Pralnacasan Vertex Pharmaceuticals

IDrugs

Volumn 6, Issue 2, 2003, Pages 154-158

  Siegmund, Britta ^a   Zeitz, Martin ^a  

^a CHARITÉ UNIVERSITÄTSMEDIZIN BERLIN   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

ACETYLTYROSYLVALYLALANYLASPARTINE ALDEHYDE; ANTIINFLAMMATORY AGENT; ANTIMETASTATIC AGENT; CORTICOSTEROID; INTERLEUKIN 1BETA CONVERTING ENZYME INHIBITOR; PLACEBO; PRALNACASAN; PRODRUG; PROTEINASE INHIBITOR; UNCLASSIFIED DRUG;

CLINICAL TRIAL; DIARRHEA; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CONTRAINDICATION; DRUG DOSE REGIMEN; DRUG EFFICACY; DRUG METABOLISM; DRUG SAFETY; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TOLERABILITY; DRUG TOXICITY; ENTERITIS; HUMAN; INFLAMMATION; MAXIMUM PERMISSIBLE DOSE; NAUSEA; NONHUMAN; OSTEOARTHRITIS; REVIEW; RHEUMATOID ARTHRITIS; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; AZEPINES; CASPASE 1; CLINICAL TRIALS, PHASE I; CLINICAL TRIALS, PHASE II; HUMANS; ISOQUINOLINES; PROTEASE INHIBITORS; PYRIDAZINES; STRUCTURE-ACTIVITY RELATIONSHIP; TREATMENT OUTCOME;

EID: 0037295235     PISSN: 13697056     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (46)

1. 170247 Vertex Pharmaceuticals Inc: Annual Report 1993. Vertex Pharmaceuticals Inc Annual Report 1993.
2. 188293 Interleukin-1β converting enzyme as an anti-inflammatory agent. Livingston D World Congr Inflamm 1995 2 Symposium 9 Talk 307
3. 237775 Structure based design of non-peptidic inhibitors of interleukin-1β converting enzyme (ICE). Mullican MD, Golec JMC, Kay DP, Jones SD, Murcko MA, Bemis G, Wilson K, Murdoch R, Harbeson S, Nyce P, Raybuck S et al Winter Conf Med Bioorganic Chem Steamboat Springs, CO, USA, January Structural and kinetic studies of human ICE.
4. 244862 Activation of interferon-γ inducing factor mediated by interleukin-1β converting enzyme. Gu Y, Kuida K, Tsutsui H, Ku G, Hsiao K, Fleming MA, Hayashi N, Higashino K, Okamura H, Nakanishi K, Kurimoto M et al Science 1997 275 5297 206-209 First description of ICE as a required protease for IL-18 activation.
5. 257441 Vertex acquires patent portfolio from Sanofi SA claiming inhibitors of IL-β converting enzyme. Vertex Pharmaceuticals Inc Press Release 1997 July 30
6. 260301 Severity and mortality of experimental pancreatitis are dependent on interleukin-1 converting enzyme (ICE). Norman J, Yang J, Fink G, Carter G, Ku G, Denham W, Livingston D J Interferon Cytokine Res 1997 17 2 113-118
7. 273064 Vertex earns $3.0 million milestone payment from Hoechst Marion Roussel for progress in ICE program for the treatment of inflammation. Vertex Pharmaceuticals Inc Press Release 1997 December 22
8. 288347 Expression of interleukin 1β and interleukin 1β converting enzyme by intestinal macrophages in health and inflammatory bowel disease. McAlindon ME, Hawkey CJ, Mahida YR 1998 42 2 214-219
9. 302985 Vertex and Hoechst Marion Roussel announce start of clinical trial with HMR-3480/VX-740, a novel compound for treatment of inflammatory diseases. Vertex Pharmaceuticals Inc Press Release 1998 October 29
10. 306496 Inflammation Research Association - Ninth International Conference (Part II), Hershey, PA, USA. IDDB Meeting Report 1998 Nov 1-5
11. 338587 Hoechst Marion Roussel and Vertex expand agreement to develop novel anti-inflammatory compounds. Vertex Pharmaceuticals Inc Press Release 1999 September 01
12. 351501 Pipeline products, phase I, II, III. Aventis Pharma AG Company World Wide Website 1999 December 23
13. 401955 Drug development pipeline. Vertex Pharmaceuticals Inc Company Communication 2001 March 09
14. 409257 Aventis Pharma R&D Day, London, May 15, 2001. Aventis Pharma AG Company Presentation 2001 May 15
15. 427421 Vertex Pharmaceuticals - Pipeline and products. Vertex Pharmaceuticals Inc Company Communication 2001 October 30
16. 429641 R&D day 2001 conclusion. Aventis Pharma AG Company Presentation 2001 May 14
17. 435164 Vertex Pharmaceuticals provides corporate update and outlook for 2002. Vertex Pharmaceuticals Inc Press Release 2002 January 08
18. 440299 FY 2001 analyst conference. Aventis Pharma AG Company Presentation 2002 February 13
19. 449230 Aventis Pharma and Vertex Pharmaceuticals to expand development of pralnacasan, oral cytokine inhibitor for inflammatory diseases. Aventis Pharma SA Press Release 2002 April 24
20. 450049 Advances in Anti-Arthritic Agents - SMi's Third Annual Conference (Part I), London, UK. Norman P IDDB Meeting Report 2002 April 23-24
21. 450735 Deutsche Bank Health Care Conference 2002. Aventis Pharma AG Company Presentation 2002 May 08
22. 451847 The ICE inhibitor, pralnacasan, reduces DSS-induced murine colitis and Th1-cell activation. Bauer C, Loher F, Schmall K, Hallwachs R, Leohr C, Siegmund B et al Gastroenterology 2002 122 (Suppl 1) Abs T971 Describes the efficacy of pralnacasan in DSS-induced colitis in mice.
23. 453094 Vertex Pharmaceuticals: Product pipeline. Vertex Pharmaceuticals Inc Company World Wide Website 2002 May 15
24. 495054 Seven potential blockbusters by 2006: Pipeline progress to help deliver sustainable growth. Aventis Pharma AG Press Release 2002 June 18
25. 458521 Vertex Pharmaceuticals reports second quarter and first half 2002 financial results. Vertex Pharmaceuticals Inc Press Release 2002 July 19
26. 460724 Drug Discovery Technology 2002 (Part V) - OVERNIGHT REPORT, Boston, MA, USA. Mongin-Bulewski C IDDB Meeting Report 2002 Aug 4-9
27. 468335 Phase IIa clinical trial results for pralnacasan in rheumatoid arthritis presented at ACR. October 29 Vertex Pharmaceuticals Inc Press Release 2002
28. 468962 Interleukin-1β converting enzyme (caspase-1) in intestinal inflammation. Biochem Pharmacol 2002 64 1 1-8 Review on the possible role of ICE in intestinal inflammation.
29. 468965 ICE/Caspase-1 inhibitors as novel anti-inflammatory drugs. Randle JC, Harding MW, Ku G, Schonharting M, Kurrle R Expert Opin Investig Drugs 2001 10 7 1207-1209 Short review on ICE inhibitors and the current status of clinical development.
30. 470328 American College of Rheumatology - 66th Annual Scientific Meeting, New Orleans, LA, USA. Sylvester B IDDB Meeting Report 2002 October 25-29
31. 470529 Vertex Pharmaceuticals provides update on progress toward pipeline and corporate objectives at Fourth Annual Investor Day. Vertex Pharmaceuticals Inc Press Release 2002 November 12
32. 472044 A novel heterodimeric cysteine protease is required for interleukin-1β processing in monocytes. Thornberry NA, Bull HG, Calaycay JR, Chapman KT, Howard AD, Kostura MJ, Miller DK, Molineuax SM,, Weidner JR, Auning J et al. Nature 1992 356 6372 768-774 Identification of ICE.
33. 472045 Structure and mechanism of interleukin-1β converting enzyme. Wilson KP, Black JA, Thomson JA, Kim EE, Griffith JP, Navia MA, Murcko MA, Chambers SP, Aldape RA, Raybuck SA et al. Nature 1994 370 6487 270-275 Description of the structure of ICE and the basis for drug targeting.
34. 472046 Interleukin-18 and interleukin-1β: Two cytokine substrates for ICE (caspase-1). Fantuzzi G, Dinarello CA J Clin Immunol 1999 19 1 1-11
35. 472047 Interleukin-18 regulation of interferon-γ production and cell proliferation as shown in interleukin-1β-converting enzyme (caspase-1)-deficient mice. Fantuzzi G, Puren AJ, Harding MW, Livingston DJ, Dinarello CA Blood 1998 91 6 2118-2125
36. 472048 Neutralization of IL-18 reduces neutrophil tissue accumulation and protects mice against lethal Escherichia coli and Salmonella typhimurium endotoxemia. Netea MG, Fantuzzi G, Kullberg BJ, Stuyt RJ, Pulido EJ, McIntyre RC Jr, Joosten LA, Van Der Meer JW, Dinarello CA J Immunol 2000 164 5 2644-2649
37. 472049 Bioactive IL-18 expression is up-regulated in Crohn's disease. Monteleone G, Trapasso F, Parello T, Biancone L, Stella A, Luliano R, Luzza F, Fusco A, Pallone F J Immunol 1999 163 1 143-147
38. 472051 IL-18, a novel immunoregulatory cytokine, is up-regulated in Crohn's disease: Expression and localization in intestinal mucosal cells. Pizarro TT, Michie MH, Bentz M, Woraratanadharm J, Smith MF Jr, Foley E, Moskaluk CA, Bickston SJ, Cominelli F J Immunol 1999 162 11 6829-6835
39. 472052 IL-1β-converting enzyme (caspase-1) in intestinal inflammation. Siegmund B, Lehr HA, Fantuzzi G, Dinarello CA Proc Natl Acad Sci USA 2001 98 23 13249-13254
40. 472054 Neutralization of interleukin-18 reduces severity in murine colitis and intestinal IFN-γ and TNF-α production. Siegmund B, Fantuzzi G, Rieder F, Gamboni-Robertson F, Lehr HA, Hartmann G, Dinarello CA, Endres S, Eigler A Am J Physiol - Regulat Integrat Comparat Physiol
41. 472058 Macrophage-derived IL-18-mediated intestinal inflammation in the murine model of Chron's disease. Kanai T, Watanabe M, Okazawa A, Sato T, Yamazaki M, Okamoto S, Ishii H, Totsuka T, Liyama R, Okamoto R, Ikeda M et al. Gastroenterology 2001 121 4 875-888
42. 472060 Blockade of endogenous IL-18 ameliorates TNBS-induced colitis by decreasing local TNF-α production in mice. Ten Hove T, Corbaz A, Amitai H, Aloni S, Belzer I, Graber P, Drillenburg P, Van Deventer SJ, Chvatchko Y, Te Velde AA Gastroenterology 2001 121 6 1372-1379
43. 472061 Treatment of T cell-dependent experimental colitis in SCID mice by local administration of an adenovirus expressing IL-18 antisense mRNA. Wirtz S, Becker C, Blumberg R, Galle PR, Neurath MF J Immunol 2002 168 1 411-420
44. 472063 Differential effects of caspase-1/interleukin-1β-converting enzyme on acinar cell necrosis and apoptosis in severe acute experimental pancreatitis. Rau B, Paszkowski A, Lillich S, Baumgart K, Moller P, Beger HG Lab Invest 2001 87 7 1001-1013
45. 472064 IL-18 regulates IL-1β-dependent hepatic melanoma metastasis via vascular cell adhesion molecule-1. Vidal-Vanaclocha F, Fantuzzi G, Mendoza L, Fuentes AM, Anasagasti MJ, Martin J, Carrascal T, Walsh P, Reznikov LL, Sim SH, Novick D Proc Natl Acad Sci USA 2000 97 2 734-739
46. 474260 Selective interleukin-1 converting enzyme (ICE/Caspase-1) inhibition with pralnacasan (HMR 3480/VX-740) reduces inflammation and joint destruction in murine type II collagen-induced arthritis (CIA). Ku G, Ford BS, Raybuck SA, Harding MW, Randle JCR Am Coll Rheumatol 2001 November 12-15 Absr 1134 Describes the dose-dependent efficacy of pralnacasan in experimental collagen-induced arthritis in mice.