Application of omeprazole in relieving toxic and side effects of tyrosine kinase inhibitor TKIs

A technology of tyrosine kinase and omeprazole, which is applied in the field of medicine, can solve the problems affecting the quality of life, immune function impairment, and easy recurrence of NSCLC patients, so as to enhance the inhibition of proliferation and apoptosis, and inhibit the symptoms of rash, The effect of improving the quality of life

Pending Publication Date: 2021-03-19
北京京佑奇康科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

And a large number of studies have shown that TKIs have great damage to immune function, which greatly affects the quality of life of NSCLC patients
At the same time, due to the ...

Method used

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  • Application of omeprazole in relieving toxic and side effects of tyrosine kinase inhibitor TKIs
  • Application of omeprazole in relieving toxic and side effects of tyrosine kinase inhibitor TKIs
  • Application of omeprazole in relieving toxic and side effects of tyrosine kinase inhibitor TKIs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073] Example 1 Bioinformatics analysis

[0074] The invention utilizes the data of lung cancer disease expression profile and TKIs drug expression profile, and applies functional genomics method to predict that omeprazole and TKIs have a certain synergistic effect.

[0075] Method steps:

[0076] The lung cancer disease expression profile and TKIs drug expression profile data obtained in the early stage of the present invention are used. First, the Impute package was used to normalize and annotate the expression profiles. Subsequently, the Limma software package was used to screen the differential genes in the expression profile, and the screening criteria for the differential genes was FDR2 FC|>1, to obtain the characteristic expression genes of lung cancer and TKIs. Then apply the EpiMed platform (EpiMed) designed based on the theory of "systems biology" and "comparative functional genomics" to conduct multi-omics correlation analysis on the characteristic expression gen...

Embodiment 2

[0079] Embodiment 2 Omeprazole combined with gefitinib clinical trial

[0080] In view of the side effects of gefitinib on the skin and gastrointestinal tract during the administration of non-small cell lung cancer patients, mainly including diarrhea and rash below grade II, the incidence rates are 55% and 46% respectively. About 12% of patients will experience nausea and so on. Severe cases will have to stop the drug due to the side effects of the digestive tract, which will adversely affect the treatment. In this part of the trial, omeprazole combined with gefitinib was used to verify its clinical performance.

[0081] Subjects: randomized 32 patients with non-small cell lung cancer who failed first-line treatment:

[0082] Medication regimen:

[0083] Scheme 1: Gefitinib monotherapy (250mg / d, 17 cases);

[0084] Scheme 2: Gefitinib monotherapy (250mg / d) combined with omeprazole (20mg / d, 15 cases);

[0085] Treatment time: The median treatment time is 32 months; ...

Embodiment 3

[0091] Embodiment 3 Omeprazole combined imatinib clinical trial

[0092] In order to further verify the clinical effect of omeprazole combined with other TKIs, this example further uses omeprazole combined with imatinib for verification.

[0093] Subjects of the clinical trial: 26 random cases of non-small cell lung cancer patients who failed first-line treatment;

[0094] Dosing regimen: scheme 1 imatinib monotherapy (400mg / d, 14 cases); scheme 2 imatinib monotherapy (400mg / d) combined with omeprazole (20mg / d, 12 cases), treatment time : The median treatment time is 32 months;

[0095] Clinical manifestations: In the imatinib monotherapy group, there were no patients with CR, 6 cases with PR, and 5 cases with SD. The total effective rate was 42.9%. Mild rash occurred in 5 patients, and diarrhea symptoms occurred in 7 patients. In the combined treatment group, 2 cases were CR, 6 cases were PR, and 4 cases were SD, and the total effective rate was 66.6%. One patient ha...

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Abstract

The invention relates to application of omeprazole in relieving toxic and side effects of a tyrosine kinase inhibitor TKIs. Omeprazole and the tyrosine kinase inhibitor are combined to find that omeprazole not only can enhance the proliferation inhibition effect and apoptosis effect of the TKIs on cancer cells, but also can greatly relieve diarrhea and rash adverse reactions of patients caused bytaking the TKIs. The invention has the advantages of good economy and high safety, and can relieve the toxic and side effects of targeted drugs, improve the living quality of patients and reduce the economic burden of patients.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to the use of omeprazole for alleviating the toxic and side effects of tyrosine kinase inhibitors. [0002] technical background [0003] Omeprazole, 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfinyl]-1H-benzimidazole, is Proton Pump Inhibitor (PPI) is a fat-soluble weakly basic drug, which currently has the strongest inhibitory effect on gastric acid secretion. Research in the prior art has found that omeprazole is easily concentrated in an acidic environment, and specifically acts on the secretory microtubules formed by the apical membrane of the gastric parietal cells and the tubular vesicles in the cytoplasm, i.e. the proton pump of the gastric parietal cells ( H+, K+-ATPase) site, and converted into the active form of sulfenamide, irreversibly combined with the sulfhydryl group of the proton pump through the disulfide bond, thereby inhibiting the act...

Claims

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Application Information

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IPC IPC(8): A61K31/4439A61K31/5377A61K31/506A61K45/06A61P35/00A61P11/00A61P1/12A61P17/00
CPCA61K31/4439A61K31/506A61K31/5377A61K45/06A61P1/12A61P11/00A61P17/00A61P35/00A61K2300/00
Inventor 卢学春迟小华
Owner 北京京佑奇康科技有限公司
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