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Cemadotin

LU103793 (NSC D-669356) is a new synthetic derivative of Dolastatin 15, an antiproliferative compound which was isolated from the mollusk Dolabella auricularia. Like Dolastatin 15, LU103793 is highly cytotoxic in vitro (IC50 = 0.1 nM). Turbidity assays with bovine brain microtubules demonstrated that LU103793 inhibits microtubule polymerization in a concentration-dependent manner (IC50 = 7 microM). Treatment with this compound also induced depolymerization of preassembled microtubules. Cell cycle analysis of tumor cell lines treated with LU103793 indicated a block in the G2-M phase. At the cellular level, it induced depolymerization of microtubules in interphase cells and development of abnormal spindles and chromosome distribution in mitotic cells. Although these effects are very similar to the cellular alterations caused by vinblastine, LU103793 does not inhibit vinblastine binding to unpolymerized tubulin in vitro. Our results suggest that LU103793 exerts its cytotoxic activity primarily through disruption of microtubule organization. See: http://www.ncbi.nlm.nih.gov/pubmed/7606731.

Current developer: Abbott Laboratories Inc.

1. Wei, Ge; Selvam, Krishnasamy Panneer; Bookbinder, Louis; Frost, Gregory I. Soluble C-terminal truncation derivatives of PH20 hyaluronidase for use in hyaluronan degradation in improving drug access to targets. U.S. Pat. Appl. Publ. (2010), 75pp. CODEN: USXXCO US 2010143457 A1 20100610 AN 2010:717638

2. Schoeller, Joergen; Pedersen, Henrik; Brix, Liselotte. Molecular vaccines for infectious disease. PCT Int. Appl. (2010), 716pp. CODEN: PIXXD2 WO 2010037402 A1 20100408 CAN 152:475600 AN 2010:522639

3. Brix, Liselotte; Schoeller, Joergen; Pedersen, Henrik. MHC multimers in cancer vaccines and immune monitoring. PCT Int. Appl. (2010), 1228pp., MEGA TAN OF 21324085W. CODEN: PIXXD2 WO 2010037395 A2 20100408 CAN 152:475577 AN 2010:490042

4. Frost, Gregory I.; Jiang, Ping; Thompson, Curtis B. Modified hyaluronidases and uses in treating hyaluronan-associated diseases and conditions. PCT Int. Appl. (2009), 292 pp. CODEN: PIXXD2 WO 2009128917 A2 20091022 CAN 151:462825 AN 2009:1297488

5. Ryan, Maureen; Smith, Maria Leia. Detection and treatment of pancreatic, ovarian and other cancers. PCT Int. Appl. (2009), 71pp. CODEN: PIXXD2 WO 2009126934 A2 20091015 CAN 151:465311 AN 2009:1262955

6. Wood, Clive R.; Dransfield, Daniel T. Metalloproteinase binding proteins and uses for preparing drug conjugates. PCT Int. Appl. (2009), 168pp. CODEN: PIXXD2 WO 2009097397 A2 20090806 CAN 151:229394 AN 2009:944359

7. Qie, Jiankun; Zhou, Wenxia; Zhao, Xiunan; He, Junlin; Zhang, Yongxiang; Liu, Keliang. Hemiasterlin Analogues with Unnatural Amino Acids at the N-Terminal and Their Inhibitory Activity on Tumor Cells. International Journal of Peptide Research and Therapeutics (2009), 15(3), 187-194. CODEN: IJPRFC ISSN:1573-3149. CAN 150:554894 AN 2009:282023

8. Liu, Jie; King, David. Site-specific attachment of drugs or other agents to engineered antibodies with C-terminal cysteine-containing extensions. PCT Int. Appl. (2009), 93pp. CODEN: PIXXD2 WO 2009026274 A1 20090226 CAN 150:253502 AN 2009:238860

9. Bai, Ruoli; Edler, Michael C.; Bonate, Peter L.; Copeland, Terry D.; Pettit, George R.; Luduena, Richard F.; Hamel, Ernest. Intracellular activation and deactivation of tasidotin, an analog of dolastatin 15: correlation with cytotoxicity. Molecular Pharmacology (2009), 75(1), 218-226. CODEN: MOPMA3 ISSN:0026-895X. CAN 150:252174 AN 2009:18782

10. Barnett, Bradley Powers; Gailloud, Philippe. Alginate and alginate lyase compositions. PCT Int. Appl. (2008), 152pp. CODEN: PIXXD2 WO 2008127290 A2 20081023 CAN 149:519014 AN 2008:1282626

11. Law, Che-Leung; Mcearchern, Julie; Drachman, Jonathan G. Conjugates of anti-CD70 antibodies with drugs and their use for the treatment of cancer and immune disorders. U.S. Pat. Appl. Publ. (2008), 81pp., Cont.-in-part of U.S. Ser. No. 546,304. CODEN: USXXCO US 2008025989 A1 20080131 CAN 148:190136 AN 2008:125686

12. Nilsson, Rune; Sandberg, Bengt; Wilbur, Scott. Conjugates of cytotoxic agents and dendrimers chain-extended with linear polymers. PCT Int. Appl. (2007), 61 pp. CODEN: PIXXD2 WO 2007080114 A2 20070719 CAN 147:197339 AN 2007:788631

13. Habib, Nabil. Treatment of cancer and other diseases. PCT Int. Appl. (2007), 86pp. CODEN: PIXXD2 WO 2007064691 A1 20070607 CAN 147:46112 AN 2007:619578

14. Kavimani, S.; Mounnissamy, V. M.; Ravitchandirane, V.; Balu, V. Marine animal and plant anticancer constituents. Amala Research Bulletin (2006), 26 83-86. CODEN: ARBMCS ISSN:0971-4987. CAN 147:124740 AN 2007:598905

15. Moeritz, Annemarie. Medicine - right out of the ocean. Medizinische Monatsschrift fuer Pharmazeuten (2007), 30(3), 103-107. CODEN: MMPHDB ISSN:0342-9601. CAN 147:514294 AN 2007:407632

16. Boyd, Sharon Elaine; Chen, Liang; Ganwar, Sanjeev; Guerlavais, Vincent; Horgan, Killian; Sufi, Bilal. Antibody-drug peptide conjugates for use as cytotoxins in cancer treatment. PCT Int. Appl. (2007), 210 pp. CODEN: PIXXD2 WO 2007038658 A2 20070405 CAN 146:402314 AN 2007:385410

17. Kaushal, Shalesh; Noorwez, Syed Mohammed. Proteasome inhibitors and other small compounds that correct protein misfolding and uses thereof. PCT Int. Appl. (2007), 60 pp. CODEN: PIXXD2 WO 2007014327 A2 20070201 CAN 146:198725 AN 2007:113642

18. Catassi, A.; Cesario, A.; Arzani, D.; Menichini, P.; Alama, A.; Bruzzo, C.; Imperatori, A.; Rotolo, N.; Granone, P.; Russo, P. Characterization of apoptosis induced by marine natural products in non small cell lung cancer A549 cells. Cellular and Molecular Life Sciences (2006), 63(19-20), 2377-2386. CODEN: CMLSFI ISSN:1420-682X. CAN 146:474951 AN 2006:1188455

19. Kaushal, Shalesh; Malhotra, Ritu; Dunn, William A. Materials and methods for enhanced degradation of mutant proteins associated with human disease. PCT Int. Appl. (2006), 87pp. CODEN: PIXXD2 WO 2006116716 A2 20061102 CAN 145:465766 AN 2006:1155706

20. Xin, Zhihong; Zhu, Weiming; Gu, Qianqun; Cui, Chengbin. Current status and developing trend for marine anticancer active agents. Zhongguo Yaoxue Zazhi (Beijing, China) (2005), 40(12), 881-885. CODEN: ZYZAEU ISSN:1001-2494. CAN 145:341915 AN 2006:521941

21. Vaghefi, Farid; Chen, Lan Bo; Sherman, Matthew L. Bis(thiohydrazide amides) for treatment of hyperplasia. PCT Int. Appl. (2006), 104 pp. CODEN: PIXXD2 WO 2006033913 A2 20060330 CAN 144:343554 AN 2006:295255

22. Rawat, Diwan S.; Joshi, Mukesh C.; Joshi, Penny; Atheaya, Himanshu. Marine peptides and related compounds in clinical trial. Anti-Cancer Agents in Medicinal Chemistry (2006), 6(1), 33-40. CODEN: AAMCE4 ISSN:1871-5206. CAN 144:120775 AN 2006:104235

23. Yaffe, Michael B.; Clapperton, Julie A.; Manke, Isaac A.; Lowery, Drew M.; Ho, Timmy; Haire, Lesley F.; Smerdon, Stephen J. The x-ray crystal structure of BRCA1 tandem BRCT repeat and BACH1 phosphopeptide complex and methods and compositions for antitumor drug design. PCT Int. Appl. (2005), 360 pp. CODEN: PIXXD2 WO 2005115454 A2 20051208 CAN 144:46998 AN 2005:1290072

24. Zask, Arie; Kaplan, Joshua; Musto, Sylvia; Loganzo, Frank. Hybrids of the hemiasterlin analogue Taltobulin and the Dolastatins are potent antimicrotubule agents. Journal of the American Chemical Society (2005), 127(50), 17667-17671. CODEN: JACSAT ISSN:0002-7863. CAN 144:129230 AN 2005:1247823

25. Lacasse, Eric; McManus, Daniel. Human protein IAP (inhibitor of apoptosis protein) nucleobase oligomers, including dsRNA, shRNA, and siRNA, and their use for enhancing apoptosis in cancer therapy. PCT Int. Appl. (2005), 112 pp. CODEN: PIXXD2 WO 2005042558 A1 20050512 CAN 142:457053 AN 2005:409543

26. Lacasse, Eric; McManus, Daniel; Durkin, Jon P. Sequences of antisense IAP (inhibitor of apoptosis protein) oligomers and their use for treatment of proliferative diseases with a chemotherapeutic agent. PCT Int. Appl. (2005), 285 pp. CODEN: PIXXD2 WO 2005042030 A1 20050512 CAN 142:457052 AN 2005:409357

27. Lee, Margaret S.; Nichols, James M.; Zhang, Yanzhen; Keith, Curtis. Combinations of chlorpromazine compounds and antiproliferative drugs for the treatment of neoplasms. PCT Int. Appl. (2005), 65 pp. CODEN: PIXXD2 WO 2005027842 A2 20050331 CAN 142:349042 AN 2005:283298

28. Kandimalla, Ekambar R.; Agrawal, Sudhir; Wang, Daqin. Synergistic treatment of cancer using immunomers in conjunction with chemotherapeutic agents. PCT Int. Appl. (2004), 106 pp. CODEN: PIXXD2 WO 2004103301 A2 20041202 CAN 142:696 AN 2004:1036851

29. Law, Che-Leung; Wahl, Alan F.; Scholler, Nathalie; Pestano, Linda A. Anti-CD70 antibodies and immunoconjugates with therapeutic agents for treatment of cancer and immune disorders. PCT Int. Appl. (2004), 159 pp. CODEN: PIXXD2 WO 2004073656 A2 20040902 CAN 141:242040 AN 2004:718323

30. Proksch, Peter; Edrada, RuAngelie; Ebel, Rainer. Drugs from the sea. Who are the producers? BIOforum Europe (2004), 8(2), 44-46. CODEN: BEIUB6 ISSN:1611-597X. CAN 142:46 AN 2004:455768

31. Wahl, Alan F.; Senter, Peter D.; Law, Che-leung; Cerveny, Charles G. Anti-CD20 antibody-drug conjugates for the treatment of cancer and immune disorders in mammal and human. PCT Int. Appl. (2004), 161 pp. CODEN: PIXXD2 WO 2004032828 A2 20040422 CAN 140:337930 AN 2004:331903

32. Marks, Randolph S.; Graham, David L.; Sloan, Jeff A.; Hillman, Shauna; Fishkoff, Steven; Krook, James E.; Okuno, Scott H.; Mailliard, James A.; Fitch, Tom R.; Addo, Ferdinand. A phase II study of the dolastatin 15 analogue LU 103793 in the treatment of advanced non-small-cell lung cancer. American Journal of Clinical Oncology (2003), 26(4), 336-337. CODEN: AJCODI ISSN:0277-3732. CAN 140:122336 AN 2004:62018

33. Cruz-Monserrate, Zobeida; Mullaney, Jeffrey T.; Harran, Patrick G.; Pettit, George R.; Hamel, Ernest. Dolastatin 15 binds in the vinca domain of tubulin as demonstrated by Hummel-Dreyer chromatography. European Journal of Biochemistry (2003), 270(18), 3822-3828. CODEN: EJBCAI ISSN:0014-2956. CAN 139:316854 AN 2003:741053

34. Aoki, Yuko; Hasegawa, Kiyoshi; Ishii, Nobuya; Mori, Kazushige. Method for selecting antitumor drug sensitivity-determining factors and method for predicting antitumor drug sensitivity using the selected factors. PCT Int. Appl. (2003), 81 pp. CODEN: PIXXD2 WO 2003076660 A1 20030918 CAN 139:255332 AN 2003:737931

35. Ishitsuka, Hideo; Okabe, Hisafumi; Shimma, Nobuo; Tsukuda, Takuo; Umeda, Isao. Method for identification of tumor targeting enzymes for design of compounds which generate anticancer substances. PCT Int. Appl. (2003), 118 pp. CODEN: PIXXD2 WO 2003043631 A2 20030530 CAN 139:7174 AN 2003:417621

36. Law, Che-Leung; Klussman, Kerry; Wahl, Alan F.; Senter, Peter; Doronina, Svetlana; Toki, Brian. Anti-CD30 antibody-cytotoxic agent conjugates for treating non-cancer immunological disorders. PCT Int. Appl. (2003), 194 pp. CODEN: PIXXD2 WO 2003043583 A2 20030530 CAN 139:5639 AN 2003:417584

37. Kerbrat, P.; Dieras, V.; Pavlidis, N.; Ravaud, A.; Wanders, J.; Fumoleau, P. Phase II study of LU 103793 (dolastatin analogue) in patients with metastatic breast cancer. European Journal of Cancer (2003), 39(3), 317-320. CODEN: EJCAEL ISSN:0959-8049. CAN 139:270382 AN 2003:83483

38. Weiner, George; Hartmann, Gunther. Methods for enhancing antibody-induced cell lysis and treating cancer. PCT Int. Appl. (2001), 312 pp. CODEN: PIXXD2 WO 2001097843 A2 20011227 CAN 136:84677 AN 2001:935435

39. Supko, Jeffrey G.; Lynch, Thomas J.; Clark, Jeffrey W.; Fram, Robert; Allen, Lee F.; Velagapudi, Raja; Kufe, Donald W.; Eder, Joseph Paul, Jr. A phase I clinical and pharmacokinetic study of the dolastatin analogue cemadotin administered as a 5-day continuous intravenous infusion. Cancer Chemotherapy and Pharmacology (2000), 46(4), 319-328. CODEN: CCPHDZ ISSN:0344-5704. CAN 134:335954 AN 2000:634571

40. Von Angerer, Erwin. New inhibitors of tubulin polymerization. Expert Opinion on Therapeutic Patents (1999), 9(8), 1069-1081. CODEN: EOTPEG ISSN:1354-3776. CAN 131:266394 AN 1999:514438

41. Barlozzari, Teresa; Banerjee, Subhashis; Haupt, Andreas. Preparation of dolastatin-15 derivatives for treatment of rheumatoid arthritis. PCT Int. Appl. (1999), 106 pp. CODEN: PIXXD2 WO 9917792 A1 19990415 CAN 130:267776 AN 1999:249095

42. Barlozzari, Teresa; Banerjee, Subhashis; Haupt, Andreas. Preparation of dolastatin-15 derivatives for treatment of rheumatoid arthritis. PCT Int. Appl. (1999), 103 pp. CODEN: PIXXD2 WO 9917709 A2 19990415 CAN 130:267774 AN 1999:244526

43. Jordan, Mary Ann; Walker, Deborah; De Arruda, Monika; Barlozzari, Teresa; Panda, Dulal. Suppression of Microtubule Dynamics by Binding of Cemadotin to Tubulin: Possible Mechanism for Its Antitumor Action. Biochemistry (1998), 37(50), 17571-17578. CODEN: BICHAW ISSN:0006-2960. CAN 130:119203 AN 1998:745399

44. Haupt, Andreas; Emling, Franz; Romerdahl, Cynthia. Preparation of linear dolastatin peptides as antitumor agents. U.S. (1998), 47 pp., Cont.-in-part of U.S. Ser. No. 431,795, abandoned. CODEN: USXXAM US 5831002 A 19981103 CAN 129:343720 AN 1998:719162

45. Barlozzari, Teresa; Haupt, Andreas. Dolastatin-15 derivatives in combination with taxanes. PCT Int. Appl. (1998), 114 pp. CODEN: PIXXD2 WO 9840092 A1 19980917 CAN 129:239875 AN 1998:621127

46. Villalona-Calero, Miguel A.; Baker, Sharyn D.; Hammond, Lisa; Aylesworth, Cheryl; Eckhardt, S. Gail; Kraynak, M.; Fram, Robert; Fischkoff, Steven; Velagapudi, Raja; Toppmeyer, Deborah; Razvillas, Betty; Jakimowicz, Krystyna; Von Hoff, Daniel D.; Rowinsky, Eric. Phase I and pharmacokinetic study of the water-soluble dolastatin 15 analog LU103793 in patients with advanced solid malignancies. Journal of Clinical Oncology (1998), 16(8), 2770-2779. CODEN: JCONDN ISSN:0732-183X. CAN 129:297904 AN 1998:554397

47. de Arruda, Monika; Cocchiaro, Celia A.; Nelson, Christine M.; Grinnell, Christine M.; Janssen, Bernd; Haupt, Andreas; Barlozzari, Teresa. LU103793 (NSC D-669356): a synthetic peptide that interacts with microtubules and inhibits mitosis. Cancer Research (1995), 55(14), 3085-92. CODEN: CNREA8 ISSN:0008-5472. CAN 123:132207 AN 1995:688156

48. Smyth J; Boneterre M E; Schellens J; Calvert H; Greim G; Wanders J; Hanauske A Activity of the dolastatin analogue, LU103793, in malignant melanoma. Annals of oncology : official journal of the European Society for Medical Oncology / ESMO (2001), 12(4), 509-11. Journal code: 9007735. ISSN:0923-7534. PubMed ID 11398885 AN 2001331247

49. Hu M K; Huang W S Synthesis and cytostatic properties of structure-simplified analogs of dolastatin 15. The journal of peptide research : official journal of the American Peptide Society (1999), 54(6), 460-7. Journal code: 9707067. ISSN:1397-002X. PubMed ID 10604591 AN 2000068091

50. Lansiaux A; Bailly C Dolastatins. Bulletin du cancer (1999), 86(11), 897-901. Journal code: 0072416. ISSN:0007-4551. PubMed ID 10586105 AN 2000054101