Sterozine 50%

Sterozine 50% Uses, Dosage, Side Effects, Food Interaction and all others data.

Sterozine 50% (INN, BAN, USAN) is a prodrug of Fluorouracil (5-FU), an antineoplastic agent used as the treatment of various cancers such as advanced gastric and colorectal cancers. It is a pyrimidine analogue used in combination therapies as an active chemotherapeutic agent in conjunction with Gimeracil and Oteracil, or along with Fluorouracil as Sterozine 50%-uracil. Sterozine 50% is usually given in combination with other drugs that enhance the bioavailability of the 5-FU by blocking the enzyme responsible for its degradation, or serves to limit the toxicity of 5-FU by ensuring high concentrations of 5-FU at a lower dose of tegafur . When converted and bioactivated to 5-FU, the drug mediates an anticancer activity by inhibiting thymidylate synthase (TS) during the pyrimidine pathway involved in DNA synthesis. 5-FU is listed on the World Health Organization's List of Essential Medicines.

Sterozine 50% is an antineoplastic agent that belongs in the class of pyrimidine analogues. It interferes with the 2'-deoxythymidylate (DTMP) synthesis in the pyrimidine pathway, resulting in inhibition of DNA synthesis . In a phase III trial investigating the clinical efficacy of S-1 (tegafur/gimeracil/oteracil) in patients with advanced or recurrent gastric cancer, treatment resulted in a high response rate and was associated with a longer overall survival and longer progression-free survival rate when used in combination with cisplatin . In a meta analysis, triple combination therapy consisting of tegafur, gimeracil and oteracil showed longer survival times and well tolerance in patients with advanced gastric cancer . Sterozine 50% and its active metabolites are potent myleosuppressive agents .

Sterozine 50%
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Sterozine 50%
Generic	Tegafur
Tegafur Other Names	Tegafur
Type
Formula	C₈H₉FN₂O₃
Weight	Average: 200.169 Monoisotopic: 200.059720321
Protein binding	Tegafur is 52.3% bound to serum proteins and 5-FU is 18.4% protein bound .
Groups	Approved, Investigational
Therapeutic Class
Manufacturer
Available Country	Japan
Last Updated:	September 19, 2023 at 7:00 am

Uses

Sterozine 50% is an antineoplastic agent used in combination with other anticancer medications to treat advanced gastric and colorectal cancers.

Indicated for the treatment of cancer usually in combination with other biochemically modulating drugs.

Indicated in adults for the treatment of advanced gastric cancer when given in combination with Cisplatin .

Indicated for the first-line treatment of metastatic colorectal cancer with Uracil and calcium folinate .

Sterozine 50% is also used to associated treatment for these conditions: Advanced Gastric Cancer

How Sterozine 50% works

The transformation of 2'-deoxyurindylate (dUMP) to 2'-deoxythymidylate (dTMP) is essential in driving the synthesis of DNA and purines in cells . Thymidylate synthase catalyzes the conversion of dUMP to dTMP, which is a precursor of thymidine triphosphate (TTP), one of the four deoxyribonucleotides required for DNA synthesis . After administration into the body, tegafur is converted into the active antineoplastic metabolite, fluorouracil (5-FU). In tumour cells, 5-FU undergoes phosphorylation to form the active anabolites, including 5-fluorodeoxyuridine monophosphate (FdUMP) . FdUMP and reduced folate are bound to thymidylate synthase leading to formation of a ternary complex which inhibits DNA synthesis . In addition, 5-fluorouridine-triphosphate (FUTP) is incorporated into RNA causing disruption of RNA functions .

Toxicity

Oral LD50 value in rat, mouse and dog are 930mg/kg, 775mg/kg, and 34mg/kg, respectively . Continuous exposure to tegafur may cause physical defects in the developing embryo (teratogenesis).

Acute toxicity from the combination use of tegafur was associated with nausea, vomiting, diarrhoea, mucositis, gastrointestinal irritation, bleeding, bone marrow depression, and respiratory failure . Overdose may lead to fatal complications . In case of overdose, appropriate therapeutic and supportive medical interventions should be implemented.

Food Interaction

Drink plenty of fluids. Drinking water is important to prevent dehydration when taking Teysuno.
Take on an empty stomach. Food does not impact the bioavailability of tegafur. Food does affect other ingredients in the combination product Teysuno. Take Teysuno at least 1 hour before or after eating.

Volume of Distribution

The volume of distribution based on apparent volume of distribution and urinary excretion data of tegafur is 16 L/m^2 .

Elimination Route

Sterozine 50% displays a dose-proportional pharmacokinetic properties. Sterozine 50% is rapidly and well absorbed into the systemic circulation, reaching the peak plasma concentration within 1 to 2 hours of administration .