First-in-Human Study of the Pharmacokinetics and Antiviral Activity of IDX375, a Novel Nonnucleoside Hepatitis C Virus Polymerase Inhibitor

J. de Bruijne; J. van de Wetering de Rooij; A. A. van Vliet; X. J. Zhou; M. F. Temam; J. Molles; J. Chen; K. Pietropaolo; J. Z. Sullivan-Bólyai; D. Mayers; H. W. Reesink

doi:10.1128/AAC.00451-12

First-in-Human Study of the Pharmacokinetics and Antiviral Activity of IDX375, a Novel Nonnucleoside Hepatitis C Virus Polymerase Inhibitor

J. de Bruijne, J. van de Wetering de Rooij, A. A. van Vliet, X. J. Zhou, M. F. Temam, J. Molles, J. Chen, K. Pietropaolo, J. Z. Sullivan-Bólyai, D. Mayers, H. W. Reesink

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Abstract

IDX375 is a potent and selective palm-binding nonnucleoside inhibitor of the hepatitis C virus (HCV) genotype 1 polymerase. This first-in-human study evaluated the safety, tolerability, and pharmacokinetics of IDX375 in healthy volunteers, as well as its antiviral activity in HCV-infected patients. IDX375, as a choline salt, was administered for 1 day to 40 healthy male volunteers (25- to 200-mg IDX375-equivalent single ascending doses and a 200-mg twice-daily [BID] dose) and three patients chronically infected with HCV genotype 1 (200 mg BID only). IDX375 was well absorbed and well tolerated by all of the study participants. A single-day 200-mg BID dose resulted in exposure-related anti-HCV activity with maximal 0.5 to 1.1 log reductions in plasma HCV RNA. These observations support further clinical investigations of IDX375

Original language	English
Pages (from-to)	4525-4528
Journal	Antimicrobial agents and chemotherapy
Volume	56
Issue number	8
DOIs	https://doi.org/10.1128/AAC.00451-12
Publication status	Published - 2012

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de Bruijne, J., van de Wetering de Rooij, J., van Vliet, A. A., Zhou, X. J., Temam, M. F., Molles, J., Chen, J., Pietropaolo, K., Sullivan-Bólyai, J. Z., Mayers, D., & Reesink, H. W. (2012). First-in-Human Study of the Pharmacokinetics and Antiviral Activity of IDX375, a Novel Nonnucleoside Hepatitis C Virus Polymerase Inhibitor. Antimicrobial agents and chemotherapy, 56(8), 4525-4528. https://doi.org/10.1128/AAC.00451-12

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title = "First-in-Human Study of the Pharmacokinetics and Antiviral Activity of IDX375, a Novel Nonnucleoside Hepatitis C Virus Polymerase Inhibitor",

abstract = "IDX375 is a potent and selective palm-binding nonnucleoside inhibitor of the hepatitis C virus (HCV) genotype 1 polymerase. This first-in-human study evaluated the safety, tolerability, and pharmacokinetics of IDX375 in healthy volunteers, as well as its antiviral activity in HCV-infected patients. IDX375, as a choline salt, was administered for 1 day to 40 healthy male volunteers (25- to 200-mg IDX375-equivalent single ascending doses and a 200-mg twice-daily [BID] dose) and three patients chronically infected with HCV genotype 1 (200 mg BID only). IDX375 was well absorbed and well tolerated by all of the study participants. A single-day 200-mg BID dose resulted in exposure-related anti-HCV activity with maximal 0.5 to 1.1 log reductions in plasma HCV RNA. These observations support further clinical investigations of IDX375",

author = "{de Bruijne}, J. and {van de Wetering de Rooij}, J. and {van Vliet}, {A. A.} and Zhou, {X. J.} and Temam, {M. F.} and J. Molles and J. Chen and K. Pietropaolo and Sullivan-B{\'o}lyai, {J. Z.} and D. Mayers and Reesink, {H. W.}",

year = "2012",

doi = "10.1128/AAC.00451-12",

language = "English",

volume = "56",

pages = "4525--4528",

journal = "Antimicrobial agents and chemotherapy",

issn = "0066-4804",

publisher = "American Society for Microbiology",

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de Bruijne, J, van de Wetering de Rooij, J, van Vliet, AA, Zhou, XJ, Temam, MF, Molles, J, Chen, J, Pietropaolo, K, Sullivan-Bólyai, JZ, Mayers, D & Reesink, HW 2012, 'First-in-Human Study of the Pharmacokinetics and Antiviral Activity of IDX375, a Novel Nonnucleoside Hepatitis C Virus Polymerase Inhibitor', Antimicrobial agents and chemotherapy, vol. 56, no. 8, pp. 4525-4528. https://doi.org/10.1128/AAC.00451-12

First-in-Human Study of the Pharmacokinetics and Antiviral Activity of IDX375, a Novel Nonnucleoside Hepatitis C Virus Polymerase Inhibitor. / de Bruijne, J.; van de Wetering de Rooij, J.; van Vliet, A. A. et al.
In: Antimicrobial agents and chemotherapy, Vol. 56, No. 8, 2012, p. 4525-4528.

Research output: Contribution to journal › Article › Academic › peer-review

TY - JOUR

T1 - First-in-Human Study of the Pharmacokinetics and Antiviral Activity of IDX375, a Novel Nonnucleoside Hepatitis C Virus Polymerase Inhibitor

AU - de Bruijne, J.

AU - van de Wetering de Rooij, J.

AU - van Vliet, A. A.

AU - Zhou, X. J.

AU - Temam, M. F.

AU - Molles, J.

AU - Chen, J.

AU - Pietropaolo, K.

AU - Sullivan-Bólyai, J. Z.

AU - Mayers, D.

AU - Reesink, H. W.

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AB - IDX375 is a potent and selective palm-binding nonnucleoside inhibitor of the hepatitis C virus (HCV) genotype 1 polymerase. This first-in-human study evaluated the safety, tolerability, and pharmacokinetics of IDX375 in healthy volunteers, as well as its antiviral activity in HCV-infected patients. IDX375, as a choline salt, was administered for 1 day to 40 healthy male volunteers (25- to 200-mg IDX375-equivalent single ascending doses and a 200-mg twice-daily [BID] dose) and three patients chronically infected with HCV genotype 1 (200 mg BID only). IDX375 was well absorbed and well tolerated by all of the study participants. A single-day 200-mg BID dose resulted in exposure-related anti-HCV activity with maximal 0.5 to 1.1 log reductions in plasma HCV RNA. These observations support further clinical investigations of IDX375

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DO - 10.1128/AAC.00451-12

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SN - 0066-4804

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JO - Antimicrobial agents and chemotherapy

JF - Antimicrobial agents and chemotherapy

IS - 8

ER -

First-in-Human Study of the Pharmacokinetics and Antiviral Activity of IDX375, a Novel Nonnucleoside Hepatitis C Virus Polymerase Inhibitor

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