How is temozolomide metabolism?

The metabolic pathway for TMZ is a pH-dependent reaction, which begins with the conversion of TMZ to MTIC, and then subsequent breakdown of MTIC to AIC. In the present study, TMZ was rapidly eliminated with a mean half-life value of 1.9 h (Table 1).

What class of drugs is temozolomide?

Temozolomide is in a class of medications called alkylating agents. It works by slowing or stopping the growth of cancer cells in your body.

How is Temodar metabolized?

Temozolomide (TMZ), sold under the brand name Temodar among others, is a medication used to treat brain tumors such as glioblastoma and anaplastic astrocytoma. It is taken by mouth or via intravenous infusion….Temozolomide.

Clinical data
Bioavailability almost 100%
Protein binding 15% (10–20%)
Metabolism hydrolysis

How do you dissolve temozolomide?

Temozolomide (TMZ) is supplied as a crystalline solid. A stock solution may be made by dissolving the TMZ in the solvent of choice. TMZ is soluble in organic solvents such as DMSO and dimethyl formamide, which should be purged with an inert gas. The solubility of TMZ in these solvents is approximately 5 mg/ml.

Is gemcitabine a prodrug?

Gemcitabine is a cytidine analog with two fluorine atoms replacing the hydroxyl on the ribose. As a prodrug, gemcitabine is transformed into its active metabolites that work by replacing the building blocks of nucleic acids during DNA elongation, arresting tumour growth and promoting apoptosis of malignant cells.

Is temozolomide a radiosensitizer?

Conclusion. Reduced radiosensitizer dosing of temozolomide concomitant with radiotherapy in glioblastoma multiforme exhibited comparable efficacy with a classic continuous daily schedule, though with better tolerability.

Is Temodar cytotoxic?

Drug Type: Temodar is an anti-cancer (“antineoplastic” or “cytotoxic”) chemotherapy drug.

What type of chemo is Temodar?

Where is temozolomide metabolized?


Clinical data
Metabolism hydrolysis
Metabolites 3-methyl-(triazen-1-yl)imidazole-4-carboxamide (MTIC, the active species); temozolomide acid
Elimination half-life 1.8 hours
Excretion mainly kidney

How do you store temozolomide?

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing. Keep out of the reach of children. Do not keep outdated medicine or medicine no longer needed.

Is temozolomide a prodrug or metabolite?

Temozolomide is a prodrug; it is spontaneously hydrolyzed at physiological pH to 3-methyl- (triazen-1-yl)imidazole-4-carboxamide (MTIC). MTIC splits into monomethylhydrazine, probably the active methylating agent, and 5-aminoimidazole-4-carboxamide (AIC). Other metabolites include temozolomide acid and unidentified hydrophilic substances.

What are the side effects of temozolomide?

The most common side effects with temozolomide are nausea, vomiting, constipation, loss of appetite, alopecia (hair loss), headache, fatigue, convulsions (seizures), rash, neutropenia or lymphopenia (low white-blood-cell counts), and thrombocytopenia (low blood platelet counts).

When should temozolomide be taken?

Temozolomide should be administered in the fasting state, at least one hour before a meal. Antiemetic therapy may be administered before, or following, administration of temozolomide.

What kind of cancer does temozolomide treat?

7.8 NCI Cancer Drugs. Temozolomide is approved to treat the following types of brain tumorsin adults: Anaplasticastrocytoma. Glioblastoma multiforme(GBM). Temozolomide is also being studied in the treatment of other types of cancer.