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Potential hepatitis C drug's step forward

April 4th, 2011

(PhysOrg.com) -- Successful initial trial for INX-189, originally synthesised in Cardiff

Inhibitex, the US biopharmaceutical company working on potential anti-viral drugs with Prof Chris McGuigan’s laboratory in the Welsh School of Pharmacy, has just announced the successful conclusion of the initial phase 1 trials of INX-189 in hepatitis C patients.

This drug, first synthesised less than three years ago in the laboratory in the Welsh School of Pharmacy, is active against Hepatitis C. This disease affects some 170 million individuals worldwide (3 per cent of the human population) and current treatment is unsatisfactory.

In the current trial, around 50 HCV patients received either a daily oral dose of INX-189, ranging from 3 mg to 100 mg, in some cases in combination with the current drug Ribavarin, for 7 days. The Company plans to present detailed results from this trial during a future scientific meeting. Preliminary data from the trial includes:

No serious adverse events.
No drug related events that increase with dose.
Dose-responsive increases in viral load reduction in the range 9-100mg per day, at both 3 days and 7 days.
Ribavirin (100mg once a day) is synergistic with INX-189 at 25mg daily.
Professor McGuigan, who is also a member of the Board of Directors of Inhibitex, warmly welcomed this news, saying: "The outcome of these multiple dose studies in patients on INX-189 are exciting and continue to show the effectiveness of the drug in patients with hepatitis C. We now need to continue with a full phase II clinical study. INX-189 has today taken a major step closer to becoming a much needed new drug for hepatitis C infection."

For recent scientific papers describing the development of INX-189 see
Design, synthesis and evaluation of a novel double pro-drug: INX-08189. A new clinical candidate for hepatitis C virus
Christopher McGuigan, Karolina Madela, Mohamed Aljarah, et al.
Bioorganic & Medicinal Chemistry Letters 20 (2010) 4850-4854
dx.doi.org/10.1016/j.bmcl.2010.06.094

and

Phosphoramidate ProTides of 2’-C-Methylguanosine as highly potent inhibitors of hepatitis C virus. Study of their in vitro and in vivo properties.
C. McGuigan, A. Gilles, K. Madela, M. Aljarah, et al.
J. Med. Chem., 2010, 4949-4957.
dx.doi.org/10.1021/jm1003792

Provided by Cardiff University

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