GSK239512 DDI Study
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The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details. |
ClinicalTrials.gov Identifier: NCT01802931 |
Recruitment Status :
Completed
First Posted : March 4, 2013
Last Update Posted : July 26, 2017
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Condition or disease | Intervention/treatment | Phase |
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Multiple Sclerosis | Drug: GSK239512 Drug: ketoconazole | Phase 1 |
Study Type : | Interventional (Clinical Trial) |
Actual Enrollment : | 22 participants |
Allocation: | Non-Randomized |
Intervention Model: | Single Group Assignment |
Masking: | None (Open Label) |
Primary Purpose: | Other |
Official Title: | An Open Label Study in Healthy Volunteers to Investigate the Effect of Ketoconazole on the Pharmacokinetics of GSK239512 |
Actual Study Start Date : | January 7, 2013 |
Actual Primary Completion Date : | April 15, 2013 |
Actual Study Completion Date : | April 15, 2013 |

Arm | Intervention/treatment |
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Active Comparator: Session 1 or Session 2
Single dose sessions without ketoconazole co-administration
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Drug: GSK239512
H3 receptor antagonist, potential victim of drug-drug interaction |
Active Comparator: Co-dose Session
Single dose session with ketoconazole co-administration
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Drug: GSK239512
H3 receptor antagonist, potential victim of drug-drug interaction Drug: ketoconazole CYP3A4 inhibitor, potential perpetrator of drug-drug interaction |
- AUC of GSK239512 [ Time Frame: Predose and up to 120 hour post dose of GSK239512 ]
- Cmax of GSK239512 [ Time Frame: Predose and up to 120 hour post dose of GSK239512 ]
- Number of participants with adverse events as a measure of safety and tolerability [ Time Frame: 15 weeks ]

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Ages Eligible for Study: | 18 Years to 45 Years (Adult) |
Sexes Eligible for Study: | Male |
Accepts Healthy Volunteers: | Yes |
Inclusion Criteria:
- Male between 18 and 45 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 cardiac monitoring. A subject with a clinical abnormality or laboratory parameters outside the reference range for the population being studied may be included only if the Investigator and the GSK Medical Monitor agree that the finding is unlikely to introduce additional risk factors and will not interfere with the study procedures.
- ALT, alkaline phosphatase and bilirubin < or = 1.5xULN (isolated bilirubin >1.5xULN is acceptable if bilirubin is fractionated and direct bilirubin <35%).
- QTcF < 450 msec.
- Male subjects with female partners of child-bearing potential must agree to use one of the contraception methods listed in the protocol. This criterion must be followed from the time of the first dose of study medication until 1 month post-last dose of GSK239512.
- Body weight > 50 kg, and body mass index (BMI) between 19.0 - 29.9 kg/m2 inclusive.
- Capable of giving informed consent and can comply with the study requirements and timetable.
Exclusion Criteria:
- A positive pre-study Hepatitis B surface antigen or positive Hepatitis C antibody result within 3 months of screening
- Current or chronic history of liver disease, or known hepatic or biliary abnormalities (with the exception of Gilbert's syndrome or asymptomatic gallstones).
- A positive pre-study drug/alcohol screen.
- A positive test for Human Immunodeficiency Virus (HIV) antibody.
- History of alcohol consumption exceeding, on average, 21 drinks/week for men (1 drink = 100 mL of wine or 240 mL of beer or 30 mL of hard liquor in Australia) within 6 months of the first dose of study medication.
- History of smoking cigarettes or using tobacco products or any nicotine-containing products (including nicotine patches) within 3 months of screening.
- The subject has participated in a clinical trial and has received an investigational product within 30 days or 5 half lives (whichever is longer) prior to the first dosing day in the current study.
- Exposure to more than four new chemical entities within 12 months prior to the first dosing day.
- 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 sensitivity to ketoconazole, or to the excipients contained in GSK239512 or Nizoral, or a history of drug or other allergy that, in the opinion of the investigator or GSK Medical Monitor, contraindicates their participation.
- Where participation in the study would result in donation of blood or blood products in excess of 500 mL within a 56 day period.
- Unwillingness or inability to follow the procedures outlined in the protocol.
- Subject is mentally or legally incapacitated.
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Have used the following medications within the last 30 days or 5 half-lives (whichever is longer) prior to screening and are not able to discontinue use throughout participation in the clinical trial:
- Any CNS stimulants (e.g., modafinil, dexamphetamine, methylphenidate).
- Known potent P-glycoprotein inhibitors (e.g. itraconazole, ketoconazole, cyclosporin, loperamide, diltiazem, verapamil, spironolactone, quinidine, bepridil, quinine, carvedilol).
- Known potent inhibitors or inducers of the CYP3A4 enzyme (see Appendix 3).
- CNS-penetrant antihistamines (e.g. bromopheniramine, chlorpheniramine, clemastine, diphenhydramine, hyrdoxyzine)
- Any other medicines that are contraindications of Nizoral (see Appendix 4).
- Unable to refrain from consumption of red wine, seville oranges, grapefruit or grapefruit juice from 7 days prior to the first dose of study medication.
- The subject has a history of significant psychiatric illness.
- Presence or history of hallucinations that, in the judgement of the investigator, may increase the safety risk to the subject.
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At risk of suicide, as indicated by:
- A documented history of attempted suicide or significant suicidal ideation during the 6 months preceding the screening visit, OR
- If in the investigator's judgment the subject is at risk of a suicide attempt based on the screen visit assessment, including the C-SSRS.
- Diagnosis of any type epilepsy
- Night shift workers within 4 weeks of first dosing
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Presence of significant and routine sleep disturbance that has a negative impact on quality of life that, in the judgement of the investigator, may increase the risk of tolerability issues during dose escalation.
- Examples of significant sleep disturbances may be: severe insomnia, nocturnal wandering, confusion, disorientation, agitation, or vivid dreams.

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.
Please refer to this study by its ClinicalTrials.gov identifier (NCT number): NCT01802931
Australia, New South Wales | |
GSK Investigational Site | |
Randwick, New South Wales, Australia, 2031 |
Study Director: | GSK Clinical Trials | GlaxoSmithKline |
Study Data/Documents: Dataset Specification

For additional information about this study please refer to the GSK Clinical Study Register

For additional information about this study please refer to the GSK Clinical Study Register

For additional information about this study please refer to the GSK Clinical Study Register

For additional information about this study please refer to the GSK Clinical Study Register

For additional information about this study please refer to the GSK Clinical Study Register

For additional information about this study please refer to the GSK Clinical Study Register

For additional information about this study please refer to the GSK Clinical Study Register
Responsible Party: | GlaxoSmithKline |
ClinicalTrials.gov Identifier: | NCT01802931 |
Other Study ID Numbers: |
117016 |
First Posted: | March 4, 2013 Key Record Dates |
Last Update Posted: | July 26, 2017 |
Last Verified: | July 2017 |
Individual Participant Data (IPD) Sharing Statement: | |
Plan to Share IPD: | Yes |
Plan Description: | Patient-level data for this study will be made available through www.clinicalstudydatarequest.com following the timelines and process described on this site. |
GSK239512 H3 receptor antagonist drug-drug interaction pharmacokinetics ketoconazole |
Multiple Sclerosis Demyelinating Autoimmune Diseases, CNS Autoimmune Diseases of the Nervous System Nervous System Diseases Demyelinating Diseases Autoimmune Diseases Immune System Diseases Ketoconazole Antifungal Agents Anti-Infective Agents |
14-alpha Demethylase Inhibitors Cytochrome P-450 Enzyme Inhibitors Enzyme Inhibitors Molecular Mechanisms of Pharmacological Action Steroid Synthesis Inhibitors Hormone Antagonists Hormones, Hormone Substitutes, and Hormone Antagonists Physiological Effects of Drugs Cytochrome P-450 CYP3A Inhibitors |