ProHealth health Vitamin and Natural Supplement Store and Health
Home  |  Log In  |  My Account  |  View Cart  View Your ProHealth Vitamin and Supplement Shopping Cart
800-366-6056  |  Contact Us  |  Help
Facebook Google Plus
Fibromyalgia  Chronic Fatigue Syndrome & M.E.  Lyme Disease  Natural Wellness  Supplement News  Forums  Our Story
Store     Brands   |   A-Z Index   |   Best Sellers   |   New Products   |   Deals & Specials   |   Under $10   |   SmartSavings Club

Trending News

10 Fibro-Friendly Foods with a Bonus: Beautiful Skin

Fight Back! Win the War Being Waged Against Your Immune System

Studies Show that Magnesium L-threonate Improves Brain Plasticity, Leading to Direct and Significant...

The role of microbiota and intestinal permeability in the pathophysiology of autoimmune and neuroimm...

Clary Sage Oil May Be Pricey, but Its Benefits Are Priceless

Component of red wine, grapes can help to reduce inflammation, study finds

Poly MVA: A Novel Therapy for Increasing Energy, Repairing DNA, and Promoting Overall Health

Pumpkin Pie Turmeric Breakfast Smoothie - Vegan + Gluten-Free

Omega-3 fatty acid stops known trigger of lupus

What’s Fenugreek Good For?

Print Page
Email Article

Next-generation PI, TMC114, shows promising antiviral activity in patients failing HIV therapy

  [ 108 votes ]   [ Discuss This Article ] • February 14, 2003

Next-generation PI, TMC114, shows promising antiviral activity in patients failing HIV therapy

Novel protease inhibitor (PI) targets resistant virus

TMC114, a next-generation protease inhibitor, has demonstrated significant antiviral activity in multiple PI-experienced HIV patients currently failing PI therapy. In the 50 patient study, the median reduction in plasma viral load was -1.35 log10 copies/ml HIV-1 RNA after 14 days treatment with TMC114 boosted with low-dose ritonavir (TMC114/r); the maximum reduction was -2.49 log10. TMC114 is being developed by Tibotec, a Belgian pharmaceutical research and development company.

The results, the first efficacy data reported for TMC114, were presented this week at the 10th Conference on Retroviruses and Opportunistic Infections by Dr Keikawus Arasteh of Vivantes Auguste-Viktoria-Klinikum, Berlin.

Antiretroviral resistance now accounts for a large proportion of HIV treatment failures and is a major concern for people living with HIV/AIDS. Cross-resistance among the currently approved PIs can render many of them ineffective.

"From the data collected so far, TMC114 seems to continue to be active in the presence of many of the strains of PI-resistant virus; these results are very encouraging," said Dr Arasteh.

The study, TMC114-C207, was a Phase IIa open label, randomized trial in 50 multiple PI-experienced HIV patients currently failing on a PI regimen. The median number of PI-resistance associated mutations at baseline was 6; all primary PI-resistance associated mutations were found among study participants. The median number of PIs previously used was 3; all patients had received at least 2 PIs and 2 NRTIs.

Patients in the study were randomised into three treatment arms (A, B, C) and one control arm, D. In arms A-C failing PIs were replaced by TMC114/r (A: 300/100 mg bid; B: 600/100 mg bid; C: 900/100 mg qd), all other antiretrovirals remained unchanged; in arm D patients continued on their failing regimen. The median change in plasma HIV-1 RNA from baseline to endpoint in arms A, B, C and D was - 1.24, - 1.50, - 1.13 and +0.02 copies/ml respectively.

Patients received TMC114/r for 14 days after which it was discontinued. None of the subjects experienced any rebound in viral load and there was no phenotypic evidence of the development of resistance to TMC114 during the two week trial. The most commonly reported AEs were GI and CNS disorders; no consistent TMC114/r related changes in blood chemistry or hematology were seen. There was one case of reversible hepatotoxicity in the TMC114/r group. TMC114 was generally well-tolerated during this study.

"These early clinical results of TMC114 in highly treatment-experienced patients are very positive" commented Wim Parys MD, Vice President of Clinical Development at Tibotec. "TMC114 was selected for clinical development on the basis of its novel in vitro antiviral profile and potency against PI-resistant HIV. These data, showing that TMC114 is active against PI-resistant virus, confirm previous results indicating that it is a next-generation PI that could potentially contribute to more effective HIV management in the future."

Further studies to evaluate long-term safety and efficacy and to define the optimal dose will be initiated later this year.

Additional TMC114 Data Presented at 10th CROI

Poster 549: TMC114, A Next Generation Protease Inhibitor: Pharmacokinetics and Safety Following Oral Administration of Multiple Doses With and Without Low Doses of Ritonavir in Healthy Volunteers.

About Tibotec  Tibotec is a pharmaceutical research and development company with headquarters in Belgium and operating subsidiaries in the United States and Ireland. The company is a subsidiary of Johnson and Johnson. Tibotec is dedicated to the discovery and development of novel, new drugs for HIV/AIDS and other infectious diseases with the ultimate aim of enhancing and extending peoples' lives. The Company is focusing on the development of HIV/AIDS compounds that are active against both wild-type and drug resistant strains of HIV.  Tibotec has two novel antiretroviral compounds in Phase II clinical development; TMC125, a non-nucleoside reverse transcriptase inhibitor (NNRTI) and TMC114, a protease inhibitor (PI).

For further information, please visit Tibotec's website:

Post a Comment

Featured Products From the ProHealth Store
Energy NADH™ 12.5mg Ultra EPA  - Fish Oil FibroSleep™

Looking for Vitamins, Herbs and Supplements?
Search the ProHealth Store for Hundreds of Natural Health Products

Article Comments

Be the first to comment on this article!

Post a Comment

Natural Pain Relief Supplements

Featured Products

Ultra EPA  - Fish Oil Ultra EPA - Fish Oil
Ultra concentrated source of essential fish oils
Vitamin D3 Extreme™ Vitamin D3 Extreme™
50,000 IU Vitamin D3 - Prescription Strength
Optimized Curcumin Longvida® Optimized Curcumin Longvida®
Supports Cognition, Memory & Overall Health
Mitochondria Ignite™ with NT Factor® Mitochondria Ignite™ with NT Factor®
Reduce Fatigue up to 45%
Ultra ATP+, Double Strength Ultra ATP+, Double Strength
Get energized with malic acid & magnesium

Natural Remedies

Vitamin K-2 – A Key Player in Cardiovascular and Bone Health Vitamin K-2 – A Key Player in Cardiovascular and Bone Health
How I Found My Long-Lost Energy How I Found My Long-Lost Energy
Natural Relief for Soreness, Pain and Swelling - Putting Out the Fire Natural Relief for Soreness, Pain and Swelling - Putting Out the Fire
The Guaifenesin Story: A centuries-old bark extract used for clearing the airways – now key to a popular FM symptom-reversal protocol The Guaifenesin Story: A centuries-old bark extract used for clearing the airways – now key to a popular FM symptom-reversal protocol
Optimize Your Immune System Naturally: Thymic Protein A Optimize Your Immune System Naturally: Thymic Protein A

ProHealth, Inc.
555 Maple Ave
Carpinteria, CA 93013
(800) 366-6056  |  Email

· Become a Wholesaler
· Vendor Inquiries
· Affiliate Program
Credit Card Processing
Be the first to know about new products, special discounts and the latest health news. *New subscribers only

CONNECT WITH US ProHealth on Facebook  ProHealth on Twitter  ProHealth on Pinterest  ProHealth on Google Plus

© 2016 ProHealth, Inc. All rights reserved. Pain Tracker App  |  Store  |  Customer Service  |  Guarantee  |  Privacy  |  Contact Us  |  Library  |  RSS  |  Site Map