12 results about "Nilotinib" patented technology

The present application belongs to the technical field of pharmaceutical analysis, and particularly relates to a kind of analytical method for determining genetic toxic impurities in nilotinib composition.The present application has good specificity, simple operation, high sensitivity, low cost, and is suitable for frequent detection in mass production, etc., for determining impurity A in compositions such as nilotinib oral suspension, nilotinib dry suspension or nilotinib capsules.The method can effectively separate the nilotinib impurity A peak from its adjacent impurity peak, and solve the problem of easy damage of the chromatographic column during the determination of nilotinib impurity A.

The application relates to the technical field of biological medicine, and discloses application of Nilotinib in preparation of a drug for inhibiting p53-AKT interaction. Relying on a double-fluorescence reporting system NanoBRET system, high-throughput screening is completed at a live cell level, and it is determined that a tyrosine kinase inhibitor Nilotinib can inhibit p53-AKT interaction. Function verification shows that Nilotinib can dose-dependently destroy a p53-AKT complex in HEK293T tool cells and U87MG, T98G and other glioma cells, release the inhibition of p53 function, and induce cell apoptosis. The above results illustrate a new path of precise intervention with the "p53-AKT interface" as a target, and provide experimental basis for redirecting Nilotinib to overcome p53-related drug resistance.

This invention provides a nilotinib capsule with reduced food-related effects and its preparation method, addressing the shortcomings of existing products. It solves the problem that existing products require avoiding the influence of food. This invention innovatively improves the dissolution and release of the drug in media with different pH values ​​by adding a specific combination of acidic pH adjusters and solubilizers to the formulation. This innovative formulation adjustment solves the problem of food affecting the release and absorption of this product, and improves the time-limited nature of administration. Therefore, this invention has great application value and promising prospects for promotion.

The invention discloses a preparation method of nilotinib, which is characterized in that easily available industrial raw materials and common intermediates are adopted, and the nilotinib is prepared through optimized carbon-nitrogen coupling reaction. The preparation method has the advantages of easily available raw materials, simple process, mild conditions and few side reactions, can better control the generation and transmission of drug impurities, and improves the drug quality and safety. Compared with the prior art, the process can effectively reduce the production cost and reduce the environmental pollution, has industrial production prospects, and can promote the economic and technical development of the raw material medicine.

Amorphous solid dispersions of nilotinib fumarate or nilotinib tartrate are provided, as well as pharmaceutical compositions thereof, wherein the compositions exhibit enhanced bioavailability in the fasted state. Preferably, the compositions may be orally administered to a patient in either the fed or fasted state, with a decrease or elimination of the food effect. Preferably, following oral administration of the pharmaceutical compositions, there is no substantial difference in the pharmacokinetic parameters (e.g., Cmax, AUC0-t and / or AUC0-infinity) of nilotinib, regardless of whether the pharmaceutical compositions are administered to a subject in the fed or fasted state.

This invention discloses the application of ZAK inhibitors in the preparation of drugs for treating EV71 virus infection, relating to the biomedical field. The ZAK inhibitors exert their effects by inhibiting the ZAK-p38 MAPK signaling pathway and by inhibiting the ZAKα-mediated ribosomal toxicity stress response (RSR). The ZAK inhibitor is nilotinib or a pharmaceutically acceptable salt thereof. Cellular and animal experiments of this invention demonstrate that EV71 infection activates the ZAKα-mediated p38 MAPK pathway (RSR), promoting viral replication and leading to multi-organ damage. ZAK inhibitors (such as nilotinib) can inhibit this pathway, reduce the expression of the viral protein VP1, and improve infection-induced renal function damage, metabolic disorders, and muscle damage. Therefore, ZAK inhibitors can be used to prepare anti-EV71 drugs.

Provided are pharmaceutical compositions which include a mixture of a lipophilic active pharmaceutical ingredient such as nilotinib, a hydrophilic polymer, one or more surfactants, and optionally an adsorbent. Also described are methods for preparing and using such pharmaceutical compositions. In one aspect, disclosed herein is an amorphous solid dispersion comprising the active pharmaceutical ingredient.

Provided are pharmaceutical compositions which include a mixture of a lipophilic active pharmaceutical ingredient such as nilotinib, a hydrophilic polymer, one or more surfactants, and optionally an adsorbent. Also described are methods for preparing and using such pharmaceutical compositions. In one aspect, disclosed herein is an amorphous solid dispersion comprising the active pharmaceutical ingredient.

The application relates to application of nilotinib in preparation of anti-neuroblastoma drugs, and discloses a novel signal axis driving neuroblastoma progression: USP39-KLF1-SNARE-Golgi diffusion, and finds a new use of nilotinib in preparation of anti-neuroblastoma drugs. The application finds that nilotinib can effectively destroy the protein interaction between USP39 and KLF1. The destruction leads to the decrease of KLF1 protein stability, the inhibition of the transcription activity of KLF1, the down-regulation of the expression of VAMP3 / VAMP8, the weakening of the SNARE complex function, the reversal of the Golgi diffusion phenotype, and the slowing down of the growth of neuroblastoma. Nilotinib is a marketed drug, and has clear human safety data, so the clinical transformation can be accelerated.

Provided herein are amorphous solid dispersions of nilotinib fumarate or nilotinib tartrate, and pharmaceutical compositions thereof, wherein the compositions exhibit enhanced bioavailability in the fasted state. Preferably, the compositions can be orally administered to a patient in the fed or fasted state with a reduction or elimination of food effect. Preferably, there is no substantial difference in the pharmacokinetic parameters (e.g., C max , AUC 0‑t , and / or AUC 0‑无穷大 ) of nilotinib following oral administration of the pharmaceutical composition, whether the pharmaceutical composition is administered to the subject in the fed or fasted state.

Disclosed herein are compositions that contain a salt of Nilotinib and a polymer, which composition have improved properties in terms of solubility and bioavailability and which are useful for treating disorders of uncontrolled cellular proliferation. Methods of using the compositions are also described

The present application relates to the biomedical technology field, and more particularly to a kind of nano drug preparation and its preparation method and application.The nano drug preparation includes rosmarinic acid and nilotinib, and the mass ratio of rosmarinic acid and nilotinib is 1:0.1-2.The present application provides a kind of composition of rosmarinic acid and nilotinib, which can synergistically activate autophagy, has the effect of neuroprotection and antioxidant stress.The drug loaded with rosmarinic acid and nilotinib provided by the present application can effectively protect dopaminergic neurons in substantia nigra, and then improve the motor symptoms of MPTP-induced PD mice, and provide a prospective scheme for PD targeted therapy.