Drug evaluation: Bevirimat - HIV Gag protein and viral maturation inhibitor

Current Opinion in Investigational Drugs

Volumn 7, Issue 8, 2006, Pages 759-765

  Temesgen, Zelalem ^a   Feinberg, Judith E ^b  

^a MAYO CLINIC   (United States)

^b UNIVERSITY OF CINCINNATI   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 O (3,3 DIMETHYLSUCCINYL)BETULIC ACID; ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; ATAZANAVIR; BEVIRIMAT; GAG PROTEIN; PLACEBO; RITONAVIR; UNCLASSIFIED DRUG;

ABDOMINAL PAIN; ANOREXIA; ANTIVIRAL ACTIVITY; BLOATING; CLINICAL TRIAL; DEFECATION DISORDER; DIARRHEA; DIZZINESS; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG CONTRAINDICATION; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG INDICATION; DRUG INDUCED HEADACHE; DRUG MARKETING; DRUG METABOLISM; DRUG POTENTIATION; DRUG SAFETY; DRUG SCREENING; DRUG SYNTHESIS; DRUG TOLERABILITY; ECG ABNORMALITY; FATIGUE; HOSPITALIZATION; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; HYPERTRIGLYCERIDEMIA; IC 50; INSOMNIA; LEG CRAMP; LIVER TOXICITY; MONOTHERAPY; MULTIPLE DRUG DOSE; MYALGIA; NAUSEA; NEPHROTOXICITY; NONHUMAN; PERIPHERAL BLOOD MONONUCLEAR CELL; PHOTOSENSITIZATION; PNEUMONIA; QUANTITATIVE ANALYSIS; RESPIRATORY TRACT INFECTION; REVIEW; SIDE EFFECT; STROKE; STRUCTURE ACTIVITY RELATION; SYNCOPE; TACHYCARDIA; TASTE DISORDER; VIRUS INHIBITION; VIRUS LOAD; VIRUS REPLICATION; VISUAL DISORDER; VOMITING; WESTERN BLOTTING;

ANIMALS; CLINICAL TRIALS, PHASE II; DRUG EVALUATION, PRECLINICAL; GENE PRODUCTS, GAG; HIV INFECTIONS; HIV-1; HUMANS; SUCCINATES; TRITERPENES;

EID: 33747601418     PISSN: 14724472     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (31)

1. 61 Anti-AIDS agents. 15. Synthesis and and-HIV activity of dihydroseselins and related analogs. Huang L, Kashiwada Y, Cosentino LM, Fan S, Chen CH, McPhail AT, Fujioka T, Mihashi K, Lee KH J MED CHEM 1994 37 23 3947-3955
2. 45 Betulinic acid and dihydrobetulinic acid derivatives as potent and-HIV agents. Kashiwada Y, Hashimoto F, Cosentino LM, Chen CH, Garrett PE, Lee KH J MED CHEM 1996 39 5 1016-1017
3. 00 Anti-human immunodeficiency virus activity of YK-FH-312 (a betulinic acid derivative), a novel compound blocking viral maturation. Kanamoto T, Kashiwada Y, Kanbara K, Gotoh K, Yoshimori M, Goto T, Sano K, Nakashima H ANTIMICROB AGENTS CHEMOTHER 2001 46 4 1225-1230
4. 53 Declining morbidity and mortality among patients with advanced human immunodeficiency virus infection. Palella FJ Jr, Delaney KM, Moorman AC, Loveless MO, Fuhrer J, Satten GA, Aschman DJ, Holmberg SD N ENGL J MED 1998 338 13 853-860
5. 30 Disposition of PA-457, a novel inhibitor of HIV-1 maturation, in rats involves extensive biliary excretion of a glucuronide. Smith PC, Bender BC, Wild CT, Allaway GP, Martin DE DRUG METAB REV 2003 35 Suppl 2 221
6. 31 PA-457: A potent HIV inhibitor that disrupts core condensation by targeting a late step in Gag processing. Li F, Goila-Gaur R, Salzwedei K, Kilgore NR, Reddick M, Matallana C, Castillo A, Zoumplis D, Martin DE, Orenstein JM, Allaway GP et al PROC NATL ACAD SCI USA 2003 100 23 13555-13560
7. 63 Panacos Pharmaceuticals amends merger agreement with VI technologies. Panacos Pharmaceuticals Inc PRESS RELEASE 2004 November 08
8. 84 Panacos's HIV maturation inhibitor gets Fast Track status. Panacos Pharmaceuticals Inc PRESS RELEASE 2005 January 06
9. 10 Panacos's PA-457 reduces viral load in phase II HIV trial. Panacos Pharmaceuticals Inc PRESS RELEASE 2005 August 22
10. 95 Selection for and characterization of HIV-1 isolates resistant to the maturation inhibitor PA-457. Salzwedel K, Goila-Gaur R, Adamson C, Li F, Castillo A, Kilgore N, Reddick M, Matallana C, Zoumplis D ANTIVIR THER 2004 9 4 S8
11. 62 Safety and antiviral activity of PA-457, the first-in-class maturation inhibitor, in a 10-day monotherapy study in HIV-1 infected patients. Beatty G, Lalezari J, Eron J, Pollard J, Saag M, Doto J, Salzwedel K, Wild C, Allaway G, Jacobson J, Martin D ICAAC 2005 45 Abs H-416d
12. 56 Panacos reports fourth quarter and full year results for 2005; company updates progress toward initiating PA-467 phase 2b clinical trial. Panacos Pharmaceuticals Inc PRESS RELEASE 2006 February 14
13. 67 Panacos reports first quarter 2006 financial results; PA-457 phase 2b trial design agreed with FDA; study projected to begin in Q2 2006. Panacos Pharmaceuticals Inc PRESS RELEASE 2006 April 26
14. 76 Anti-AIDS agents, 11. Betulinic acid and platanic acid as anti-HIV principles from Syzigium claviflorum, and the anti-HIV activity of structurally related triterpenoids. Fujioka T, Kashiwada Y, Kilkuskie RE, Cosentino LM, Ballas LM, Jiang JB, Janzen WP, Chen IS, Lee KH J NAT PROD 1994 67 2 243-247
15. 29 The determinants of activity of the HIV-1 maturation inhibitor PA-457 map to residues flanking the Gag CA-SP1 cleavage site. Li F, Zoumplis D, Matallana C, Adamson C, Kilgore N, Reddick M, Freed E, Allaway G, Wild C INT CONF RETROVIRUSES OPPORTUNISTIC INFECT 2005 12 Abs 256
16. 42 In vitro and in vivo pre-clinical analyses of PA-457, a novel betulinic acid derivative that potently inhibits HIV-1 replication. Wild CT, Kilgore NR, Reddick MS, Salzwedel KD, Turpin JA, Kashiwada Y, Lee KH, Smith PC, Martin DE, Allaway GP INT AIDS SOC CONF HIV PATHOGENESIS TREAT 2002 14 Abs MoPeA3030
17. 05 Determinants of activity, in vitro metabolism and in vivo disposition of the novel maturation inhibitor PA-457. Martin DE, Smith P, Goila-Gaur R, Salzwedel K, Li F, Kilgore N, Reddick M, Matallana C, Castillo A, Zoumplis D, Allaway G et al INT CONF RETROVIRUSES OPPORTUNISTIC INFECT 2005 11 Abs 545
18. 75 The safety, tolerability and pharmacokinetics of multiple oral doses of PA-457, a first-in-class HIV maturation inhibitor, in healthy volunteers. Martin DE, Ballow CH, Blum R, Doto J, Wild CT, Allaway GP INT CONF RETROVIRUSES OPPORTUNISTIC INFECT 2005 12 Abs 551
19. 82 The safety, tolerability and pharmacokinetics of PA-457, a first-in-class HIV maturation inhibitor, in healthy volunteers. Martin DE, Ballow CH, Blum R, Doto J, Wild CT, Allaway GP INT CONGR DRUG THER HIV INFECT 2004 7 Abs
20. 86 In vitro and in vivo disposition of PA-457, a novel inhibitor of HIV-1 maturation. Martin DE, Smith P, Wild C, Allaway G EJIAS 2004 15 Abs MPeA5644
21. 88 The first-in-class maturation inhibitor, PA-457, is a potent inhibitor of HIV replication both in vitro and in vivo. Martin DE, Smith P, Wild C, Allaway G EJIAS 2004 15 Abs WaPeA5643
22. 55 The first in class maturation inhibitor, PA-457, is a potent inhibitor of HIV drug-resistant isolates and acts synergistically with approved HIV drugs in vitro. Kilgore N, Reddick M, Zuiderhof M, Li F, Yunus AS, Matallana C, Zoumplis D, Castillo A, Salzwedel K, Wild C INT CONF RETROVIRUSES OPPORTUNISTIC INFECT 2006 13 Abs 509
23. 58 Pharmacokinetics/pharmacodynamics of PA-457 In a 10-day multiple does monotherapy trial in HIV-infected patients. Smith P, Forrest A, Beatty G, Jacobson J, Lalezari J, Eron J, Pollard R, Saag M, Doto J, Martin DE INT CONF RETROVIRUSES OPPORTUNISTIC INFECT 2006 13 Abs 52
24. 62 Pharmacokinetic/pharmacodynamic effects of PA-457 in HIV-infected patients following a single oral dose. Ogundele A, Smith PF, Forrest A, Martin DE INT AIDS SOC CONF HIV PATHOGENESIS TREAT 2006 3 Abs TuPe3.1B01
25. 64 Viral resistance to PA-457, a novel inhibitor of HIV-1 maturation. Adamson CS, Salzwedel K, Golia-Gaur R, Ablan S, Li F, Castillo A, Wild C, Freed EO COLD SPRING HARBOR LAB MEET - RETROVIRUSES 2005
26. 71 Determinants of activity of the HIV-1 maturation inhibitor PA-457 map to the Gag protein CA-SP1 domain. Li F, Matallana C, Zoumplis D, Kilgore NR, Reddick M, Adamson CS, Salzwedel K, Martin DE, Allaway GP, Freed EO, Wild CT COLD SPRING HARBOR LAB MEET - RETROVIRUSES 2005
27. 92 Potent in vivo antiviral activity of the HIV-1 maturation inhibitor PA103001-01. Stoddart CA, Bare J, Martin DE KEYSTONE SYMP - HIV PATHOGENESIS 2004
28. 50 3-O-(3′,3′-dimethysuccinyl) betulinic acid inhibits maturation of the human immunodeficiency virus type 1 Gag precursor assembled in vitro. Sakalian M, McMurtrey CP, Deeg FJ, Maloy CW, Li F, Wild CT, Salzwedel K J VIROL 2006 80 12 5716-5722
29. 39 Panacos begins phase IIb HIV trial of bevirimat. Panacos Pharmaceuticals Inc PRESS RELEASE 2006 June 12
30. 56 PA-457, the first-in-class maturation inhibitor, exhibits antiviral activity following a single oral dose in HIV-1-infected patients. Martin D, Jacobson J, Schurmann D, Osswald E, Doto J, Wild C, Allaway G INT CONF RETROVIRUSES OPPORTUNISTIC INFECT 2005 12 Abs 159
31. 07 Biotechnology quarterly: Will Biotech lose its pricing power? Schmidt E, Nadeau P, Schimmer J, Hsia C, Gershell SG COWEN CO 2005 October 01