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Novel PD-1 tumor immunosuppressant and drug preparation method thereof

An immunosuppressant, PD-1 technology, applied in anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., can solve the problems of limited reports and embarrassment of PD-1 inhibitors, achieve inhibition of cancer cell immunity and humoral immunity, improve The effect of killing ability and improving antigen phagocytosis ability

Inactive Publication Date: 2018-09-07
HENAN TIANSHENG TAIFENG PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] PD-1 inhibitors are already on the market in the United States. Due to the embarrassing status and complex mechanism of PD-1 inhibitors, the English version of the drug instructions has brought a lot of trouble to users. When using drugs, due to PD- 1 Inhibitors are not yet on the market in the mainland, and many patients need to communicate with the attending doctor to ask the attending doctor to help the patient use the PD-1 inhibitor, and the English instructions will also cause some troubles for the doctor. Therefore, PD-1 inhibitors in the mainland It has not been used yet, and only some English instructions can be found on the website, and the Chinese literature reports of PD-1 inhibitors are very limited

Method used

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  • Novel PD-1 tumor immunosuppressant and drug preparation method thereof
  • Novel PD-1 tumor immunosuppressant and drug preparation method thereof
  • Novel PD-1 tumor immunosuppressant and drug preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

5 copies

[0033] The preparation method of the immunosuppressant medicine comprises the following steps:

[0034] (1) Add the PD-1 monoclonal antibody into a glass container, add a small amount of water, adjust the solution concentration to 250 g / ml with sodium carbonate buffer solution with a pH of 9.0, dialyze overnight at a low temperature of 1°C, and then dissolve the PD-1 monoclonal antibody Anti-transfer into a shock container, avoid light and shake for 4 hours, and store it at -20°C for standby;

[0035] (2) Take the metabolic antagonist, disperse it in 30ml of chloroform, add alkaloid, incubate at room temperature for 25min, then add platinum agent, stir magnetically at a constant temperature at room temperature, add dropwise 10% ammonia water to adjust the pH to 9.2, Continue to stir for 10 minutes, then transfer to a water bath on a rotary evaporator to 80°C, drain the air in the bottle and continue to rotate, remove the organic phase, and set aside;

[0036]...

Embodiment 2

[0038]

[0039]

[0040] The preparation method of the immunosuppressant medicine comprises the following steps:

[0041] (1) Add PD-1 monoclonal antibody into a glass container, add a small amount of water, adjust the solution concentration to 200g / ml with sodium carbonate buffer solution with a pH of 9.2, dialyze overnight at 4°C, and then dissolve PD-1 monoclonal antibody Anti-transfer into a shock container, avoid light and shake for 3 hours, and store it at -20°C for standby;

[0042](2) Take the metabolic antagonist, disperse it in 30ml of chloroform, add alkaloid, incubate at room temperature for 30min, then add platinum agent, stir magnetically at a constant temperature at room temperature, add dropwise 10% ammonia water to adjust the pH to 9.0, Continue to stir for 15 minutes, then transfer to a water bath on a rotary evaporator to 80°C, drain the air in the bottle and continue to rotate, remove the organic phase, and set aside;

[0043] (3) Take the material o...

Embodiment 3

[0045]

[0046]

[0047] The preparation method of the immunosuppressant medicine comprises the following steps:

[0048] (1) Add PD-1 monoclonal antibody into a glass container, add a small amount of water, adjust the solution concentration to 250g / ml with sodium carbonate buffer solution with a pH of 9.0, dialyze overnight at 2°C, and then dissolve PD-1 monoclonal antibody Anti-transfer into a shock container, avoid light and shake for 4 hours, and store it at -20°C for standby;

[0049] (2) Take the metabolic antagonist, disperse it in 30ml of chloroform, add alkaloid, incubate at normal temperature for 25min, then add platinum agent, stir magnetically at constant temperature at room temperature, add dropwise 10% ammonia water to adjust the pH to 9.0, Continue to stir for 15 minutes, then transfer to a water bath on a rotary evaporator to 80°C, drain the air in the bottle and continue to rotate, remove the organic phase, and set aside;

[0050] (3) Take the material ...

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Abstract

The invention relates to the technical field of drug inhibitors, in particular to a novel PD-1 tumor immunosuppressant and a drug preparation method thereof. The immunosuppressant is prepared from byweight, 30-45 parts of PD-1 monoclonal antibody, 2-6 parts of alkaloid, 4-7 parts of antibiotic, 3-9 parts of alkylating agent, 1-5 parts of platinum agent and 5-9 parts of metabolic antagonist; the alkaloid consists of one or more of paclitaxel, vincristine and docetaxel; the antibiotic consists of one or more of epirubicin, idarubicin and mitomycin; the alkylating agent is one or two of ifosfamide and dacarbazine; the platinum agent is one or two of cisplatin and oxaliplatin; the metabolic antagonist is one or more of gemcitabine, cytarabine and tegafur. The immunosuppressant can block the interaction between PD-L1 molecules expressed on tumor cells and receptors on activated T cells, inhibit the apoptosis of the activated T cells and improve the killing capability of the tumor cells.

Description

technical field [0001] The invention relates to the technical field of drug inhibitors, in particular to a novel PD-1 tumor immunosuppressant and a preparation method thereof. Background technique [0002] Tumor immunotherapy is to mobilize the body's immune system to enhance anti-tumor immunity, thereby inhibiting and killing tumor cells. Tumor immunotherapy is one of the most promising research directions in the field of tumor treatment. PD-1 is obtained in the apoptotic T cell hybridoma, and it is named as the programmed death-1 receptor because of its association with apoptosis, and the PD-1 programmed death receptor is an important immunosuppressive Factor, a member of the CD28 superfamily. [0003] PD-1 inhibitors are a breakthrough mechanism of anticancer drugs, and have shown efficacy in multiple indications such as melanoma, kidney cancer, lung cancer, head and neck cancer, bladder cancer, and breast cancer. The breadth, depth, and durability of its response are ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K39/395A61P35/00A61K31/337A61K31/475A61K31/704A61K31/407A61K31/675A61K31/4164A61K33/24A61K31/7068
CPCA61K39/395A61K31/337A61K31/407A61K31/4164A61K31/475A61K31/675A61K31/704A61K31/7068A61K33/24A61P35/00A61K2300/00
Inventor 沙薇梁建华杨艳丽韩永春
Owner HENAN TIANSHENG TAIFENG PHARM TECH CO LTD
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