Phase I Study to Evaluate Safety, Pharmacokinetics and Pharmacodynamics of GSK2256098 in Healthy Volunteers

NCT00996671 | Completed Phase 1

• 1 other identifier: 113581
• Study Type: interventional
• Target: 38
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study is to test the safety of a new drug and to look at how the drug is handled by your body. This is the first time the drug will be given to people, the drug has been safely given to animals over many days at higher doses than will be given in the study. The study will be done in healthy men and woman to determine what effects, good or bad, it has on thier health. This study will find out: If the drug has any side effects after one dose of the drug is given? How much of the drug gets into the bloodstream, and how long does the body take to get rid of it? If the drug causes any changes to a substance that is in skin, hair or blood.

Conditions

Cancer

Keywords

focal adhesion kinase inhibitor; healthy volunteers; first time in human

Outcome Measures

Primary Outcomes (2)

• To characterize the safety of single doses of GSK2256098 in adult healthy subjects

  within 10-14 days following administration of study drug

• To characterize the single dose pharmacokinetics of GSK2256098 in blood and urine in adult healthy subjects

  14 days after administration of study drug

Secondary Outcomes (4)

• To examine the dose proportionality of GSK2256098 pharmacokinetic parameters following single dose administration in healthy subjects

  14 days

• To explore dose- and concentration-effect relationships for various safety parameters, if appropriate

  14 days

• To estimate the effect of high fat/calorie meal on the pharmacokinetics, safety, and tolerability of a single dose of GSK2256098.

  14 days

• To explore and potentially identify small molecules or cytokines in plasma which may serve as biomarkers for future studies

  14 days

Study Arms (2)

Dose Escalation Cohorts

EXPERIMENTAL

single dose administration escalating doses starting at 20 mg and continue escalation; the highest dose in this study will not exceed the mean Day 1 exposure in male dogs at the NOAEL dose (6 mg/kg/day).

Drug: GSK2256098; Drug: Placebo

Food effect Cohort

EXPERIMENTAL

Dose to be selected based on emerging safety and PK data; subjects will be given FDA standard high fat meal followed by single dose of study drug.

Drug: GSK2256098

Interventions

GSK2256098 DRUG

focal adhesion kinase inhibitor given as a single dose

Dose Escalation Cohorts; Food effect Cohort

Placebo DRUG

Placebo to be used as comparator for GSK2256098

Dose Escalation Cohorts

Eligibility Criteria

• Age: 18 Years - 65 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• 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.
• AST, ALT, alkaline phosphatase and bilirubin less than or equal to 1.5 X ULN (isolated bilirubin \>1.5 X ULN is acceptable if bilirubin is fractionated and direct bilirubin \< 35%).
• Urine microalbumin: creatinine ratio \< 300 mg/g.
• Male or female between 18 and 65 years of age inclusive, at the time of signing the informed consent.
• 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; or postmenopausal defined as 12 months of spontaneous amenorrhea \[in questionable cases a blood sample with simultaneous follicle stimulating hormone (FSH) \> 40 MlU/ml and estradiol \< 40 pg/ml (\<140 pmol/L) is confirmatory\].
• Male subjects must agree to use one of the contraception methods listed in Section 8.1. This criterion must be followed from the time of the first dose of study medication until the end of the follow-up period.
• Body weight greater than or equal to 50 kg and body mass index (BMI) within the range 18.5 to 30.0 kg/m2 (inclusive).
• Capable of giving written informed consent, which includes compliance with the requirements and restrictions listed in the consent form.
• Average QTcF \< 450 msec (based on averaged results of three ECGs).

You may not qualify if:

• A positive pre-study Hepatitis B surface antigen or positive Hepatitis C antibody result within three 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 HIV antibody.
• History of alcohol consumption within six months of the study defined as:
• an average weekly intake of \> 21 units for males or \> 14 units for females. One unit is equivalent to 8 g of alcohol: a half-pint (\~240 ml) of beer, 1 glass (125 ml) of wine or 1 (25 ml) measure of spirits.
• 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, five half-lives or twice the duration of the biological effect of the investigational product (whichever is longer).
• Exposure to more than four new chemical entities or investigational products within 12 months prior to the first dosing day.
• Use of prescription or non-prescription drugs, including vitamins, herbal and dietary supplements (including St John's Wort) within seven days (or 14 days if the drug is a potential enzyme inducer) or five 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 any of the study medications, 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.
• Where participation in the study would result in donation of blood or blood products in excess of 500 mL within a 56 day period.
• Pregnant females as determined by positive serum hCG test at screening or positive urine hCG test prior to dosing.
• Lactating females.
• Unwillingness or inability to follow the procedures outlined in the protocol.
• Subject is mentally or legally incapacitated.

Sponsors & Collaborators

• GlaxoSmithKline: lead

Study Sites (1)

GSK Investigational Site

Melbourne, Victoria, 3004, Australia

Location

Related Links

• Results for study 113581 can be found on the GSK Clinical Study Register.
• Researchers can use this site to request access to anonymised patient level data and/or supporting documents from clinical studies to conduct further research.

MeSH Terms

Conditions

Neoplasms

Interventions

GSK2256098

Study Officials

• GSK Clinical Trials

  GlaxoSmithKline

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: SINGLE
• Who Masked: PARTICIPANT
• Purpose: TREATMENT
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: October 15, 2009
• First Posted: October 16, 2009
• Study Start: November 6, 2009
• Primary Completion: March 17, 2010
• Study Completion: March 17, 2010
• Last Updated: June 14, 2017

Record last verified: 2017-06

Data Sharing

• IPD Sharing: Will share

Locations

AU (1)