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New HIV Maturation Inhibitor MPC-9055
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Myriad Genetics Announces Topline Results of Phase 1 Trial of Vivecon for HIV: HIV Maturation Inhibitor
Trial Indicates Favorable Safety and Pharmacokinetics Profiles
SALT LAKE CITY, UT, Sep 17, 2008 (MARKET WIRE via COMTEX News Network) -- Myriad Genetics, Inc. (NASDAQ: MYGN) (www.myriad.com) announced today that it has successfully completed dose escalation in the Phase 1 human clinical trial of Vivecon(TM), its HIV viral maturation inhibitor, in healthy volunteers. The trial demonstrated a favorable safety profile with Vivecon in 55 subjects enrolled across 9 cohorts.
The Phase 1 trial was designed as a single ascending dose study to assess the safety, tolerability and pharmacokinetic parameters of the compound in healthy volunteers. The overall safety profile was favorable with no serious adverse events or clinically significant changes in laboratory values or ECG. The observed pharmacokinetic profile supports continued development. Vivecon has good oral bioavailability and the study demonstrated enhanced absorption of Vivecon when taken with food. This is an additional positive for the drug candidate since that is the preferred option to dosing on an empty stomach.
Based on these results, Myriad is proceeding to a Phase 2a study, a multiple ascending dose trial in treatment-naive HIV-infected individuals. The Phase 2a trial will further evaluate the safety, pharmacokinetic parameters and Vivecon's ability to inhibit viral replication. This clinical development plan may allow a relatively rapid overall development timeline and accelerated initiation of pivotal studies.
"Our anti-HIV program is proceeding well, led by Vivecon as a viral maturation inhibitor," said Adrian Hobden, Ph.D., President of Myriad Pharmaceuticals, Inc. "The Phase 1 data indicates a well-tolerated drug candidate with excellent characteristics for use in the potential treatment of HIV infection."
Vivecon has been tested extensively for anti-viral activity and safety with both in-vitro and in-vivo models, in preclinical studies. It demonstrated anti-viral activity of less than 10 nanomolar IC50 against the HIV virus, with at least a 1,000-fold therapeutic safety index. Vivecon was also shown to be active against viral strains that are resistant to currently marketed anti-HIV drugs, including nucleoside reverse transcriptase inhibitors such as AZT(TM), non-nucleoside reverse transcriptase inhibitors such as Efavirenz(TM) and protease inhibitors such as Ritonavir(TM).
Vivecon (MPC-9055)
Vivecon is a novel, potent, small-molecule drug candidate designed by Myriad Pharmaceuticals for the oral treatment of human immunodeficiency virus 1 (HIV-1) infection. Vivecon is currently in Phase 1 clinical development.
About Vivecon (MPC-9055)
Vivecon is a potent small-molecule maturation inhibitor being developed for the oral treatment of HIV infection. Vivecon targets a unique cleavage event in the HIV life cycle, inhibiting the processing of a Capsid-Spacer 1 intermediate of the Gag protein. This results in a noninfectious virion, and prevents subsequent rounds of HIV infection. Vivecon does not inhibit HIV protease. As a viral maturation inhibitor, Vivecon has the potential to be the first drug in a new class of agents for the treatment of HIV-1 infection.
Vivecon has been tested extensively in preclinical in vitro and in vivo studies to establish antiviral activity and assess safety. It demonstrated potent antiviral activity, with an average HIV IC 50 value of 10 nanomolar and an approximate 1,000-fold in vitro therapeutic index. Vivecon was also shown to be active against viral strains that are resistant to the currently marketed anti-HIV drugs, including nucleoside reverse transcriptase inhibitors such as AZT, non-nucleoside reverse transcriptase inhibitors such as Efavirenz, and protease inhibitors such as Ritonavir. Vivecon has been well-tolerated and exhibits a favorable safety profile in a variety of preclinical studies.
Myriad's anti-viral drug discovery program began with the discovery of the interaction between the HIV Gag protein and the human host protein, TSG101, in the viral budding/maturation pathway of HIV. This research was first published on October 5, 2001 [1], and expanded upon in September, 2003 [2]. Both articles were featured as the cover article in the journal Cell. Myriad scientists have made subsequent discoveries regarding the biology of HIV viral particle maturation, viral fusion with host cells and intra-cellular events in the life cycle of HIV which has enabled Myriad to identify additional novel targets which may inhibit HIV infection.
Clinical Trial
The current clinical development plan for Vivecon is designed to expedite the drug candidate through the clinical development path. The first Phase 1 trial is formatted as a single ascending dose in healthy volunteers and is designed to assess the safety, tolerability, and pharmacokinetics of the compound.
References
1. Garrus J.E., et al, Tsg101 and the Vacuolar Protein Sorting Pathway Are Essential for HIV-1 Budding. Cell 2001 107 : 55-65. PMID: 11595185
2. von Schwedler , U.K. , et al, The Protein Network of HIV Budding. Cell 2003 114 : 701-713. PMID: 14505570
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