46 results about "Bound drug" patented technology

Described herein are compositions and methods for use in targeted drug delivery using cell receptor binding drug delivery conjugates containing hydrophilic spacer linkers for use in imaging, diagnosing, and/or treating diseases and disease states caused by pathogenic cell populations.

The invention discloses a novel conjugate composed of a hydrophilic polymer and resveratrol, a pharmaceutical composition including the conjugate, their preparation methods and applications in the preparation of drugs for treating tumor, diabetes and cardio cerebrovascular disease, wherein the hydrophilic polymer is selected from the group consisting of polyethylene glycol, polyglutamic acid, polyaspartic acid, polypropylene glycol, polyvinyl alcohol, polypropylene morpholine, polyethylene glycol-amino acid oligopeptide and their copolymer. Through modification of the hydrophilic polymer, a bound drug can be protected, stability and water solubility of the conjugate are raised, and active period of the conjugate in organisms is prolonged.

Linkers for binding drugs to cell binding agents are modified to hydrophilic linkers by incorporating a polyethylene glycol spacer. The potency or the efficacy of the cell-binding agent-drug conjugates is surprisingly enhanced several folds in a variety of cancer cell types, including those expressing a low number of antigens on the cell surface or cancer cells that are resistant to treatment. A method for preparing maytansinoids bearing a thioether moiety and a reactive group which allows the maytansinoid to be linked to a cell-binding agent in essentially a single step is also provided.

The invention belongs to the field of medical chemistry, and particularly relates to a compound with the good hepatitis C virus inhibition effect, a preparation method of the compound, a composition comprising the compound and application of the compound or the composition as a medicine for treating hepatitis C virus infectious diseases. The compound has the excellent antiviral activity, meanwhile has the low cytotoxicity, is good in safety, good in plasma protein binding effect and suitable for patent medicine and has the quite good clinical application prospect.

According to a method for detecting the plasma protein binding rate of meropenem or imipenem by combining a liquid chromatography-mass spectrometry technology with an ultrafiltration technology, the liquid chromatography-tandem mass spectrometry detection technology is combined with the ultrafiltration technology, and the total concentration of meropenem or imipenem in plasma and the free concentration of drugs in ultrafiltrate are respectively detected. And an MOPs stabilizer is added during sample treatment, so that the problem of poor drug stability is solved, and the determination result is more accurate. The method can be used for rapidly detecting the protein binding rate of the drug at high throughput, and is particularly suitable for unstable drug molecules.

The invention discloses a novel 2-(2,4,5-substituted phenylamino)pyrimidine derivative as well as a preparation method and application thereof to preparation of an anti-tumor drug and belongs to the field of medicines. The novel 2-(2,4,5-substituted phenylamino)pyrimidine derivative has a structure shown as a general formula (I): (the formula (I) is shown in the description), wherein in the formula (I), R is independently selected from methyl and deuterated (D) methyl and can be the same or different at the same time; R1 is independently selected from H, D, methyl, C2 to C5 alkyl, Cl and F, Brand CF3; R2 is independently selected from H and D and can be the same or different at the same time. The compound or pharmaceutically acceptable salt thereof or a composition thereof is applied to preparation of a drug for treating cancers, and has advantageous physical properties (such as relatively high permeability and/or relatively low plasma protein binding) and relatively high selectivityand relatively low toxic characteristics; especially, the compound has a very good application prospect in the aspect of treating non-small-cell lung cancer.

A method is provided for increasing the safety and efficacy of albumin-binding drugs such as those used as anti-cancer, anti-infective, or anti-hypertensive drugs, or for numerous other conditions. In the preferred method, the invention modulates those drugs which bind at the IB site on human serum albumin by co-administering a compound which is highly tolerable to humans and which can bind competitively with those albumin-binding drugs at the IB binding site so as to increase the safety and efficacy of the drug. The invention is advantageous in that by administering the highly tolerable compound in a sufficient amount to compete with the targeted drug, the latter can be administered at a much lower dosage while maintaining or exceeding its potency. Compositions containing the combination of highly tolerable compound and albumin-bind drugs are also disclosed.

Saliva offers an alternative specimen for the therapeutic monitoring of cyclosporine (CsA) in children and patients with difficult venous access. For a highly protein-bound drug such as CsA, saliva provides a practical approach for measuring the unbound concentration. Liquid chromatography-tandem mass spectrometry (LC-MS/MS) is ideally suited for the measurement of drugs in saliva. A solid-phase extraction technique, analytic liquid chromatography over an Aqua Perfect column, maintained at 65° C., and electrospray tandem mass spectrometry were used to quantify CsA in saliva. The method used cyclosporine C (CsC) as the internal standard. Mobile phase comprised of a 97:3 voL mixture of methanol and 30 mmol/L ammonium acetate at a flow rate of 0.5 mL/min. Chromatograms using mass transitions of m/z 1219.9→m/z 1202.9 for CsA and m/z 1235.9→m/z 1218.9 for CsC were obtained. The calibration curve was linear from 1 to 300 μg/L with correlation coefficient values ranging from 0.9732 to 0.9968). The lower limit of quantification was 1 μg/L and limit of detection was 0.6 μg/L with an average extraction recovery of 84.7±2.6% for CsA and 93.7±4.4% for CsC from the saliva matrix. The accuracy of the method ranged from 92% to 104.7%, and the intra- and interim coefficients of variation were 6.9-12.2% and 8.3-12.1%, respectively. The correlation coefficient value between the CsA concentration measurements in 15 paired blood-saliva samples from kidney transplant recipients was 0.695 (P=0.006). The noninvasive and simple method of saliva collection coupled with the LC-MS/MS quantification technique for CsA analysis would generate novel data that could benefit patients undergoing CsA therapy.

The invention discloses a logistic regression-based pharmacokinetic parameter prediction method for a drug compound in the technical field of drug research and development, and the method comprises the following steps: 1, file input: inputting a molecular three-dimensional structure file of the drug compound; 2, calculation of a descriptor: calculating the descriptor of a molecule through CDK; 3,a training process: dividing text data and label data contained in the data set into a training set and a verification set; training a model by using the training set data, and outputting a parameterprediction model; adopting an Adam optimizer to optimize the model, and optimizing the model through 20-stage training. According to the method, a neural multi-task logistic regression algorithm is utilized, and rules can be automatically designed under the condition of little or no manual intervention. Through the molecular structure of the drug compound, the pharmacokinetic lipophilicity, solubility, plasma protein binding rate, transdermal property and other parameter values of the drug compound are accurately predicted.

The invention discloses a method for detecting the plasma protein binding rate of nine effect components in Sheepear Inula Herb extract. The method comprises the following steps: preparing a SheepearInula Herb extract sample medicine solution; preparing a standard control solution by using the nine effect components, and preparing a buffer solution; and establishing a method for simultaneously detecting the respective content of the Sheepear Inula Herb extract nine effect components in human plasma, rat plasma and the buffer solution by ultrahigh performance liquid chromatography-mass spectrometry (UPLC-MS/MS) analysis technology; and detecting the protein binding rates of the Sheepear Inula Herb extract nine effect components in the human plasma and rat plasma by an equilibrium dialysistechnology to establish the method for detecting the protein binding rate of Sheepear Inula Herb extract nine effect components in the human plasma and rat plasma. The method for detecting the plasmaprotein binding rate of nine effect components in Sheepear Inula Herb extract provides a demonstrative research for the detection of the plasma protein binding rate of traditional Chinese medicinal multiple effect components in different species animals, and is of great significance to study the druggability of traditional Chinese medicinal active components.