9 results about "Melphalan" patented technology

The present application for a patent of invention relates to the use of melphalan in the preparation of an intravitreal medicament for the prevention of vitreoretinal proliferation. It belongs to the technical field of pharmaceuticals, particularly ophthalmic medicines, and comprises melphalan at a concentration of 5 μg / 0.1 mL, intended for intravitreal injectable administration during pars plana vitrectomy.

The invention discloses a eeFISH (fluorescence in situ hybridization) whole brain tissue transparentizing multiple fluorescence in situ hybridization method and a kit. The hybridization method comprises the steps of whole brain tissue perfusion fixation, decoloration, nucleic acid anchoring, hydrogel crosslinking, electrophoresis-driven transparentizing, probe permeation through osmotic pressure regulation, electrophoresis hybridization and the like. The method specifically comprises the following steps: 1) carrying out covalent anchoring on nucleic acid through a melphalan-succinimide ester compound, and carrying out three-dimensional cross-linking immobilization with an acrylamide-bisacrylamide hydrogel system so as to maintain tissue molecule information and a space structure; (2) molecules such as lipid are removed through electrophoresis, and rapid tissue transparentizing is achieved; and 3) promoting the probe to permeate into the deep layer of the tissue and specifically hybridize under osmotic pressure and electrophoresis conditions. According to the application, high-efficiency electrophoresis driving and osmotic pressure regulation are taken as core characteristics, in-situ detection of whole-brain three-dimensional space molecular information can be directly, efficiently and quickly realized, and the problems of difficulty in compatibility of transparency and hybridization, slow probe permeation, insufficient signal background noise elution and the like are effectively solved; the method is widely applicable to space in-situ detection and analysis of nucleic acid and protein.

The present invention relates to a conjugate of cell-penetrating peptide and melphalan and a formulation comprising the same. Specifically, the present invention relates to a conjugate formed by covalently linking cell-penetrating peptide derivative to melphalan, a formulation comprising the conjugate, a method for treating diseases with the conjugate, and the application of the formulation in treating diseases.

The invention provides melflufen, or a salt thereof, or a pharmaceutical formulation comprising melflufen, or a salt thereof, for use in the treatment and / or prophylaxis of immunoglobulin light chain (AL) amyloidosis. The invention also provides dosage regimens and kits that find utility in the treatment and / or prophylaxis of AL amyloidosis, and methods for the treatment and / or prophylaxis of AL amyloidosis, and uses of melflufen, or a salt thereof, for the manufacture of a medicament for the treatment of AL amyloidosis.

The invention discloses a supramolecular polypeptide-drug coupled prodrug nano material for treating multiple myeloma as well as a preparation method and application of the supramolecular polypeptide-drug coupled prodrug nano material. According to the nano material, hyaluronic acid modified by beta-cyclodextrin is taken as a skeleton, and a melphalan-dexamethasone double-drug coupling compound coupled with an adamantane modified GFLG short peptide connexon is loaded through a supramolecular host-guest effect. The nano material has good stability and drug entrapment capacity under physiological conditions, and can realize quick-response drug release under the condition of simulating an enzymatic environment in myeloma cells. The nano material can realize efficient cellular uptake and specific drug activated release, so that proliferation of multiple myeloma cells is inhibited, and a new strategy for delivery of the multiple myeloma nano drug with a synergistic treatment effect is provided.

The invention is directed to stable, liquid pharmaceutical compositions comprising melphalan, at least one cyclodextrin, at least one non-aqueous solvent, water and / or at least one aqueous buffer, at least one antioxidant, optionally, at least one chelating agent, and, optionally, at least one inorganic salt. The invention is also directed to the use of the compositions of the invention for the treatment of cancers, their preparation, and dosage forms containing them.

The invention relates to a milobain transdermal delivery preparation which comprises the following components in percentage by weight: 8-12% of milobain or benzene sulfonate thereof (in terms of free alkali), 40-60% of an acrylic acid pressure-sensitive adhesive matrix, 8-12% of a polyvinylpyrrolidone crystal inhibitor, 9-22% of a solubilizer composition and 9-22% of a penetration enhancer composition, and the sum of the components is 100%. The preferable prescription of the transdermal drug delivery preparation has the following beneficial effects: (1) the crylic acid pressure-sensitive adhesive matrix is used as a drug carrying basis, and the crystal inhibitor is combined to effectively inhibit drug crystallization and separation, so that the long-term physical stability and uniformity of the preparation are ensured; (2) the solubilizing composition cooperates with the crystal inhibitor to maintain the supersaturated state of the medicine, so that the dissolving bottleneck of the miloabalin is overcome, and a foundation is laid for efficient transdermal release; (3) the penetration enhancer composition significantly improves the cumulative release rate, and shows excellent and stable penetration enhancing effect and long-acting release characteristic when being matched with different solubilizers; and (4) the adhesive force is moderate: the adhesive force of the preferable prescription is 9-14N, so that the adhesive strength and the comfort can be balanced, and the requirements of skin patches are met.

(3R, 4S)-3-(4-hydroxy-3,5-dimethoxyphenyl)-4-(4-hydroxyphenyl)-8-methyl-3,4-dihydro-2H- chromen-7-ol (TRX-E-002-1) for use in a method of treatment for a hematological cancer being acute myeloid leukemia or multiple myeloma in a subject in need thereof, the method comprising administering to the subject an effective amount of TRX-E-002-1. The method may further comprise administering to the subject an effective amount of a second compound selected from the group consisting of (i) a BCL-2 inhibitor such as venetoclax, navitoclax or obatoclax, (ii) a deoxycytidine analogue chemotherapeutic such as cytarabine or gemcitabine, (iii) a hypomethylating agent such as azacitidine or decitabine, (iv) an anthracycline chemotherapeutic such as daunorubicin, doxorubicin, epirubicin, idarubicin, valrubicin or mitoxantrone, (v) a proteasome inhibitor such as carfilzomib, bortezomib, and ixazomib, (vi) an immunomodulatory drug such as pomalidomide, lenalidomide, and thalidomide and(vii) a corticosteroid drug such as dexamethasone or prednisone, and (viii) an alkylator such as bendamustine, cyclophosphamide, melphalan, and melflufen. Corresponding combination pharmaceutical compositions.

The invention discloses an active oxygen response type tumor diagnosis and treatment integrated microneedle patch and a preparation method and application thereof. The microneedle patch comprises a microneedle; the active oxygen response type prodrug FDOCl-19 comprises a phenothiazine structure, and the active oxygen response type prodrug FDOCl-19 is loaded on the microneedle. In a microenvironment with high ROS expression in a tumor area, FDOCl-19 is activated to release a large amount of anti-cancer drug melphalan and fluorophore methylene blue in a short time, melphalan effectively prevents growth of tumors, methylene blue can realize in-situ fluorescence imaging of the tumors, and the microneedle patch has the characteristics of on-demand drug delivery and high safety, and can be applied to the field of tumor treatment. And painless, noninvasive and precise treatment of superficial tumors is realized.