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Important Therapeutic Target For Breast Cancer: Newly Appreciated Membrane Estrogen Receptor
New research at Rhode Island Hospital has uncovered the biological effects of a novel membrane estrogen receptor, a finding that has potential implications for hormonal therapy for breast cancer. The study is published in the July edition of the journal Molecular Endocrinology. This new study by Edward Filardo, MD, and his research team further supports earlier published work by the group that linked the transmembrane receptor, GPR30/GPER-1, to specific estrogen binding, rapid estrogen signaling and breast cancer metastasis. "What is exciting about this new work," says Filardo, "is that it provides some insight into the influence of GPR30 at the cellular level. It shows that estrogen action through GPR30 allows for breast tumor cell survival, and not breast tumor cell proliferation." Prior studies by Filardo"s group showed that estrogen acts through GPR30 to promote the rapid release of preformed growth factors that are tethered to the surface of breast cancer cells. Their latest study was conducted in an effort to better understand the mechanism by which GPR30 triggered the release of epidermal growth factor (EGF) polypeptides from the surface of breast cancer cells.
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96-Week Safety And Efficacy Findings Presented For INTELENCE(TM) (etravirine) As Part Of HIV Combination Therapy

Ninety-six week pooled results from two Phase 3 studies (DUET-1 and DUET-2) showed that significantly more treatment-experienced HIV-1-infected adults with non-nucleoside reverse transcriptase inhibitor (NNRTI) and protease inhibitor (PI) resistance had an undetectable viral load (DUET-1 and -2 Study Design The DUET-1 and -2 studies, identical in design and conducted across the Americas, Australia, Canada, Europe, Thailand and Europe, assessed the 24-week efficacy and safety of INTELENCE in combination with a BR in treatment-experienced adult HIV-1 patients with documented evidence of NNRTI and PI resistance. They were large randomized, controlled studies and the primary endpoint was the proportion of patients who achieved a confirmed undetectable viral load (less than 50 copies/mL). Patients with HIV-1 who were eligible for the DUET trials had a viral load of greater than 5,000 copies/mL, were on a stable antiretroviral therapy regimen, and had evidence of at least one NNRTI-resistance-associated mutation, either at screening or from historical resistance tests as well as evidence of three or more primary PI mutations (D30N, V32I, L33F, M46I/L, I47A/V, G48V, I50L/V, V82A/F/L/S/T, I84V, N88S, or L90M) at screening. Participants in the DUET studies were randomized to receive INTELENCE 200 mg twice daily (599 patients) or placebo (604 patients), each given in addition to a BR. For all patients, the BR included darunavir/ritonavir, plus at least two investigator-selected antiretroviral drugs (N(t)RTIs with or without enfuvirtide). The study was designed to evaluate INTELENCE efficacy and safety over 48 weeks with an optional extension to 96 weeks. The study remained double-blinded until the last study participant reached week 48; after this point, the study was unblinded. DUET-1 and -2: 96-Week Efficacy Data The 96-week pooled analysis of the DUET studies showed the following efficacy results: -- Fifty-seven percent of patients in the INTELENCE arm had an undetectable viral load (DUET-1 and -2: 96-Week Safety Data -- In the DUET studies, the most commonly reported adverse events (greater than or equal to 10 percent) among patients in the INTELENCE arm vs. placebo arm, regardless of causality, were rash (21 percent vs. 12 percent), diarrhea (19 percent vs. 24 percent), nausea (15 percent vs. 14 percent), nasopharyngitis (14 percent vs. 12 percent), headache (12 percent vs. 14 percent), cough (11 percent vs. 9 percent) and herpes simplex (10 percent vs. 10 percent). -- The incidence of nervous system and psychiatric AEs was comparable between the INTELENCE and placebo arms. Nineteen percent of patients in the INTELENCE arm experienced nervous system disorders and 20 percent reported psychiatric disorders, compared to 21 percent of patients in the placebo arm who experienced either AE. Important Safety Information INTELENCE does not cure HIV infection or AIDS, and does not prevent passing HIV to others. Warnings & Precautions -- Severe Skin Reactions: Severe and potentially life-threatening skin reactions, including Stevens-Johnson Syndrome, hypersensitivity reaction, and erythema multiforme, have occurred (Use in Specific Populations -- Hepatic Impairment: INTELENCE should be used with caution in patients with severe hepatic impairment (Child-Pugh Class C) as pharmacokinetics of INTELENCE have not been evaluated in these patients. Adverse Reactions -- The most common adverse events (>10%) of any intensity that occurred at a higher rate than placebo at 24-weeks were rash (16.9% vs. 9.3%) and nausea (13.9% vs. 11.1%). -- The most common treatment-emergent adverse reactions (Grade 2-4) that occurred in patients receiving an INTELENCE-containing regimen vs. placebo at 24-weeks were rash (9.0% vs. 3.1%), diarrhea (5.2% vs. 9.6%), nausea (4.7% vs. 3.5%), fatigue (3.3% vs. 4.0%), abdominal pain (3.0% vs. 2.5%), peripheral neuropathy (2.8% vs. 1.8%), hypertension (2.8% vs. 2.2%), headache (2.7% vs. 4.1%), and vomiting (2.3% vs. 2.0%). Drug Interactions -- INTELENCE should not be co-administered with the following ARVs: tipranavir/ritonavir, fosamprenavir/ritonavir, atazanavir/ritonavir, full-dose ritonavir (600 mg bid), protease inhibitors administered without ritonavir, and other NNRTIs. -- INTELENCE should not be co-administered with carbamazepine, phenobarbital, phenytoin, rifampin, rifapentine, rifabutin (when part of a regimen containing protease inhibitor/ritonavir) or products containing St. John"s wort (Hypericum perforatum). -- INTELENCE and lopinavir/ritonavir should be co-administered with caution. -- Co-administration of INTELENCE with other agents such as substrates, inhibitors, or inducers of CYP3A4, CYP2C9, and/or CYP2C19 may alter the therapeutic effect or adverse events profile of INTELENCE or the co-administered drug(s). This is not a complete list of potential drug interactions. About Tibotec Therapeutics Tibotec Therapeutics, a division of Ortho Biotech Products, L.P., headquartered in Bridgewater, N.J., is dedicated to delivering innovative virology therapeutics that help healthcare professionals address serious unmet needs in people living with HIV. About Tibotec Pharmaceuticals Tibotec Pharmaceuticals, based in Cork, Ireland, is a pharmaceutical research and development company, with offices in Yardley, PA, USA and its main research and development operations in Mechelen, Belgium. Tibotec is dedicated to the discovery and development of innovative HIV/AIDS drugs and anti-infectives for diseases of high unmet medical need. Tibotec Therapeutics


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