CN115487195A - New application and medicine of mozavaptan compounds - Google Patents

New application and medicine of mozavaptan compounds Download PDF

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CN115487195A
CN115487195A CN202211197699.6A CN202211197699A CN115487195A CN 115487195 A CN115487195 A CN 115487195A CN 202211197699 A CN202211197699 A CN 202211197699A CN 115487195 A CN115487195 A CN 115487195A
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mozavaptan
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彭聪
陈翔
晏铭洁
周冰静
刘念
张旭
伍劼
陶倩
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Xiangya Hospital of Central South University
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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Abstract

The invention relates to a new application and a medicine of a mozavaptan compound, wherein the mozavaptan compound is selected from at least one of mozavaptan and derivatives thereof. Clinical experiments prove that the mozavaptan compound which is commonly used as a V2 receptor antagonist (non-peptide AVP2 receptor antagonist) can inhibit the proliferation of malignant melanoma cells such as SK-MEL-5 cells, SK-MEL-28 cells, A375 cells and the like, further can effectively inhibit the growth of malignant skin tumors, and clinical experiments on mice show that the mozavaptan compound has no obvious toxic or side effect, thereby providing a new breakthrough direction for preventing and treating the skin tumors.

Description

New application and medicine of mozavaptan compounds
Technical Field
The invention relates to the technical field of pharmacy, and in particular relates to a new application of a mozavaptan compound and a medicine.
Background
Skin tumor is a cell proliferative disease occurring in skin, is a common disease, is a new organism which often occurs in intradermal or subcutaneous tissues, has a plurality of types, is clinically divided into benign tumor and malignant tumor, can continuously proliferate to cause metastasis, and threatens life, and is called malignant skin tumor or skin cancer. Malignant skin tumors are dermatological diseases that are difficult to treat, and mainly include: basal cell carcinoma, squamous cell carcinoma, malignant melanoma, paget's disease, etc.
Among them, malignant melanoma, usually abbreviated as melanoma, is a highly malignant skin tumor, abbreviated as malignant melanoma, which often occurs on the skin, mucous membrane and internal organs. Malignant melanoma is the main type of malignant tumor of the skin, and can be formed by the evolution of congenital or acquired benign melanocytic nevus, or the malignant melanoma is formed by the malignant alteration of dysplastic nevus, and in recent years, the incidence rate and the death rate of malignant melanoma are increased year by year. The treatment of malignant melanoma lacks specific drug treatment, and early surgical excision is mainly adopted, but the prognosis is poor, and postoperative recurrence brings huge challenges to treatment.
Accordingly, there is a need for improvement in the art.
Disclosure of Invention
Based on the above, the invention provides a new application and a drug of a mozavaptan compound, and aims to provide a new direction for preventing and treating skin tumors.
The technical scheme of the invention for solving the technical problems is as follows.
In one aspect of the invention, the invention provides an application of a mozavaptan compound in preparation of a drug for preventing and treating skin tumors, wherein the mozavaptan compound is selected from at least one of mozavaptan and derivatives thereof.
In some of these embodiments, the skin tumor comprises melanoma.
In some of these embodiments, the derivative of mozavaptan comprises a pharmaceutically acceptable salt of mozavaptan or a pharmaceutically acceptable ester compound of mozavaptan.
In some of these embodiments, the mozavaptan class compound is selected from at least one of mozavaptan and mozavaptan hydrochloride.
In some embodiments, the skin tumor prevention and treatment drug is a drug for inhibiting melanoma cell proliferation.
In some of these embodiments, the melanoma cells are at least one of SK-MEL-5 cells, SK-MEL-28 cells, and A375 cells.
In another aspect of the invention, a medicament for preventing and treating skin tumors is provided, and an active ingredient of the medicament for preventing and treating skin tumors comprises a mozavaptan compound, wherein the mozavaptan compound is at least one selected from the group consisting of mozavaptan and derivatives thereof.
In some embodiments, the components of the drug for preventing and treating skin tumor further comprise a pharmaceutically acceptable matrix, wherein the pharmaceutically acceptable matrix is selected from at least one of sustained release agent, excipient, filler, adhesive, wetting agent, disintegrating agent, absorption enhancer, adsorption carrier, surfactant, lubricant and solvent for injection.
In some embodiments, the drug for preventing and treating skin tumor is injection, and the matrix comprises solvent for injection.
In some of these embodiments, the solvent for injection comprises at least one of water for injection, oil for injection, ethanol, propylene glycol, dimethyl sulfoxide, and polyethylene glycol.
The skilled person of the present application finds: mozavaptan compounds which are commonly used as V2 receptor antagonists (non-peptide AVP2 receptor antagonists) can effectively prevent and treat malignant skin tumors including malignant melanoma, and the mozavaptan compounds can inhibit the proliferation of malignant melanoma cells such as SK-MEL-5 cells, SK-MEL-28 cells, A375 cells and the like, and animal experiments show that the mozavaptan compounds can effectively inhibit the tumor growth of B16F10 tumor-bearing C57 mice, have no obvious toxic or side effect, and provide a new breakthrough direction for preventing and treating skin tumors.
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In order to more clearly illustrate the embodiments of the present invention or the technical solutions in the prior art, the drawings used in the description of the embodiments or the prior art will be briefly described below, and it is obvious that the drawings in the following description are some embodiments of the present invention, and other drawings can be obtained by those skilled in the art without creative efforts.
FIG. 1 is a graph showing the inhibition of proliferation of melanoma A375 cells in the test group and the control group in example 1;
FIG. 2 is a graph showing the inhibition of proliferation of SK-MEL-5 cells in melanoma as measured by the test and control groups in example 1;
FIG. 3 is a graph showing the inhibition of proliferation of SK-MEL-28 cells, which are melanoma, in the test group and the control group of example 1;
FIG. 4 is a graph showing the actual comparison of the volumes of B16F 10-bearing tumors after treatment in the test group and the control group in example 2;
FIG. 5 is a graph showing a comparison of the change in body weight of C57BL/6 mice in the test group and the control group in example 2.
Detailed Description
Reference will now be made in detail to embodiments of the invention, one or more examples of which are described below. Each example is provided by way of explanation, not limitation, of the invention. In fact, it will be apparent to those skilled in the art that various modifications and variations can be made in the present invention without departing from the scope or spirit of the invention. For instance, features illustrated or described as part of one embodiment, can be used on another embodiment to yield a still further embodiment.
It is therefore intended that the present invention cover the modifications and variations of this invention provided they come within the scope of the appended claims and their equivalents. Other objects, features and aspects of the present invention are disclosed in or are apparent from the following detailed description. It is to be understood by one of ordinary skill in the art that the present discussion is a description of exemplary embodiments only, and is not intended as limiting the broader aspects of the present invention.
Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs. The terminology used in the description of the invention herein is for the purpose of describing particular embodiments only and is not intended to be limiting of the invention. As used herein, the term "and/or" includes any and all combinations of one or more of the associated listed items.
The terms "comprises," "comprising," or any other variation thereof, are intended to cover a non-exclusive inclusion, such that a process, method, article, or apparatus that comprises a list of elements does not include only those elements but may include other elements not expressly listed or inherent to such process, method, article, or apparatus. Without further limitation, an element defined by the phrases "comprising a," "8230," "8230," or "comprising" does not exclude the presence of additional like elements in a process, method, article, or apparatus that comprises the element. The indefinite articles "a" and "an" preceding an element or component of the invention are not intended to limit the number requirement (i.e., the number of occurrences) of the element or component. Thus, "a" or "an" should be read to include one or at least one, and the singular form of an element or component also includes the plural unless the number clearly indicates only the singular. "plurality" means at least two, e.g., two, three, etc., unless specifically limited otherwise.
The weight of the related components mentioned in the description of the embodiments of the present invention may not only refer to the specific content of each component, but also represent the proportional relationship of the weight among the components, and therefore, the content of the related components is scaled up or down within the scope disclosed in the description of the embodiments of the present invention as long as it is in accordance with the description of the embodiments of the present invention. Specifically, the weight described in the description of the embodiment of the present invention may be a unit of mass known in the chemical industry field, such as μ g, mg, g, and kg.
Other than as shown in the operating examples, or where otherwise indicated, all numbers expressing quantities of ingredients, physical and chemical properties, and so forth used in the specification and claims are to be understood as being modified in all instances by the term "about". For example, unless indicated to the contrary, the numerical parameters set forth in the foregoing specification and attached claims are approximations that can be suitably varied by those skilled in the art utilizing the teachings disclosed herein to achieve the desired properties. The use of numerical ranges by endpoints includes all numbers within that range and any range within that range, for example, 1 to 5 includes 1, 1.1, 1.3, 1.5, 2, 2.75, 3, 3.80, 4, and 5, and the like.
As shown in the background art, the treatment of malignant melanoma lacks specific drug treatment, and early surgical excision is mainly adopted, but the prognosis is poor, and postoperative recurrence brings huge challenges to treatment. Therefore, the development of effective drugs against malignant melanoma has been a problem for those skilled in the art.
However, the development process for new drugs is time consuming for those skilled in the art, including: the method comprises the steps of selecting a target, then carrying out lead compound research, then carrying out structure-activity relationship research and active compound screening, then selecting a candidate drug, and then carrying out preclinical research, and the mass production challenge is also faced after new drug development, so that a long time is spent from research and development to market, and no new specific drug is marketed so far.
Therefore, the technical scheme of the application is obtained by breaking the conventional rules, creatively proposing 'new application of old medicine', and finding that the mozavaptan compound which is commonly used as a V2 receptor antagonist (non-peptide AVP2 receptor antagonist) can effectively prevent and treat malignant skin tumors including malignant melanoma.
The invention provides an application of a mozavaptan compound in preparation of a drug for preventing and treating skin tumors, wherein the mozavaptan compound is selected from at least one of mozavaptan and derivatives thereof.
The skilled person in the present application finds: mozavaptan compounds which are commonly used as V2 receptor antagonists (non-peptide AVP2 receptor antagonists) can effectively prevent and treat malignant skin tumors including malignant melanoma, and the mozavaptan compounds can inhibit the proliferation of malignant melanoma cells such as SK-MEL-5 cells, SK-MEL-28 cells, A375 cells and the like, and animal experiments show that the mozavaptan compounds can effectively inhibit the tumor growth of B16F10 tumor-bearing C57 mice, have no obvious toxic or side effect, and provide a new breakthrough direction for preventing and treating skin tumors.
The research result shows that: the mozavaptan compound has obvious drug effect of preventing and treating skin tumor, is a mass-produced marketed drug, has relatively clear toxicology and pharmacology, and reduces the research and development cost.
In some of these examples, the derivative of mozavaptan comprises a pharmaceutically acceptable salt of mozavaptan or a pharmaceutically acceptable ester compound of mozavaptan.
In some examples, pharmaceutically acceptable salts of mozavaptan include, but are not limited to, at least one of mozavaptan hydrochloride, mozavaptan sulfate, mozavaptan phosphate, mozavaptan nitrate.
In some of these examples, the mozavaptan class compound is selected from at least one of mozavaptan and mozavaptan hydrochloride.
Mozavaptan (mozavaptan) and derivatives thereof are novel vasopressin V2 receptor antagonists, and mozavaptan hydrochloride is a non-peptide V2 receptor antagonist, has a urinary excretion effect, can increase blood sodium ion concentration, and generates beneficial hemodynamic changes. Wherein the Mozavaptan CAS number is 137975-06-5, and the molecular formula is C 27 H 29 N 3 O 2 The structural formula is as follows:
Figure BDA0003871081070000071
mozavaptan hydrochloride (Mozavaptan hydrochloride), CAS number 138470-70-9, molecular formula C 27 H 30 ClN 3 O 2 Molecular weight 464.00, structural formula:
Figure BDA0003871081070000072
in some specific examples thereof, the mozavaptan compound is mozavaptan hydrochloride.
In some of these embodiments, the skin tumor comprises melanoma.
In some embodiments, the skin tumor preventing and treating drug is a drug for inhibiting melanoma cell proliferation.
In some embodiments, the melanoma cell is at least one of SK-MEL-5 cell, SK-MEL-28 cell and A375 cell.
SK-MEL-5 cells, SK-MEL-28 cells and A375 cells are human melanoma cells.
The invention provides a drug for preventing and treating skin tumor, wherein the active ingredient of the drug for preventing and treating skin tumor comprises a mozavaptan compound, and the mozavaptan compound is selected from at least one of mozavaptan and derivatives thereof.
In some embodiments, the composition of the drug for preventing and treating skin tumor further comprises a pharmaceutically acceptable matrix, wherein the pharmaceutically acceptable matrix is selected from at least one of sustained release agent, excipient, filler, adhesive, humectant, disintegrant, absorption enhancer, adsorption carrier, surfactant, lubricant and solvent for injection.
It is understood that the pharmaceutically acceptable matrix can be selected from one of sustained release agent, excipient, filler, binder, wetting agent, disintegrant, absorption enhancer, adsorption carrier, surfactant, solvent for injection and lubricant, or two or more of sustained release agent, excipient, filler, binder, wetting agent, disintegrant, absorption enhancer, adsorption carrier, surfactant and lubricant; and is not limited to the above list, and the kind of the specific substrate may be selected according to the administration form of the drug for preventing and treating skin tumor.
The sustained-release agent, excipient, filler, binder, wetting agent, disintegrant, absorption enhancer, adsorption carrier, surfactant, lubricant and solvent for injection are briefly described herein, and include, but are not limited to, the following species.
Fillers include, but are not limited to, at least one of starch, pregelatinized starch, lactose, microcrystalline cellulose, calcium carbonate, mannitol, dextrin, and sucrose; disintegrants include, but are not limited to, at least one of sodium carboxymethyl starch, crospovidone, sodium bicarbonate, sodium carboxymethyl starch, croscarmellose sodium, and low substituted hydroxypropyl cellulose; lubricants include, but are not limited to, at least one of magnesium stearate, talc, aerosil, hydrogenated vegetable oils, polyethylene glycols, and sodium lauryl sulfate; the surfactant includes, but is not limited to, at least one of carbomer, poloxamer, sodium lauryl sulfate, sodium dodecylbenzene sulfonate, lecithin, polysorbate, sorbitan fatty acid, cholesterol, sucrose fatty acid ester and polyoxyethylene fatty acid ester; binders include, but are not limited to, at least one of starch, methylcellulose, povidone, hypromellose, hydroxypropylcellulose, sodium carboxymethylcellulose, ethylcellulose, polyethylene glycol, and gelatin; humectants include, but are not limited to, ammonium alginate cyclomethicone, glycerin, polydextrose, propylene glycol, sodium hyaluronate, sodium lactate, sorbitol, trehalose, triacetin, triethanolamine, and xylitol; sustained release agent excipients include, but are not limited to, hydrophilic gel matrix tablets, erodible matrix tablets, insoluble matrix tablets, polymer films, and the like.
In some examples, the medicament for preventing and treating skin tumor can also comprise a preservative.
It is understood that preservatives include, but are not limited to, methylparaben, ethylparaben, propylparaben, benzoic acid, sodium benzoate, sorbic acid, potassium sorbate.
In some embodiments, the pharmaceutical composition for preventing and treating skin tumor is in the form of tablet, granule, capsule, injection, oral liquid, ointment, cream or suspension.
In some examples, the pharmaceutical dosage form for preventing and treating skin tumor is tablet. It is understood that when the pharmaceutical dosage form for preventing and treating skin tumor is tablet, disintegrating agent, lubricant, filler, etc. can be included.
The dosage forms of the medicines for preventing and treating skin tumor can be divided into a gastrointestinal administration dosage form and a non-gastrointestinal administration dosage form according to the administration route.
The gastrointestinal administration dosage form refers to a dosage form that the medicinal preparation enters the gastrointestinal tract after oral administration and plays a role of a whole body by local or absorption, such as common powder, tablets, granules, capsules, solutions, emulsions, suspensions and the like.
Parenteral forms of administration are understood to mean all other forms, except for the oral route of administration, which can act locally at the site of administration or can be absorbed to exert a systemic effect, for example by injection; such as injections, including intravenous injection, intramuscular injection, subcutaneous injection, intradermal injection, intracavity injection and other injection routes.
In some specific examples, the skin tumor preventing and treating medicine is oral liquid, and the matrix includes sodium carboxymethyl cellulose.
In some examples, the skin tumor prevention and treatment drug is administered in the form of a liniment, an oral preparation or an injection.
Further, injections include, but are not limited to, intravenous injections.
In some embodiments, the drug for preventing and treating skin tumor is injection, and the matrix comprises solvent for injection.
In some embodiments, the solvent for injection comprises at least one of water for injection, oil for injection, and other non-aqueous solvents for injection.
The water for injection includes purified water, for example, water treated by distillation, electrodialysis, ion exchange or reverse osmosis.
Oils for injection include vegetable oils, such as: at least one of sesame oil, tea oil, olive oil, corn oil and soybean oil.
Other non-aqueous injectable solvents include water-soluble organic solvents including at least one of glycerol, ethanol, propylene glycol, dimethyl sulfoxide, and polyethylene glycol.
In some embodiments, the solvent for injection comprises at least one of water for injection, oil for injection, ethanol, propylene glycol, and polyethylene glycol.
While the present invention will be described in connection with particular embodiments thereof, it is to be understood that the invention is not limited to the disclosed embodiments, but is intended to cover by the appended claims the scope of the invention, and that certain changes and modifications of the various embodiments of the invention, which fall within the true spirit and scope of the invention, will be suggested to those skilled in the art and this disclosure.
DETAILED DESCRIPTION OF EMBODIMENT (S) OF INVENTION
Example 1
Preparation of experimental materials:
reagent: DMEM medium was purchased from Biological industries; fetal bovine serum was purchased from Biological Industries; pancreatin digest was purchased from Beyotime corporation; PBS (phosphate buffered saline) powder was purchased from Servicebio corporation; moravaptan hydrochloride solution (10 mM, solvent DMSO dimethyl sulfoxide) was purchased from MCE; CCK8 reagent was purchased from Bimake.
Wherein, mM is the concentration unit, namely: mmol/L.
Cell line: melanoma cell lines SK-MEL-5, SK-MEL-28 and A375 cells were obtained from the dermatology laboratory of Xiangya Hospital, university of Central and south, respectively using DMEM medium containing 10% FBS (fetal bovine serum) at constant temperature of 37 ℃ with 5% CO 2 Culturing under the condition of (3) and reserving for use.
The instrument comprises the following steps: an ultra-clean bench; a cell incubator; a centrifuge; a cell counter; a negative pressure suction device; a microplate reader.
Consumable material: a cell culture dish; a 96-well plate; 15ml centrifuge tube; cell counting plate.
Example 1
Detecting the inhibition effect of the mozavaptan hydrochloride on the cell proliferation of human melanoma SK-MEL-5, SK-MEL-28 and A375
The test process comprises the following steps: separately treating melanoma SK-MEL-5 and SK-MEL-28 and A375 cells were seeded into 96-well plates at 3X 103 cells/well and cultured using DMEM medium containing 10% FBS, at 37 5% 2 Culturing under the condition, dividing the test group and the control group, and setting 5 multiple wells in each group.
After 16h of culture, mozavaptan hydrochloride stock solution (10 mM) was added to the culture medium of 3 test groups of melanoma SK-MEL-5, SK-MEL-28 and A375 cells, respectively, to a final concentration of 10. Mu.M, the culture medium was added only to the control group, CCK8 was added at 24h, 48h, 72h, respectively, and incubated in an incubator for 2h, and then absorbance values (OD) were measured using a microplate reader for each well in each control group and test group at a wavelength of 450 nm. The absorbance value can reflect the number of living cells, and lower absorbance values indicate lower numbers of living cells, i.e., indicate greater inhibition of cell proliferation.
The inhibition of the proliferation of melanoma a375 cells by the test group and the control group is shown in fig. 1. Wherein A1 represents a control group, and A2 represents a test group to which a mozavaptan hydrochloride solution is added. As can be seen from FIG. 1, compared with the control group, the mozavaptan hydrochloride with the concentration of 10 μ M has an obvious inhibition effect on the proliferation activity of A375 cells, and is in an aging relationship within 0-72 h, and the statistical P value of the two is less than 0.05, which shows that the difference between the two is significant and has statistical significance.
The inhibition of proliferation of the melanoma SK-mel-5 cells by the test group and the control group is shown in FIG. 2. Wherein, B1 represents a control group, and B2 represents a test group added with the mozavaptan hydrochloride solution. As can be seen from FIG. 2, compared with the control group, the mozavaptan hydrochloride with the concentration of 10 μ M has an obvious inhibition effect on the proliferation activity of SK-mel-5 cells, an aging relation is formed within 0-72 h, the statistical P value of the two is less than 0.05, and the fact that the difference between the two is obvious and has statistical significance is shown.
The proliferation inhibition of the melanoma SK-mel-28 cells in the test group and the control group is shown in FIG. 3. Wherein C1 represents a control group, and C2 represents a test group to which a mozavaptan hydrochloride solution is added. As can be seen from FIG. 3, compared with the control group, the mozavaptan hydrochloride with the concentration of 10 μ M has an obvious inhibition effect on the activity of SK-mel-28 cells, an aging relation is formed within 0-72 h, the statistical P value of the two is less than 0.05, and the fact that the difference between the two is obvious and has statistical significance is shown.
Example 2
Detecting the inhibitory effect of mozavaptan hydrochloride on the tumor growth in B16F10 tumor-bearing C57BL/6 mice:
the test process comprises the following steps: 10 mice of C57BL/6 were prepared, shaved on the back and sterilized with iodophor, and then mouse melanoma cells B16F10 were injected subcutaneously to construct a mouse melanoma model, and after the tumor grew to reach, the mice were randomly divided into 2 groups of 5 mice each, which were a test group and a control group.
The test group was administered a daily treatment with a solution of mozavaptan hydrochloride (in corn oil) by intraperitoneal injection, at 0.5mg per 1kg of mouse body weight, once a day; the control group was given daily corn oil treatment in an amount equivalent to the test group. Five controls were formed for 5 mice in the experimental group and 5 of their corresponding controls.
Wherein, the actual comparison graph of the tumor volumes of the test group and the control group is shown in fig. 4, and the volume sizes of the tumor real objects compared in the five groups are shown in table 1:
TABLE 1
1 2 3 4 5
Test group 72.7mm 3 97.0mm 3 134.5mm 3 399.4mm 3 456.5mm 3
Control group 642.9mm 3 688.7mm 3 799.4mm 3 999.4mm 3 1071.8mm 3
As can be seen from the results of fig. 4 and table 1: the mozavaptan hydrochloride can effectively inhibit the growth of tumors in mice.
The Body weights of the mice of each group were measured, and a graph comparing the change in Body weight of the mice of the test group and the control group is shown in FIG. 5, wherein the abscissa day after treatment represents the number of Days, and the ordinate Body weight represents the Body weight of the mice; data from duplicate experiments are presented as mean (N = 5) ± SD; * P is less than 0.05.
As can be seen from figure 5, the mozavaptan hydrochloride does not substantially affect the body weight of the mice, and the side shows that the mozavaptan hydrochloride has no obvious toxic or side effect on the mice and does not affect the normal physiological activities of the mice.
The technical features of the embodiments described above may be arbitrarily combined, and for the sake of brevity, all possible combinations of the technical features in the embodiments described above are not described, but should be considered as being within the scope of the present specification as long as there is no contradiction between the combinations of the technical features.
The above-mentioned embodiments only express several embodiments of the present invention, so as to understand the technical solutions of the present invention specifically and in detail, but not to be understood as the limitation of the protection scope of the invention. It should be noted that various changes and modifications can be made by those skilled in the art without departing from the spirit of the invention, and these changes and modifications are all within the scope of the invention. It should be understood that the technical solutions provided by the present invention, which are obtained by logical analysis, reasoning or limited experiments, are within the scope of the present invention as set forth in the appended claims. Therefore, the protection scope of the present patent shall be subject to the content of the appended claims, and the description and drawings can be used to explain the content of the claims.

Claims (10)

1. The application of the mozavaptan compound in preparing the medicines for preventing and treating the skin tumors is characterized in that the mozavaptan compound is selected from at least one of mozavaptan and derivatives thereof.
2. The use of claim 1, wherein the skin tumor comprises melanoma.
3. The use of claim 1, wherein said derivative of mozavaptan comprises a pharmaceutically acceptable salt of mozavaptan or a pharmaceutically acceptable ester compound of mozavaptan.
4. The use according to any one of claims 1 to 3, wherein the mozavaptan class of compounds is selected from at least one of mozavaptan and mozavaptan hydrochloride.
5. The use according to any one of claims 1 to 3, wherein the skin tumor preventing and treating drug is a drug for inhibiting the proliferation of melanoma cells.
6. The use according to claim 5, wherein the melanoma cells are at least one of SK-MEL-5 cells, SK-MEL-28 cells and a375 cells.
7. The medicine for preventing and treating the skin tumor is characterized in that the active ingredient of the medicine for preventing and treating the skin tumor comprises a mozavaptan compound, and the mozavaptan compound is selected from at least one of mozavaptan and derivatives thereof.
8. The agent for preventing and treating skin tumor according to claim 7, wherein the ingredients of the agent for preventing and treating skin tumor further comprise pharmaceutically acceptable base, and the pharmaceutically acceptable base is at least one selected from the group consisting of sustained release agent, excipient, filler, binder, humectant, disintegrant, absorption enhancer, adsorption carrier, surfactant, lubricant and solvent for injection.
9. The agent for preventing and treating skin tumor according to claim 8, wherein the agent for preventing and treating skin tumor is an injection, and the base comprises a solvent for injection.
10. The agent for preventing and treating skin tumor according to any one of claims 7 to 9, wherein the solvent for injection comprises at least one of water for injection, oil for injection, ethanol, propylene glycol, dimethyl sulfoxide and polyethylene glycol.
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Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20160022635A1 (en) * 2014-07-28 2016-01-28 University Of Miami Use of arginine vasopressin receptor antagonists for the treatment of prostate cancer
CN112121051A (en) * 2020-09-30 2020-12-25 郑州大学 Application of mozavatan in preparation of anti-digestive tract tumor medicine

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20160022635A1 (en) * 2014-07-28 2016-01-28 University Of Miami Use of arginine vasopressin receptor antagonists for the treatment of prostate cancer
CN112121051A (en) * 2020-09-30 2020-12-25 郑州大学 Application of mozavatan in preparation of anti-digestive tract tumor medicine

Non-Patent Citations (2)

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Title
G.MARRONCINI等: "The V2 receptor antagonist tolvaptan counteracts proliferation and invasivity in human cancer cells", 《JOURNAL OF ENDOCRINOLOGICAL INVESTIGATION》 *
SONALI SINHA等: "Targeting the vasopressin type-2 receptor for renal cell carcinoma therapy", 《ONCOGENE》 *

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