Method for thermochemoradiation treatment of rectal cancer

FIELD: medicine, oncology, radiology.

SUBSTANCE: the suggested thermochemoradiation treatment should be fulfilled in three stages at intervals between each of them being 10-14 d: during the 1st stage it is necessary to carry out distance gamma-therapy daily at fractionating the dosage during 1-3 d per 4 Gy, then during 4-22 d per 2 Gy up to TFD being 50 isoGy, radiosensitization with 5-fluorouracil daily at the dosage of 125 mg intravenously at flow-type technique 30 min before the séance of radiation treatment and local thermotherapy with transrectal sensor once/2 d, every other day, just before gamma-therapy; during the 2nd stage it is necessary to conduct radiosensitization and local thermotherapy similarly, as it was during the first stage, as for irradiation it should be carried out as intracavitary gamma-therapy daily per 3 Gy up to TFD being 18-24 Gy; during the 3d stage one should fulfill radiosensitization with fluorouracil as during the first and second stages and carry out distance gamma-therapy daily per 2 Gy so that TFD from all three stages should achieve 74 isoGy.

EFFECT: higher efficiency of therapy.

3 ex

 

The invention relates to medicine, namely to the combined thermochemical therapy, and is intended for the most effective conduct of multicomponent treatment in cancer of the anal canal, medium and nizhneamudarinskogo departments rectum different stages.

Known accepted methods of combined treatment of cancer of the anal canal, the lower and srednetemperaturnogo departments of the rectum. The standard surgical treatment of this pathology is abdomino-perineal extirpation of the rectum or abdomino-anal resection for cancer of srednetemperaturnogo division of the rectum [1]. When purely surgical treatment of relapses occur in 18.3-28.6% of patients. In the combined treatment before surgery, patients spend intensely concentrated course of remote gamma-therapy for 5g X 5 times, regardless of the stage of the primary tumor [2]. The recurrence of tumors in the treatment algorithm arise in 7.1-17.2% of cases. As radiosensibility in some clinics use local hyperthermia (42-45° (C) to the primary tumor with the use of a rectal probe and microwave radiation (460 MHz, 915 MHz), while hyperthermia is carried out on 3, 4, 5 sessions intensely concentrated course of remote gamma-therapy (HR) [3]. Relapses when this was observed in 2.9-7.1% of patients. The disadvantages of the use of the microwave m is should be attributed to the strengthening of tenesmus, the appearance of pronounced rectitem and more pronounced overall radiation reaction. Closest to the claimed method is a method termolecular treatment of prostate tumors [patent No. 2238776] through a combination of thermotherapy and remote radiation therapy according to a certain scheme. However, application of this scheme for the treatment of rectal cancer is associated with a significant risk of radiation damage up to heavy.

The aim of the proposed method is to optimize the treatment of rectal cancer and increase its effectiveness. The essence of the proposed method lies in the fact that the treatment is carried out stage, with breaks between stages in 10-14 days. At the 1st stage to perform remote gamma-therapy daily with dose fractionation in 1-3 days at 4 Gy, then 4-22 days Gr 2 to SOD 50 sogr. At the 2nd stage produces intracavitary gamma therapy daily for 3 Gr and SOD 18-24 Gy. On the 3rd stage again to perform remote gamma-therapy daily 2 Gy to SOD from all three phases 74 sogr. When this radiation is combined with local therapy transrectal probe at a known mode radiation [patent No. 2238776] on the first two stages through the day, starting from the 4th day of treatment, and combine at all stages with radiosensibility 5-fluorouracil 125 mg daily intravenous bolus 30 minutes before the session is radiotherapy. Operative treatment of cancer of the anal canal 1 tbsp. after applying this method does not perform, and in other cases, the way Supplement surgery 3 weeks after the 1st stage.

Scientific and technical information search showed that the invention is not known and is not clear from the current level of science and technology that demonstrates compliance with this method, the criterion of "novelty". Due to the presence of these distinctive features in the proposed method, and also use them in combination and sequence of actions, we can make a conclusion about conformity of the proposed method inventive step.

The method is as follows. At the 1st stage to perform remote gamma-therapy daily with dose fractionation in 1-3 days at 4 Gy, then 4-22 days Gr 2 to SOD 50 sogr. Daily, the patient is given intravenous bolus radiosensibility 5-fluorouracil at a dose of 125 mg 30 minutes prior to the session of radiotherapy, and 1 every 2 days (one day) just before gamma therapy is local therapy using transrectal probe mode 40 MHz for 60 minutes with the temperature in the rectum 50-59°C.

Then after an interval of 10-14 days of conducting the 2nd stage of treatment in which radiosensibility and lo the social therapy also perform, as at the 1st stage, and irradiation is carried out in the form of intracavitary gamma therapy daily for 3 Gr and SOD 18-24 Gy.

After 10-14 days interval, perform the 3rd step, which performs radiosensibility 5-fluorouracil, as on the 1st and 2nd stages and conduct remote gamma-therapy daily 2 Gy so that the SOD from all three stages of treatment reached 74 sogr.

Operative treatment of cancer of the anal canal 1 tbsp. after applying this method does not perform, and in other cases, the way Supplement surgery 3 weeks after the 1st stage.

The proposed method is carried out on 16 patients: 5 patients with tumors of the anal canal T1-2N0; 4 patients with T3N0-2; 5 patients with tumor nizhneamudarinskogo Department rectal T1-4N0-2 and 2 patients with tumor of srednetemperaturnogo Department of T1-4N0-2. Complications during the proposed method have been identified. The effectiveness of the treatment were assessed according to the results of pathological studies and the results of the examination within 6 months; in all cases achieved a cure.

Give examples of the use of the proposed method.

Example 1. Patient O., 37 years. Diagnosis: cancer of the anal canal T3N0M0. The course combined termokhimicheskogo the treatment approach. Transrectal therapy was performed after SOD 12 Gy, 5 times in 2 n the Delhi immediately prior radiation therapy within 60 min, the temperature in the rectum from 50 to 59°C. After 3 weeks, the operation - abdomino-perineal extirpation of the rectum. The histological conclusion squamous cell carcinoma of the anal canal in stages defined therapeutic pathomorphosis (4 items), without metastases in the lymph nodes.

Example 2. Patient C., 50 years. Diagnosis: cancer of the anal canal, T2N0M0, 1 tbsp. Histological conclusion squamous orogovevshi cancer. The course termokhimicheskogo treatment to SOD 74 sogr by the described method. At the end of treatment showed complete tumor resorption, cytological conclusion, tumor cells were detected, surgical treatment was not conducted. Control examination after 6 months data for recurrence and distant metastasis no.

Example 3. Patient F., 64 years. Diagnosis: cancer nizhneamudarinskogo Department rectum TNM, 2 tbsp. Degree of local spread of the tumour and the presence of increased adrectal lymph nodes in the preoperative period is set when the transrectal us. The course termokhimicheskogo treatment. Extirpation of the rectum is performed after 3 weeks. The histological conclusion - moderately differentiated adenocarcinoma, pathomorphosis 4 degrees, without metastasis in adrectal lymph nodes.

Thus, the application of the proposed method to optimize cancer treatment right in the gut and increase its effectiveness.

Literature

NEs VI colorectal Cancer kicsi // Diagnostics and treatment of cancer of the colon and rectum. - M.: Medicine. - 1981. - S-187.

2. Burdov B.A., Yurchenko NI Radiation therapy in combined treatment of direct kicsi // Surgery. - 1989. No. 5. - P.39-43.

3. Badgers Y.A. Combined and complex treatment of patients with rectal cancer: author. Diss...Prof. the honey. Sciences. - M.,1991. - s-253.

4. Patent for invention No. 2238776. The way jermolajevas therapy of prostate tumors.

The way termokhimicheskogo treatment of rectal cancer by combining radiation therapy with radiosensibility and local thermotherapy, characterized in that is carried out in three stages with breaks between each of them 10-14 days, the 1st of which perform remote gamma-therapy daily with dose fractionation in 1-3 days at 4 Gy, then 4-22 days Gr 2 to SOD 50 sohr, radiosensibility 5-fluorouracil daily dose of 125 mg intravenous bolus over 30 min before the session of radiation therapy and local therapy transrectal probe 1 every 2 days, every other day, directly before gamma-ray therapy; on the 2nd stage radiosensibility and local thermotherapy perform the same as the 1st stage, and irradiation is carried out in the form of intracavitary gamma therapy daily for 3 Gr and SOD 18-24 Gy; at the 3rd stage perform radiosensibility 5-torural the ohms on the 1st and 2nd stages and conduct remote gamma-therapy daily Gr 2 thus, to SOD from all three stages of treatment reached 74 sogr.



 

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1 ex, 1 tbl

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1 ex, 1 tbl

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24 cl, 7 sch, 28 ex

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5 tbl, 9 dwg

FIELD: organic chemistry, medicine, pharmacy.

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27 cl, 1 tbl, 17 ex

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EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

21 cl, 1 tbl, 76 ex

FIELD: organic chemistry, chemical technology.

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EFFECT: improved method of synthesis.

3 ex

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to an intermediate compound, i. e. tert.-butyl-(E)-(6-{2-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]-pyrimidine-5-yl}-(4R,6S)-2,2-dimethyl[1,3]dioxane-4-yl]acetate that can be used in synthesis of compound of the formula (IV)

eliciting inhibitory effect on activity of HMG-CoA-reductase and, therefore, can be used for preparing pharmaceutical agents for treatment, for example, hypercholesterolemia, hyperproteinemia and atherosclerosis. Also, invention relates to a method for preparing indicated intermediate compound by reaction of the new parent compound - diphenyl-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidine-5-ylmethyl]phosphine oxide with tert.-butyl-2-[(4R,6S)-6-formyl-2,2-dimethyl-1,3-dioxane-4-yl]acetate in the presence of a strong base in simple ether or aromatic solvents or their mixtures at temperature in the range from -200C to -900C. Also, invention relates to a method for preparing of compound of the formula (IV) wherein R1 means hydrogen atom or pharmaceutically acceptable cation and to a method for preparing intermediate compounds of the formula (VI):

wherein each P1 and P2 represents independently (C1-C4)-alkyl or group:

and wherein P3 represents (C1-C8)-alkyl. Applying new intermediate compounds and proposed methods provide enhancing quality and yield of compounds.

EFFECT: improved preparing methods.

9 cl, 1 tbl, 8 ex

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