Mitozytrex -----胃癌或胰腺癌转移性腺癌

Mitozytrex (丝裂霉素)——胃癌或胰腺癌转移性腺癌

Mitozytrex™

(mitomycin for injection)

DESCRIPTION

Mitozytrex is a sterile dry mixture of Mitomycin, USP and hydroxypropyl â

cyclodextrin (HPbCD) (glucopyranose polymers used as solubilizing agent),

which when reconstituted with Sterile Water for Injection provides a solution for

intravenous administration. Mitozytrex is supplied in vials containing 5 mg of

mitomycin. Each 5 mg vial of Mitozytrex contains mitomycin 5 mg and HPbCD

2 g.

CLINICAL PHARMACOLOGY

Mitomycin selectively inhibits the synthesis of deoxyribonucleic acid (DNA). The

guanine and cytosine content correlates with the degree of mitomycin-induced

cross-linking. At high concentrations of the drug, cellular RNA and protein

synthesis are also suppressed.

In humans, mitomycin is rapidly cleared from the serum after intravenous

administration. Time required to reduce the serum concentration by 50% after a

30 mg bolus injection is 17 minutes. After injection of 30 mg, 20 mg, or 10 mg

I.V., the maximal serum concentrations were 2.4 mg/mL, 1.7 mg/mL, and 0.52

mg/mL, respectively. Clearance is effected primarily by metabolism in the liver,

but metabolism occurs in other tissues as well. The rate of clearance is inversely

proportional to the maximal serum concentration because, it is thought, of

saturation of the degradation pathways.

Approximately 10% of a dose of mitomycin is excreted unchanged in the urine.

Since metabolic pathways are saturated at relatively low doses, the percent of a

dose excreted in urine increases with increasing dose. In children, excretion of

intravenously administered mitomycin is similar. Approximately 80-90% of

HPbCD, the solubilizing agent in Mitozytrex, is eliminated through the kidneys,

and greater than 93% is excreted unchanged in the urine within 12 hours after

dosing.

© 2002 SuperGen, Inc. November 2002

GO-P-05