Nelfinavir mesylate

Expert Opinion on Pharmacotherapy

Volumn 1, Issue 7, 2000, Pages 1429-1440

  Tebas, Pablo ^a   Powderly, William G ^a  

^a WASHINGTON UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

Antiretroviral therapy; HIV; Nelfinavir; Protease inhibitors

Indexed keywords

NELFINAVIR; PROTEINASE INHIBITOR;

DRUG COMBINATION; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; PHASE 1 CLINICAL TRIAL; PHASE 2 CLINICAL TRIAL; PHASE 3 CLINICAL TRIAL; REVIEW; VIROLOGY;

CLINICAL TRIALS, PHASE I; CLINICAL TRIALS, PHASE II; CLINICAL TRIALS, PHASE III; DRUG COMBINATIONS; HIV INFECTIONS; HIV PROTEASE INHIBITORS; HUMANS; NELFINAVIR;

EID: 0034568957     PISSN: 14656566     EISSN: None     Source Type: Journal    
DOI: 10.1517/14656566.1.7.1429     Document Type: Article

References (50)

1. PALELLA FJ, Jr., DELANEY KM, MOORMAN AC et ah. Declining morbidity and mortality among patients with advanced human immunodeficiency virus infection. HIV Out-patient Study Investigators. N. Engl. J. Med. (1998) 338:853-860. Excellent summary of the profound impact of Pis in the outcome of HIV infection.
2. ANONYMOUS: Update: trends in AIDS incidence United States, 1996. MMWR - Morbidity & Mortality Weekly Report (1997) 46:801-867.
3. CARPENTER CCJ, COOPER DA, FISCHL MA et al.: Antiretroviral therapy in adults - Updated recommendations of the International AIDS Society - USA PaneL JAMA (2000) 283:381-390.
4. SAFRIN S, GRUNFELD C: Fat distribution and metabolic changes in patients with HIV infection. AIDS (1999) 13:2493-2505. The best summary of the metabolic complications associated with antiretroviral treatment. Good summary and complete references.
5. CARR A, MILLER J, LAW M, COOPER DA: A syndrome of lipoatrophy, lactic acidaemia and liver dysfunction associated with HIV nucleoside analogue therapy: contribution to protease inhibitor-related lipodystrophy syndrome. ATOS(2000) 14:F25-F32.
6. TEBAS P, POWDERLY WG, CLAXTON S et ah. Accelerated bone mineral loss in HIV-infected patients receiving potent antiretroviral therapy. AIDS (2000) 14:F63-F67. A new complication of antiretroviral treatment.
7. ROBERTS NA, MARTIN JA, KINCHINGTON D et al.-. Rational design of pcptidc-based HIV proteinase inhibitors. Science (1990) 248:358-361.
8. GEHLHAAR DK, VERKHIVKER GM, REJTO PA et al.: Molecular recognition of the inhibitor AG-1343 by HIV-1 protease: conformationally flexible docking by evolutionary programming. Chcm. Biol. (1995) 2:317-32-4.
9. SHETTY BV, KOSA MB, KHALIL DA, WEBBER S: Preclinical pharmacokinetics and distribution to tissue of AG1343, an inhibitor of human immunodeficiency virus type 1 protease. Antlmicrob. Agents Chcmother. (1996) 40:110-114.
10. KALDOR SW, KALISH VJ, DAVIES JF et al.: Viracept (Nelfinavir Mesylate, AG1343) - a potent, orally bioavailable inhibitor of HIV-1 protease.J. Med. Chcm. (1997) 40:3979-3985.
11. QUART BD, CHAPMAN SK, PETERKIN J, WEBBER S, OLIVER S: Phase I safety, tolerance, pharmacokinetics and food effect studies of AG1343 - a novel protease inhibitor. Natl. Conf. Hum. Retroiintscs Relat. Infect. (1995) 167:2.
12. KERR B, LEE C, YUEN G étal.: Overview of in vitro and/ i7ro drug interaction studies of nclfinavir mesylate (NFV), a new HIV-1 protease inhibitor. 4th Conference on Retrovirus and Opportunistic Infections. (1997) 133.
13. ZHANG K, WU E, PATICK A et al.: Plasma metabolites of nelfinavir, a potent HIV protease inhibitor, in HIV positive patients: quantitatlon by LC-MS/MS and antiviral activities. 6th European ISSX Meeting. Gothenburg, (June 30 -July 3 1997). Abstract no. 128.
14. Viracept (nelfinavir mesylate): Prescribing information. Agouron Pharmaceuticals Inc., La Jolla, CA, USA (1999).
15. MASERATI R, VILLANI P, SEMINARI E, PAN A, LO CAPUTO S, REGAZZI MB: High plasma levels of nelfinavir and efavirenz in two HIV-positive patients -with hepatic disease. AIDS (.1999) 13:870-871.
16. MCCANCE-KATZ EF, FARBER S, SELWYN PA, O'CONNOR A: Decrease in mcthadone levels with nelfinavir mesylate. Am.]. Psychiatry (2000) 157:481.
17. SAAH A, RIDDLER S, HAVLIR DV etal.: Co-administration of indinavir and nelfinavir: pharmacokinetics, tolerability, antiviral activity and preliminary viral resistance. 12lh World AIDS Conference. Geneva, Switzerland (June 28 -July 3 1998). Abstract no. 22352.
18. KROGSTAD P, KERR B, ANDERSON R etal.: Phase I Study of the HIV-Protease Inhibitor Nelfinavir Mesylate (NFV) in HW+ Children. 4th Conference on Retrovinis and Opportunistic Infections. Washington DC, USA (January 23 - 26 1997).
19. STARR SE, FLETCHER CV, SPECTOR SA et al.: Combination therapy with efavirenz, nelfinavir and nucleoside reverse-transcriptase inhibitors in children infected with human immunodeficiency virus Type 1. Pédiatrie AIDS Clinical Trials Group 382 Team. A'. Engl. J. Med. (1999)341:1874-1881. The largest trial of nelfinavir use in children.
20. MARKOWITZ M, CONANT M, HURLEY A et al.: A preliminary evaluation of nelfinavir mesylate, an inhibitor of human immunodeficiency virus (HTV)-1 protease, to treat HIV infection.J. Infect. Dis. (1998) 177:1533-1540.
21. GATHE J, BURKHARDT B, HAWLEY P, CONANT M, PETERKIN J, CHAPMAN S: A randomized phase n study of Viracept, a novel HIV protease inhibitor, used in combination with stavudine vs. stavudine alone. Program and Abstracts of the XI International Conference on AIDS. Vancouver, British Columbia (July 7-12 1996).
22. MARKOWITZ M, CAO Y, HURLEY A, O'DONOVAN R, HO D: Triple therapy with nelfinavir (Viracept) in combination with AZT and 3TC in 12 antiviral-naive subjects chronically infected with HIV-1. llth International Conference on AIDS. Vancouver, British Columbia (1997).
23. HENRY K, LAMARCA A, MYERS R, CHAPMAN S: The safety of VIRACEPT (nelfinavir mesylate, NFV) in pivotal Phase II/III double-blind randomized controlled trials as monotherapy and in combination with either d4T or AZT/3TC. 4th Conference on Retmvinis and Opportunistic Infections. (1997) 108.
24. POWDERLY W, SENSION M, CONANT M, STEIN A, CLENDENINN N: The efficacy of viracept (nelfinavir mesylate) in pivotal phase n/in double-blind randomized controlled trials as monotherapy and in combination with d4T or AZT/3TC. 4th Conference on Retrovinis and Opportunistic Infections. Washington DC, USA (January23 - 26, 1997).
25. GULICK RM, MELLORS JW, HAVLIR D et al.-. Simultaneous vs. sequential initiation of therapy with Indinavir, zidovudine and lamivudine for HIV-1 infection: 100-week follow-up. JAMA (1998) 280:351.
26. POWDERLY VG, SAAG MS, CHAPMAN S, YU G, QUART B, CLENDENINN NJ: Predictors of optimal virological response to potent antiretroviral therapy. AIDS (.1999) 13:1873-1880. The only article published so far from AG-511, the pivotal trial that led to the approval of nelfinavir.
27. PETERSEN A, JOHNSON M: Long-term comparison of b.i.d. and t.i.d. dosing Viracept (nelfinavir) in combination with stavudine (d4T) and lamivudine (3TC) in HIV patients. 12lh International Conference on AIDS. Geneva, Switzerland (1998). Abstract no. 12224
28. JOHNSON M, NELSON M, PETERS B et al.: A comparison of b.i.d. and t.Ld. dosing of nelfinavir mesylate when given in combination with stavudine (d4T) and lamivudine (3TC) for up to 48 weeks. 38th Interscience Conference on Antimicrobial Agents and Chemotherapy. San Diego, USA (September 24 - 27 1998).
29. CLUMECK N: AVANTI 3, A randomised, double-blind, comparative trial to evaluate the efficacy, safety and tolerance of AZT/3TC vs. AZT/3TC/nelfinavir in antiretroviral naive patients. 5th Conference on Retrovinis and Opportunistic Infections. Chicago, IL, USA (1998).
30. ALBRECHT M, KATZENSTEIN D, BOSCH R, LIOU S, HANLMER S: ACTC 364-nelfinavir and/or efavirenz in combination with new NRTIs in nucleoside experienced subjects: week-48 ultrasensitive HIV RNA results. 7th Conference on Rctroiintses and Opportunistic Infections. San Francisco, CA, USA (January 30 - February 2 2000).
31. EYSTER E, JEMSEKJ, KAGAN S et ah. Initial effectiveness and tolerability of nelfinavir in combination with efavirenz (Sustiva, DMP 266) in antiretroviral therapy naïve or nucleo-side analogue experienced HIV-1 infected patients: characterization in a Phase II, open-label, multicenter study at 24 weeks (Study DMP 266-024). 12th World AIDS Conference. Geneva, Switzerland (June 28 -July 3 1998). Abstract no. 22386.
32. GATELL J, KURITZKES D, GREEN S et al.-. Twice daüy dosing of delavirdine (DLV) in combination with nelfinavir (NFV), didatiosinc (ddl) and stavudine (d4T) results in significant decreases in viral burden. 39th Interscience Conference on Antimicrobial Agents and Chemotherapy. San Francisco, CA, USA (September 26 - 29 1999).
33. MOYLE G, ON BEHALF OF THE SPICE STUDY TEAM: Study of protease inhibitor (PI) combination in Europe (SPICE): soft galatin capsule (SQV-SGC) plus nelfinavir (NFV) in HIV-infected individuals. 12th World AIDS Conference. (June 18 -July 3 1998).
34. MOYLE G, POZNIAK A, OPRAVIL M et al.: The SPICE study: 48-week activity of combinations of saquinavir soft gelatin and nelfinavir with and without nucleoside analogues.J.Acquired Immune Deficiency Syndromes (2000) 23:128-137.
35. GALLANT J, HEALTH-CHIOZZI M, ANDERSON R, FIELDS C, FLEXNER C: Phase n study of ritonavir-nelfinavir combination therapy: an update. 12th International Conference on AIDS. Geneva, Switzerland (1998). Abstract no. 12207.
36. ROCA B, GOMEZ CJ, ARNEDO A: A randomized, comparative study of lamivudine plus stavudine, with indinavir or nelfinavir, in treatment-experienced HIV-infected patients. AJDS(.2000) 14:157-161.
37. PODZAMCZER D, FERRER E, CONSIGUO E et al.: Preliminary results of a randomized multicenter study comparing combivir (2DV/3TC) plus nelfinavir or nevirapine in HIV-infected naive patients (COMBINE study). 7th Conference on Rctroviniscs and Opportunistic Infections. San Francisco, CA, USA (January 30 - February 2 2000). Abstract 510.
38. STASZEWSKi S, MORALES-RAMIREZ J, TASHIMA KT ct a!.: Efavirenz plus zidovudine and lamivudine, efavirenz plus Indinavir and indinavir plus zidovudine and lamivudine in the treatment of HIV-1 infection in adults. Study 006 Team. Ar. Engt. J. Med. (1999) 341:1865-1873. Results of DMP-006 that led to the approval of efavirenz as an antiretroviral drug.
39. WALMSLEY S, BADLEY A, BEAU. G et al.: Efficacy of ABT-378/r vs. nelfinavir (NFV) in antiretroviral (ARV>naive subjects; results of a phase III blinded randomized clinical triaL Program and abstracts of the 40th Interscience Conference on Antimicrobial Agents and Chemotherapy. Toronto, Ontario, Canada (September 17 -20, 2000). Abstract 693.
40. 40. HAMMER S, SQUIRES K, DEGRUTTOLA V et al.: Randomized trial of abacavir (ABC) and nelfinavir (NFV) in combination with efavirenz (EFV) and adefovir dipivoxil (ADV) as salvage therapy In patients with virologie failure receiving Indinavir (IDV). 6th Conference on Retrovimscs and Opportunistic Infections. Chicago, IL, USA (January 31 - February 4 1999).
41. GULICK RM, HU Xf, FISCUS SA et al.: Salvage therapy with saquinavir SGC (SQV) in combination with ritonavir (RTV) or nelfinavir (NFV) plus delavirdine (DLV), adefovir dipivoxil (ADV) or both. ACTG 359. 7th Conference on Rctrovimses and Opportunistic Infections. San Francisco, CA, USA (January 30 - February 2 2000).
42. HAUBRICH R, KEMPER C, WITT M et al.: Differences in protease inhibitor (PI) phenotypic susceptibility after failure of the first Pi-containing regimen. 39th Interscience Conference on Antimicrobial Agents and Chemotherapy. San Francisco, CA, USA (September 1999).
43. COHEN C, HUNT S, SENSION M et al.: Phenotypic resistance testing significantly improves response to therapy: a randomized trial (VIRA 3001). 7th Conference on Retmvinises and Opportunistic Infections. San Francisco, CA, USA (2000).
44. PATICK A, DURAN M, CAO Y et al: Genotypic Analysis of HIV-1 variants isolated from patients treated with the protease inhibitor nelfinavir, alone or in combination with d4T or AZT and 3TC. 4th Conference on Retrovirus and Opportunistic Infections. Washington DC, USA (January23 - 26, 1997).
45. TEBAS P, PATICK AK, KANE EM et al.: Virologie responses to a ritonavir-saquinavir-containing regimen in patients who had previously failed nelfinavir. /UD.IU999) 13:F23-28. In spite of its small size it continues to be the only prospective nelfinavir failure study published so far.
46. ROBINSON BS, RICCARDI KA, GONG YF et al.: BMS-232632, a highly potent human immunodeficiency virus protease inhibitor that can be used hi combination with other available antiretroviral agents. Antimicrobial Agents & Chemotherapy (2000) 44:2093-2099.
47. GONG YF, ROBINSON BS, ROSE RE et al.: In vitro resistance profile of the human immunodeficiency virus Type 1 protease inhibitor BMS-232632. Antimlcrob. Agents Chemothcr. (2000) 44:2319-2326.
48. THOMPSON M, MURPHY R, GULICK R et al: Analysis of duration of virologie response in two phase II studies of ABT-378/ritonavir (ABT-378/r) at 72 weeks. Abstract TuPeB3197. XIII International AIDS Conference. Durban, South Africa (July 9-14 2000).
49. STASZEWSKI S, MORALES-RAMIREZ JO, GODOFSKY EV et al: Longer time-to-trcatment failure and durability of response with efavirenz + ZDV + 3TC: First analysis of full 1266 patient cohort from Study 006. 39th International Conference of Antimicrobial Agents and Chemotherapy. San Francisco, CA, USA (September 26 - 29 1999).
50. POWDERLY VG, TEBAS P: Nelfinavir, a new protease inhibiton early clinical results. AIDS (1999) 13(Suppl. l):S41-48.