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Nitrosoureas, triazenes, alkyl sulfonates, aziridines and related alkylatorsIn useNatural productNeeds review

Streptozocin

Also known as Zanosar, streptozotocin, STZ, NSC-37917

A glucose-linked methylnitrosourea originally found in a soil bacterium. Trials and reviews describe its use, usually with other drugs, for advanced pancreatic islet-cell carcinoma and other neuroendocrine tumours.

From discovery to approval

  1. c. 1959 · Earliest report found

    A 2013 review describes streptozotocin as a naturally occurring compound produced by the soil bacterium Streptomyces achromogenes. Vavra and colleagues titled their report on it a new antibacterial antibiotic, and Herr and colleagues reported its isolation, in the Antibiotics Annual volume dated 1959-1960.[1][2][3][4]

  2. 1982-05-07 · FDA regular · 23 years after first description

    Streptozocin for injection (Zanosar), NDA 050577, original approval, classed as a new molecular entity with standard review in the Drugs@FDA history. The label is not available there, so the indication at approval is not stated here. The type regular is an inference: no accelerated-approval wording was found.[5]

How it works

A glucose analogue carrying a methylnitrosourea group that methylates DNA. In animal studies it enters pancreatic beta cells through the GLUT2 glucose transporter; the review adds that human beta cells express little GLUT2 and are not affected when it is used for islet-cell carcinoma.[1]

Where it came from and why

It was found as an antibiotic, not as a cancer drug. A 1963 paper (NSC-37917) concerns its diabetogenic action. The review says that after its discovery it was used as a chemotherapeutic alkylating agent in metastasising pancreatic islet-cell tumours.

Cancers

  • Advanced pancreatic islet-cell carcinoma

    Randomised US trials compared streptozocin alone with streptozocin plus fluorouracil (1980) and streptozocin plus doxorubicin, streptozocin plus fluorouracil, or chlorozotocin (1992). A 1968 Lancet report and a 1973 series of 52 patients are titled as treating islet-cell tumours with streptozotocin.[6]

  • Neuroendocrine tumours

    A 2012 review says streptozocin-based chemotherapy has been used for over 30 years in neuroendocrine tumours and reports that chemotherapy appears to give the highest response rate, particularly in pancreatic neuroendocrine tumours.[7]

Worth knowing

  • In a 1980 trial of 84 patients with advanced islet-cell carcinoma, the response rate was 63% with streptozocin plus fluorouracil and 36% with streptozocin alone, and complete responses were 33% and 12%; median survival was 26 and 16 1/2 months, a difference that was not statistically significant.[6]
  • In a 1992 trial of 105 patients, streptozocin plus doxorubicin gave a higher regression rate than streptozocin plus fluorouracil (69% vs 45%, P = 0.05), a longer time to progression (median 20 vs 6.9 months, P = 0.001) and longer survival (median 2.2 vs 1.4 years, P = 0.004).[8]
  • A 2013 review describes streptozotocin as a glucose analogue taken up by pancreatic beta cells through the GLUT2 transporter, and discusses its use to induce diabetes in experimental animals.[1]
  • A 2012 review says there are no trials comparing chemotherapy with best supportive care in pancreatic neuroendocrine tumours, although multi-agent streptozocin regimens are associated with improved survival compared with control therapy.[7]
  • Drugs@FDA lists the approved Zanosar product (NDA 050577) as discontinued. DailyMed lists a Zanosar product from Esteve Pharmaceuticals, last published in September 2026, under the marketing category "unapproved drug for use in drug shortage".[9]

References

  1. Eleazu CO, Eleazu KC, Chukwuma S, Essien UN. Review of the mechanism of cell death resulting from streptozotocin challenge in experimental animals, its practical use and potential risk to humans. J Diabetes Metab Disord. 2013;12(1):60. PubMedDOI
  2. VAVRA JJ, DEBOER C, DIETZ A, HANKA LJ, SOKOLSKI WT. Streptozotocin, a new antibacterial antibiotic. Antibiot Annu. 1959;7:230-5. PubMed
  3. HERR RR, EBLE TE, BERGY ME, JAHNKE HK. Isolation and characterization of streptozotocin. Antibiot Annu. 1959;7:236-40. PubMed
  4. RAKIETEN N, RAKIETEN ML, NADKARNI MV. Studies on the diabetogenic action of streptozotocin (NSC-37917). Cancer Chemother Rep. 1963;29:91-8. PubMed
  5. U.S. Food and Drug Administration. Drugs@FDA: Approval date(s) and history, letters, labels, reviews for NDA 050577 (streptozocin; Zanosar). Page read 2026-10-26. Source
  6. Moertel CG, Hanley JA, Johnson LA. Streptozocin alone compared with streptozocin plus fluorouracil in the treatment of advanced islet-cell carcinoma. N Engl J Med. 1980;303(21):1189-94. PubMedDOI
  7. Weatherstone K, Meyer T. Streptozocin-based chemotherapy is not history in neuroendocrine tumours. Target Oncol. 2012;7(3):161-8. PubMedDOI
  8. Moertel CG, Lefkopoulo M, Lipsitz S, Hahn RG, Klaassen D. Streptozocin-doxorubicin, streptozocin-fluorouracil or chlorozotocin in the treatment of advanced islet-cell carcinoma. N Engl J Med. 1992;326(8):519-23. PubMedDOI
  9. Esteve Pharmaceuticals, S.A. Zanosar (streptozocin) powder, for solution: SPL label with Dear Health Care Provider Letter. DailyMed, set ID f31d3bff-6fc6-c35f-e053-2995a90a596b, published 25 September 2026 (marketing category: unapproved drug for use in drug shortage). Source
  10. Broder LE, Carter SK. Pancreatic islet cell carcinoma. II. Results of therapy with streptozotocin in 52 patients. Ann Intern Med. 1973;79(1):108-18. PubMedDOI
  11. Murray-Lyon IM, Eddleston AL, Williams R, Brown M, Hogbin BM, Bennett A, et al. Treatment of multiple-hormone-producing malignant islet-cell tumour with streptozotocin. Lancet. 1968;2(7574):895-8. PubMedDOI