MedKoo product information:

Sagopilone

sagopilone is a fully synthetic low-molecular-weight epothilone with potential antineoplastic activity. Sagopilone binds to tubulin and induces microtubule polymerization while stabilizing microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2/M arrest, and apoptosis. The agent is not a substrate for the P-glycoprotein (P-gp) efflux pump and so may exhibit activity in multidrug-resistant (MDR) tumors. The epothilone class of metabolites was originally isolated from the myxobacterium Solangium cellulosum. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus) .

Current developer:   

1. Galmarini, Carlos M. Sagopilone, a microtubule stabilizer for the potential treatment of cancer. Current Opinion in Investigational Drugs (BioMed Central) (2009), 10(12), 1359-1371. CODEN: COIDAZ ISSN:2040-3429. AN 2010:726309

2. Richter, Annett; Olbrich, Carsten; Krause, Michael; Hoffmann, Jens; Kissel, Thomas. Polymeric Micelles for parenteral delivery of Sagopilone: Physicochemical characterization, novel formulation approaches and their toxicity assessment in vitro as well as in vivo. European Journal of Pharmaceutics and Biopharmaceutics (2010), 75(2), 80-89. CODEN: EJPBEL ISSN:0939-6411. AN 2010:643014

3. Richter, Annett; Wiedekind, Achim; Krause, Michael; Kissel, Thomas; Haag, Rainer; Olbrich, Carsten. Non-ionic dendritic glycerol-based amphiphiles: Novel excipients for the solubilization of poorly water-soluble anticancer drug Sagopilone. European Journal of Pharmaceutical Sciences (2010), 40(1), 48-55. CODEN: EPSCED ISSN:0928-0987. CAN 153:69993 AN 2010:465236

4. Eschenbrenner, Julia. Mode of action analysis of the synthetic epothilone Sagopilone. (2009), No pp. CAN 152:397468 AN 2010:438250

5. Richter, Annett; Olbrich, Carsten; Krause, Michael; Kissel, Thomas. Solubilization of Sagopilone, a poorly water-soluble anticancer drug, using polymeric micelles for parenteral delivery. International Journal of Pharmaceutics (2010), 389(1-2), 244-253.

6. Hammer, Stefanie; Sommer, Anette; Fichtner, Iduna; Becker, Michael; Rolff, Jana; Merk, Johannes; Klar, Ulrich; Hoffmann, Jens. Comparative Profiling of the Novel Epothilone, Sagopilone, in Xenografts Derived from Primary Non-Small Cell Lung Cancer. Clinical Cancer Research (2010), 16(5), 1452-1465. 

7. Qi, Wenyuan; Meng, Zhiyun; Dou, Guifang. Clinical research progress of epothilone analogues. Guoji Yaoxue Yanjiu Zazhi (2009), 36(5), 336-339. CODEN: GYYZBO ISSN:1674-0440. CAN 152:559866 AN 2010:145484

8. Koitka, Matthias; Hochel, Joachim; Gieschen, Hille; Borchert, Hans-Hubert. Improving the ex vivo stability of drug ester compounds in rat and dog serum: Inhibition of the specific esterases and implications on their identity. Journal of Pharmaceutical and Biomedical Analysis (2010), 51(3), 664-678. 

9. Arnold, D.; Voigt, W.; Kiewe, P.; Behrmann, C.; Lindemann, S.; Reif, S.; Wiesinger, H.; Giurescu, M.; Thiel, E.; Schmoll, H.-J. Weekly administration of sagopilone (ZK-EPO), a fully synthetic epothilone, in patients with refractory solid tumours: results of a phase I trial. British Journal of Cancer (2009), 101(8), 1241-1247. 

10. Silvani, Antonio; Gaviani, Paola; Fiumani, Anna; Scaioli, Vidmer; Lamperti, Elena; Eoli, Marica; Botturi, Andrea; Salmaggi, Andrea. Systemic sagopilone (ZK-EPO) treatment of patients with recurrent malignant gliomas. Journal of Neuro-Oncology (2009), 95(1), 61-64. CODEN: JNODD2 ISSN:0167-594X. CAN 152:397257 AN 2009:1134643

11. Michaud, Laura Boehnke. The epothilones: how pharmacology relates to clinical utility. Annals of Pharmacotherapy (2009), 43(7/8), 1294-1309. 

12. Strube, Anne; Hoffmann, Jens; Stepina, Elizaveta; Hauff, Peter; Klar, Ulrich; Kaekoenen, Sanna-Maria. Sagopilone Inhibits Breast Cancer Bone Metastasis and Bone Destruction Due to Simultaneous Inhibition of Both Tumor Growth and Bone Resorption. Clinical Cancer Research (2009), 15(11), 3751-3759. 

13. Hoffmann, Jens; Fichtner, Iduna; Lemm, Margit; Lienau, Philip; Hess-Stumpp, Holger; Rotgeri, Andrea; Hofmann, Birte; Klar, Ulrich. Sagopilone crosses the blood-brain barrier in vivo to inhibit brain tumor growth and metastases. Neuro-Oncology (Durham, NC, United States) (2009), 11(2), 158-166. 

14. Fumoleau, Pierre. Treatment beyond taxanes, emerging new cytotoxic agents. EJC Supplements (2009), 7(1), 8-13. 

15. Cheng, Kit L.; Bradley, Thomas; Budman, Daniel R. Novel microtubule-targeting agents - the epothilones. Biologics: Targets & Therapy (2008), 2(4), 789-811. CODEN: BTTICT ISSN:1177-5491. CAN 151:235111 AN 2009:388282

16. Mulzer, Johann; Altmann, Karl-Heinz; Hoefle, Gerhard; Mueller, Rolf; Prantz, Kathrin. Epothilones - A fascinating family of microtubule stabilizing antitumor agents. Comptes Rendus Chimie (2008), 11(11-12), 1336-1368. CODEN: CRCOCR ISSN:1631-0748. CAN 150:175860 AN 2008:1488319

17. Klar, Ulrich; Hoffmann, Jens; Giurescu, Marius. Sagopilone (ZK-EPO): from a natural product to a fully synthetic clinical development candidate. Expert Opinion on Investigational Drugs (2008), 17(11), 1735-1748. 

18. Alexander, Emma J. Sagopilone: Microtubule-stabilizing agent epothilone oncolytic. Drugs of the Future (2008), 33(6), 496-505. 

19. Hoffmann, Jens; Vitale, Ilio; Buchmann, Bernd; Galluzzi, Lorenzo; Schwede, Wolfgang; Senovilla, Laura; Skuballa, Werner; Vivet, Sonia; Lichtner, Rosemarie B.; Vicencio, Jose M.; Panaretakis, Theocharis; Siemeister, Gerhard; Lage, Hermann; Nanty, Lisa; Hammer, Stefanie; Mittelstaedt, Kevin; Winsel, Sebastian; Eschenbrenner, Julia; Castedo, Maria; Demarche, Carine; Klar, Ulrich; Kroemer, Guido. Improved Cellular Pharmacokinetics and Pharmacodynamics Underlie the Wide Anticancer Activity of Sagopilone. Cancer Research (2008), 68(13), 5301-5308. 

20. Pronzato, Paolo. New therapeutic options for chemotherapy-resistant metastatic breast cancer: the epothilones. Drugs (2008), 68(2), 139-146. 

21. Richter Annett; Olbrich Carsten; Krause Michael; Hoffmann Jens; Kissel Thomas Polymeric micelles for parenteral delivery of Sagopilone: physicochemical characterization, novel formulation approaches and their toxicity assessment in vitro as well as in vivo. European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V (2010), 75(2), 80-9. Journal code: 9109778. E-ISSN:1873-3441. PubMed ID 20188169 AN 2010360628 In-process for

22. Richter Annett; Wiedekind Achim; Krause Michael; Kissel Thomas; Haag Rainer; Olbrich Carsten Non-ionic dendritic glycerol-based amphiphiles: novel excipients for the solubilization of poorly water-soluble anticancer drug Sagopilone. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences (2010), 40(1), 48-55.

23. Tomillero A; Moral M A Gateways to clinical trials. Methods and findings in experimental and clinical pharmacology (2010), 32(1), 47-86. 

24. Richter Annett; Olbrich Carsten; Krause Michael; Kissel Thomas Solubilization of sagopilone, a poorly water-soluble anticancer drug, using polymeric micelles for parenteral delivery. International journal of pharmaceutics (2010), 389(1-2), 244-53. Journal code: 7804127. E-ISSN:1873-3476. PubMed ID 20100557 AN 2010183491

25. Hammer Stefanie; Sommer Anette; Fichtner Iduna; Becker Michael; Rolff Jana; Merk Johannes; Klar Ulrich; Hoffmann Jens Comparative profiling of the novel epothilone, sagopilone, in xenografts derived from primary non-small cell lung cancer. Clinical cancer research : an official journal of the American Association for Cancer Research (2010), 16(5), 1452-65. Journal code: 9502500. ISSN:1078-0432. PubMed ID 20179216 AN 2010146742

26. Schmid P; Kiewe P; Possinger K; Korfel A; Lindemann S; Giurescu M; Reif S; Wiesinger H; Thiel E; Kuhnhardt D Phase I study of the novel, fully synthetic epothilone sagopilone (ZK-EPO) in patients with solid tumors. Annals of oncology : official journal of the European Society for Medical Oncology / ESMO (2010), 21(3), 633-9. 

27. Galmarini Carlos M Sagopilone, a microtubule stabilizer for the potential treatment of cancer. Current opinion in investigational drugs (London, England : 2000) (2009), 10(12), 1359-71. 

28. Koitka Matthias; Hochel Joachim; Gieschen Hille; Borchert Hans-Hubert Improving the ex vivo stability of drug ester compounds in rat and dog serum: inhibition of the specific esterases and implications on their identity. Journal of pharmaceutical and biomedical analysis (2010), 51(3), 664-78. Journal code: 8309336. E-ISSN:1873-264X. PubMed ID 19850433 AN 2009745192 In-process for

29. Arnold D; Voigt W; Kiewe P; Behrmann C; Lindemann S; Reif S; Wiesinger H; Giurescu M; Thiel E; Schmoll H-J Weekly administration of sagopilone (ZK-EPO), a fully synthetic epothilone, in patients with refractory solid tumours: results of a phase I trial. British journal of cancer (2009), 101(8), 1241-7.

30. Silvani Antonio; Gaviani Paola; Fiumani Anna; Scaioli Vidmer; Lamperti Elena; Eoli Marica; Botturi Andrea; Salmaggi Andrea Systemic sagopilone (ZK-EPO) treatment of patients with recurrent malignant gliomas. Journal of neuro-oncology (2009), 95(1), 61-4. 

31. Cheng Kit L; Bradley Thomas; Budman Daniel R Novel microtubule-targeting agents - the epothilones. Biologics : targets & therapy (2008), 2(4), 789-811. Journal code: 101321511. ISSN:1177-5475. PubMed ID 19707459 AN 2009580379 In-process for

32. Tomillero A; Moral M A Gateways to clinical trials. Methods and findings in experimental and clinical pharmacology (2009), 31(5), 341-56. Journal code: 7909595. ISSN:0379-0355. PubMed ID 19649342 AN 2009529776

33. Michaud Laura Boehnke The epothilones: how pharmacology relates to clinical utility. The Annals of pharmacotherapy (2009), 43(7), 1294-309. 

34. Strube Anne; Hoffmann Jens; Stepina Elizaveta; Hauff Peter; Klar Ulrich; Kakonen Sanna-Maria Sagopilone inhibits breast cancer bone metastasis and bone destruction due to simultaneous inhibition of both tumor growth and bone resorption. Clinical cancer research : an official journal of the American Association for Cancer Research (2009), 15(11), 3751-9. 

35. Hoffmann Jens; Fichtner Iduna; Lemm Margit; Lienau Philip; Hess-Stumpp Holger; Rotgeri Andrea; Hofmann Birte; Klar Ulrich Sagopilone crosses the blood-brain barrier in vivo to inhibit brain tumor growth and metastases. Neuro-oncology (2009), 11(2), 158-66.

36. Tomillero A; Moral M A Gateways to Clinical Trials. Methods and findings in experimental and clinical pharmacology (2008), 30(9), 715-24.

37. Klar Ulrich; Hoffmann Jens; Giurescu Marius Sagopilone (ZK-EPO): from a natural product to a fully synthetic clinical development candidate. Expert opinion on investigational drugs (2008), 17(11), 1735-48. 

38. Hoffmann Jens; Vitale Ilio; Buchmann Bernd; Galluzzi Lorenzo; Schwede Wolfgang; Senovilla Laura; Skuballa Werner; Vivet Sonia; Lichtner Rosemarie B; Vicencio Jose M; Panaretakis Theocharis; Siemeister Gerhard; Lage Hermann; Nanty Lisa; Hammer Stefanie; Mittelstaedt Kevin; Winsel Sebastian; Eschenbrenner Julia; Castedo Maria; Demarche Carine; Klar Ulrich; Kroemer Guido Improved cellular pharmacokinetics and pharmacodynamics underlie the wide anticancer activity of sagopilone. Cancer research (2008), 68(13), 5301-8.

39. Pronzato Paolo New therapeutic options for chemotherapy-resistant metastatic breast cancer: the epothilones. Drugs (2008), 68(2), 139-46.