Experimental study of cisplatin, cisplatin for the platinum metal complexes, with a broad spectrum anti-tumor, the characteristics of effective anaerobic cells. 1969 Rosenberg platinum complex was first reported on the S180 has anti-tumor activity in mice, in the 20th century and the early 70s with a new anticancer drug is recommended for clinical use. Cisplatin on various experimental tumors inhibited, SI80, LI2IO, P388, Dunning leukemia, ECA, ARS, melanoma B16, Lewis lung cancer , ADJ / DCGA myeloma, chicken Rous sarcoma, neuroblastoma supraventricular film , Walker carcinosarcoma 256 in rats induced breast cancer were significantly reduced. Not only in the vaccination of the SI80 immediately after the medication has _100% inhibition rate of 90%, even if the tumor grew again when the medication, can significantly inhibit tumor growth, to shrink the tumor, tumor necrosis.
Experimental study of cisplatin on mouse leukemia LI2l0, P388 not only prolong survival, but also to make long-term survival of some animals, 28 mice have a strong role in colon cancer. Cisplatin by intraperitoneal or intravenous injection of the best, no significant effect of oral. LD50 intraperitoneal administration in mice is 13_14mg/kg.
Cisplatin and VP-16 combined with ADM or colon cancer in mice, 28 have synergistic anti-tumor effect in mice with combined CTX Ridgeway osteosarcoma, P388, LI2IO also synergy. Cisplatin can also strengthen the ICRF-159, CPT, MTX ,6-TG anti-tumor effect. Uranium along with VCR, ADM, ACD no cross-resistance and anti-tumor agent with the melted very different role.
Burnt agent cisplatin has a similar dual role of functional groups, and cells with pro-nuclear groups, the main base and the role of DNA chain, copy the template to change its normal function, causing obstacles to DNA replication, thus inhibiting cell division . Cisplatin in the center of the molecule to its anti-tumor effects of lead atoms is important, and only have the effect of cis, trans is invalid. Cisplatin is cell cycle non-specific drugs.
Experimental study of cisplatin, along with the uranium isotope labeled pharmacokinetic study of the human body after treatment, blood was two compartment model decay, the distribution half-life of 25_49min, elimination half-life of 58_73h, about 90% of drugs blood and plasma protein binding. The slow elimination of drug in the body, urinary excretion of white 6h after administration 15% -27%, 24h 18% -34%, discharge, emit only 5 days after administration of 27% -54%. Some people think that the elimination phase half-life hydration reduced diuretic, platinum excreted faster, reducing the renal toxicity. Cisplatin can be distributed in the body of the organization, kidney, liver, ovary, uterus, skin, bone tissue distribution of more selective distribution in tumor tissue element. Intraperitoneal administration of drug concentrations within the abdominal organs when compared with 2.5-8 times higher when administered intravenously, the treatment of ovarian cancer benefit. Immunosuppressive effects of cisplatin occurs rapidly, short duration, only 18-72h.