Esophageal cancer chemotherapy drug etoposide injection drug VP-16 is a semi-synthetic derivatives of podophyllotoxin, one is a cell cycle specific drugs, 1970 to enter clinical. VP-16 in the cell targets of a DNA topoisomerase II, interfere with DNA topoisomerase DNA break to reconnect E response to inhibition of mitosis, the cell division ceased in the late S phase or early G2 phase.
Preclinical animal studies show that, VP-16 has a variety of experimental animal tumor inhibition, such as L1210, P388, P1534 leukemia, S37, S180, Walker carcinosarcoma, B16 melanoma, Ehrlich ascites carcinoma. Esophageal cancer chemotherapy drug etoposide injection can cure more than half of L1210 leukemia in mice, on the S37, S180 tumor inhibition rate of 61% – 72%, so that the survival of mice suffering from leukemia P1534 compared with the control group increased by 83% – 110% of mice Lewis lung cancer lung metastasis was inhibited. VP-16 broad-spectrum anti-tumor, and with Ara-C, CTX, DDP and BCND have synergistic effect.
VP-16 in rats after intravenous injection, blood concentration was two-compartment open model attenuation, t1/2 = 1.3h, t1 / 2 (3 = 4.3h. Oral bioavailability of the drug an average of 48%, giving static After injection of the drug, t1/2 = (1.4 0.4) h, t1 / 2 (3 = (5.7 1.8) h.
Esophageal cancer chemotherapy drug etoposide injection, 74% – 90% of the drug and plasma protein binding, only blood, cerebrospinal fluid drug concentration of 2% – 10%. Mainly with the urine excretion, 72h 45% discharged, of which 2 / 3 as the prototype drug, only 1.5% _16% by fecal excretion.