Navigation Links
Pharmacokinetic/Pharmacodynamic Data Support Further Development of Tobira's Next-Generation CCR5 Receptor Antagonist
Date:2/17/2010

SAN FRANCISCO, Feb. 17 /PRNewswire/ -- Pharmacokinetic/pharmacodynamic (PK/PD) data for TBR-652, which is being developed by Tobira Therapeutics for the treatment of HIV infection, show a strong relationship between drug exposure and viral suppression with this next-generation CCR5 receptor antagonist. These data were presented here today at the 17th Conference on Retroviruses and Opportunistic Infections (CROI).

"These data demonstrate a clear and consistent relationship between TBR-652 plasma concentrations and antiviral activity," said David Martin, PharmD, Tobira Therapeutics, lead author of the PK/PD study. "TBR-652's potent, dose-dependent decreases in viral load, obtained without the need for a ritonavir-boost, illustrate the potential for this compound in fixed-dose antiretroviral drug combinations for the treatment of HIV disease."

In a Phase IIa trial involving 54 treatment-experienced HIV infected patients, a 10-day course of once-daily, TBR-652 monotherapy produced a median nadir decline from baseline in HIV viral load of up to 1.8 log10 copies/mL (Abstract 53, CROI 2010). Using a simple inhibitory Emax model, steady state plasma concentrations of TBR-652 were highly correlated with reductions from baseline in HIV RNA levels. The PK/PD model estimated a maximal antiviral effect (Emax) for TBR-652 of ~ 1.5 log10 copies/mL.  The plasma concentrations of TBR-652 associated with this Emax were easily achieved at doses of greater than or equal to 75 mg/day.  Investigators also observed significant viral load suppression persisting throughout the study's 30-day observation period.

"These PK/PD data for TBR-652 align with previously presented results and support the ongoing development of this exciting compound," said James Sapirstein, President and CEO of Tobira Therapeutics. "These latest data further differentiate TBR-652 from other CCR5 antagonists and provide insights into the future path forward for this drug."

About the trial

Study 652-2-201 was a double-blind, placebo-controlled, dose-escalation trial in which patients were randomized to receive once-daily TBR-652 in the following dosing cohorts: 25 mg (n=8), 50 mg (n=8), 75 mg (n=9), 100 mg (n=10), and 150 mg (n=9); 10 patients were randomly assigned to receive placebo.  All patients were HIV treatment-experienced, though none had previously been treated with a CCR5 antagonist.  

TBR-652 monotherapy produced dose-dependent declines in HIV RNA with a median nadir decline from baseline in HIV viral load of up to 1.8 log10 copies/mL.  In addition, dose-dependent changes in MCP-1 concentrations were also observed, demonstrating TBR-652's dual CCR5/CCR2 mechanism of action and potential anti-inflammatory benefits.  Most adverse events in the study were mild in severity (Grade 1). There were no clinically significant trends in adverse events, laboratory tests, vital signs or electrocardiogram measurements. Additionally, there were no liver function test elevations of Grade 1 or greater.

About Tobira Therapeutics, Inc.

Tobira Therapeutics is a private biopharmaceutical company which is focused on developing and commercializing innovative antiviral compounds to treat HIV disease.  The company was founded in 2006 by Eckard Weber, M.D., a partner at the venture capital firm Domain Associates, to develop novel treatments for HIV disease. Tobira has assembled a highly experienced management team with decades of clinical and commercial development experience specifically in HIV/AIDS drug development.

www.tobiratherapeutics.com

SOURCE Tobira Therapeutics, Inc.

RELATED LINKS
http://www.tobiratherapeutics.com

'/>"/>

SOURCE Tobira Therapeutics, Inc.
Copyright©2010 PR Newswire.
All rights reserved

Related medicine news :

1. HIV therapy in pregnancy-data support WHO recommendations
2. Longaberger Expands Horizon of Hope Campaign to Build Support for American Cancer Societys Breast Cancer Initiatives
3. Data from Patient Subsets of e-HEALING, a Worldwide Registry, Support Use of OrbusNeichs Genous(TM) Bio-Engineered R Stent(TM) as Alternative to Drug- Eluting Stents
4. Family-based treatment more effective than supportive psychotherapy in treating bulimia
5. Therap Services Continues to Hire Experienced Developmental Disability Industry Clinicians for its Customer Support Team
6. Tata Consultancy Services to Support Roches Global Capacity Building Initiative
7. TriWest Creates First-of-its-Kind Partnership to Offer Military Leaders With Grief Support Program
8. AIDS Healthcare Foundation Applauds City Commissioners Support of Diversity, Urges Call for Mayors Resignation
9. Hundreds of MADD Supporters Meet in St. Louis on Sept. 6-8
10. HealthFitness CEO Supports Move Toward Cultural Shift, and Science-Based Health Management Programming
11. Regional Center of Orange County Expands Family Support Resources to Meet Growing Needs
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:6/24/2016)... Maryland (PRWEB) , ... June 24, 2016 , ... ... Angels is actively feeding the Frederick area economy by obtaining investment capital for ... over the past 2½ years that have already resulted in more than a ...
(Date:6/24/2016)... ... June 24, 2016 , ... ... the upcoming 2016 Miss Arizona pageant as its official Medspa Sponsor. Dr. Josh ... Mesa, and Chandler, Arizona. , Dr. Olson says the decision to support ...
(Date:6/24/2016)... ... ... Today, InhaleLabs.com (Inhale) offilially launched its site, which aims to ... high quality water pipes within an ideal price range. The site is completely free ... two brothers, Nick and Mike Hunter, who use medical cannabis to heal ailments of ...
(Date:6/23/2016)... CA (PRWEB) , ... June 23, 2016 , ... An ... that may expose a possible link between head and neck cancer in individuals with ... in the study were evaluated based on whether they had gum disease, brushed their ...
(Date:6/23/2016)... McKinney, Texas (PRWEB) , ... June 23, 2016 , ... ... the special operations community. He turned towards the water to find peace and set ... funds for a veterans charity and turned to the internet. He came across the ...
Breaking Medicine News(10 mins):
(Date:6/24/2016)... 2016  Arkis BioSciences, a leading innovator in ... durable cerebrospinal fluid treatments, today announced it has ... is led by Innova Memphis, followed by Angel ... investors.  Arkis, new financing will accelerate the commercialization ... release of its in-licensed Endexo® technology. ...
(Date:6/23/2016)... BEVERLY HILLS, Calif. , June 23, 2016 ... faced the many challenges of the current process. Many of ... option because of the technical difficulties and high laboratory costs ... would have to offer it at such a high cost ... to afford it. Dr. Parsa Zadeh , ...
(Date:6/23/2016)... 2016 Roche (SIX: RO, ROG; OTCQX: RHHBY) ... Elecsys BRAHMS PCT (procalcitonin) assay as a dedicated testing ... With this clearance, Roche is the first IVD company ... for sepsis risk assessment and management. PCT ... PCT levels in blood can aid clinicians in assessing ...
Breaking Medicine Technology: