TMC-114 (Tibotec)

Current Opinion in Investigational Drugs

Volumn 5, Issue 8, 2004, Pages 879-886

  Shurtleff, Amy C ^a  

^a UNITED STATES ARMY MEDICAL RESEARCH INSTITUTE OF INFECTIOUS DISEASES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; DARUNAVIR; SULFONAMIDE;

CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; HUMAN; PATENT; PHASE 1 CLINICAL TRIAL; PHASE 2 CLINICAL TRIAL; RANDOMIZED CONTROLLED TRIAL; REVIEW; STRUCTURE ACTIVITY RELATION;

ANTI-HIV AGENTS; CLINICAL TRIALS, PHASE I; CLINICAL TRIALS, PHASE II; HUMANS; PATENTS; RANDOMIZED CONTROLLED TRIALS; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES;

EID: 16644386448     PISSN: 14724472     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (41)

1. 122181 3-Tetrahydrofuran and pyran urethanes as high-affinity P-2ligands for HIV-1 protease inhibitors. Ghosh AK, Thompson WJ, McKee SP, Duong TT, Lyle TA, Chen JC, Darke PL, Zugay JA, Emini EA, Schleif WA et al J MED CHEM 1993 36 2 292-294
2. 133378 Cyclic sulfolanes as novel and high affinity P2 ligands for HIV-1 protease inhibitors. Ghosh AK, Thompson WJ, Lee HY, McKee SP, Munson PM, Duong TT, Darke PL, Zugay JA, Emini EA, Schleif WA et al J MED CHEM 1993 36 7 924-927
3. 159728 Selection of multiple human immunodeficiency virus type 1 variants that encode viral proteases with decreased sensitivity to an inhibitor of the viral protease. Kaplan AH, Michael SF, Wehbie RS, Knigge MF, Paul DA, Everitt L, Kempf DJ, Norbeck DW, Erickson JW, Swanstrom R PROC NATL ACAD SCI USA 1994 91 12 5597-5601
4. 162397 Characterization of human immunodeficiency virus type 1 variants with increased resistance to a C2-symmetric protease inhibitor. Ho DD, Toyoshima T, Mo H, Kempf DJ, Norbeck D, Chen CM, Wideburg NE, Burt SK, Erickson JW, Singh MK J VIROL 1994 68 3 2016-2020
5. 171227 Cyclic sulfone-3-carboxamides as novel P-2 ligands for Ro-318959 based HIV-1 protease inhibitors. Ghosh AK, Thompson WJ, Munson PM, Liu W, Huff JR BIOORG MED CHEM LETT 1995 5 1 83-88
6. 203734 In vivo emergence of HIV-1 variants resistant to multiple protease inhibitors. Condra JH, Schleif WA, Blahy OM, Gabryelski LJ, Graham DJ, Quintero JC, Rhodes A, Robbins HL, Roth E, Shivaprakash M et al NATURE 1995 374 6522 569-571
7. 235348 Drug-resistance patterns of saquinavir and other HIV proteinase inhibitors. Roberts NA AIDS 1995 9 Suppl 2 S27-S32
8. 349754 Relative potency of protease inhibitors in monocytes/ macrophages acutely and chronically infected with human immunodeficiency virus. Perno CF, Newcomb FM, Davis DA, Aquaro S, Humphrey RW, Calio R, Yarchoan R J INFECT DIS 1998 178 2 413-422
9. 400965 Clinical Implications of HIV Drug Resistance - Third European Symposium, Frankfurt, Germany. Boriskin Y IDDB MEETING REPORT 2001 February 23-25
10. 404924 Antiviral Research 14th International Conference - OVERNIGHT REPORT, Satellite Symposium, Seattle, WA, USA. Muhsin M IDDB MEETING REPORT 2001 April 8-12
11. 406988 Summary of the Antiviral Research 14th International Conference, Seattle, WA, USA. Croasdell G IDDB MEETING REPORT 2001 April 8-12
12. 434093 Interscience Conference on Antimicrobial Agents and Chemotherapy - 41st Meeting (Part VI) - OVERNIGHT REPORT, Poster Presentation, Chicago, IL, USA. Garvey R IDDB MEETING REPORT 2001 December 16-19
13. 441792 TMC-125 shows antiviral effect in patients failing HIV therapy. Tibotec-Virco NV PRESS RELEASE 2002 February 28
14. 445845 Antiviral Research - 15th International Conference (Part V), Prague, Czech Republic. Este JA IDDB MEETING REPORT 2002 March 17-21
15. 448283 Influence of binding to human plasma proteins by protease inhibitors may be overestimated in current IQ models. de Bethune MP, Xie D, Azijn H, Wigerinck P, Hoetelmans R, Pauwels R INT CONF RETROVIRUSES OPPORTUNISTIC INFECT 2002 9 Abs 449-W
16. 465743 Interscience Conference on Antimicrobial Agents and Chemotherapy - 42nd Meeting (Part VII), San Diego, CA, USA. Mackay J IDDB MEETING REPORT 2002 September 27-30
17. 478825 Next-generation PI, TMC114, shows promising antiviral activity in patients failing HIV therapy. Tibotec Pharmaceuticals Ltd PRESS RELEASE 2003 February 14
18. 479516 Retroviruses and Opportunistic Infections - Tenth Conference (Part I), Boston, MA, USA. Este JA IDDB MEETING REPORT 2003 February 10-14
19. 479770 Retroviruses and Opportunistic Infections - Tenth Conference, Boston, MA, USA. Susman E IDDB MEETING REPORT 2003 February 10-14
20. 484782 Overcoming drug resistance in HIV-1 chemotherapy: The binding thermodynamics of amprenavir and TMC-126 to wild-type and drugresistant mutants of the HIV-1 protease. Ohtaka H, Velazquez-Campoy A, Xie D, Freire E PROTEIN SCI 2002 11 8 1908-1916
21. 484791 Antiviral activity of UIC-PI, a novel inhibitor of the human immunodeficiency virus type 1 protease. Ghosh AK, Pretzer E, Cho H, Hussain KA, Duzgunes N ANTIVIRAL RES 2002 54 1 29-36
22. 484793 Safety, tolerability and pharmacokinetics of escalating single oral doses of TMC114, a novel protease inhibitor (PI) highly active against HIV-1 variants resistant to other PIs. Van Der Geest R, van der Sandt I, Gille D, Groen K, Tritsmans L, Stoffels P ICAAC 2001 41 Abs 347
23. 505286 Proteinase Inhibitors - Second International Industry Conference, From Hits to Leads to Drugs, Zurich, Switzerland. Nestler H P IDDB MEETING REPORT 2003 September 3-4
24. 506518 Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro. Koh Y, Nakata H, Maeda K, Ogata H, Bilcer G, Devasamudram T, Kincaid JF, Boross P, Wang YF, Tie Y, Volarath P ANTIMICROB AGENTS CHEMOTHER 2003 47 10 3123-3129
25. 524484 Retroviruses and Opportunistic Infections - 11th Annual Conference, San Francisco, California, USA. Susman E IDDB MEETING REPORT 2004 February 8-12
26. 533219 Potent HIV protease inhibitors incorporating high-affinity P2-ligands and (R)-(hydroxyethylamino)sulfonamide isotere. Ghosh AK, Kincaid JF, Cho W, Walters DE, Krishnan K, Hussain KA, Koo Y, Cho H, Ruddall C, Holland L, Buthod J BIOORG MED CHEM LETT 1998 8 6 687-690
27. 533449 TMC114, a next generation HIV protease inhibitor: Pharmacokinetics and safety following oral administration of multiple doses with and without low doses of ritonavir in healthy volunteers. Hoetelmans R, Van der Sandt I, De Pauw M, Struble K, Peeters M, Van der Geest R INT CONF RETROVIRUSES OPPORTUNISTIC INFECT 2003 10 Abs 549
28. 533484 First clinical results on antiretroviral activity, pharmacokinetics and safety of TMC114, an HIV-1 protease inhibitor, in multiple PI-experienced patients. Arasteh K, Clumeck N, Pozniak A, Jaeger H, De Pauw M, Muller H, Peeters M, Hoetelmanns R, De Meyer S, van der Sandt I, Comhaire S, van der Geest R INT CONF RETROVIRUSES OPPORTUNISTIC INFECT 2003 10 Abs 8
29. 533673 High resolution crystal structures of HIV-1 protease with a potent non-peptide inhibitor (UIC-94017) active against multi-drug-resistant clinical strains. Tie Y, Boross PI, Wang YF, Gaddis L, Hussain AK, Leshchenko S, Ghosh AK, Louis JM, Harrison RW, Weber IT J MOL BIOL 2004 338 2 341-352
30. 533674 Antiviral activity of TMC114, a potent next-generation protease inhibitor, against more than 4000 recent recombinant clinical isolates exhibiting a wide range of (protease inhibitor) resistance profiles. De Meyer S, Van Marck H, Veldeman J, McKenna P, Pauwels R, de Bethune MP ANTIVIRAL THER 2003 8 3 S20
31. 533675 TMC114 binds within the substrate envelope of HIV-1 protease, which could account for its efficacy against multi-protease inhibitorresistant virus. King N, Prabu Jeyabalan M, Wigerinck P, de Bethune MP, Schiffer CA ANTIVIRAL THER 2003 8 3 S19
32. 533676 TMC114, a potent next-generation protease inhibitor: Characterization of antiviral activity in multiple protease inhibitorexperienced patients participating in a phase IIa study. De Meyer S, Peeters M, Jordens C, McKenna P, van der Geest R, Pauwels R, de Bethune MP ANTIVIRAL THER 2003 8 3 S18
33. 541109 HIV-1 protease inhibitors in development. Rusconi S, Cactmancio S EXPERT OPIN INVESTIG DRUGS 2002 11 3 387-395
34. 544496 TMC114 (UIC96017): A novel nonpeptidic protease inhibitor potent against multi-PI resistant HIV in vitro. Koh N, Maeda K, Bilcer T, Ghosh M INT CONF RETROVIRUSES OPPORTUNISTIC INFECT 2003 10 Abs 553
35. 544732 TMC114, a high potent protease inhibitor (PI) with an excellent profile against HIV variants highly resistant to current PIs. de Bethune MP, Wigerinck P, Jonckheere H, Tahri A, Maes L, Pauwels R, Erickson J ICAAC 2001 41 Abs 1677
36. 544946 Molecular basis of HIV-1 protease drug resistance: Structural analysis of mutant proteases complexed with cyclic urea inhibitors. Ala PJ, Huston EE, Klabe RM, McCabe DD, Duke JL, Rizzo CJ, Korant BD, DeLoskey RJ, Lam PY, Hodge CN, Chang CH BIOCHEMISTRY 1997 36 7 1573-1580
37. 544950 Crystal structures of complexes of a peptidic inhibitor with wildtype and two mutant HIV-1 proteases. Hong L, Treharne A, Hartsuck JA, Foundling S, Tang J BIOCHEMISTRY 1996 35 33 10627-10633
38. 544952 Thermodynamic basis of resistance to HIV-1 protease inhibition: Calorimetric analysis of the V82F/I84V active site resistant mutant. Todd MJ, Luque I, Velazquez-Campoy A, Freire E BIOCHEMISTRY 2000 39 39 11876-11883
39. 544956 The development of cyclic sulfolanes as novel and high-affinity P2 ligands for HIV-1 protease inhibitors. Ghosh AK, Lee HY, Thompson WJ, Culberson C, Holloway MK, McKee SP, Munson PM, Duong TT, Smith AM, Darke PL et al J MED CHEM 1994 37 8 1177-1188
40. 544957 Structure-based design of HIV-1 protease inhibitors: Replacement of two amides and a 10 pi-aromatic system by a fused bistetrahydrofuran. Ghosh AK, Thompson WJ, Fitzgerald PM, Culberson JC, Axel MG, McKee SP, Huff JR, Anderson PS J MED CHEM 1994 37 16 2506-2508
41. 546531 A potent human immunodeficiency virus type 1 protease inhibitor, UIC-94003 (TMC-126), and selection of a novel (A28S) mutation in the protease active site. Yoshimura K, Kato R, Kavlick MF, Nguyen A, Maroun V, Maeda K, Hussain KA, Ghosh AK, Gulnik SV, Erickson JW, Mitsuya H J VIROL 2002 76 3 1349-1359