safety/effectiveness of oral chemokine coreceptor 5 (ccr5) antagonist incb009471 in r5-tropic hiv infected patients

Conditions: HIV Infections

Summary: this study will evaluate the safety, pharmacokinetics and efficacy of the ccr5 antagonist incb009471 in hiv-1 infected patients who are antiretroviral therapy naïve, or who are not currently on a haart regimen and have not received any antiretroviral agents for 3 months prior to the screening visit. subjects will receive study medication (incb009471) admnistered orally or placebo once daily with food for 14 days. clinical safety laboratories, 12-lead electrocardiograms, physical examinations and virologic assessments, including viral load, viral tropism and cd4+ cell count determinations will be performed at the screening visit and at regularly scheduled visits throughout the study. a blood sample will also be obtained and stored to potentially determine the genotype of the ccr5 receptor. the primary objectives are: 1. assess the safety and tolerability of 3 doses of incb009471 or placebo when administered orally, once daily, as monotherapy for 14 days; 2. determine the pharmacokinetics of 3 doses of incb009471 or placebo when administered orally, once daily, as monotherapy for 14 days; 3. evaluate the anti-retroviral activity of 3 doses of incb009471 or placebo when administered orally, once daily, as monotherapy for 14 days


Eligibility criteria:
inclusion criteria: asymptomatic hiv-1 infected individuals that are treatmen naïve (ie less than 2 weeks prior arv exposure) or treatment experienced subjects who are not currently on haart and have not received any arvs for 3 months prior to screening. * males between 18 years and 65 years of age, utilizing adequate contraceptive methods. * post menopausal or surgically sterile females between 18 years and 65 years of age. women of childbearing potential, utilizing adequate contraceptive methods. * cd4-lymphocyte count \>350 cells/mm3 * hiv-1 rna copies/ml \> 10,000. * hiv-1 is ccr5 tropic virus only. * ccr5 antagonist treatment naive. * bmi \> 16 to \< 32 kg/m2. * have no clinically significant findings on screening evaluations, which in the opinion of the investigator would interfere with the subject's ability to comply with the protocol. * able to comprehend and willing to sign an informed consent form. exclusion criteria: * current or recent (\<30 days) opportunistic infection. * presence of cxcr4- or dual-tropic hiv-1 virus at screening or baseline assessments. * subjects with chronic renal insufficiency * personal history of cardiac diseases. * history or presence of an abnormal ecg. * history of unstable ischemic heart disease or uncontrolled hypertension. * history of malignancy, with the exception of cured basal cell or squamous cell carcinoma of the skin. * subjects who have received radiation therapy or cytotoxic chemotherapeutic agents and have not recovered from side effects. * current treatment or treatment within 30 days or 5 half-lives with another investigational medication or current enrollment in another investigational drug protocol. * subjects with unstable medical condition (s), which , in the opinion of the investigator would compromise their participation in the trial

Keywords: hiv-infection viral load ccr5 viral tropism hiv-1 infection treatment naive