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Becatecarin

Description of Becatecarin: Becatecarin  is a synthetic diethylaminoethyl analogue of the indolocarbazole glycoside antineoplastic antibiotic rebeccamycin. Becatecarin intercalates into DNA and stabilizes the DNA-topoisomerase I complex, thereby interfering with the topoisomerase I-catalyzed DNA breakage-reunion reaction and initiating DNA cleavage and apoptosis. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Current developer:    Exelixis Inc.

 1. Mann, David Marshall. Gene expression profiling in the pulmonary artery in the selection of therapies for vascular-related diseases. PCT Int. Appl. (2009), 115pp. CODEN: PIXXD2 WO 2009121031 A1 20091001 CAN 151:418165 AN 2009:1194632

2. Robey, Robert W.; Obrzut, Tomasz; Shukla, Suneet; Polgar, Orsolya; Macalou, Sira; Bahr, Julian C.; Pietro, Attilio; Ambudkar, Suresh V.; Bates, Susan E. Becatecarin (rebeccamycin analog, NSC 655649) is a transport substrate and induces expression of the ATP-binding cassette transporter, ABCG2, in lung carcinoma cells. Cancer Chemotherapy and Pharmacology (2009), 64(3), 575-583. CODEN: CCPHDZ ISSN:0344-5704. CAN 152:254419 AN 2009:689908

3. Li, Chiang Jia; Mikule, Keith; Li, Youzhi. Compositions and methods using Stat3 pathway inhibitors or cancer stem cell inhibitors for combination cancer treatment. PCT Int. Appl. (2009), 81pp. CODEN: PIXXD2 WO 2009036101 A1 20090319 CAN 150:345478 AN 2009:332545

4. Burstein, Harold J.; Overmoyer, Beth; Gelman, Rebecca; Silverman, Paula; Savoie, Jennifer; Clarke, Kathryn; Dumadag, Leda; Younger, Jerry; Ivy, Percy; Winer, Eric P. Rebeccamycin analog for refractory breast cancer: a randomized phase II trial of dosing schedules. Investigational New Drugs (2007), 25(2), 161-164. CODEN: INNDDK ISSN:0167-6997. CAN 146:287832 AN 2006:1347363

5. Dowlati, Afshin; Chapman, Robert; Subbiah, Shanmuga; Fu, Pingfu; Ness, Anne; Cortas, Tania; Patrick, Lauren; Reynolds, Sherrie; Xu, Natalie; Levitan, Nathan; Ivy, Percy; Remick, Scot C. Randomized phase II trial of different schedules of administration of rebeccamycin analogue as second line therapy in non-small cell lung cancer. Investigational New Drugs (2005), 23(6), 563-567. CODEN: INNDDK ISSN:0167-6997. CAN 144:480540 AN 2006:65782

6. Ricart, Alejandro D.; Hammond, Lisa A.; Kuhn, John G.; Takimoto, Chris H.; Goetz, Andrew; Forouzesh, Bahram; Forero, Leonardo; Ochoa-Bayona, Jose L.; Berg, Kristin; Tolcher, Anthony W.; Rowinsky, Eric K. Phase I and Pharmacokinetic Study of Sequences of the Rebeccamycin Analogue NSC 655649 and Cisplatin in Patients with Advanced Solid Tumors. Clinical Cancer Research (2005), 11(24, Pt. 1), 8728-8736. CODEN: CCREF4 ISSN:1078-0432. CAN 144:460400 AN 2005:1318349

7. Rewcastle, Gordon W. Becatecarin(Helsinn Healthcare). IDrugs (2005), 8(10), 838-847. CODEN: IDRUFN ISSN:1369-7056. CAN 144:183759 AN 2005:1173150

8. Moreau, Pascale; Holbeck, Susan; Prudhomme, Michelle; Sausville, Edward A. Cytotoxicities of three rebeccamycin derivatives in the National Cancer Institute screening of 60 human tumor cell lines. Anti-Cancer Drugs (2005), 16(2), 145-150. CODEN: ANTDEV ISSN:0959-4973. CAN 142:348304 AN 2005:40758

9. Masferrer, Jaime L. Method using a cyclooxygenase 2 (COX-2) inhibitor and a topoisomerase II inhibitor as a combination therapy in the treatment of neoplasia. U.S. Pat. Appl. Publ. (2003), 85 pp., Cont.-in-part of U.S. Ser. No. 865,177. CODEN: USXXCO US 2003225150 A1 20031204 CAN 140:726 AN 2003:950066

10. Hussain, Maha; Vaishampayan, Ulka; Heilbrun, Lance K.; Jain, Vikash; LoRusso, Patricia M.; Ivy, Percy; Flaherty, Lawrence. A phase II study of rebeccamycin analog (NSC-655649) in metastatic renal cell cancer. Investigational New Drugs (2003), 21(4), 465-471. CODEN: INNDDK ISSN:0167-6997. CAN 141:16967 AN 2003:833153

11. Goel, Sanjay; Wadler, Scott; Hoffman, Anthony; Volterra, Fabio; Baker, Cheryl; Nazario, Elliot; Ivy, Percy; Silverman, Alyson; Mani, Sridhar. A Phase II Study of Rebeccamycin Analog NSC 655649 in Patients with Metastatic Colorectal Cancer. Investigational New Drugs (2003), 21(1), 103-107. CODEN: INNDDK ISSN:0167-6997. CAN 139:358114 AN 2003:245064

12. Merchant, Joseph; Tutsch, Kendra; Dresen, Amy; Arzoomanian, Rhoda; Alberti, Dona; Feierabend, Chris; Binger, Kim; Marnoccha, Rebecca; Thomas, James; Cleary, Jim; Wilding, George. Phase I clinical and pharmacokinetic study of NSC 655649, a rebeccamycin analogue, given in both single-dose and multiple-dose formats. Clinical Cancer Research (2002), 8(7), 2193-2201. CODEN: CCREF4 ISSN:1078-0432. CAN 137:163468 AN 2002:601198

13. Long, Byron H.; Rose, William C.; Vyas, Dolatrai M.; Matson, James A.; Forenza, Salvatore. Discovery of antitumor indolocarbazoles: rebeccamycin, NSC 655649, and fluoroindolocarbazoles. Current Medicinal Chemistry: Anti-Cancer Agents (2002), 2(2), 255-266. CODEN: CMCACI ISSN:1568-0118. CAN 137:134289 AN 2002:267591

14. Tolcher, Anthony W.; Eckhardt, S. Gail; Kuhn, John; Hammond, Lisa; Weiss, Geoffrey; Rizzo, Jinee; Aylesworth, Cheryl; Hidalgo, Manuel; Patnaik, Amita; Schwartz, Garry; Felton, Sally; Campbell, Elizabeth; Rowinsky, Eric K. Phase I and pharmacokinetic study of NSC 655649, a rebeccamycin analog with topoisomerase inhibitory properties. Journal of Clinical Oncology (2001), 19(11), 2937-2947. CODEN: JCONDN ISSN:0732-183X. CAN 135:282652 AN 2001:505322

15. Dowlati, Afshin; Hoppel, Charles L.; Ingalls, Stephen T.; Majka, Susan; Li, Xiaolin; Sedransk, Nell; Spiro, Timothy; Gerson, Stanton L.; Ivy, Percy; Remick, Scot C. Phase I clinical and pharmacokinetic study of rebeccamycin analog NSC 655649 given daily for five consecutive days. Journal of Clinical Oncology (2001), 19(8), 2309-2318. CODEN: JCONDN ISSN:0732-183X. CAN 135:235854 AN 2001:353904

16. Bailly, Christian; Goossens, Jean-Francois; Laine, William; Anizon, Fabrice; Prudhomme, Michelle; Ren, Jinsong; Chaires, Jonathan B. Formaldehyde-Induced Alkylation of a 2'-Aminoglucose Rebeccamycin Derivative to Both A T and G C Base Pairs in DNA. Journal of Medicinal Chemistry (2000), 43(24), 4711-4720. CODEN: JMCMAR ISSN:0022-2623. CAN 134:65796 AN 2000:713583

17. Venkataram, Ubrani V.; Franchini, Miriam K.; Bogardus, Joseph B. Stable solutions of rebeccamycin analog and preparations thereof. Can. Pat. Appl. (1990), 18 pp. CODEN: CPXXEB CA 2015632 A1 19901110 CAN 115:120044 AN 1991:520044

18. Venkataram, Ubrani V.; Franchini, Miriam K.; Bogardus, Joseph B. Anticancer solutions containing stabilized 8-N-(diethylaminoethyl)rebeccamycin. Eur. Pat. Appl. (1990), 7 pp. CODEN: EPXXDW EP 397147 A2 19901114 CAN 115:35719 AN 1991:435719

19. Kaneko, Takushi; Wong, Henry; Utzig, Jacob; Schurig, John; Doyle, Terrence W. Water soluble derivatives of rebeccamycin. Journal of Antibiotics (1990), 43(1), 125-7. CODEN: JANTAJ ISSN:0021-8820. CAN 112:217391 AN 1990:217391

20. Kaneko, Takushi; Wong, Henry S.; Utzig, Jacob J. Preparation of rebeccamycin analogs as antitumors and pharmaceutical compositions containing them. Eur. Pat. Appl. (1988), 14 pp. CODEN: EPXXDW EP 269025 A2 19880601 CAN 110:135647 AN 1989:135647

21. Dowlati Afshin; Posey James; Ramanathan Ramesh K; Rath Linda; Fu Pingfu; Chak Amitabh; Krishnamurthi Smitha; Brell Joanna; Ingalls Stephen; Hoppel Charles L; Ivy Percy; Remick Scot C Phase II and pharmacokinetic trial of rebeccamycin analog in advanced biliary cancers. Cancer chemotherapy and pharmacology (2009), 65(1), 73-8. Journal code: 7806519. E-ISSN:1432-0843. PubMed ID 19399502 AN 2009627380 MEDLINE (Copyright (C) 2010 U.S. National Library of Medicine on SciFinder (R))

22. Tomillero A; Moral M A Gateways to clinical trials. Methods and findings in experimental and clinical pharmacology (2009), 31(4), 263-98.

23. Tomillero A; Moral M A Gateways to clinical trials. Methods and findings in experimental and clinical pharmacology (2008), 30(8), 643-72. Journal code: 7909595. ISSN:0379-0355. PubMed ID 19088949 AN 2009036942 MEDLINE (Copyright (C) 2010 U.S. National Library of Medicine on SciFinder (R))

24. Tomillero A; Moral M A Gateways to clinical trials. Methods and findings in experimental and clinical pharmacology (2008), 30(5), 383-408. Journal code: 7909595. ISSN:0379-0355. PubMed ID 18806898 AN 2008617220 MEDLINE (Copyright (C) 2010 U.S. National Library of Medicine on SciFinder (R))

25. Borthakur Gautam; Alvarado Yesid; Ravandi-Kashani Farhad; Cortes Jorge; Estrov Zeev; Faderl Stefan; Ivy Percy; Bueso-Ramos Carlos; Nebiyou Bekele B; Giles Francis Phase 1 study of XL119, a rebeccamycin analog, in patients with refractory hematologic malignancies. Cancer (2008), 113(2), 360-6.

26. Langevin Anne-Marie; Bernstein Mark; Kuhn John G; Blaney Susan M; Ivy Percy; Sun Junfeng; Chen Zhengjia; Adamson Peter C A phase II trial of rebeccamycin analogue (NSC #655649) in children with solid tumors: a Children's Oncology Group study. Pediatric blood & cancer (2008), 50(3), 577-80. 

27. Bayes Miriam; Rabasseda X; Prous J R Gateways to clinical trials. Methods and findings in experimental and clinical pharmacology (2007), 29(3), 231-45. Journal code: 7909595. ISSN:0379-0355. PubMed ID 17520107 AN 2007308528 MEDLINE (Copyright (C) 2010 U.S. National Library of Medicine on SciFinder (R))

28. Bayes M; Rabasseda X; Prous J R Gateways to clinical trials. Methods and findings in experimental and clinical pharmacology (2006), 28(7), 451-95. 

29. Anizon Fabrice; Moreau Pascale; Sancelme Martine; Laine William; Bailly Christian; Prudhomme Michelle Rebeccamycin analogues bearing amine substituents or other groups on the sugar moiety. Bioorganic & medicinal chemistry (2003), 11(17), 3709-22. 

30. Langevin Anne-Marie; Weitman Steven D; Kuhn John G; Weintraub Susan T; Baruchel Sylvain; Furman Wayne; Bernstein Mark; Blaney Susan; Vietti Teresa Phase I trial of rebeccamycin analog (NSC #655649) in children with refractory solid tumors: a pediatric oncology group study. Journal of pediatric hematology/oncology : official journal of the American Society of Pediatric Hematology/Oncology (2003), 25(7), 526-33.

31. Weitman S; Moore R; Barrera H; Cheung N K; Izbicka E; Von Hoff D D In vitro antitumor activity of rebeccamycin analog (NSC# 655649) against pediatric solid tumors. Journal of pediatric hematology/oncology : official journal of the American Society of Pediatric Hematology/Oncology (1998), 20(2), 136-9. 

32. Krishnan B S; Moore M E; Lavoie C P; Long B H; Dalterio R A; Wong H S; Rosenberg I E Fluorescence polarization studies of the binding of BMS 181176 to DNA. Journal of biomolecular structure & dynamics (1994), 12(3), 625-36.