Rilapladib is a potent and selective inhibitor of lipoprotein associated phospholipase A2 (Lp-PLA2), which was previously under development for the treatment of atherosclerosis and is currently being developed for the treatment of Alzheimer's disease.

This study is a single-center, open-label, two-part study. The two study parts will run independently. Subjects dosed in one part of this study will not be permitted to participate in the other part.

Part A will investigate the pharmacokinetic profile of rilapladib and its metabolites, SB-664601 and GSK1174379, after single dose and steady state dosing of rilapladib 250 milligram (mg) along with the biliary and urinary elimination pathways of rilapladib 250 mg. Part B will determine the effect of repeat administration of itraconazole on the PK of a single oral dose of rilapladib 25 mg.

Healthy male and female subjects, aged 18-65 years, will be recruited for this study. Ten subjects will be recruited for Part A and 20 subjects will be recruited for Part B.

Inclusion Criteria:

• Male or female aged between 18 and 65 years of age inclusive, at the time of signing the informed consent.
• Healthy as determined by a responsible and experienced physician, based on a medical evaluation including medical history, physical examination, laboratory tests and Electrocardiogram (ECG). A subject with a clinical abnormality or laboratory parameter(s) which is/are not specifically listed in the inclusion or exclusion criteria, outside the reference range for the population being studied may be included only if the Investigator in consultation with the Glaxosmithkline (GSK) Medical Monitor agree and document that the finding is unlikely to introduce additional risk factors and will not interfere with the study procedures.
• A subject with an alanine aminotransferase (ALT), alkaline phosphatase or bilirubin laboratory result outside the reference range may be included only if the Investigator and GSK Medical Monitor agree and document that the finding is unlikely to introduce additional risk factors.
• A female subject is eligible to participate if she is of: Non-childbearing potential defined as pre-menopausal females with a documented tubal ligation or hysterectomy [for this definition, "documented" refers to the outcome of the investigator's/designee's review of the subject's medical history for study eligibility, as obtained via a verbal interview with the subject or from the subject's medical records]; or postmenopausal defined as 12 months of spontaneous amenorrhea [in questionable cases a blood sample with simultaneous follicle stimulating hormone (FSH) > 40 milli-International units/milliliter (MIU/mL) and estradiol < 40 picogram (pg)/mL (<147 picomole/Litre [pmol/L]) is confirmatory].
• Body weight >= 50 kilogram (kg) and body mass index (BMI) within the range 19-32 kg/square meter (m^2) (inclusive).
• Based on single QT duration corrected for heart rate by Fridericia's formula (QTcF): QTcF <450millisecond (msec); or QTcF <480 msec in subjects with right bundle branch block.
• Capable of giving written informed consent, which includes compliance with the requirements and restrictions listed in the consent form.

Exclusion Criteria:

Criteria Based Upon Medical History

• Current or chronic history of liver disease, or known hepatic or biliary abnormalities (with the exception of Gilbert's syndrome or asymptomatic gallstones), or prior cholecystectomy.
• History of asthma, anaphylaxis or anaphylactoid reactions, or severe allergic responses.
• Lifetime history of suicide attempt or active suicidal ideation within the past six months.
• Current major depressive episode or a previous episode of depression requiring medical intervention.
• History of sensitivity to heparin or heparin-induced thrombocytopenia (if the clinical research unit uses heparin to maintain intravenous cannula patency).
• History of sensitivity to compounds with a chemical structure related to rilapladib or itraconazole, or components thereof, or a history of drug or other allergy that, in the opinion of the investigator or GSK Medical Monitor, contraindicates their participation.
• Any contraindications for itraconazole administration.
• Requiring the use of oral or injectable strong Cytochrome P450 3A4 (CYP3A4) inhibitors or use of other CYP3A4 inhibitors/inducers within 14 days prior to dosing.
• Unable to refrain from the use of prescription or non-prescription drugs, including vitamins, herbal and dietary supplements (including St. John's Wort) within 7 days (or 14 days if the drug is a potential enzyme inducer) or 5 half-lives (whichever is longer) prior to the first dose of study medication, unless in the opinion of the investigator and GSK Medical Monitor the medication will not interfere with the study procedures or compromise subject safety.
• History of regular alcohol consumption within 6 months of the study defined as an average weekly intake of >14 drinks for males or >7 drinks for females. One drink is equivalent to 12 gram (g) of alcohol: 12 ounces (360 mL) of beer, 5 ounces (150 mL) of wine or 1.5 ounces (45 mL) of 80 proof distilled spirits.

Criteria Based Upon Diagnostic Assessments

• A positive pre-study Hepatitis B surface antigen, positive Hepatitis C antibody result, or positive test for Human Immunodeficiency Virus (HIV) antibody.
• Urinary cotinine levels indicative of smoking or history or regular use of tobacco- or nicotine-containing products within 6 months prior to screening.
• A positive pre-study drug or alcohol screen.

Other Criteria

• Where participation in the study would result in donation of blood or blood products in excess of 500 mL within a 56 day period.
• The subject has participated in a clinical trial and has received an investigational product within the following time period prior to the first dosing day in the current study: 30 days, 5 half-lives or twice the duration of the biological effect of the investigational product (whichever is longer).
• Previous participation in this study.
• Exposure to more than four new chemical entities within 12 months prior to the first dosing day.
• Consumption of red wine, seville oranges, grapefruit or grapefruit juice and/or pummelos, exotic citrus fruits, grapefruit hybrids or fruit juices within 7 days prior to the first dose of study medication until collection of the final pharmacokinetic sample.