New HIV Drug Development

Global HIV/AIDS Medicine

Volumn , Issue , 2008, Pages 123-134

  Wit, Ferdinand W N M ^a   Lange, Joep M A ^b   Volberding, Paul A ^c,d  

^a Agendia   (Netherlands)

^b UNIVERSITY OF AMSTERDAM   (Netherlands)

^c UNIVERSITY OF CALIFORNIA   (United States)

^d SAN FRANCISCO VETERANS AFFAIRS MEDICAL CENTER   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

EID: 84884420294     PISSN: None     EISSN: None     Source Type: Book    
DOI: 10.1016/B978-1-4160-2882-6.50016-2     Document Type: Chapter

References (77)

1. Youle M, Arastéh K, Clotet B, et al. Potential barriers and motivators to enfuvirtide use: Physician and patient perspectives of injectable antiretrovirals (ARVs). Program and abstracts of the European AIDS Clinical Society, 10th European AIDS Conference, Dublin, Ireland: 17-20 November 2005;Poster PE73/24.
2. Home R, Clotet R, Cohen C, et al. Treatment-experienced patient perceptions of self-injectable therapy. Program and abstracts of the European AIDS Clinical Society, 10th European AIDS Conference, Dublin, Ireland: 17-20 November 2005;Poster PE73/25.
3. Lazzarin A, Clotet B, Cooper D, et al. TORO 2 Study Group. Efficacy of enfuvirtide in patients infected with drug-resistant HIV-1 in Europe and Australia. N Engl J Med 2003, 348:2186-2195.
4. Lalezari JP, Henry K, O'Hearn M, et al. TORO 1 Study Group. Enfuvirtide, an HIV-1 fusion inhibitor, for drug-resistant HIV infection in North and South America. N Engl J Med. N Engl J Med 2003, 349:1100-2185. [Erratum in:].
5. Katlama C, Berger D, Bellos N, et al. Efficacy of TMC114/r in 3-class experienced patients with limited treatment options: 24-week planned interim analysis of 296-week multinational dose-finding trials. Program and abstracts of the 12th Conference on Retroviruses and Opportunistic Infections, Boston, MA: 22-25 February 2005;Abstract 164LB.
6. Cahn P, Hicks C. 48 Week meta-analyses demonstrate superiority of protease inhibitor (PI) Tipranavir + Ritonavir (TPV/r) over an optimized PI (CPI/r) regimen in antiretroviral (ARV) experienced patients. 10th European AIDS Conference, Dublin, Ireland: 17-20 November 2005;Abstract No. PS 3/8.
7. Jacobson JM, Lowy I, Fletcher CV, et al. Single-dose safety, pharmacology, and antiviral activity of the human immunodeficiency virus (HIV) type 1 entry inhibitor PRO 542 in HIV-infected adults. J Infect Dis 2000, 182:326-329.
8. Jacobson JM, Israel RJ, Lowy I, et al. Treatment of advanced human immunodeficiency virus type 1 disease with the viral entry inhibitor PRO 542. Antimicrob Agents Chemother 2004, 48:423-429.
9. Kuritzkes DR, Jacobson J, Powderly WG, et al. Antiretroviral activity of the anti-CD4 monoclonal antibody TNX-355 in patients infected with HIV type 1. J Infect Dis 2004, 189:286-291.
10. Godofsky E, Zhang X, Sorenson M, et al. In vitro antiretroviral activity of the humanized anti-CD4 monoclonal antibody, TNX-355, against CCR5, CXCR4, and dual-tropic isolates and synergy with enfuvirtide. 45th Interscience Conference on Antimicrobial Agents and Chemotherapy, Washington, DC: 16-29 December 2005;Abstract LB-26.
11. Norris, D, Morales J, Gathe J, et al. TNX-355 in combination with optimized background regimen (OBR) exhibits greater antiviral activity than OBR alone in HIV treatment experienced patients. Program and abstracts of the 45th Interscience Conference of Antimicrobial Agents and Chemotherapy Washington, DC: 16-19 December 2005, Abstract LB 2-26.
12. Hanna G, Lalezari J, Hellinger J, et al. Antiviral activity, safety and tolerability of a novel oral small molecule HIV-1 attachment inhibitor BMS-488043 in HIV-1 infected subjects, 11th Conference on Retroviruses and Opportunistic Infections, San Francisco, CA: 2004;Abstract 141.
13. Lin PF, Ho HT, Gong YF, et al. Characterization of a small molecule HIV-1 attachment inhibitor BMS-488043: virology, resistance and mechanism of action, 11th Conference on Retroviruses and Opportunistic Infections, San Francisco, CA: 2004;Abstract 534.
14. Doms RW, Trono D The plasma membrane as a combat zone in the HIV battlefield. Genes Dev 2000, 14:2677-2688.
15. Scarlatti G, Tresoldi E, Bjorndal A, et al. In vivo evolution of HIV-1 co-receptor usage and sensitivity to chemokine-mediated suppression. Nat Med 1997, 3:1259-1265.
16. Liu R, Paxton WA, Choe S, et al. Homozygous defect in HIV-1 coreceptor accounts for resistance of some multiply-exposed individuals to HIV-1 infection. Cell 1996, 86:367-377.
17. Lederman MM, Veazey RS, Offord R, et al. Prevention of vaginal SHIV transmission in rhesus macaques through inhibition of CCR5. Science 2004, 306:485-487.
18. Hendrix CW. Clinical pharmacokinetics and pharmacodynamics of chemokine inhibitors: implications for rational dosing. Program and abstracts of the 12th Conference on Retroviruses and Opportunistic Infections, Boston, MA: 22-25 February 2005;Abstract 58.
19. Schurmann D, Rouzier R, Nougarede R, et al. SCH-D: Antiviral activity of a CCR5 receptor antagonist, 11th Conference on Retroviruses and Opportunistic Infections, San Francisco, CA: 2004;Abstract 140LB.
20. Peters C, Kawabata T, Syntin P Assessment of immunotoxic potential of maraviroc (UK-427857) in cynomolgus monkeys. Program and abstracts of the 45th Interscience Conference of Antimicrobial Agents and Chemotherapy, Washington, DC: 16-19 December 2005;Abstract H-1100.
21. Walker DK, Abel S, Comby P, et al. Species differences in the disposition of the CCR5 antagonist, UK-427857, a new potential treatment for HIV. Drug Metab Dispos 2005, 33:587-595.
22. Dorr P, Macartney M, Rickett G et al. UK-427857. A novel small molecule HIV entry inhibitor is a specific antagonist of the chemokine receptor CCR5. Program and abstracts of the 10th Conference on Retroviruses and Opportunistic Infections, Boston, MA: 10-14 February 2003;Oral Presentation 12.
23. Westby M, Smith-Burchnell C, Hamilton D, et al. Structurally related HIV co-receptor antagonists bind to similar regions of CCR5 but have differential activities against UK-427857-resistant primary isolates. Program and abstracts of the 12th Conference on Retroviruses and Opportunistic Infections, Boston, MA: 22-25 February 2005;Abstract 96.
24. Westby M, Mori J, Smith-Burchnell C, et al. Maraviroc (UK-427857)-resistant HIV-1 variants, selected by serial passage, are sensitive to CCR5 antagonists and T-20. Antivir Ther 2005, 10:S72.
25. Petropoulos CJ, Huang W, Toma J, et al. Resistance to HIV chemokine receptor antagonists. Program and abstracts of the 12th Conference on Retroviruses and Opportunistic Infections, Boston, MA: 22-25 February 2005;Abstract 59.
26. Fätkenheuer G, Pozniak A, Johnson M, et al. Evaluation of dosing frequency and food effect on viral load reduction during short-term monotherapy with UK-427857 a novel CCR5 antagonist. Program and abstracts of the XV International AIDS Conference, Bangkok, Thailand: 11-16 July 2004;Abstract TuPeB4489.
27. Macartney MJ, Dorr PK, Smith-Burchnell C, et al. In vitro antiviral profile of UK-427857, a novel CCR5 antagonist. Abstracts of the 43rd Annual Interscience Conference on Antimicrobial Agents and Chemotherapy (43rd ICAAC), Chicago, IL: 14-17 September 2003. Abstract H-875.
28. Westby M, Whitcomb J, Huang W, et al. Reversible predominance of CXCR4. Utilising variants in a non-responsive dual tropic patient receiving the CCR5 antagonist UK-427857. 11th Conference on Retroviruses and Opportunistic Infection, San Francisco CA: 8-11 February 2004;Abstract 538.
29. Lewis ME, Van der Ryst E, Youle M, et al. Phylogenetic analysis and co-receptor tropism of HIV-1 envelope sequences from two patients with emergence of CXCR4 using virus following treatment with the CCR5 antagonist UK-427857 Program and abstracts of the 44th Annual ICAAC Meeting, Washington, DC 30 October-2 November, 2004;Abstract H-584b.
30. Sparks S, Adkison K, Shachoy-Clark A, et al. Prolonged duration of CCR5 occupancy by 873140 in HIV-positive subjects. Program and abstracts of the 12th Conference on Retroviruses and Opportunistic Infections, Boston, MA: 22-25 February 2005;Abstract 77.
31. Demarest J, Sparks S, Watson C, et al. Prolonged and unique binding of a novel CCR5 antagonist, 873140. Program and abstracts of the 44th Interscience Conference of Antimicrobial Agents and Chemotherapy, Washington, DC: 30 October-2 November 2004;Abstract H-211.
32. Lalezari J, Thompson M, Kumar P, et al. Antiviral activity and safety of 873140, a novel CCR5 antagonist, during short-term monotherapy in HIV-infected adults. AIDS 2005, 19:1443-1448.
33. Steel HM. Special presentation on aplaviroc-related hepatotoxicity. Program and abstracts of the European AIDS Clinical Society 10th European AIDS Conference, Dublin, Ireland: 17-20 November 2005;Special presentation.
34. Moreno C, Gustot T, Nicaise C, et al. CCR deficiency exacerbates T-cell medicated hepatitis in mice. Hepatology 2005, 42:854-862.
35. Schols D, Claes S, De Clercq E, et al. AMD-3100, a CXCR4 antagonist, reduced HIV viral load and X4 virus levels in humans. Program and abstracts of the 9th Conference on Retroviruses and Opportunistic Infections, Seattle, Washington: 24-28 February 2002;Abstract 2.
36. Schols D, Claes S, Hatse S, et al. Anti-HIV activity profile of AMD070, an orally bioavailable CXCR4 antagonist H. 10th Conference on Retroviruses and Opportunistic Infections, Boston, MA: 2003;Abstract 563.
37. Stone N, Dunaway S, Flexner C, et al. Biologic activity of an orally bioavailable CXCR4 antagonist in human subjects. Program and abstracts of the 5th International Workshop on Clinical Pharmacology of HIV Therapy, Rome, Italy: 1-3 April 2004;Abstract 5.3.
38. Strizki J, Wojcik L, Marozsan A, et al. Properties of in vitro generated HIV-1 variants resistant to the CCR5 antagonists SCH 351125 and SCH 417690. Antivir Ther 2005, 10:566.
39. LaBranche C, Davison D, Ferris R, et al. Studies with 873140, a novel CCR5 antagonist, demonstrate synergy with enfuvirtide and potent inhibition of enfuvirtide-resistant R5-tropic HIV-1. Antivir Ther 2005, 10:S73.
40. Gulick R, Eron J, Bartlett JA, et al. Complete analysis of T-1249-101: safety, pharmacokinetics and antiviral activity of T-1249, a peptide inhibitor of HIV membrane fusion. 42nd Interscience Conference on Antimicrobial Agents and Chemotherapy, San Diego, CA: 2002;Abstract H-1075.
41. Miralles GD, DeMasi R, Sista P, et al. Baseline genotype and prior antiretroviral history do not affect virological response to T-1249. Antivir Ther 2002, 6:S4.
42. Miralles GD, Lalezari JP, Bellos N, et al. T-1249 demonstrates potent antiviral activity over 10 day dosing in most patients who have failed a regimen containing enfuvirtide (ENF): planned interim analysis of T1249-102, a phase I/II study. 10th Conference on Retroviruses and Opportunistic Infections, Boston, MA: 10-14 February 2003;Abstract 14LB.
43. Sista P, Melby T, Dhingra U, et al. The fusion inhibitors T-20 and T-1249 demonstrate potent in vitro antiviral activity against clade B HIV-1 isolates resistant to reverse transcriptase and protease inhibitors and non-B clades. Antivir Ther 2001, 6:S3.
44. Colucci P, Pottage J, Robison H, et al. Program and abstracts of the 45th Interscience Conference on Antimicrobial Agents and Chemotherapy, Washington, DC: 16-19 December 2005;Abstract LB-27.
45. Murphy RL, Schürmann D, Beard A, et al. Tolerance and potent anti-HIV-1 activity of Reverset following 10 days of mono-therapy in treatment-naive individuals. Program and abstracts of the 11th Conference on Retroviruses and Opportunistic Infections, San Francisco, CA: 8-11 February 2004;Abstract 137.
46. Murphy RL, Schurmann D, Beard A, et al. Potent anti-HIV-1 activity of Reverset TM following 10 days of monotherapy in treatment-naive individuals. Program and abstracts of the XV International AIDS Conference, Bangkok, Thailand. 11-16 July 2004;Abstract MoOrB1056.
47. Cohen C, Katlama C, Murphy R, et al. Antiretroviral activity and tolerability of Reverset (Dd4FC), a new fluoro-cytidine nucleoside analog when used in combination therapy in treatment-experienced patients: results of phase IIb study RVT-203. Program and abstracts of the 3rd International AIDS Society Conference on the HIV Pathogenesis and Treatment, Rio de Janeiro, Brazil: 24-27 July 2005;Abstract WeOaLB0103.
48. Bethell R, Adams J, De Muys J, et al. Pharmacological evaluation of a dual deoxycytidine analogue combination: 3TC and SPD754. Program and abstracts of the 11th Conference on Retroviruses and Opportunistic Infections, San Francisco, CA: 8-11 February 2004;Abstract 138.
49. Bethell R, De Rooj E, Smolders K, et al. Comparison of the in vitro mitochondrial toxicity of SPD754 in HepG2 cells with nine other nucleoside reverse transcriptase inhibitors. Program and abstracts of the 44th Interscience Conference of Antimicrobial Agents and Chemotherapy, Washington, DC. 30 October-2 November 2004;Abstract H-207.
50. Cahn P, Lange J, Cassetti I, et al. Anti HIV-1 activity of SPD754, a new NRTI: results of a 10-day monotherapy study in treatment-naive HIV patients. Program and abstracts of the 2nd IAS Conference on HIV Pathogenesis and Treatment, Paris, France: 13-16 July 2003;Abstract LB15.
51. Eron J, Merigan T, Kilby M, et al. Clinical HIV suppression after short-term monotherapy with DAPD. 40th Interscience Conference on Antimicrobial Agents and Chemotherapy, Toronto: 2000;Abstract 690.
52. Gripshover B, Santana J, Ribaudo H, et al. A randomized, placebo-controlled trial of amdoxovir vs placebo with enfuvirtide plus optimized background therapy for HIV-infected subjects failing current therapy (AACTG 5118). Program and abstracts of the 12th Conference on Retroviruses and Opportunistic Infections; 22-25 February 2005; Boston, MA. Abstract 553.
53. Sankatsing SU, Weverling GJ, Peeters M, et al. TMC125 exerts similar initial antiviral potency as a five-drug, triple class Antiretroviral regimen. AIDS 2003, 17:2623-2627.
54. Gazzard B, Pozniak A, Rosenbaum W, et al. An open-label assessment of TMC 125-a new, next-generation NNRTI, for 7 days in HIV-1 infected individuals with NNRTI resistance. AIDS 2003, 17:49-54.
55. Nadler JP, Grossman HA, Hicks C, et al. Efficacy and tolerability of TMC125 in HIV patients with NNRTI and PI resistance at 24 weeks: TMC125-C223. 10th European AIDS Conference/Europe an AIDS Clinical Society, Dublin, Ireland: 2005;Abstract LBPS3/7A.
56. Grossman HA, Hicks C, Nadler, et al. Efficacy and tolerability of TMC125 in HIV patients with NNRTI and H resistance at 24 weeks: TMC125-c223. Program and abstracts of the 45th Interscience Conference of Antimicrobial Agents and Chemotherapy, Washington DC: 16-19 December 2005;Abstract H-416C.
57. de Béthune MP, Andries K, Azijn H. TMC278, a new potent NNRTI, with an increased barrier to resistance and good pharmacokinetic Profile. Program and abstracts of the 12th Conference on Retroviruses and Opportunistic Infections, Boston, MA: 22-25 February 2005;Abstract 556.
58. Goebel F, Yakovlev A, Pozniak A, et al. TMC278: potent anti-HIV activity in Antiretroviral therapy-naive patients. Program and abstracts of the 12th Conference on Retroviruses and Opportunistic Infections, Boston, MA: 22-25 February 2005;Abstract 160.
59. Hernandez J, Amador L, Amantea M, et al. Short-course monotherapy with AG1549, a novel nonnucleoside reverse transcriptase inhibitor (NNRTI), in Antiretroviral naive patients. Program and abstracts of the 7th Conference on Retroviruses and Opportunistic Infections: 30 January-2 February 2000; Abstract 669.
60. Pesano R, Piraino S, Hawley P, et al. 24 week safety, tolerability, and efficacy of capravirine as add-on therapy to nelfinavir and 2 nucleoside reverse transcriptase inhibitors in patients failing a non-nucleoside reverse transcriptase inhibitor-based regimen. Program and abstracts of the 12th Conference on Retroviruses and Opportunistic Infections, Boston, MA: 22-25 February 2005;Abstract 555.
61. Denning J, Kim J, Sanderson B, et al. A double-blind, parallel, randomized, placebo-controlled, single ascending dose study to investigate 695634X and 678248X safety, tolerability and pharmacokinetics following oral administration of 695634G to healthy male subjects (NN210001). Program and abstracts of the XV International AIDS Conference, Bangkok, Thailand: 11-16 July 2004;Abstract TuPeB4480.
62. Romines K, St. Clair M, Hazen R, et al. Antiviral characterization of GW8248, a novel benzophenone non-nucleoside reverse transcriptase inhibitor. Program and abstracts of the 2nd International AIDS Society Conference on HIV Pathogenesis and Treatment, Paris, France: 13-16 July 2003; Abstract 535.
63. Kim Y, Symonds W, Steel H, et al. Safety and pharmacokinetics (PK) of 695634 following repeat oral dose administration to healthy subjects. Program and abstracts of the 44th Interscience Conference on Antimicrobial Agents and Chemotherapy, Washington, DC: 30 October -2 November 2004;Abstract A23.
64. Becker S, Lalezari J, Walworth C, et al. Antiviral activity and safety of GW695634, a novel next generation NNRTI, in NNRTI-resistant HIV-1 infected patients. Program and abstracts of the 3rd International AIDS Society Conference on the HIV Pathogenesis and Treatment, Rio de Janeiro, Brazil: 24-27 July 2005;Abstract WePe62C03.
65. Bonneau P, Robinson P, Duan J, et al. Antiviral characterization and human experience with BILR 355 BS, a novel next-generation non-nucleoside reverse transcriptase inhibitor with a broad anti HIV-1 profile. Program and abstracts of the 12th Conference on Retroviruses and Opportunistic Infections, Boston, MA: 22-25 February 2005;Abstract 558.
66. Coulombe R, Fink D, Landry S, et al. Crystallographic study with BILR 355 BS, a novel nonnucleoside reverse transcriptase inhibitor (NNRTI) with a broad anti HIV-1 profile. Program and abstracts of the 3rd International AIDS Society Conference on the HIV Pathogenesis and Treatment, Rio de Janeiro, Brazil: 24-27 July 2005;Abstract WePp0105.
67. Jochmans D, Kestelyn B, Marchand B, et al. Identification and biochemical characterization of a new class of HIV inhibitors: nucleotide-competing reverse transcriptase inhibitors. Program and abstracts of the 12th Conference on Retroviruses and Opportunistic Infections, Boston, MA: 22-25 February 2005;Abstract 156.
68. Jochmans D, Van Schoubroeck B, Ivens T, et al. ATP enhances the inhibitory effect of NcRTIs (nucleotide-competing RT inhibitors). Antivir Ther 2005, 10:S93.
69. Deval J, Jochmans D, Hertogs K, et al. Mechanistic differences between novel nucleotide-competing reverse transcriptase inhibitors (NcRTIs) and classical chain-terminators. Antivir Ther 2005, 10:S94.
70. Himmel D, Sarafianos S, Clark A, et al. Crystal structure of a complex of HIV-1 reverse transcriptase with an RNase H inhibitor bound at a novel site on the enzyme. Program and abstracts of the 12th Conference on Retroviruses and Opportunistic Infections, Boston, MA: 22-25 February 2005;Abstract 157.
71. Little S, Drusano G, Schooley R, et al. Antiretroviral effect of L-000870810, a novel HIV-1 integrase inhibitor, in HIV-1-infected patients. Program and abstracts of the 12th Conference on Retroviruses and Opportunistic Infections, Boston, MA: 22-25 February 2005;Abstract 161.
72. Morales-Ramirez JO, Teppler H, Kovacs C, et al. Antiretroviral effect of MK-0518, a novel HIV-1 integrase inhibitor, in ART-naive HIV-1 infected patients. Program and abstracts of the European AIDS Clinical Society 10th European AIDS Conference, Dublin, Ireland: 17-20 November 2005;Abstract LBPS1/6.
73. Li F, Goila-Gaur R, Salzwedel K, et al. PA-457: a potent HIV inhibitor that disrupts core condensation by targeting a late step in Gag processing. Proc Natl Acad Sci USA 2003, 100:13555-13560.
74. Beatty G, Lalezari J, Eron J, et al. Safety and antiviral activity of PA-457, the first-in-class maturation inhibitor, in a 10-Day monotherapy study in HIV-1 infected patients. Program and abstracts of the 45th Interscience Conference of Antimicrobial Agents and Chemotherapy, Washington, DC: 16-19 December 2005;Abstract H-416D.
75. Cooper D, Hicks C, Lazzarin A, et al. 24-week RESIST study analyses: the efficacy of tipranavir/ritonavir (TPV/r) is superior to lopinavir/ritonavir LPV/r), and the TPV/r treatment response is enhanced by inclusion of genotypically active antiretrovirals in the optimized background regimen (OBR). Program and abstracts of the 12th Conference on Retroviruses and Opportunistic Infections, Boston, MA: 22-25 February 2005;Abstract 560.
76. Walmsley S, Leith J, Katlama C, et al. pharmacokinetics and safety of tipranavir/ritonavir (TPV/r) alone or in combination with saquinavir (SQV), amprenavir (APV), or lopinavir (LPV): interim analysis of BI1182.51. Program and abstracts of the XV International AIDS Conference, Bangkok, Thailand: 11-16 July 2004; Abstract WeOrB1236.
77. Ward D, Lalezari J, Thompson M et al. Preliminary antiviral activity and safety of 640385/ritonavir in HIV-infected patients (Study HPR10006): an 8-week interim analysis. 45th Annual Interscience Conference on Antimicrobial Agents and Chemotherapy, Washington, DC: 16-19 December 2005;Abstract H-412 (oral).