Customization: | Available |
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CAS No.: | 85622-93-1 |
Formula: | C6h6n6o2 |
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Product Name | Temozolomide |
Appearance | White Power |
CAS No. | 85622-93-1 |
MF | C6H6N6O2 |
MW | 194.15 |
Pharmacological action:
Temozolomide is an alkylating agent of imidazolium tetrazine with antitumor activity. It is rapidly converted to the active product MTIC (3-methyl -(triazine-1 -) imidazole-4-formamide) at systemic physiological pH. The cytotoxic effect of MTIC is mainly manifested by alkylation of guanine 6th oxygen atom and 7th nitrogen atom on DNA molecule. It plays cytotoxic role by mismatch repair of methylated adduct.
Pharmacokinetics:
Preclinical data suggest that this product can quickly cross the blood-brain barrier and enter the cerebrospinal fluid. After oral administration of this product in adult patients, it is rapidly absorbed, and the peak blood concentration can be reached as early as 20 minutes after taking the drug (the average time is 0.5-1.5 hours). Plasma clearance, volume of distribution and half-life are dose-independent. This product has a low protein binding rate (10%-20%), so it is not expected to interact with drugs with high protein binding rates. C- The excretion of C in the stool within 7 days after oral administration of this product is 0.8%, indicating that the drug is fully absorbed. After oral administration, the protodrug in urine within 24 hours accounts for about 5%-10% of the dose, and the rest is excreted into the urine in the form of AIC (4-amino-5-imidazole-carboxyamide hydrochloride) or other polar metabolites.
Population analysis of pharmacokinetics showed that plasma clearance was not related to age, renal function, or smoking.
Pediatric patients have a higher AUC than adult patients, but the maximum tolerated dose (MTD) per cycle is 1000 mg/m for both children and adults.