43 results about "Approved drug" patented technology

This disclosure describes the use of azithromycin, roxithromycin, and telithromycin, including derivatives thereof, as senolytic drugs. BrdU was used to induce senescence in model human fibroblast cell lines. Also disclosed are methods for screening compounds for senolytic activity. The SRB assay was used to measure cell viability through protein content. Azithromycin roxithromycin, and telithromycin, clinically-approved pharmaceuticals, were found to be senolytic drugs. However, the closely-related parent compound, erythromycin, showed no senolytic activity. Azithromycin strongly induced both aerobic glycolysis and autophagy in human fibroblasts, but showed bi-phasic effects including on mitochondrial oxygen consumption rates with inhibitory activity at 50 μM and stimulatory activity at 100 μM. The xCELLigence real-time assay system showed that azithromycin preferentially targets senescent cells, removing approximately 97% (nearly a 25-fold reduction in senescent cells).

The present disclosure provides methods of treating anemia in a patient in need thereof, comprising administering to the patient in need thereof an effective amount of salmeterol or a pharmaceutically acceptable salt thereof. Salmeterol or a pharmaceutically acceptable salt thereof may be administered conjointly with an erythropoiesis-stimulating agent, optionally wherein the anemia is refractory to the erythropoiesis-stimulating agent. Also provided are methods of promoting differentiation of an erythroid progenitor cell toward a mature red blood cell in a patient in need thereof, comprising administering an effective amount of salmeterol or a pharmaceutically acceptable salt thereof. The present disclosure further provides methods comprising administering salbutamol or a pharmaceutically acceptable salt thereof. Salmeterol, salbutamol, or a pharmaceutically acceptable salt thereof may be administered conjointly with other FDA-approved drugs such as luspatercept, lenalidomide, daprodustat, vadadustat, an erythropoiesis-stimulating agent (ESA), and / or a hypomethylating agent.

This disclosure describes the use of azithromycin, roxithromycin, and telithromycin, including derivatives thereof, as senolytic drugs. BrdU was used to induce senescence in model human fibroblast cell lines. Also disclosed are methods for screening compounds for senolytic activity. The SRB assay was used to measure cell viability through protein content. Azithromycin roxithromycin, and telithromycin, clinically-approved pharmaceuticals, were found to be senolytic drugs. However, the closely-related parent compound, erythromycin, showed no senolytic activity. Azithromycin strongly induced both aerobic glycolysis and autophagy in human fibroblasts, but showed bi-phasic effects including on mitochondrial oxygen consumption rates with inhibitory activity at 50 μM and stimulatory activity at 100 μM. The xCELLigence real-time assay system showed that azithromycin preferentially targets senescent cells, removing approximately 97% (nearly a 25-fold reduction in senescent cells).

The invention belongs to the field of biological medicine, and particularly relates to a fusobacterium nucleatum FtsZ protease inhibitor and application thereof. On the basis of the idea of new use of old drugs, drugs approved by FDA are subjected to structure-based virtual screening and molecular dynamics simulation, and sorafenib, ponatinib, ceritinib and ibastine can be stably combined to active sites of fusobacterium nucleatum FtsZ protease; in-vitro experiments also show that sorafenib, ponatinib, ceritinib and ibastine are inhibitors with the fusobacterium nucleatum FtsZ protease, so that new antibacterial applications of sorafenib, ponatinib, ceritinib and ibastine are explored. The invention not only provides a new angle for antibiotic discovery, but also provides an example for rapid development of a novel FtsZ protease inhibitor.

The p300 inhibitor specifically regulates the expression of genes that induce fibrosis, thereby acting only on fibrotic tissues and reducing the risk of adverse effects on normal tissues. Because the inhibitor blocks multiple fibrotic signaling pathways, it may be effective for fibrosis in various organs such as the liver, lungs, and kidneys. In addition, by modulating gene expression, the inhibitor has the potential to address the fundamental cause of the fibrotic process. The present invention is characterized in that bronopol is first identified as a specific example of such a p300 inhibitor. In particular, bronopol is an FDA-approved drug with established safety, and therefore is expected to reduce the time and cost required for conducting clinical trials.

Described herein methods of treating urothelial carcinoma with an approved drug product containing a fibroblast growth factor receptor (FGFR) inhibitor. Also described herein are methods of selling or offering for sale an approved drug product containing a fibroblast growth factor receptor (FGFR) inhibitor.

The present invention relates to a compound for treating fungal disease, wherein said compound provide target-specific inhibition of fungal adhesion, biofilm formation, and filamentation without affecting their growth, at very low concentration. The compound of the present invention is selected from FDA approved drugs Cangrelor. Further, the present invention provides a composition comprising compound of the present invention and a pharmaceutically acceptable carrier. Further, the present invention provides a method of treating fungal infections using the compound and / or composition of the present invention. Furthermore, uses of the compound and / or composition is also being provided in the present disclosure.

An intelligent dosing platform system for prior authorization and pharmacy benefit management comprising intelligent injection devices with prior authorization modules configured to receive medication release approval from pharmacies, distributing agents, and payor entities. The system analyzes authorization requirements by evaluating individual payor policies, pharmacy benefit manager formulary restrictions, step therapy requirements, medical necessity criteria, seasonality factors, and timing considerations. An automated decision engine determines authorization approval or denial based on real-time policy evaluation and aggregated device usage data from multiple injection devices. An action coordinator triggers downstream processes including preventing device shipment, updating electronic health records, and coordinating billing system updates. A financial reconciliation module ensures one-to-one correspondence between authorization approvals and fulfillment activities, matching approved medications with actually shipped or administered medications while preventing payment for unapproved medications.

The present disclosure describes the use of azithromycin, roxithromycin and telithromycin (including their derivatives) as anti-aging drugs. BrdU was used to induce senescence in a model human fibroblast cell line. A method for screening compounds with anti-aging activity is also disclosed. The SRB assay is used to determine cell viability by protein content. The clinically approved drugs azithromycin, roxithromycin and telithromycin have been found to be anti-aging drugs. However, the closely related parent compound erythromycin does not show anti-aging activity. Azithromycin strongly induces both aerobic glycolysis and autophagy in human fibroblasts, but shows a bidirectional effect, including 50 μM inhibitory activity and 100 μM stimulatory activity on mitochondrial oxygen consumption rate. The xCELLigence real-time assay system showed that azithromycin preferentially targeted senescent cells, removing approximately 97% of senescent cells (a nearly 25-fold reduction in senescent cells).

The invention discloses a gp130-loaded engineered extracellular vesicle and application thereof, belongs to the technical field of biological medicines, and relates to a medicine, which comprises a scaffold protein EN144 membrane externally hung gp130 protein-loaded engineered extracellular vesicle, the scaffold protein EN144 membrane externally hung gp130 protein-loaded engineered extracellular vesicle, and the gp130 protein-loaded engineered extracellular vesicle. The sequence of the scaffold protein EN144 is SEQ ID NO: 1; according to the present invention, the EN144-EVhgp130 provides the anti-inflammatory effect in a variety of diseases; the consistency of in-vivo and in-vitro research results shows that the EN144-EVhgp130 and the EN144-EVmgp130 can be used for effectively inhibiting the generation of sepsis inflammatory factors on RNA (Ribonucleic Acid) and protein levels; compared with a clinically approved drug TCZ, the EN144-EVhgp130 shows a higher survival rate and more remarkable inflammation improvement in a sepsis mouse model, and the IC50 of the EN144-EVhgp130 is lower than that of the TCZ.

The present invention discloses a program-controllable protein rapid secretion and release PASS system, including a protein rapid secretion and release system regulated by clinically approved drugs, a protein rapid secretion and release system regulated by blue light, and a protein rapid secretion and release system that recognizes protein antigen signals. The PASS system of the present invention has the ability to respond to a variety of inducers and achieve rapid release of a variety of user-defined proteins by directly regulating protein secretion rather than inducing protein transcriptional expression. The PASS system of the present invention can quickly and efficiently regulate the secretion and release of target proteins, and has the characteristics of orthogonality, non-toxicity, high efficiency, low background leakage, and rapid induction of protein rapid secretion and release, providing an artificially controllable protein drug rapid, transient protein rapid delivery technology platform for basic research, genetic engineering, and regenerative medicine, and has great potential application value for treating diseases caused by insufficient protein secretion or damage.

The invention relates to the technical field of biology, in particular to application of losamine as a tyrosinase inhibitor. An FDA approved drug database is screened through an artificial intelligence model, the potential inhibitory activity of the compound on tyrosinase is found, and experiments prove that the compound has good tyrosinase inhibitory activity and transdermal ability.

The application discloses application of FTY720 as a PP2A phosphatase activator in preparation of a medicine for treating type I neurofibromatosis. The application first uses FTY720 for treatment of type I neurofibromatosis, and proves that FTY720 significantly inhibits formation of neurofibromas by non-specifically activating PP2A phosphatase. In-vivo experimental results show that FTY720 as a single drug can significantly inhibit tumor growth, and a synergistic effect is presented when FTY720 is combined with a MEK inhibitor, and tumor growth is almost completely inhibited. In-vitro cell experiments show that FTY720 as a single drug or in combination with MEKi treatment can inhibit tumor Schwann cells from forming tumor spheres, inhibit cell proliferation and migration, and induce tumor cell apoptosis. The application overcomes the drug resistance problem existing in the prior art MEK inhibitor, and provides a new treatment strategy for type I neurofibromatosis. FTY720 is an FDA-approved drug, and has good safety and drugability, and has high clinical conversion potential.

The invention relates to an application of a patent medicine Tenapanor approved by FDA in preparing a medicament for resisting platelet and arterial thrombosis. The medicament can be used for effectively inhibiting platelet activation and aggregation and arterial thrombosis block formation. The invention relates to an FDA approved patent medicine Tanipanol capable of effectively inhibiting platelet activation and aggregation induced by a natural agonist ADP and carotid artery and mesenteric artery thrombosis. Tanipamox is used as a novel candidate drug for resisting formation of platelets and arterial thrombosis blocks in fundamental research of thrombotic diseases, and has potential application value in prevention and treatment of arterial thrombosis related diseases.

The present disclosure provides the first asymmetric total synthesis and target identification of the curcusone natural products. The novel convergent synthesis is built upon a cheap and abundant chiral pool molecule (8) and features a thermal [3,3]-sigmatropic rearrangement and an FeCl3-promoted global hydrolysis / adol condensation cascade to rapidly construct the critical cycloheptadienone core. By performing chemoproteomics with the alkyne probe 37, we identified the previously “undruggable” oncogenic protein BRAT1 as a key cellular target of 1d. Furthermore, 1d inhibits BRAT1 in cancer cells, thereby reducing cancer cell migration, increasing susceptibility to DNA damage, and inducing chemosensitization to the approved drug etoposide. Compound 1d is the first known small-molecule inhibitor for BRAT1, a master regulator of the DDR and DNA repair. Composition matters and methods of uses are within the scope of this disclosure.

The invention belongs to the field of biological medicines, and particularly relates to application of a long-chain non-coding RNA SLCO4A1-AS1 inhibitor in preparation of a medicine for treating lung cancer. According to the application, the action mechanism of the long non-coding RNA SLCO4A1-AS1 is discussed, and it is found that the long non-coding RNA SLCO4A1-AS1 is combined with ALKBH5, so that synthesis of asparagine by lung cancer cells is promoted, and cell growth is maintained. According to the invention, structural data of long non-coding RNA SLCO4A1-AS1 and ALKBH5 and a drug structure database approved by FDA to appear in the market are further subjected to simulation docking and screening, and a micromolecular drug, namely allpasvir, which potentially inhibits the combination of SLCO4A1-AS1 and ALKBH5 is obtained. The invention finds that the allpasvir can inhibit the growth of lung cancer cells at a cellular level; in an animal model, the ellpasvir can significantly inhibit tumor growth and reduce the tumor volume.

The invention discloses an unsupervised drug similarity evaluation method based on a graph neural network, only real drug molecules are used for training, and performance fluctuation and insufficient generalization caused by negative sample dependence are avoided. According to the method, SMILES representation of an approved drug is analyzed into a molecular graph with atomic attributes, structural perception features are extracted through a three-layer graph neural network, graph-level representation is obtained through average pooling, and a drug molecule representation center is calculated to construct a minimum hypersphere space. In the scoring stage, drug similarity scores are calculated according to the distance between candidate molecular characterization and the center and boundary parameters, and continuous interpretable quantitative evaluation is achieved. The method has the advantages of high stability, strong generalization ability and good adaptability, and can be widely applied to virtual drug screening and candidate molecule optimization.

The present disclosure relates to therapeutic methods and clinically useful molecular switches, for which activity or degradation of a switch-presenting polypeptide can be precisely induced via administration or withdrawal of an FDA-approved drug. Certain aspects of the disclosure relate to an engineered drug-inducible heterodimeric system including a first polypeptide presenting a CRBN polypeptide disrupted for or lacking a DDB1-interacting domain and a second polypeptide presenting a CRBN polypeptide substrate, where binding between the CRBN polypeptide and the CRBN polypeptide substrate are inducible via administration of an FDA-approved thalidomide analog immunomodulatory drug (IMiD). Another aspect of the disclosure relates to a chimeric antigen receptor (CAR) that presents a minimal fragment of the CRBN polypeptide substrate IKZF3 capable of triggering proteasomal degradation of CAR upon administration of an FDA-approved IMiD.

Systems and methods are provided for automatically generating reports of new drug applications, including memory storing program instructions and at least one processor programmed or configured to retrieve plural data files from a server associated with the Food and Drug Administration (FDA), wherein the plural data files include data associated with new drug applications; determine that at least one data file includes data for an approved 505(b)(2) drug application; generate a list of data files including a subset of plural data files, wherein each data file in the subset of plural data files represents a new drug application; input the subset of plural data files including data for approved 505(b)(2) drug applications into at least one natural language processing (NLP) model; and generate, with the at least one NLP model, a text summary of each data file of the subset of plural data files.

This invention relates to the field of biomedicine, specifically to a class of prodrug structures with ROS signal-responsive properties, their preparation methods, and applications. The prodrug molecules with ROS signal-responsive properties developed in this invention can rapidly release bioactive molecules in ROS-rich environments, achieving targeted therapeutic effects. This method has good universality and has been verified to be able to prodrugize various molecules, including four approved drug molecules, improving drug solubility, biocompatibility, reducing cytotoxicity, and enhancing targeted therapeutic effects. Based on the structural characteristics of these molecules, they can also complex with PVA hydrogels to further achieve responsive and controllable drug release.

The present invention proposes a drug dimer nano-therapeutic agent based on ferrocene and its preparation method and application, which belongs to the field of drug development technology. The present invention proposes a drug delivery system based on ferrocene drug dimer, and especially develops a multi-mode ferroptosis nano-inducer (FSS), and explores its potential for inducing ferroptosis to treat colorectal cancer. Ferrocene-modified SAS prodrug and SN38 prodrug are prepared by chemically coupling SAS or SN38 with ferrocene dicarboxylic acid by bis(2-hydroxyethyl) disulfide through esterification reaction. The prodrug has the characteristic of responding to the specific release of high levels of GSH in the tumor microenvironment, and optimizes the pharmacokinetics and pharmacokinetic properties of clinically approved drugs. The clinical drug dimer based on ferrocene involved in the present invention has certain self-assembly characteristics, and the two drug dimers are co-assembled to prepare a nano-therapeutic agent with potential for combined application, which shows good application potential and prospect in the treatment of colorectal cancer.

This invention discloses the application of OXR1 as a target in the preparation of drugs for treating osteoclast-related bone diseases. This invention reveals for the first time the crucial role of OXR1 in osteoclast differentiation: OXR1 directly binds to the KEAP1 protein, promoting the interaction between KEAP1 and p62, thereby mediating mitophagy, clearing excess reactive oxygen species generated during osteoclast differentiation, and maintaining mitochondrial homeostasis. Inhibiting OXR1 expression or function can effectively block osteoclast differentiation and reduce bone loss. Based on this, this invention provides two intervention strategies targeting OXR1: one is gene therapy using adeno-associated viruses carrying shRNA targeting OXR1; the other is screening and validating the novel use of the FDA-approved drug velpatasvir as an OXR1 inhibitor. In vitro and in vivo experiments confirmed that both significantly inhibit osteoclast activity and improve the osteoporotic phenotype in ovariectomized mice.

A drug combination prediction method and device integrating molecular docking and expression profile data, the method comprising: obtaining structural information of disease targets and structural information of FDA approved drugs, performing molecular docking targeted screening; using a disease related gene set as a reference imprint, using a differential gene set of approved drugs as a drug imprint, calculating the correlation between the reference imprint and the drug imprint to obtain an imprint matching score; Z-score conversion of the drug molecular docking and the imprint matching score respectively to obtain SDi and SSi, summing SDi and SSi and sorting to obtain a drug combination prediction result. The present application establishes a drug function prediction tool, which integrates intrinsic activity and downstream biological effect factors into the molecular docking strategy, compared with single molecular docking, the hit rate of the top 10, 30 and 100 positive drugs of the present application is increased by 2.8 times, 2.5 times and 1.9 times respectively.

Acquired hearing loss due to chemotherapy or noise exposure is a major health problem, and Cisplatin chemotherapy often causes permanent hearing loss in cancer patients. However, there are no FDA-approved drugs for the treatment or prevention of Cisplatin- or noise-induced hearing loss. In one aspect, use of Niclosamide, Ingenol, and Elesclomol as an active agent to treat a hearing impairment and to prevent a hearing impairment, and methods of treating and / or preventing hearing impairments or disorders using the compositions are disclosed. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

This invention discloses uses for nicardipine in preparing anti-lung cancer products. This invention provides uses for nicardipine in the preparation of products to treat non-small cell lung cancer. From carrying out cancer drug repositioning for the FDA- and CFDA-approved drug nicardipine, experiments for this invention show, based on screening of non-anti-cancer drugs for various cancer cell lines (tissue types) and mutation sites, that nicardipine has a new use as an anti-small cell lung cancer and / or anti-non small cell lung cancer medication, thus achieving a new purpose for an old drug.

Autism (ASD) symptoms of aggression-toward others or self, and paranoia with social isolation, are presently treated with antipsychotic medications such as haloperidol, Thorazine, and newer generation antipsychotics risperidone and aripiprazole (latter two are the only FDA approved drugs for treating autism irritability / aggression). But these antipsychotics including the newer generation, after a two or more years of use, often lead to irreversible tardive dyskinesia, other dystonias, loss of effectiveness, and brain volume loss. The present invention overcomes the irreversible tardive dyskinesia and dystonias and loss of effectiveness with long term-use of antipsychotics, by replacing the antipsychotic completely with a three (3) drug novel composition consisting of fluoxetine or sertraline with guanfacine and oxcarbazepine. This novel composition markedly reduces aggression and paranoia / social isolation in ASD adults and adolescents without concomitant antipsychotic use that often causes irreversible tardive dyskinesia, eventual tachyphylaxis, or brain volume loss from antipsychotic long-term use.

Described herein are methods of treating non-metastatic castrate-resistant prostate cancer using an approved drug product comprising apalutamide, enzalutamide or darolutamide. Also described here are drug products containing apalutamide enzalutamide or darolutamide, and methods of selling or offering for sale an anti-androgen drug product.

The invention relates to the field of drug development, and discloses a molecular druggability potential scoring method based on a comparative learning variational auto-encoder, which comprises the following steps: constructing a sample set comprising drug molecules and non-drug molecules, preprocessing the sample set and predicting to obtain ADMET characteristic spectrums, evaluating and sequencing the importance of the ADMET characteristic spectrums, and determining the druggability potential of the drug molecules according to the druggability potential of the drug molecules and the non-drug molecules. Screening out a druggability related characteristic set; a UniMol-based multi-task learning model is adopted to predict ADMET properties, an RDKit chemoinformatics tool is adopted to calculate physicochemical properties and synthesis feasibility scores, and a one-dimensional molecular feature vector is formed through fusion; taking the one-dimensional molecular feature vector as the input of a variational auto-encoder model adopting a fused triple contrast learning mechanism for training, and constructing a potential space; and mapping the approved drug molecules and the to-be-evaluated molecules into a potential space, and calculating druggability scores based on the Euclidean distance between the to-be-evaluated molecules and the distribution center and the local drug molecule density. The method is suitable for druggability comprehensive evaluation of drug screening, pilot optimization and molecular design.

The invention provides application of Jintiange capsules in delaying skeletal muscle senescence. The invention has the beneficial effects that the Jintiange capsule simulates the traditional Chinese medicine tiger bone powder through the bionic tiger bone powder, effectively delays skeletal muscle senescence, and can be directly applied clinically by using the medicine verified by clinical examination and approval. The Jintiange capsule is composed of various animal bones and has the characteristics of multiple components and multiple target points, so that no serious safety problem is found in clinical application of the Jintiange capsule. In addition, the old people have good compliance after taking the Jintiange capsule, and the long-term taking of the Jintiange capsule has feasibility for delaying skeletal muscle aging.

An algorithm for identifying treatment targets for diseases and FDA-approved drugs that can be re-purposed for off-label use is described, as well as methods of using drugs identified by the algorithm to treat diseases including cancer. Also described are synergistic combinations of FDA-approved drugs for treating diffuse pleural mesothelioma.