SOUTH SAN FRANCISCO, Calif.--(EON: Enhanced Online News)--Tobira Therapeutics today announced that the American Chemical Society’s journal Molecular Pharmaceutics published an article detailing the cenicriviroc (CVC) drug product formulation and process optimization. This article provides insight into formulation and process advancements, which represent significant breakthroughs in enabling once daily dosing with a single tablet in multiple indications, including the treatment of HIV. These data also establish the basis for future product pipeline diversification by allowing fixed-dose combinations in indications where conveniently administered single tablet multidrug combinations are the standard of care. Tobira’s lead product, cenicriviroc, is a novel oral, once daily, fixed-dose combinable, dual antagonist of chemokine receptors CCR2 and CCR5 being developed for the treatment of HIV-1 infection, graft versus host disease (GVHD), fibrosis and certain oncology indications in which CCR2 and CCR5 play a biological role.
The product candidate that was developed by authors Mark Menning and Sean Dalziel, Ph.D., of Tobira, dramatically improved the physical stability of CVC and absorption resilience across normal gastric pH ranges in a pentagastrin/famotidine beagle dog model. The proprietary formulation and process techniques used in this development are essential to producing the necessary characteristics for conventional dosage form scale-up and production expansion for a broad range of commercial applications. These data were published in the current online issue of Molecular Pharmaceutics in the article titled Fumaric Acid Microenvironment Tablet Formulation and Process Development for Crystalline Cenicriviroc Mesylate, a BCS IV Compound.
Cenicriviroc (CVC) is a novel, oral, once-daily, fixed-dose combinable, dual inhibitor of chemokine receptors CCR2 and CCR5 being developed for the treatment of HIV-1 infection, GVHD, fibrosis, and other indications in which CCR2 and CCR5 play a role. CVC was designed to bind to two cellular chemokine receptors: CCR5 and CCR2. The CCR5 receptor is a key avenue for entry of HIV into human T-cells and is also expressed on macrophages and other immune cells and plays a role in inflammatory responses. CCR2 is expressed on monocytes and other immune cells and is also implicated in inflammation-mediated diseases. Tobira’s most advanced program is for the treatment of HIV, evaluating CVC in fixed-dose combination tablets with other HIV antiretrovirals, for use in complete regimens for treatment of HIV infection. Annually, the U.S. CDC and UNAIDS estimate 47,500 and 2.5 million new HIV infections occur in the U.S. and globally, respectively. Tobira is also evaluating CVC for the prevention of acute GVHD and for the treatment of fibrosis and certain oncology indications.
About Tobira Therapeutics
Tobira Therapeutics is a privately held biopharmaceutical company developing innovative therapies for treatment of HIV infection, GVHD, fibrosis and certain oncology indications. The company’s lead development candidate is cenicriviroc (CVC), a novel, oral, once-daily, fixed-dose combinable, dual inhibitor of chemokine receptors CCR2 and CCR5. Tobira has financial support from a syndicate of leading life science investors including Domain Associates, Frazier Healthcare Ventures, Montreux Equity Partners, Novo Ventures and Canaan Partners. Learn more at www.TobiraTherapeutics.com.