Pafuramidine for pneumocystis jiroveci pneumonia in HIV-infected individuals

Expert Review of Anti-Infective Therapy

Volumn 5, Issue 6, 2007, Pages 921-928

  Chen, Donald ^a   Marsh, Rebecca ^a   Aberg, Judith A ^a  

^a NEW YORK UNIVERSITY   (United States)

Author keywords

DB289; Diamidine; Pafuramidine; Pneumocystis jiroveci

Indexed keywords

2,5 BIS(4 AMIDINOPHENYL)FURAN; AMIDINE; ATOVAQUONE; CLINDAMYCIN; CORTICOSTEROID; COTRIMOXAZOLE; DAPSONE; DIAMIDINE DERIVATIVE; FOLINIC ACID; FURAMIDINE; PAFURAMIDINE; PENTAMIDINE; PLACEBO; PRIMAQUINE; PRODRUG; TRIMETHOPRIM; TRIMETREXATE; UNCLASSIFIED DRUG;

AMINOTRANSFERASE BLOOD LEVEL; AMYLASE BLOOD LEVEL; ANEMIA; BONE MARROW SUPPRESSION; CLINICAL TRIAL; DIARRHEA; DRUG ABSORPTION; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DOSE COMPARISON; DRUG ERUPTION; DRUG EXCRETION; DRUG HALF LIFE; DRUG HYPERSENSITIVITY; DRUG MECHANISM; DRUG PROTEIN BINDING; DRUG STRUCTURE; DRUG TOLERABILITY; DRUG USE; DRUG WITHDRAWAL; ELECTROLYTE DISTURBANCE; FEVER; HEADACHE; HEART ARRHYTHMIA; HEMOLYSIS; HEPATITIS; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTED PATIENT; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; HYPERGLYCEMIA; HYPERKALEMIA; HYPOGLYCEMIA; KIDNEY FAILURE; LEUKOPENIA; METHEMOGLOBINEMIA; MORBIDITY; MORTALITY; NAUSEA; NONHUMAN; PANCREATITIS; PERIPHERAL NEUROPATHY; PNEUMOCYSTIS JIROVECI; PNEUMOCYSTIS PNEUMONIA; REVIEW; SIDE EFFECT; SINGLE DRUG DOSE; THROMBOCYTOPENIA; UNSPECIFIED SIDE EFFECT; UREMIA; VOMITING;

ANIMALS; ANTIFUNGAL AGENTS; BENZAMIDINES; CLINICAL TRIALS AS TOPIC; HIV; HIV INFECTIONS; HUMANS; PNEUMOCYSTIS JIROVECII; PNEUMONIA, PNEUMOCYSTIS;

EID: 37349120064     PISSN: 14787210     EISSN: 17448336     Source Type: Journal    
DOI: 10.1586/14787210.5.6.921     Document Type: Review

References (35)

1. Tidwell R, Boykin D. Dicationic DNA minor groove binders as antimicrobial Agents. In: Small Molecule DNA and RNA Binders. Demeunynck M (Ed.). John Wiley & Sons, NJ, USA 414-460 (2004).
2. Soeiro MN, De Souza EM, Stephens CE, Boykin DW. Aromatic diamidines as antiparasitic agents. Exp. Opin. Investig. Drugs 14(8), 957-972 (2005).
3. Kaplan JE, Hanson D, Dworkin MS et al. Epidemiology of human immunodeficiency virus-associated opportunistic infections in the United States in the era of highly active antiretroviral therapy. Clin. Infect. Dis. 30(Suppl. 1), S5-S14 (2000).
4. Miller RF, Allen E, Copas A, Singer M, Edwards SG. Improved survival for HIV infected patients with severe Pneumocystis jirovecii pneumonia is independent of highly active antiretroviral therapy. Thorax 61(8), 716-721 (2006).
5. Huang L, Hecht FM. Why does Pneumocystis carinii pneumonia still occur? AIDS 14(16), 2611-2612 (2000).
6. Lundberg BE, Davidson AJ, Burman WJ. Epidemiology of Pneumocystis carinii pneumonia in an era of effective prophylaxis: the relative contribution of non-adherence and drug failure. AIDS 14(16), 2559-2566 (2000).
7. Morris A, Lundgren JD, Masur H et al. Current epidemiology of Pneumocystis pneumonia. Emerging Infect. Dis. 10(10), 1713-1720 (2004).
8. Benson CA, Kaplan JE, Masur H et al. Treating opportunistic infections among HIV-infected adults and adolescents: recommendations from CDC, the National Institutes of Health, and the HIV Medicine Association/Infectious Diseases Society of America. MMWR Recomm. Rep. 53(RR-15), 1-112 (2004).
9. Thomas CF Jr, Limper AH. Pneumocystis pneumonia. N. Engl. J. Med. 350(24), 2487-2498 (2004).
10. Barry S, Johnson M. Pneumocystis carinii pneumonia: a review of current issues in diagnosis and management. HIV Med. 2(2), 123-132 (2001).
11. Safrin, S, Lee BL, Sande MA. Adjunctive folinic acid with trimethoprim-sulfamethoxazole for Pneumocystis carinii pneumonia in AIDS patients is associated with an increased risk of therapeutic failure and death. J. Infect. Dis. 170(4), 912-917 (1994).
12. Klein NC, Duncanson FP, Lenox TH et al. Trimethoprim-sulfamethoxazole versus pentamidine for Pneumocystis carinii pneumonia in AIDS patients: results of a large prospective randomized treatment trial. AIDS 6(3), 301-305 (1992).
13. Huang L, Crothers K, Atzori C et al. Dihydropteroate synthase gene mutations in Pneumocystis and sulfa resistance. Emerging Infect. Dis. 10(10), 1721-1728 (2004).
14. Wharton JM, Coleman DL, Wofsy CB et al. Trimethoprim-sulfamethoxazole or pentamidine for Pneumocystis carinii pneumonia in the acquired immunodeficiency syndrome. A prospective randomized trial. Ann. Intern. Med. 105(1), 37-44 (1986).
15. Toma E, Thorne A, Singer J et al. Clindamycin with primaquine vs. trimethoprim-sulfamethoxazole therapy for mild and moderately severe Pneumocystis carinii pneumonia in patients with AIDS: a multicenter, double-blind, randomized trial (CTN 004). CTN-PCP Study Group. Clin. Infect. Dis. 27(3), 524-530 (1998).
16. Safrin S, Finkelstein DM, Feinberg J et al. Comparison of three regimens for treatment of mild to moderate Pneumocystis carinii pneumonia in patients with AIDS: a double-blind, randomized trial of oral trimethoprim-sulfamethoxazole, dapsone-trimethoprim, and clindamycin-primaquine. Ann. Intern. Med. 124(90) 792-802 (1996).
17. Sattler FR, Frame P, Davis R et al. Trimetrexate with leucovorin versus trimethoprim-sulfamethoxazole for moderate to severe episodes of Pneumocystis carinii pneumonia in patients with AIDS: a prospective, controlled multicenter investigation of the AIDS Clinical Trials Group Protocol 029/031. J. Infect. Dis. 170(1), 165-172 (1994).
18. Hughes W, Leoung G, Kramer F et al. Comparison of atovaquone (566C80) with trimethoprim-sulfamethoxazole to treat pneumocystis carinii pneumonia in patients with AIDS. N. Engl. J. Med. 328(21), 1521-1527 (1993).
19. Midgley I, Fitzpatrick K, Taylor LM et al. Pharmacokinetics and metabolism of the prodrug DB289 (2,5-bis[4-(N-methoxyamidino)phenyl]furan monomaleate) in rat and monkey and its conversion to the antiprotozoal/antifungal drug DB75 (2,5-bis(4-guanylphenyl)furan dihydrochloride). Drug Metab. Dispos. 35(6), 955-967 (2007).
20. Zhou L, Lee K, Thakker DR, Boykin DW, Tidwell RR, Hall JE. Enhanced permeability of the antimicrobial agent 2,5-bis(4-amidinophenyl)furan across caco-2 cell monolayers via its methylamidoxime prodrug. Pharm. Res. 19(11), 1689-1695 (2002).
21. Hildebrandt E, Boykin DW, Kumar A, Tidwell RR, Dykstra CC. Identification and characterization of an endo/exonuclease in Pneumocystis carinii that is inhibited by dicationic diarylfurans with efficacy against Pneumocystis pneumonia. J. Eukaryot. Microbiol. 45(1), 112-121 (1998).
22. Turner PR, Denny WA. The mutagenic properties of DNA minor-groove binding ligands. Mutat. Res. 355(1-2), 141-169 (1996).
23. Connor TH. Trizna Z. Pentamidine isethionate is negative in tests for microbial mutagenicity and chromosomal breakage in vitro. Toxicol. Lett. 63(1), 69-74 (1993).
24. Lanteri CA, Trumpower BL, Tidwell RR, Meshnick SR. DB75, a novel trypanocidal agent, disrupts mitochondrial function in Saccharomyces cervisiae. Antimicrob. Agents Chemother. 48(10), 3968-3974 (2004).
25. Lanteri CA, Stewart ML, Brock JM et al. Roles for the Trypanosoma brucei P2 transporter in DB75 uptake and resistance. Mol. Pharmacol. 70(5), 1585-1592 (2006).
26. 5 reductase. Drug Metab. Dispos. 33(12), 1886-1893 (2005).
27. Wang MZ, Saulter JY, Etsuko Usuki et al. CYP4F enzymes are the major enzymes in human liver microsomes that catalyze the O-demethylation of the antiparasitic prodrug DB289 [2,5-bis(4-amidinophenyl)furan-bis-O- methylamidoxime]. Drug Metab. Dispos. 34(12), 1985-1994 (2006).
28. Tidwell RR, Jones SK, Naiman NA et al. Activity of cationically substituted bis-benzimidazoles against experimental Pneumocystis carinii pneumonia. Antimicrob. Agents Chemother. 37(8), 1713-1716 (1993).
29. Boykin DW, Kumar A, Spychala J et al. Dicationic diarylfurans as anti-Pneumocystis carinii agents. J. Med. Chem. 38(6), 912-916 (1995).
30. Boykin DW, Kumar A, Hall JE et al. Anti-pneumocystis activity of bis-amidoximes and bis-O-alkylamidoximes prodrugs. Bioorg. Med. Chem. Lett. 6(24), 3017-3020 (1996).
31. Yeramian P, Kruse M, Kecskes A et al. Safety and clinical pharmacokinetics of DB289, a new orally bioavailable dication. Presented at: 41st Annual Meeting of the Interscience Conference on Antimicrobial Agents and Chemotherapy. Chicago, IL, USA, 16-19 December (2001) (Abstract F-2163).
32. Yeramian P, Meshnick, Krudsood S et al. Efficacy of DB289 in Thai patients with Plasmosium vivax or acute, uncomplicated Plasmodium falciparum infections. J. Infect. Dis. 192(2), 319-22 (2005).
33. Yeates C. DB-289 Immtech International. IDrugs 6, 1086-1093 (2003).
34. Blum J, Pizzagalli F, Thompson M et al. Efficacy and safety of DB289, a new oral drug for treatment of first stage sleeping sickness: preliminary results from Phase II trials. Presented at: Medicine and Health in the Tropics Meeting. Marseille, France, September 15 2005 (Abstract O-101).
35. Yeramian P, Leon J, Huarcaya E et al. Efficacy and safety of DB289, a new oral drug for treatment of Pneumocystis jiroveci pneumonia in AIDS patients. Clin. Microbiol. Infect. 11(5), 96 (2005) (Abstract O405).