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Ketoconazole

Phase 1

Cancer | Small molecule | Oncology |GSK plc|Last Updated: Nov 13, 2017

Success Probability

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Trial Design

CONTROLLED
Total Trials1
Total Enrollment48

FDA Designations

No designations recorded

Clinical trial landscape

Ketoconazole · 3 trials · 4 indications

Phase 1 3
NCT01340846A Pharmacokinetics Study of the Effects of GSK2118436 on Warfarin, the Effects of Ketoconazole and Gemfibrozil on GSK2118436, and the Effects of Repeat Doses of GSK2118436 in Subjects With BRAF Mutant Solid TumorsCancer
COMPLETED48 Analytics
NCT00501397A Study of the Effects of Ketoconazole Taken Orally Has on the PK Profiles of a Dose of GSK189075 in Healthy VolunteersType 2 Diabetes Mellitus
COMPLETED22 Analytics
NCT00404378Study Of Healthy Subjects To Assess The Effect Of Ketoconazole And The Way The Body Will React To Casopitant [GW679769]Nausea and Vomiting, Chemotherapy-Induced
COMPLETED15 Analytics
PHASE1COMPLETED
A Pharmacokinetics Study of the Effects of GSK2118436 on Warfarin, the Effects of Ketoconazole and Gemfibrozil on GSK2118436, and the Effects of Repeat Doses of GSK2118436 in Subjects With BRAF Mutant Solid Tumors
CancerUnlock trial analytics
PHASE1COMPLETED
A Study of the Effects of Ketoconazole Taken Orally Has on the PK Profiles of a Dose of GSK189075 in Healthy Volunteers
Type 2 Diabetes MellitusUnlock trial analytics
PHASE1COMPLETED
Study Of Healthy Subjects To Assess The Effect Of Ketoconazole And The Way The Body Will React To Casopitant [GW679769]
Nausea and Vomiting, Chemotherapy-InducedUnlock trial analytics

Study Endpoints

Primary Endpoints

Maximum plasma concentration (Cmax) of S-warfarin with and without GSK2118436
Up to 168 hours after dosing on Day 1 (warfarin alone) and Day 22 (warfarin in combination with GSK2118436)
Area under the concentration time curve (AUC) of S-warfarin with and without GSK2118436
Up to 168 hours after dosing on Day 1 (warfarin alone) and Day 22 (warfarin in combination with GSK2118436)
Maximum plasma concentration (Cmax) of GSK2118436 with and without an inhibitor
Up to 12 hours after dosing on Day 18 (GSK2118436 alone) and Day 22 (GSK2118436 in combination with inhibitor)
Area under the concentration time curve (AUC) of GSK2118436 with and without an inhibitor
Up to12 hours after dosing on Day 18 (GSK2118436 alone) and Day 22 (GSK2118436 in combination with inhibitor)
Cmax of GSK2118436 and metabolites after single and multiple 75mg HPMC dose
Up to 24 hours after dosing on Day 1 and up to 12 hours after dosing on Day 18
AUC of GSK2118436 and metabolites after single and multiple 75mg HPMC dose
Up to 24 hours after dosing on Day 1 and up to 12 hours after dosing on Day 18
Time to Cmax (Tmax) of GSK2118436 and metabolites after single and multiple 75mg HPMC dose
Up to 24 hours after dosing on Day 1 and up to 12 hours after dosing on Day 18
Half-life of GSK2118436 and metabolites after single 75mg HPMC dose
Up to 24 hours after dosing on Day 1
Cmax of GSK2118436 and metabolites after single and multiple 150mg HPMC dose
Up to 24 hours after dosing on Day 1 and up to 12 hours after dosing on Day 18
AUC of GSK2118436 and metabolites after single and multiple 150mg HPMC dose
Up to 24 hours after dosing on Day 1 and up to 12 hours after dosing on Day 18
Tmax of GSK2118436 and metabolites after single and multiple 150mg HPMC dose
Up to 24 hours after dosing on Day 1 and up to 12 hours after dosing on Day 18
Half-life of GSK2118436 and metabolites after single 150mg HPMC dose
Up to 24 hours after dosing on Day 1
Plasma blood samples for GSK189075 at Day 1 Session 1, Days 5 & 6 Session 3
at Day 1 Session 1, Days 5 & 6 Session 3 urine collections for volume
urine collections for volume, glucose, & creatinine at Day 1 Session 1, Days 5 & 6 Session 3.
at Day 1 Session 1, Days 5 & 6 Session 3.
Plasma levels will be measured for casopitant at Period 1: Day 1, 2 & 3.
Period 1: Day 1, 2 & 3
Plasma levels will be measured for casopitant and ketoconazole at Period 2: Day 4, 5, 6, 7, & 8.
Period 2: Day 4, 5, 6, 7, & 8.

Secondary Endpoints

Cmax of R-warfarin with and without GSK2118436
Up to 168 hours after dosing on Day 1 (warfarin alone) and Day 22 (warfarin in combination with GSK2118436)
Time to Cmax (Tmax) of R-warfarin
Up to 168 hours after dosing on Day 1 (warfarin alone) and Day 22 (warfarin in combination with GSK2118436)
Trough concentration of GSK2118436
Up to168 hours after dosing on Day 22
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Study Design & Arms

AllocationNON_RANDOMIZED
MaskingNONE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Part AEXPERIMENTALWarfarin dosed at 15mg
Part BEXPERIMENTALKetoconazole dosed at 400mg
Part CEXPERIMENTALGemfibrozil dosed at 600mg
Part DEXPERIMENTALGSK2118436 dosed alone
Cohort 1 Treatment Period 1EXPERIMENTALSubjects will receive single oral dose of 100 milligram (mg) of Casopitant. There will be wash out period of 7 days.
Cohort 1 Treatment Period 2EXPERIMENTALSubjects will receive ketoconazole 400 mg once daily on Days 1 - 7. On Day 4 subjects will receive a single dose of oral casopitant 100 mg along with ketoconazole.
Cohort 2 Treatment Period 1EXPERIMENTALSubjects will receive single oral dose of 50 mg of Casopitant. There will be wash out period of 7 days.
Cohort 2 Treatment Period 2EXPERIMENTALSubjects will receive ketoconazole 400 mg once daily on Days 1 - 7. On Day 4 subjects will receive a single dose of oral casopitant 50 mg along with ketoconazole.

Interventions

NameTypeDescription
WarfarinDRUGWarfarin dosed at 15mg on Day 1 and Day 22
KetoconazoleDRUGKetoconazole dosed at 400mg daily on Days 19 through 22
GemfibrozilDRUGGemfibrozil dosed at 600mg twice daily on Days 19 through 22
GSK2118436 150mgDRUGGSK2118436 dosed at 150mg twice daily
GSK2118436 75mgDRUGGSK2118436 dosed at 75mg twice daily
GSK189075DRUG -
casopitant 100 mgDRUGCasopitant tablets will be available with dose strength of 50 mg. Subjects will receive two 50 mg tablets for the dose of 100 mg. On Day 4 of Treatment Period 2, the dose of casopitant and ketoconazole is to be taken at the same time
Casopitant 50 mgDRUGCasopitant tablets will be available with dose strength of 50 mg and will receive single dose. On Day 4 of Treatment Period 2, the dose of casopitant and ketoconazole is to be taken at the same time.
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites11

Inclusion Criteria: * Male or female at least 18 years of age at the time of signing the informed consent form; * Capable of giving written informed consent, which includes compliance with the requirements and restrictions listed in the consent form; * Body weight \>/= 45 kg and a body mass index \...

Countries:United StatesAustraliaUnited Kingdom
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Frequently asked questions about Ketoconazole

What is Ketoconazole used for?

Ketoconazole is an investigational small molecule being studied in Phase 1 clinical trials for conditions including chemotherapy-induced nausea and vomiting, type 2 diabetes mellitus, chronic obstructive pulmonary disease, and cancer. It is being developed by GSK plc (GSK) and has been evaluated in healthy volunteers and patients with BRAF mutant solid tumors.

Who makes Ketoconazole?

Ketoconazole is being developed by GSK plc, which trades under the ticker GSK. The company has sponsored Phase 1 clinical trials involving the drug across multiple indications, including oncology and metabolic and respiratory conditions.

What phase is Ketoconazole in?

Ketoconazole is in Phase 1 clinical development. It is investigational and not approved for any use. One Phase 1 study has been completed, with no active trials currently listed.

What clinical trials is Ketoconazole in?

Ketoconazole has been studied in completed Phase 1 trials including NCT00404378, NCT00501397, NCT00866515, and NCT01340846. These trials assessed drug interactions and pharmacokinetics in healthy volunteers and in patients with BRAF mutant solid tumors.

Is Ketoconazole the same as casopitant or GSK189075?

Ketoconazole is not the same as casopitant or GSK189075. It was studied as an interacting drug in trials of those investigational agents, such as NCT00404378 with casopitant and NCT00501397 with GSK189075, to assess how ketoconazole affects their pharmacokinetics.