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A kind of drug combination containing plinabulin and application thereof

A drug and drug resistance technology, applied in the field of drug combinations containing plinabulin, can solve the problems of long-term malignant tumors, poor selectivity of tumor cells, drug resistance or drug resistance, etc., to achieve convenient drug administration and improve The effect of bioavailability

Active Publication Date: 2022-04-01
ZUNYI MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, Plinabulin, like other chemotherapeutic drugs, has poor selectivity to tumor cells, and will inevitably damage normal cells of the human body while killing cancer cells, resulting in adverse drug reactions. Moreover, these toxic Side effects are positively correlated with the dosage of Plinabulin
At the same time, the treatment of malignant tumors takes a relatively long time. During the long-term treatment, drug resistance or drug resistance will inevitably gradually occur. People must also change different drugs from time to time to avoid drug resistance or drug resistance.

Method used

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  • A kind of drug combination containing plinabulin and application thereof
  • A kind of drug combination containing plinabulin and application thereof
  • A kind of drug combination containing plinabulin and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] When the combination of Plinabulin and Tetrandrine is used in human treatment, the dosage of the two drugs is determined according to the phase II clinical data or instructions. The specific situation is: according to the Phase II clinical data of Plinabulin, Plinabulin The daily recommended dosage of Nabuline is 32-48mg, continuous medication for 4 weeks, 2 weeks of drug withdrawal, 6 weeks as a course of treatment. According to the instruction manual of tetrandrine, the daily recommended dosage of tetrandrine is 200 mg, administered twice a week for 2 consecutive weeks, and stopped for 1 week, repeating this twice, 6 weeks as a course of treatment. According to the average adult body weight of 60kg, the daily recommended dosage of Plinabulin is converted into clinical daily dosage per kilogram of body weight, and the daily dosage of Plinabulin is: 0.53-0.8mg / kg body weight / day. According to the average adult body weight of 60kg, the daily recommended dosage of tetrand...

experiment example 1

[0045] Experimental Example 1 Cell Experiment

[0046] 1. Cell selection and active culture

[0047] The experiments selected vincristine-resistant human gastric cancer cells SGC-7901 / VCR, human gastric cancer cells SGC-7901, human breast cancer cells MDA-MB-231, doxorubicin-resistant human chronic myelogenous leukemia cells K-562 / ADR, human Histiocytic lymphoma cells U-937. Vincristine-resistant human gastric cancer cells SGC-7901 / VCR, human gastric cancer cells SGC-7901, and human breast cancer cells MDA-MB-231 were cultured in DMEM+10% FBS complete medium. Human histiocytic lymphoma cells U-937 were cultured in 1640+10% FBS complete medium. Doxorubicin-resistant human chronic myeloid leukemia cells K-562 / ADR were cultured in IMDM+10% FBS complete medium. The above cells were kept at 37°C with 5% CO 2 , cultured in a cell incubator with saturated humidity.

[0048] 2. Experimental method

[0049] After each tumor cell line is in a stable state, spread the cells in a 96...

experiment example 2

[0079] Experimental example 2 Nude mouse transplantation tumor experiment

[0080] In the course of this experiment, the injection dose was based on the US Food and Drug Administration (FDA) "Estimating the Safe Starting Dose in Clinical Trials for Therapeutics in Adult Healthy Volunteers" (Estimating the Safe Starting Dose in Clinical Trials for Therapeutics in Adult Healthy Volunteers) ), the injection dose conversion ratio of human body and nude mice (ie, nude mice in experimental verification) required to achieve the same biological effect is calculated as 1:12.3. Based on this conversion ratio, the dosage of the nude mice used in the experiment was converted by comparing the dosage of the human body. Data were analyzed with Graphpad Prism 8.0 software, P<0.05 was considered significant difference (*P<0.05; **P<0.01; ***P<0.001).

[0081] In each embodiment, the dosage of tetrandrine is: 40.96mg / kg (3.33mg / kg×12.3) according to the body weight of nude mice, and the dosage...

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Abstract

The invention relates to the technical field of cancer chemotherapeutic drugs, and discloses a drug combination containing plinabulin and an application thereof. The active ingredients of this drug combination include plinabulin and tetrandrine. The combined use of tetrandrine and plinabulin can inhibit and kill various malignant tumor cells, and can reduce the dosage of drugs, shorten the treatment cycle, reduce toxic and side effects, and reduce the adverse reactions caused by toxic and side effects. In terms of avoiding drug resistance or drug resistance, there is a new option.

Description

technical field [0001] The invention relates to the technical field of cancer chemotherapeutic drugs, in particular to a drug combination containing plinabulin and an application thereof. Background technique [0002] Cancer is one of the diseases that seriously endanger people's health today. Chemotherapy is one of the methods to treat malignant tumors (cancer). It uses chemical drugs to prevent the proliferation, infiltration and metastasis of cancer cells, and finally kills cancer cells. treatment. However, the therapeutic effect of chemotherapy on cancer often leads to the failure of chemotherapy due to the following aspects: 1) the restrictive dose of chemotherapy drugs is too large, and the patient cannot tolerate sufficient treatment dose and course of treatment; 2) the selectivity of chemotherapy drugs is poor, which will cause serious toxicity Side effects; 3) Multidrug resistance (MDR) of tumor cells to chemotherapeutic drugs. [0003] Plinabulin is a diketopiper...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/496A61K31/4748A61K9/08A61K9/00A61P35/00A61P35/02
CPCA61K31/496A61K31/4748A61K9/08A61K9/0019A61K9/0053A61P35/00A61P35/02A61K2300/00
Inventor 高宁雷令姜秀星王梅申立文
Owner ZUNYI MEDICAL UNIVERSITY
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