Esophageal cancer chemotherapy drug irinotecan in the experimental study

By | January 22, 2012

Experimental study of irinotecan, CPT-II as a semi-synthetic camptothecin derivative, as topoisomerase I inhibitors. Preclinical studies have shown, CPT-II and its active metabolite SN38 on a variety of experimental tumors has obvious anti-tumor activity, such as _80 fibrosarcoma, Lewis lung, NH134 liver , Co-4 colon cancer, Mx-l in breast cancer , ST-16 gastric cancer, broad-spectrum anti-tumor.
In addition, it is rarely expressed in vivo MDR (multidrug resistance) gene in tumor identification, VCR or ADM-resistant P338 murine leukemia equally effective. In vitro CPT-II along with some chemotherapy drugs, such as lead, Ara celecoxib, fluorouracil dark homes and E of topoisomerase inhibitor combination has synergistic or additive effect.
Experimental study of irinotecan, CPT-11 with anti-cholinesterase activity, have anti-cholinesterase drugs that prolong the activity of choline glass king from neuromuscular blockade, nondepolarizing neuromuscular blockers may be be antagonistic, should pay attention to that combination.
Experimental study of irinotecan, intravenous CPT-II, the majority of drugs quickly into the active metabolite SN380 drugs mainly in the gastrointestinal tract, liver, kidney and endocrine glands, stability, volume of distribution 157L/ml, total body clearance average of 15L / l (m h), plasma half-life of the final re-4.2h.
This product is mainly by biliary excretion, fecal excretion of more than 60%, 24h urinary excretion rate of CPT-II and SN38 were 19.9% and 0.25%.

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