CORK, Ireland—Tibotec Pharmaceuticals and Gilead Sciences,Inc. announced today that they have entered into a license agreement togetherto develop and commercialize a new once-daily single tablet fixed-dose antiretroviralcombination product. The new product contains PREZISTA (darunavir), Tibotec'sprotease inhibior, and cobicistat, Gilead's investigationalpharmacoenhancing—or "boosting"—agent.
Within the agreement, subject to regulatory approval,Tibotec will be handling the formulation, manufacturing, registration,distribution and commercialization of the PREZISTA and cobicstat fixed-dosecombination product worldwide. Gilead will retain sole rights formanufacturing, developing and commercializing cobicistat both as a stand-aloneproduct as well as for use in concert with other drugs and agents.
"We are excited to be able to study and develop PREZISTAwith an alternative boosting agent in a combination product which has thepotential to reduce the number of tablets patients take," said Johan Van Hoof,M.D., Global Therapeutic Area Head, Infectious Diseases and Vaccines, JanssenPharmaceutica N.V., in a press release regarding the agreement. "Tibotec iscommitted to developing new and innovative HIV treatment options, especiallythose which provide simplified treatment regimens that may help patients tobetter manage their HIV treatment."
When co-administered with ritonavir, and with otherantiretroviral agents, PREZISTA is indicated for the treatment of humanimmunodeficiency virus (HIV-1) infection. In the United States, a once dailydosing of PREZISTA is indicated for both treatment-naïve adult patients as wellas treatment-experienced adult patients with no darunavir resistance associatedsubstitutions. In the European Union, a once daily dosing of PREZISTA isrecommended for treatment-naïve adult patients, and may be used intreatment-experienced adult patients with no darunavir resistance associatedsubstitutions and who also have plasma HIV-1 RNA < 100,000 copies/ml andCD4+ cell count greater than or equal to 100 cells x 10(6)/l.
Gilead's cobicistat, which the website lists as apharmacokinetic enhancer, is currently in Phase III clinical trials. In theabstract of a letter published online May 17, 2010 in ACS MedicinalChemistry Letters, authors from Gileaddescribe cobicistat as a "potent and selective inhibitor of human cytochromeP450 3A enzymes." The abstract further describes the compound as being devoidof anti-HIV activity, which makes it more suitable for use in "boostinganti-HIV drugs without risking selection of potential drug-resistnat HIVvariants." The authors also note that cobicistat presents reduced liability fordrug interactions, may be more tolerable than ritonavir and "has high aqueoussolubility."
"PREZISTA is one of the leading protease inhibitors andco-formulating it with cobicistat in a new combination product demonstrates ourcommitment to HIV and innovations that will provide new options for patients,"said Van Hoof in a press release.
In addition to this agreement, Gilead and Tibotec are alsodiscussing terms for developing and commercializing a single-tablet regiment(STR) that combines PREZISTA with Gilead's Emtriva (emtricitabine), cobicistatand its investigational agent GS 7340. gilead would be responsible fordeveloping and commercializing the new STR worldwide. The agreement to developthe fixed-dose combination of PREZISTA and cobicistat depends upon the signingof an agreement on the PREZISTA, Emtriva, GS 7340 and cobicistat STR.
Tibotec is one of the firms that compose the JanssenPharmaceutical Companies of Johnson & Johnson. The company's main R&Dfacilities are located in Beerse, Belgium, with additional offices inTitusville, N.J. and Cork.