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OSI-930

OSI-930 is a selective thiophene-derived tyrosine kinase inhibitor with potential antineoplastic activity. Tyrosine kinase inhibitor OSI-930 inhibits stem cell factor receptor (c-Kit) and the vascular endothelial growth factor receptor 2 (VEGFR2), which may result in the inhibition of both tumor cell proliferation and tumor angiogenesis. Both c-Kit and VEGFR2 are overexpressed in a variety of cancers. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

OSI-930 is a novel inhibitor of the receptor tyrosine kinases Kit and kinase insert domain receptor (KDR), which is currently being evaluated in clinical studies. OSI-930 selectively inhibits Kit and KDR with similar potency in intact cells and also inhibits these targets in vivo following oral dosing.

 Current developer:   OSI Pharmaceuticals, Inc

 1. Dihel, Larry; Kittleson, Christine; Mulvihill, Kristen; Johnson, William W. Oxidative metabolism of the trifluoromethoxy moiety of OSI-930. Drug Metabolism and Drug Interactions (2009), 24(2-4), 95-121. CODEN: DMDIEQ ISSN:0792-5077. AN 2010:437994

2. Gruber, Harry E.; Jolly, Douglas; Perez, Omar. Recombinant replication-competent retroviral vectors expressing therapeutic products for treatment of proliferative disorders. PCT Int. Appl. (2010), 194pp. CODEN: PIXXD2 WO 2010036986 A2 20100401 CAN 152:423197 AN 2010:402977

3. Patel, Jay; Korlipara, Vijaya L. Design, synthesis, and evaluation of OSI-930 analogs as dual c-Kit and KDR (VEGFR-2) tyrosine kinase inhibitors. Abstracts of Papers, 238th ACS National Meeting, Washington, DC, United States, August 16-20, 2009 (2009), MEDI-144. CODEN: 69LVCL AN 2009:984314

4. Steinberg, Joyce L.; Gupta, Neeraj; Pradhan, Rajendra S.; Enschede, Sari H.; Humerickhouse, Rod A. Pharmaceutical dosage form for oral administration of tyrosine kinase inhibitor. PCT Int. Appl. (2009), 38pp. CODEN: PIXXD2 WO 2009100176 A2 20090813 CAN 151:253972 AN 2009:976624

5. Bosch Genover, Jaime; Fernandez Lobato, Mercedes. Treatment of portal hypertension and related conditions by combined inhibition of the VEGF and PDGF signaling pathways. PCT Int. Appl. (2009), 30pp. CODEN: PIXXD2 WO 2009092442 A1 20090730 CAN 151:212495 AN 2009:918301

6. Garton, Andrew J.; Franklin, Maryland. Combined treatment with an EGFR kinase inhibitor and an inhibitor of c-kit. U.S. Pat. Appl. Publ. (2009), 40 pp. CODEN: USXXCO US 2009136517 A1 20090528 CAN 151:1315 AN 2009:652406

7. Haley, John; Thomson, Stuart. Biological markers predictive of anti-cancer response to kinase inhibitors. PCT Int. Appl. (2008), 106pp. CODEN: PIXXD2 WO 2008127719 A1 20081023 CAN 149:486833 AN 2008:1281025

8. Bradner, James Elliot; Shen, John Paul; Perlstein, Ethan Oren; Rubinsztein, David; Sarkar, Sovan; Schreiber, Stuart L. Modulators for regulating autophagy, and therapeutic uses and combinations. PCT Int. Appl. (2008), 159pp. CODEN: PIXXD2 WO 2008122038 A1 20081009 CAN 149:440403 AN 2008:1211287

9. Medower, Christine; Wen, Lian; Johnson, William W. Cytochrome P450 Oxidation of the Thiophene-Containing Anticancer Drug 3-[(Quinolin-4-ylmethyl)-amino]-thiophene-2-carboxylic Acid (4-Trifluoromethoxy-phenyl)-amide to an Electrophilic Intermediate. Chemical Research in Toxicology (2008), 21(8), 1570-1577. CODEN: CRTOEC ISSN:0893-228X. CAN 149:298699 AN 2008:932957

10. Tiollier, Jerome; Sicard, Helene; Bonnafous, Cecile. Improved methods of using phosphoantigen for the treatment of cancer. PCT Int. Appl. (2008), 107pp. CODEN: PIXXD2 WO 2008059052 A1 20080522 CAN 148:577360 AN 2008:614166

11. Liepold, Bernd; Rosenberg, Joerg; Knobloch, Martin; Nehen, Christian. Pharmaceutical dosage form for oral administration of tyrosine kinase inhibitor. PCT Int. Appl. (2008), 28pp. CODEN: PIXXD2 WO 2008055966 A1 20080515 CAN 148:546116 AN 2008:586637

12. Yee, Karen W. L.; Giles, Francis J. Antiangiogenic therapy for hematologic malignancies. Antiangiogenic Cancer Therapy (2008), 655-732. CODEN: 69JTOH CAN 148:78 AN 2007:1039236

13. Maitland, Mardi Gomberg; Ratain, Mark; Garcia, Joe Gn; Maitland, Michael; Moreno, Liliana. Compositions and methods for treating pulmonary hypertension. PCT Int. Appl. (2007), 81 pp. CODEN: PIXXD2 WO 2007087575 A2 20070802 CAN 147:203944 AN 2007:845310

14. Brown, Jeffrey Lester; Emery, Stephen Charles; Blakey, David Charles. Combination of anti-angiopoietin 2 human monoclonal antibody and of VEGF-A, KDR and/or FLT1 antagonist for treating cancer. PCT Int. Appl. (2007), 88 pp. CODEN: PIXXD2 WO 2007068895 A1 20070621 CAN 147:93969 AN 2007:671771

15. Uenaka, Toshimitsu; Yamamoto, Yuji; Matsui, Junji. Method for assaying anti-tumor effect of angiogenesis inhibitor. PCT Int. Appl. (2007), 147pp. CODEN: PIXXD2 WO 2007015578 A1 20070208 CAN 146:221063 AN 2007:150229

16. Owa, Takashi; Ozawa, Yoichi; Semba, Taro. Simultaneous use of sulfonamide-containing compound and angiogenesis inhibitor. PCT Int. Appl. (2006), 270 pp. CODEN: PIXXD2 WO 2006030941 A1 20060323 CAN 144:324798 AN 2006:268466

17. Garton, Andrew J.; Crew, Andrew P. A.; Franklin, Maryland; Cooke, Andrew R.; Wynne, Graham M.; Castaldo, Linda; Kahler, Jennifer; Winski, Shannon L.; Franks, April; Brown, Eric N.; Bittner, Mark A.; Keily, John F.; Briner, Paul; Hidden, Chris; Srebernak, Mary C.; Pirrit, Carrie; O'Connor, Matthew; Chan, Anna; Vulevic, Bojana; Henninger, Dwight; Hart, Karen; Sennello, Regina; Li, An-Hu; Zhang, Tao; Richardson, Frank; Emerson, David L.; Castelhano, Arlindo L.; Arnold, Lee D.; Gibson, Neil W. OSI-930: A novel selective inhibitor of Kit and kinase insert domain receptor tyrosine kinases with antitumor activity in mouse xenograft models. Cancer Research (2006), 66(2), 1015-1024. CODEN: CNREA8 ISSN:0008-5472. CAN 144:100564 AN 2006:55726

18. Petti, Filippo; Thelemann, April; Kahler, Jen; McCormack, Siobhan; Castaldo, Linda; Hunt, Tony; Nuwaysir, Lydia; Zeiske, Lynn; Haack, Herbert; Sullivan, Laura; Garton, Andrew; Haley, John D. Temporal quantitation of mutant Kit tyrosine kinase signaling attenuated by a novel thiophene kinase inhibitor OSI-930. Molecular Cancer Therapeutics (2005), 4(8), 1186-1197. CODEN: MCTOCF ISSN:1535-7163. CAN 143:339119 AN 2005:720263

19. Dihel Larry; Kittleson Christine; Mulvihill Kristen; Johnson William W Oxidative metabolism of the trifluoromethoxy moiety of OSI-930. Drug metabolism and drug interactions (2009), 24(2-4), 95-121. Journal code: 8904736. ISSN:0792-5077. PubMed ID 20408495 AN 2010279470 In-process for

20. Thomson Stuart; Petti Filippo; Sujka-Kwok Izabela; Epstein David; Haley John D Kinase switching in mesenchymal-like non-small cell lung cancer lines contributes to EGFR inhibitor resistance through pathway redundancy. Clinical & experimental metastasis (2008), 25(8), 843-54. Journal code: 8409970. E-ISSN:1473-7276. PubMed ID 18696232 AN 2008767029

21. Medower Christine; Wen Lian; Johnson William W Cytochrome P450 oxidation of the thiophene-containing anticancer drug 3-[(quinolin-4-ylmethyl)-amino]-thiophene-2-carboxylic acid (4-trifluoromethoxy-phenyl)-amide to an electrophilic intermediate. Chemical research in toxicology (2008), 21(8), 1570-7. Journal code: 8807448. E-ISSN:1520-5010. PubMed ID 18672911 AN 2008522497

22. Garton Andrew J; Crew Andrew P A; Franklin Maryland; Cooke Andrew R; Wynne Graham M; Castaldo Linda; Kahler Jennifer; Winski Shannon L; Franks April; Brown Eric N; Bittner Mark A; Keily John F; Briner Paul; Hidden Chris; Srebernak Mary C; Pirrit Carrie; O'Connor Matthew; Chan Anna; Vulevic Bojana; Henninger Dwight; Hart Karen; Sennello Regina; Li An-Hu; Zhang Tao; Richardson Frank; Emerson David L; Castelhano Arlindo L; Arnold Lee D; Gibson Neil W OSI-930: a novel selective inhibitor of Kit and kinase insert domain receptor tyrosine kinases with antitumor activity in mouse xenograft models. Cancer research (2006), 66(2), 1015-24. Journal code: 2984705R. ISSN:0008-5472. PubMed ID 16424037 AN 2006035498

23. Rice Michael C; Bockman Jeffrey Anticancer Drug Discovery and Development - SRI's Seventh Annual Summit. IDrugs : the investigational drugs journal (2005), 8(10), 805-8. Journal code: 100883655. ISSN:1369-7056. PubMed ID 16254797 AN 2005576174

24. Petti Filippo; Thelemann April; Kahler Jen; McCormack Siobhan; Castaldo Linda; Hunt Tony; Nuwaysir Lydia; Zeiske Lynn; Haack Herbert; Sullivan Laura; Garton Andrew; Haley John D Temporal quantitation of mutant Kit tyrosine kinase signaling attenuated by a novel thiophene kinase inhibitor OSI-930. Molecular cancer therapeutics (2005), 4(8), 1186-97. Journal code: 101132535. ISSN:1535-7163. PubMed ID 16093434 AN 2005428008