化合物详情

Streptozotocin is produced by the soil microorganism, Streptomyces achromogenes var. 128, first isolated from soil samples collected near Blue Rapids, Kansas, USA.

Symptoms of overdose include nausea and vomiting, anorexia, myelosuppression; and nephrotoxicity.

Antibiotic resistance

Likelihood score: D (possible cause of clinically apparent liver injury).

NTP Carcinogen - Reasonably anticipated to be a human carcinogen.

Intravenous. Poor oral absorption (17-25%).

Streptozotocin is a naturally occurring chemical that is particularly toxic to the insulin-producing beta cells of the pancreas. It is used in medical research to produce an animal model for Type 1 diabetes in large dose as well as Type 2 diabetes with multiple low doses. Streptozotocin is similar enough to glucose to be transported into the cell by the glucose transport protein GLUT2, but is not recognized by the other glucose transporters. This explains its relative toxicity to beta cells, since these cells have relatively high levels of GLUT2. Streptozotocin is a glucosamine-nitrosourea (i.e. alkylating) compound. As with other alkylating agents in the nitrosourea class, it is toxic to cells by causing damage to the DNA, though other mechanisms may also contribute.

Oral Slope Factor Reference: CALEPA

Uric acid nephrolithiasis developed in a 75 yr old man who had received a large cumulative dose of streptozotocin for treatment of metastatic islet cell carcinoma of the pancreas. Oligoanuric renal failure mediated by massive intraureteral uric acid deposits occurred despite normal serum concentrations of uric acid. This case implicates the uricosuric effects of streptozotocin in the pathogenesis of uric acid nephropathy and suggests that renal uric acid excretion should be monitored routinely in patients receiving large cumulative doses of this drug.

2B, possibly carcinogenic to humans. (L135)

Reference: DOI:10.1016/j.drudis.2011.05.007

LD50 Dog male iv 50 mg/kg