sensitivity of drug-resistant tumors to first-line drugs such as sunitinib, and shows a significant anticancer effect in in-vivo and in-vitro models, and has important clinical transformation value.

Dendrimer compositions and methods for the treatment of one or more inflammatory and / or angiogenic diseases and / or disorders of the eye include hydroxyl-terminated dendrimers complexed or conjugated with one or more active agents for the treatment or alleviation of one or more symptoms of the diseases of the eye, and / or for diagnosing the diseases and / or disorders of the eye. The dendrimers may include one or more ethylene diamine-core poly(amidoamine) (PAMAM) hydroxyl-terminated generation-4, 5, 6, 7, 8, 9, or 10 dendrimers. The active agents may be VEGFR tyrosine kinase inhibitors including sunitinib or analogues thereof. Preferably, the compositions are suitable for administration via a systemic route to target activated microglia / macrophages in retina / choroid.

The present invention discloses the use of a chromatin remodeling factor BPTF as a diagnostic marker for sunitinib resistance in renal cancer. The present invention discloses the use of an active ingredient that downregulates or blocks the expression of BPTF molecules in renal cancer cells in the preparation of relevant kits and drugs for diagnosing and treating sunitinib resistance in renal cancer. The present invention provides a new diagnostic and therapeutic means for targeted drug resistance in renal cancer.

The invention relates to a gas chromatography detection method for the residual quantity of 2-chloropyrrole in a sunitinib intermediate 5-formyl-2, 4-dimethyl-1H-pyrrole-3-carboxylic acid, and belongs to the technical field of detection. An electron capture detector is adopted, an antioxidant is added in a headspace sampling mode, the oxidation problem of a sample is avoided, and the trace 2-chloropyrrole is detected. The method is sensitive, accurate, good in repeatability, low in instrument operation cost, simple and rapid in detection process and capable of better controlling the 2-chloropyrrole residual quantity in the production of the sunitinib intermediate 5-formyl-2, 4-dimethyl-1H-pyrrole-3-carboxylic acid.

Dendrimer compositions and methods for treating one or more ocular inflammatory and / or angiogenic diseases and / or conditions, including hydroxyl-terminated dendrimers complexed or conjugated to one or more active agents for treating or reducing one or more symptoms of an ocular disease, and / or for diagnosing an ocular disease and / or condition. The dendrimers can include one or more ethylenediamine core poly(amidoamine) (PAMAM) hydroxyl-terminated generation 4, 5, 6, 7, 8, 9, or 10 dendrimers. The active agent can be a VEGFR tyrosine kinase inhibitor, including sunitinib or an analog thereof. Preferably, the compositions are suitable for administration via a systemic route to target activated microglia / macrophages in the retina / choroid.

Selective and potent inhibitors of G protein-coupled receptor kinase 5 (GRK5), a pharmaceutical composition comprising same, and a method of use, such as in the treatment of heart disease or cancer.

The invention discloses an anti-tumor composition and application thereof. The active ingredients of the composition are sunitinib with a treatment effective dose and zingiberenone A for enhancing the treatment effect of the sunitinib. The concentration ratio of zingiberenone A to sunitinib is 1: (0.5-2.5). According to the anti-tumor composition provided by the invention, the zingiberenone A and sunitinib are combined for use, so that the drug sensitivity of tumors can be improved, a synergistic effect on inhibiting the multiplication capacity and migration capacity of human kidney cancer cells 786-O is achieved, and a new strategy is provided for treating renal cell carcinoma.

The present application relates to a kind of cell membrane-coated pH-responsive nanogel and its preparation method, the pH-responsive nanogel is that chitosan is crosslinked by crosslinking agent to form nanogel, then load polypeptide ENO1, and further load drug sunitinib, finally, it is prepared by coating kidney cancer cell membrane.The pH-responsive nanogel prepared in the present application as the carrier of polypeptide and drug, with the advantages of good biocompatibility, high drug loading rate, etc., in the tumor microenvironment response dissociation release drug, real-time monitoring is carried out to focus area during treatment.

To provide dendrimer compositions and methods for drug delivery to the eye.SOLUTION: Dendrimer compositions and methods for the treatment of one or more inflammatory and / or angiogenic diseases and / or disorders of the eye include hydroxyl-terminated dendrimers complexed or conjugated with one or more active agents for the treatment or alleviation of one or more symptoms of the diseases of the eye, and / or for diagnosing the diseases and / or disorders of the eye. The dendrimers may include one or more ethylene diamine-core poly(amidoamine) (PAMAM) hydroxyl-terminated generation-4, 5, 6, 7, 8, 9, or 10 dendrimers. The active agents may be VEGFR tyrosine kinase inhibitors including sunitinib or analogues thereof. Preferably, the compositions are suitable for administration via a systemic route to target activated microglia / macrophages in retina / choroid.SELECTED DRAWING: None

The invention provides application of cevaltinib in preparation of a medicine for treating tendinopathy, the tendinopathy is a tendon degenerative disease caused by tendon stem cell senescence and tendon degeneration, and the medicine for treating the tendinopathy can target tendon stem cells, inhibit tyrosine kinase receptors and inhibit expression of tendon stem cell senescence markers p16 and p21. Therefore, histological pathologic progresses such as tendon degeneration and the like are inhibited. The invention further provides a medicine, and the effective component of the medicine is the cevaltinib. According to the application disclosed by the invention, the remarkable effect of the cevaltinib in the aspect of treating the tendinopathy is found for the first time, and the senescence of tendon stem cells is inhibited and the tendon degeneration is delayed by highly selectively inhibiting MET tyrosine kinase. In addition, the used cevaltinib is high in biological safety, the synthesis method is mature, intensive production has been achieved, the requirements for storage and transportation conditions are not high, and the cost of the cevaltinib serving as a medicine is greatly reduced.

A genomic biomarker comprising a set of 5-50 genes is provided for predicting responsiveness to an anti-cancer treatment that includes a combination of palbociclib and sunitinib. These genes are differentially expressed in tumors that respond to the combination therapy compared to those that do not. At least some of the genes in the biomarker are significantly overexpressed in non-responsive tumors relative to responsive ones. This genomic biomarker helps determine whether a subject diagnosed with a cancerous disease will benefit from the combination therapy prior to its administration, enabling the optimization of medical treatment and supporting precision medicine.