JPS62161725A - Preventive agent for malignant tumor - Google Patents

Abstract

PURPOSE:The titled pharmaceutical for oral use, containing porphyrin or a salt thereof as an active ingredient and capable of preventing the occurrence, growth,, metastasis and recurrence of malignant tumor. CONSTITUTION:A pharmaceutical containing prophyrin or a salt thereof. The prophyrinis a generic name of porphyrin derivatives and examples thereof include etiporphyrin, mesoporphyrin, protoporphyrin, deuteroporphyrin, hematoporphyrin, coproporphyrin, uroporphyrin, etc. The administration thereof in a small daily dose, e.g. up to about 60mg, is found to be capable of remark ably suppressing or inhibiting the growth of tumor in the object. The porphyrin or salt thereof in a small daily dose is capable of normally holding the character of cells and adjustment of function or promoting the normalization thereof, preventing the occurrence or malignant tumor, e.g. cancer, or suppressing the growth, metastasis and recurrence thereof.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a drug for preventing the occurrence, growth, metastasis and recurrence of malignant tumors in the human body.

Once malignant tumors such as cancer occur, they are extremely difficult to treat and often lead to death.
Currently, surgery, radiotherapy, chemotherapy, etc. are being used to treat such tumors, but satisfactory results have not yet been obtained.

Chemotherapy is currently being studied the most, with much research being focused on the development of anticancer drugs.

However, none of the anticancer drugs that have been proposed so far is effective against many types of cancer, but only against a specific type of cancer. Therefore, considering the easy migration and reoccurrence of cancer, it is difficult to completely cure cancer using anticancer drugs. Furthermore, these anticancer drugs have the major drawback of often causing side effects and damaging the human body.

Currently, in order to effectively treat cancer, early detection of cancer is proposed. However, it is difficult to detect cancer early, and the detection rate is only about 10% of the cancer mortality rate. Therefore, medical efforts to detect such cancers early cannot be said to be very effective in reducing the statistical cancer mortality rate.

From a medical point of view, it is of course wise to focus more efforts on preventing illness than on treating it after it occurs. In particular, as mentioned above, it is extremely difficult to treat tumors, so it is very meaningful to prevent their occurrence or suppress their growth to a stage before it becomes malignant, and the success rate is very low. It's also expensive. It has long been said that malignant tumors in the human body, regardless of their cause, occur when damage is caused not at the cellular level but at the organizational level. If the organization can be maintained in a normal state, i.e., if the smooth turnover of tissue cells can be maintained, then the development of malignant tumors can be prevented, or even if they occur at all. 6 Regarding human cancers, the slower the growth rate, the slower the growth rate.
It can be said that the amount of malignant dust is that low, and therefore,
The retardation of the growth rate has great significance in terms of cancer treatment. However, until now, cell function regulation (re)
No effective drug has been proposed for preventing the occurrence and growth of malignant tumors by maintaining or promoting the normalization of the malignant tumor.

An object of the present invention is to provide a drug that prevents the occurrence, growth, metastasis, and recurrence of tumors in the human body by maintaining or promoting normalization of cell functions.

By pre-administering porphyrin or its salt in small amounts every day, for example up to about 60 mg,
It has been found that tumor growth in a subject can be significantly inhibited or inhibited. Therefore, according to the present invention, by ingesting small amounts of porphyrin or its physiological salts every day, it is possible to maintain or promote the normalization of cellular characteristics and functions, and to prevent malignant tumors such as cancer. prevent the occurrence, or inhibit its growth, metastasis, and recurrence;
Thereby, the health of the human body can be maintained.

Porphyrin in the present invention is a general term for porphin derivatives, and is widely present in animals and plants.

These porphyrins include, for example, ethiborphyrin,
Included are memphorphyrin, protoporphyrin, deuteroporphyrin, hematoporphyrin, knob-mouth porphyrin, uroporphyrin, and the like. The salts also include physiological salts such as sodium salts and potassium salts. A preferred porphyrin is the sodium salt of protoporphyrin (C34II, , N40.N
a, ) and are commercially available under many trade names. To date, porphyrins have been used to treat certain diseases of the liver, such as cholelithiasis, but have not been used for such purposes as in the present invention. Furthermore, it has long been established that this porphyrin is harmless to the human body.

Our extensive research on protoporphyrin has shown that it plays a role in the development and growth of tumors in the human body, primarily by promoting function in the lymphatic system, which violates the body's homeostasis. It can be concluded that it is controlled. The human body's lymphatic system has the effect of keeping various organs at a certain size, and this effect also works on cancerous tissue. The effects obtained by using porphyrins in the present invention are achieved through such a mechanism.

In this sense, the porphyrin used in the present invention is completely different from conventionally proposed anticancer agents that directly attack and destroy localized cancer cells in its fundamental mechanism of action. Therefore, the types of tumors whose development and growth can be prevented by the porphyrin used in the present invention are not limited to any particular type, and in fact, according to this invention, the occurrence of other diseases such as lymphoma, leukemia, and hypertension can also be prevented. Preventable.

According to the invention, the porphyrins, alone or in the form of a mixture with a carrier, can be prepared in solid form, for example tablets, pills,
It is taken orally as a powder or capsule.

The maximum amount of porphyrin ingested per day is not particularly limited, since even an excessive amount does not cause any particular harm to the human body. however.

From an economical point of view, 100mg or less per day1 usually 60m
It is best to take it in an amount of less than 1g. The lower limit intake of profilin is usually 5 mg or more, preferably 10 mg or more, considering its effectiveness for the human body. Of course, in special cases this intake may be above or below the ranges mentioned. In the average adult.

20I a day! It has been clinically determined that the entire amount of ingested Ig is excreted into bile within 24 hours, leaving no residue.

The drug according to the present invention has an excellent effect of preventing tumor development and growth, and has great industrial significance.

Next, the present invention will be explained in more detail with reference to Examples.

Example 1 (1) The drug according to the present invention was administered to a human body. in this case,
The patient was a 42-year-old woman who underwent surgery to remove breast cancer, and to prevent recurrence, all of her lymphatic system and some of her muscles were also removed at the same time. Also,
She had lymphatic sparks throughout her body.

During the first week, Long in the morning and 10 hours after 12 hours of administration.
A total of 20 mg was administered orally daily.

During the second week, 30 mg was administered daily in three divided doses.

The lymphatic pilot line gradually became smaller, and the pilot line in the right armpit almost disappeared. Subjects stated that their appetite increased, they slept better, and their general health improved. Thereafter, the dose was reduced to 20 mg, then 10 mg,
The total dose was 20mg, including LOmg in the evening. All lymphatic starters have disappeared. Thereafter, medication was continued to prevent recurrence. No side effects were observed.

(2) The subject was a 72-year-old woman with bladder cancer.

Chemotherapy was administered, but in this case it was painful.

It was accompanied by some adverse side effects such as bleeding and fatigue.

Bleeding was seen in the mouth and throat as well as in the urine.

During the first week, the drug according to the invention was given orally twice in each dose of 10 mg, for a total of 20 mg per day in chemotherapy.

After 3 days, the bleeding stopped and there were no side effects (and the pain was alleviated).

During the 2nd week and 3rd M, the daily dosage was 30 mg.

This was given in 10 mg portions.

(3) Breast cancer patients with axillary nitric lymph metastasis. Experiments according to the present invention were conducted with three women as subjects.

The first woman was 53 years old and took 10 mg twice daily.
A total of 20 mg was given. She lived for two years.

The second woman was 43 years old and was given 40 mg orally twice daily, 20 mg at night and 10 mg during the day.

Two years and three months later, the patient is still alive.

The third woman attempts to have all her axillary lymph removed.” J o
The patient had a metastatic cancer in his right armpit after surgery for ``ne s''''. He was given IQmg twice daily for a total of 20mg for 3 months, and then 10mg twice daily for a total of 30mg. The patient is still alive 1 year and 6 months after taking the medication.

(4) The subject was a 56-year-old man with inoperable gastric cancer. During the first 5 months, 20mg 3 times, total 60mg
mg was given orally during the day, and the daily dosage was reduced to 30 mg for the first six months, and thereafter to 20 mg per day.

Even now, two and a half years after receiving the medication, the patient is still alive.

(5) The subject was an 18-year-old male who had osteosarcoma and underwent surgery for it. A total of 20 mg of 10 n+g was given each day. No side effects were observed, and the patient is still alive and well even now, three years after taking the medication.

(6) The subject was a 63-year-old man with stomach cancer. Surgery was not performed because of his weakened condition. X-rays confirmed the progress of the cancer. A total of 20 mg was given orally twice daily at 10+++ g. After 3 months of administration, X-ray photographs confirmed that the cancer had not progressed any further than at the beginning.

Example 2 Borman m aged 50-60 years who underwent surgery
Thirty patients with type 2 gastric cancer (10 female patients) were randomly divided into two groups, and one group received 200 mg daily.
of 5-fluorouracil, and the other group received PP! ll (protoporphyrin) was administered at 2 rng daily.

PPN was administered in tablet form once daily after meals. The results are shown in Figure 1. In this figure, the horizontal axis shows the survival period (in units of two parts), but the vertical axis is simply expanded to make it easier to see, and does not have any meaning. isn't it. Also, 0 indicates a patient receiving PPN.

× indicates control. As can be seen from Figure 1,
Most patients who did not receive PPN died within 2 years (average 1.5 years), whereas most patients who received PPN were still alive 3 years after starting treatment.

Example 3 20 Stage II breast cancer patients (age 40-50)
After undergoing surgery, the patients were randomly divided into two groups. One group received 2000 doses of X-rays, and the other group received the same X-ray treatment plus 20 mg of PPN as a tablet once daily after meals. The results are shown in FIG. From FIG. 2, it can be seen that most of the patients who did not receive PPN died three years after the surgery, but all of the patients who received PPN were still alive at that time.

Example 4 Twenty lung cancer patients (5 female patients) aged 40 to 50 who underwent surgery were divided into two groups without any activity.

One group received X-ray therapy, and the other group received 20 mg of PPN as a tablet once daily after meals in addition to X-ray therapy. The results are shown in Figure 3.
After 2 years, all patients who did not receive PPN had died, but most of the patients who received PPN were still alive after 4 years.

Example 5 20 patients with inoperable uterine cancer (age 40-60)
The patients were randomly divided into two groups, one group received LOOOR X-ray therapy, and the patients in the other group received X-ray therapy and 20 mg of PPN in the form of a tablet was administered daily after meals. The results are shown in FIG. The survival period was calculated from the time when the patient was diagnosed as inoperable. As can be seen from Figure 4, all of the patients who did not receive PPN died within about two and a half years, but more than half of the patients who received PPN survived.

From the above results, it can be seen that administering PPN to terminally ill cancer patients significantly improves the patient's survival rate. This is the metastasis and proliferation of cancer cells, PP
This shows that it can be effectively suppressed by N administration.

[Brief explanation of drawings]

1 to 4 are graphs showing the results of administration of protoporphyrin (PPN) to cancer patients in Examples 2 to 4, respectively. In Figures 1 to 4, the horizontal axis is survival period (unit: year)
In addition, the x mark shows the result for a control patient not administered protoporphyrin, and the ○ mark shows the result for a patient administered protoporphyrin. Applicant's agent Patent attorney Toshiaki Ikeura (and 1 other person) Figure 1 Figure 2 Figure 3 Figure 4 Year of life

Claims (1)

[Claims] (1) An orally ingested malignant tumor preventive agent consisting of a solid substance containing porphyrin or a physiological salt thereof.