Potent new hepatitis C drug completes first clinical trials successfully
September 4, 2010
(ChattahBox Health News) – Inhibitex has initiated a Phase I double-blind, placebo-controlled, single ascending dose study to evaluate the safety and pharmacokinetic activity of INX-189 in healthy volunteers under an IND that it filed earlier this year with the FDA. The study, which is being conducted in the U.S., will evaluate up to six escalating doses of INX-189, ranging from 3 mg up to200 mg. Each dose cohort will include eight subjects, six of which will receive INX-189 and two that will receive placebo.
Completion of the initial phase (phase 1a) of trials of INX-189, discovered and first prepared by researchers at Cardiff University’s Welsh School of Pharmacy in 2008, means the chances of it becoming an approved medicine have significantly improved.
Approximately 170 million people worldwide are affected with Hepatitis C, which can lead to liver cancer, cirrhosis and death. It is the leading cause of liver transplantation in western countries. The current treatment involves two drugs ribavirin and interferon, which has to be given as an injection. Side effects are often severe and lead to patients failing to complete the treatment.
Professor Chris McGuigan of the Welsh School of Pharmacy, academic lead on the project, said: “This is still a very early stage of the trials process but none the less a significant development. Successfully completing phase 1a demonstrates that the drug is safe, with no drug-related side effects at all in a single dose of 100mg.
“The efficiency of drug release in this study has also confirmed that one single dose a day is most likely enough in treating the virus.
“We believe that INX-189 offers the possibility of more potency against Hepatitis, more rapid action in the liver, and fewer side effects than existing treatments.”
In 2008, laboratory tests showed INX-189 killed 90 per cent of the virus at very low (nanomolar) concentration, making it the most potent compound of its kind developed to date.
US pharmaceutical company Inhibitex, which owns the licence to INX-189 and has been working with the Cardiff team, has announced it is looking forward to a second trial (phase 1b), which would evaluate the compound’s effectiveness in Hepatitis C patients.
Cardiff University and Inhibitex filed a patent on INX-189 earlier this year. It has been cleared for human clinical trials by the Food and Drug Administration in the US.
Inhibitex is developing a series of proprietary protides of nucleoside inhibitors that target the RNA-dependent RNA polymerase (NS5b) of HCV. The Company believes that its protides possess several pharmacological advantages over nucleosides alone, including greater potency, a more rapid conversion into its active form in the liver and potentially less toxicity due to reduced systemic exposure of the nucleoside. INX-189 is a protide of a 2′-C-methylguanosine analogue, which the Company believes is the most potent HCV nucleotide polymerase inhibitor described in the literature to date. The Company believes that preclinical studies of INX-189 support its potential as a highly potent, once-per-day oral therapy highly amenable to combination with other antivirals for the treatment of patients with chronic hepatitis C infection.
Inhibitex, Inc., headquartered in Alpharetta, Georgia, is a biopharmaceutical company focused on developing products to prevent and treat serious infectious diseases. The Company’s pipeline includes FV-100, which is in Phase II clinical development for the treatment of shingles, and INX-189, a nucleotide polymerase inhibitor in development for the treatment of chronic hepatitis C infections. Both programmes were in licensed from and pursued collaboratively with Cardiff University. The Company also has additional HCV nucleotide polymerase inhibitors in preclinical development and has licensed the use of its proprietary MSCRAMM® protein platform to Pfizer for the development of staphylococcal vaccines. For additional information about the Company, please visit www.inhibitex.com.
Cardiff University is recognized in independent government assessments as one of Britain’s leading teaching and research universities and is a member of the Russell Group of the UK’s most research intensive universities. Among its academic staff are two Nobel Laureates, including the winner of the 2007 Nobel Prize for Medicine, Professor Sir Martin Evans.
Founded by Royal Charter in 1883, today the University combines impressive modern facilities and a dynamic approach to teaching and research. The University’s breadth of expertise in research and research-led teaching encompasses: the humanities; the natural, physical, health, life and social sciences; engineering and technology; preparation for a wide range of professions; and a longstanding commitment to lifelong learning.