None listed
Conditions
Interventions
Intervention1: RBx 10017609: Oral Tablets of 15mg, 30 mg, 60 mg, 125 mg, 200 mg, 400 mg, 800 mg and 1600 mg strength. Single dose
Control Intervention1: Placebo: Oral Tablets of 15mg, 30 mg, 60 mg, 12
Sponsors
Ranbaxy Laboratories Ltd
Eligibility
Inclusion criteria
Inclusion criteria: 1. Healthy males in the age range of 18 -45 years with Body Mass Index (BMI)* between 19 ? 28 kg/m2. 2. Full comprehension: ability to comprehend the full nature and purpose of the study, including possible risks and side effects; ability to co-operate with the Investigator and to comply with the requirements of the entire study. 3. Have voluntarily given written informed consent to participate in this study. 4. Be of normal health as determined by medical history, have sitting systolic blood pressure of &#8805; 100 mmHg to < 140 mmHg and diastolic blood pressure of &#8805; 60 mmHg or < 90 mmHg, pulse rate &#8805;60 & &#8804; 90 bpm, clinical examination and laboratory investigations performed within 21 days prior to the commencement of the study. * BMI = Body weight (in kg)/ Height (in m2) Additional Inclusion criteria for Food effect study (Part-2). 5. Have a non-vegetarian diet habit.
Exclusion criteria
Exclusion criteria: 1. History of hypersensitivity to any drug or history of asthma or allergic reactions/atopy 2. Any evidence of organ dysfunction or any clinically significant deviation from the normal, in physical or clinical determinations. 3. Presence of disease markers of HIV 1 or 2, Hepatitis B or C viruses or venereal infection. 4. Presence of values which are out of acceptable limits for haemoglobin, RBC, hematocrit, mean corpuscular haemoglobin (MCH), Mean corpuscular volume (MCV), mean corpuscular haemoglobin concentration (MCHC), bleeding time (BT), clotting time (CT), activated partial thromboplastin time (aPTT), prothrombin time (PT), total white blood cells (WBC) count, differential WBC count or platelet count. 5. Positive for urinary screen testing of drugs of abuse (opiates or cannabinoids). 6. Presence of values which are out of acceptable limits for blood urea nitrogen (BUN), serum creatinine, uric acid, sodium, potassium, calcium, phosphorus, chloride, bicarbonate, alkaline phosphatase (ALP), aspartate amino transferase (AST), alanine amino transferase (ALT), total bilirubin, gamma glutamyl transferase (GGT), albumin, globulin, total protein, cholesterol, triglycerides, lactate dehydrogenase (LDH), creatinine phosphokinase (CPK), glucose (Part 1 and 2) and Cystatin C (Part 1). 7. Clinically abnormal chemical and microscopic examination of urine. 8. Clinically abnormal ECG (12 lead), QTc >440 msec and abnormal Chest X-Ray. 9. History of or any complaints suggestive of gastrointestinal, hepatic, renal, cardiovascular, pulmonary, neurological (including generalized or partial epilepsy), endocrine, vision abnormality, rheumatological, urogenital or haematological disease. 10. Presence of significant infection or known inflammatory process. 11. History of joint pain, stiffness and reduced mobility. 12. Presence of acute gastrointestinal symptoms at the time of screening and/or admission (e.g. nausea, vomiting, diarrhoea, heart burn). 13. Presence of chronic constipation (less than 3 times a week for 12 weeks) at the time of screening and/or admission. 14. Inability to communicate well with investigator (i.e. language problem, poor mental development, psychiatric illness or poor cerebral function) that may impair the ability to provide, written informed consent. 15. Use of tobacco in any form (including cigarette smoking) in the last 6 months. 16. History of drug dependence or habitual alcohol abuse. 17. History of intake of chronic medication. 18. Use of any regular medication (OTC or prescription) with in 14 days or any drug metabolizing enzyme modifying medications within 30 days prior to Day 1 of this study. 19. Participation in any clinical trial within 12 weeks preceding Day 1 of this study. 20. Volunteers who, through completion of this study, would have donated and/or lost more than 350 mL of blood in the past 3 months.
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Safety and tolerability assessed on the basis of AEs, vital signs (BP, pulse rate, respiratory rate, and body temperature), ECG and clinical laboratory results after single dose administration of RBx 10017609Timepoint: admission, pre dose, 1, 2, 4, 6, 8, 10, 12, 24, 30, 36, 48, 60 and 72 hrs post-dose | — |
Secondary
| Measure | Time frame |
|---|---|
| Pharmacokinetic parameters In plasma for parent and metabolite: Cmax, Tmax, AUC0-t, AUC0-&#8734;, T1/2. In plasma for parent: CL/F and Vd/F. In urine: Total parent drug excreted unchanged (X0) and total demethylated metabolite excreted in urine, renal clearance (CLR) of the parent. Pharmacodynamic parameters Total MMP and MMP-9 activity inhibition in plasma and saliva. Timepoint: pre-dose, 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 36, 48 hrs post-dose for drug estimation. Sample points can be extended to 72, 96 and 120 hrs | — |
Countries
India
Contacts
Public ContactMr. Raghu Kochar
Outcome results
None listed