Streptozocin (Synonyms: Estreptozocin, NSC 37917, NSC 85998, Streptozocin, STZ, U 9889)

Streptozocin, a potent DNA-methylating antibiotic, is a naturally occurring nitrosoamide used for extensively to produce diabetes in experimental models.^[1]

In vitro, STZ was toxic with IC50 values of 11.7, 904 and 1024 μg/ml for HL60, K562 and C1498 cells respectively.^[3]

In vivo efficacy test it shown that when combined with a protocol for induction of diuresis, dogs were treated safely with 500 mg/m2 of streptozocin, intravenously, every 3 weeks, and it may be have a potential efficacy on the treatment of dogs with metastatic pancreatic islet cell tumors.^[1]

In vivo experiment it indicated that mice were administrated streptozocin with 65 mg/kg intraperitoneally for 8-11 days or 14-17 days, streptozocin improved the impaired development of preimplantation embryos on 8-11 days. However, after 14-17 days, the incidence of degenerated embryos was increased in both streptozocin-treated mice groups.^[2] Treatment with 60 mg/kg of streptozocin intravenously also induces an early hyperglycaemia when the hepatic glycogen storage is almost depleted that is during the fasting state.^[4] For the treatment of advanced islet-cell carcinoma, the combination of streptozocin and doxorubicin is more efficious than the current standard regimen of streptozocin plus fluorouracil.^[5] There is little value for patients with malignant carcinoid tumors by combination treatment with streptozocin and 5-fluorouracil.^[6]

References:
[1].Moore AS, et al. Streptozocin for treatment of pancreatic islet cell tumors in dogs: 17 cases (1989-1999). J Am Vet Med Assoc. 2002 Sep 15;221(6):811-8.
[2].Veselá J, et al. Subdiabetogenic streptozocin treatment impairs preimplantation development of mouse embryos. Physiol Res. 1993;42(1):23-7.
[3].Diab RA, et al. Immunotoxicological effects of streptozotocin and alloxan: in vitro and in vivo studies. Immunol Lett. 2015 Feb;163(2):193-8.
[4].Wong KK. Reduction by streptozocin of blood glucose utilization during the appearance of the streptozocin induced early hyperglycaemia in fasting rats. Biochem Mol Biol Int. 1996 May;39(1):191-5.
[5].Moertel CG, et al. Streptozocin-doxorubicin, streptozocin-fluorouracil or chlorozotocin in the treatment of advanced islet-cell carcinoma. N Engl J Med. 1992 Feb 20;326(8):519-23.
[6].Oberg K, et al. Cytotoxic treatment in patients with malignant carcinoid tumors. Response to streptozocin--alone or in combination with 5-FU. Acta Oncol. 1987;26(6):429-32.