Recently, the oral drug for the treatment of advanced gastric cancer-S-1 capsule has finally been successfully listed in China. This kind of Tigio capsule with the trade name of "Weikangda" was produced by Shandong New Times Pharmaceutical Co., Ltd. (a subsidiary of Lunan Pharmaceutical Group) and obtained the production approval from the State Pharmaceutical Products Administration in August 2008. The successful listing of S- 1 capsule has added a powerful weapon for patients with gastric cancer to overcome persistent diseases.

Mechanism and therapeutic advantages of S- 1 capsule;

S- 1, also known as TS- 1, is an oral anticancer agent of fluorouracil derivatives, including tegafur (FT-207) and two regulators: jimpamine (CDHP) and octreotide (Oxo). As we all know, at present, most standard regimens for the treatment of gastrointestinal tumors include fluorouracil (5-Fu) or its derivatives.

After oral administration of S- 1, tegafur is slowly transformed into fluorouracil in vivo, which plays an anti-tumor role. CDHP can inhibit the catabolism of 5-Fu released by FT-207 under the action of dihydropyrimidine dehydrogenase, increase the concentration of 5-Fu in plasma and prolong the maintenance time of effective drug concentration. Oxo can reduce the damage of 5-Fu to gastrointestinal mucosa, inhibit the phosphorylation of 5-Fu and reduce its side effects on gastrointestinal tract. Therefore, S- 1 capsule has the following advantages:

(1) It can maintain high blood concentration and improve its anticancer activity;

② obviously reduce the drug toxicity;

③ Easy to take.

Comparison of application of S- 1 capsule at home and abroad

S- 1 capsule was developed and produced by Japan Dapeng Pharmaceutical Industry Co., Ltd. as early as 1999, and has been widely used in advanced gastric cancer, head and neck cancer, colorectal cancer, non-small cell lung cancer and other major diseases. However, due to various reasons, Japanese-made S-Gio capsules have not been able to enter the China market, which makes many patients lose the opportunity of treatment. The price of nearly 20,000 yuan per box (120 capsules) is unbearable for many patients.

Vianda (S-Gio capsule) produced by Shandong New Times Pharmaceutical Co., Ltd. went on the market, which filled the vacancy in the domestic market and the price was relatively cheaper. Vianda (S-Gio Capsule) has two different doses of pills, 20mg and 25 mg, and each dose of pills has three specifications of packaging, which is convenient for patients with different doses to choose.

S- 1 Description of capsule:

Drug name

Generic name: S- 1 capsule

Product name: Weikangda

English name: gimeracil and oteracil porassium capsules

Chinese Pinyin: Tiji 'ao Capsule

Component -S- 1 capsule is a compound preparation, and its components are tegafur, jimpamine and potassium oteracil.

The capsule is a hard capsule, and the contents are white or white-like particles or fine powder.

Indications of unresectable locally advanced or metastatic gastric cancer.

standard

1, each capsule contains tegafur 20 mg, jimpamine 5.8 mg, and oteracil potassium 19.6 mg.

2. Each capsule contains 25 mg of tegafur, 7.25 mg of jimpamine and 24.5 mg of oteracil potassium.

dosage

Drug therapy alone:

The reference dose (1 dose) of the first dose for adults should be calculated according to the body surface area in the table below, twice a day, 1 dose after breakfast and dinner, for a total of 28 days, and then stop taking the drug 14 days. This is a cycle that can be repeated.

Reference dose for initial administration of body surface area (unit: tegafur)

& lt1.25m2 40mg/time

1.25-& lt； 1.5m2 50mg/time

& gt1.5m2 60mg/time

The dose can be increased or decreased according to the patient's condition, and the dose is set at 40, 50, 60 and 75mg/ time. When the dosage needs to be increased, if there are no abnormal clinical examination values (hematological examination, liver and kidney function examination) and digestive tract symptoms related to S- 1 capsule, and there is no safety problem, the dosage can be increased one time in turn according to the reference amount, but the maximum dosage shall not exceed 75mg/ time; When reducing the dose, reduce one dose in turn according to the reference amount, and the minimum dose is 40mg/ time.

When increasing or decreasing the dosage, please refer to the following table:

Reduce the baseline dose increment of initial administration.

Stop taking 40mg/time and 50mg/time.

Stop taking medicine ←40mg/ time 50mg/ time 60mg/ time.

Stop taking drugs ←40mg/ time ←50mg/ time ← 60mg/ time ← 75mg/ time.

Note: The above dosage is calculated by tegafur, and the dosage should be increased or decreased in turn according to the above table in each cycle.

Combined medication:

Oral administration of S- 1 capsule 80mg/m2/ day, twice a day, 1 time after breakfast and dinner, for a total of 14 days, and drug withdrawal for 7 days; Cisplatin: 75mg/m2, intravenous drip for three days (day 1, day 2, day 3). Every 3 weeks is 1 cycle, and at least 2 cycles should be treated.

Pharmacology and toxicology

Pharmacological action:

1, anti-tumor effect

S- 180 sarcoma,  sarcoma, AH- 130 ascites liver cancer, Sato lung cancer (rats), Lewis lung cancer, colon cancer 26 (mice) and other subcutaneous transplanted tumors, as well as human gastric cancer, colorectal cancer, breast cancer, lung cancer, pancreatic cancer and renal cancer (nude mice).

In addition, S- 1 capsule can prolong the survival time of Lewis lung cancer model and L5 178Y liver metastasis model (mice), and inhibit the tumor proliferation of human gastric cancer and colorectal cancer cell transplantation model (nude mice).

2. Mechanism of action

S- 1 capsule is a compound preparation consisting of tegafur, jimpamine and potassium oteracil. After oral administration, tegafur is slowly transformed into 5-FU in vivo, which plays an anti-tumor role.

Dicyandiamide is mainly distributed in the liver, which selectively antagonizes the 5-FU catabolic enzyme DPD, thus increasing the concentration of tegafur converted into 5-FU, and then keeping the phosphorylated metabolite 5-FUMP of 5-FU at a high concentration in the tumor, thus enhancing the anti-tumor effect.

After oral administration, potassium oteracil has selective antagonistic effect on orotate phosphoribosyltransferase distributed in digestive tract, thus selectively inhibiting the transformation from 5-FU to 5-FUMP. As a result of the above actions, the anti-tumor effect is enhanced after oral administration of S- 1 capsule, but the digestive tract toxicity is reduced.

Toxicological research:

The results of acute toxicity test showed that the LD50 of mice was 44 1-55 1mg/kg, and that of beagle dogs was 53mg/kg.

The results of long-term toxicity test showed that S- 1 capsule was given orally to SD rats and Beagle dogs 13-52 weeks, and the main toxic target organ was bone marrow hematopoietic stem cells.

Store at room temperature and seal.

Packaging: aluminum-plastic packaging. 20mg specification (based on tegafur): 14 capsules/box, 28 capsules/box, 42 capsules/box.

25mg specification (based on tegafur): 12 capsules/box, 24 capsules/box, 36 capsules/box.

Valid for 24 months.

Registration authentication number

20mg specification: National Medicine Zhunzi H20080802

25mg specification: National Medicine Zhunzi H20080803

Production enterprise

Enterprise name: Shandong New Age Pharmaceutical Co., Ltd.