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GSK2118436

Phase 3

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

Success Probability

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Trial Design

RandomizedCONTROLLEDDMC
Total Trials6
Total Enrollment493

FDA Designations

No designations recorded

Clinical trial landscape

GSK2118436 · 8 trials · 3 indications

Phase 3 1Phase 2 2Phase 1 5
NCT01227889A Study Comparing GSK2118436 to Dacarbazine (DTIC) in Previously Untreated Subjects With BRAF Mutation Positive Advanced (Stage III) or Metastatic (Stage IV) MelanomaCancer
COMPLETED251 Analytics
PHASE3COMPLETED
A Study Comparing GSK2118436 to Dacarbazine (DTIC) in Previously Untreated Subjects With BRAF Mutation Positive Advanced (Stage III) or Metastatic (Stage IV) Melanoma
CancerUnlock trial analytics

Study Endpoints

Primary Endpoints

Progression-free Survival (PFS) as Assessed by the Investigator
Time interval between the date of randomization and the earlier of the date of disease progression or the date of death due to any cause (up to 9.9 months)

PFS is defined as the interval of time between the date of randomization and the earlier of the date of disease progression or the date of death due to any cause. Disease progression was based on radiographic or photographic evidence, and assessments were made by the investigator according to Response Evaluation Criteria in Solid Tumors (RECIST) version 1.1. PD is defined as at least a 20% increase in the sum of the diameters of target lesions, taking as a reference, the smallest sum of diameters recorded since the treatment started (e.g., percent change from nadir, where nadir is defined as the smallest sum of diameters recorded since treatment start). In addition, the sum must have an absolute increase from nadir of 5 millimeters (mm). For participants who did not progress or die, PFS was censored at the date of last contact. Data are presented as median and 96% confidence interval.

Progression-free Survival (PFS) as Assessed by an Independent Radiologist: Randomized Phase
Time interval between the date of randomization and the earlier of the date of disease progression or the date of death due to any cause (up to 9.9 months)

PFS is defined as the interval of time between the date of randomization and the earlier of the date of disease progression or the date of death due to any cause. Disease progression was based on radiographic or photographic evidence, and assessments were made by an independent radiologist according to RECIST version 1.1. PD is defined as at least a 20% increase in the sum of the diameters of target lesions, taking as a reference, the smallest sum of diameters recorded since the treatment started (e.g., percent change from nadir, where nadir is defined as the smallest sum of diameters recorded since treatment start). In addition, the sum must have an absolute increase from nadir of 5 mm. For participants who did not progress or die, PFS was censored at the date of last contact.

Number of Participants With BRAF V600E Mutation-positive Melanoma With Overall Intracranial Response (OIR), as Assessed by the Investigator
From the time of the Baseline assessment until disease progression or end of study treatment (average of 18.3 weeks)

OIR is defined as the number of participants whose intracranial response was a confirmed complete response (CR) or partial response (PR) assessed by investigators using modified Response Evaluation Criteria in Solid Tumors (RECIST), version 1.1. CR is defined as disappearance of all lesions. PR is defined as at least a 30% decrease in the sum of the diameters of target lesions, taking as a reference, the Baseline sum of the diameters (e.g., percent change from Baseline). For the primary analysis, OIR was measured when all participants in both treatment arms had two post-Baseline disease assessments. Participants who had an intracranial response of not evaluable or a missing response were treated as non-responders. Confirmation assessments were to be performed no less than 4 weeks after the criteria for response were initially met and may have been performed at the next protocol scheduled assessment.

Number of Participants With a Best Overall Response of Confirmed Complete Response (CR) or Partial Response (PR) as Assessed by the Investigator for Participants Who Had a BRAF V600E Mutation
Up to 60 months

A participant was defined as a responder if he/she achieved either a CR (the disappearance of all target lesions. Any pathological lymph nodes must be \<10 millimeter (mm) in the short axis.) or PR (at least a 30 percent decrease in the sum of the diameters of target lesions, taking as a reference, the Baseline sum of the diameters \[e.g., percent change from Baseline\]). To be assigned a status of PR or CR, a confirmatory disease assessment was required at Week 12 if an initial response was seen at the Week 6 scan. Initial responses (CR/PR) that occured at Week 12 or later were required to be confirmed not less than 4 weeks and not more than 6 weeks after the criteria for response were first met. The analysis was performed on Primary efficacy Population which comprised of all participants who received at least one dose of GSK2118436 (All Treated Participants Population) and had a BRAF V600E mutation.

Part 1: Safety and tolerability of GSK2118436 as assessed by changes in physical examination findings
Screening, Day 1 and Week 6.

Safety and tolerability parameter will include a complete (head, eyes, ears, nose, throat, skin, thyroid, neurological, lungs, cardiovascular, abdomen \[liver and spleen\], lymph nodes, extremities, height and weight) and brief (skin, lungs, cardiovascular system, abdomen \[liver and spleen\] and weight) physical examination at Baseline and at the end of Part 1 of the study.

Part 1: Safety and tolerability of GSK2118436 as assessed by changes in vital signs measurements
Screening, pre-dose and 8 hours post-dose on Study Day 1, 8, 15, and Week 6.

Safety and tolerability parameter will include measurement of vital signs (recording of systolic and diastolic blood pressure, temperature, and pulse rate) at Baseline and at the end of Part 1 of the study.

Part 1: Safety and tolerability of GSK2118436 as assessed by changes in ECG readings
Screening, Day 1, 8 Day 15 and Week 6. On study days 1 and 8, ECG will be obtained at 30 minutes pre-dose and 2-hours (hrs) post-dose administration.

Safety and tolerability parameter will include ECGs readings (heart rate and measurement of RR, PR, QRS, QT, and QTc intervals) at Baseline and at the end of Part 1 of the study.

Part 1: Safety and tolerability of GSK2118436 as assessed by changes in clinical laboratory assessments
Day 1, 8, 15 and and Week 6.

Safety and tolerability parameter will include laboratory values (hematology, clinical chemistry, coagulation, liver function tests, cardiac enzyme and beta-hCG/serum or urine pregnancy test for female subjects of childbearing potential only) at Baseline and at end of Part 1 of the study.

Part 2: Change from Baseline in QTcF interval at each time point for GSK2118436
Baseline (Study Day -1)/pre-dose (Study Days 1 and 8) (within 30 minutes prior to administration of study treatment) and 1, 1.5, 2, 3, 4, 6, 8, 10 and 24-hrs post-dose. Day 2 and 9, 24 hr post dose Holter ECG.

Change from Baseline in QTcF interval at each time point for GSK2118436 will be calculated as average of 3 Holter ECG replicates per time point minus the value at Baseline.

Number of participants with adverse events as a measure of safety and tolerability
First 28 days for Dose-limiting toxicity, Adverse Events for 1 year

Adverse Events will be graded by the investigator according to the NCI-CTCAE (version 4.0)

The percent of absolute bioavailability (F) of GSK2118436 following single-dose oral HPMC capsule and a concomitant IV microdose
Up to 72 hours
• Excretion of radioactivity in urine following oral administration of [14C]GSK2118436
Pre-dose, and post-dose for a minimum of 96 hours, and a maximum of 240 hours after dosing.
• Excretion of radioactivity in feces following oral administration of [14C]GSK2118436
Pre-dose, and post-dose for a minimum of 96 hours, and a maximum of 240 hours after dosing.
PK data, AEs, changes in laboratory values and vital signs, physical exam, clinical testing and PD data
21 days

Secondary Endpoints

Overall Survival
Time interval between the date of randomization and the date of death due to any cause (up to 22.1 months)
Number of Participants With a Best Overall Response of Confirmed Complete Response (CR) or Confirmed Partial Response (PR) as Assessed by the Investigator: Randomized Phase
From randomization until the first documented evidence of a confirmed complete response or partial response (median of 6.6 weeks)
Number of Participants With a Best Overall Response of Confirmed CR or PR as Assessed by an Independent Radiologist: Randomized Phase
From randomization until the first documented evidence of a confirmed complete response or partial response (median of 12.0 weeks)
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelCROSSOVER
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
GSK2118436EXPERIMENTALSubjects in this arm will receive GSK2118436 150 mg twice daily.
Dacarbazine (DTIC)ACTIVE_COMPARATORSubjects will receive intravenous dacarbazine (DTIC) 1000 mg/m2 every 3 weeks
CrossoverEXPERIMENTALSubjects who initially receive DTIC will be allowed to receive GSK2118436 after initial progression.
Single ArmEXPERIMENTALSingle arm with 2 cohorts; Cohort A no previous brain therapy and Cohort B previous brain therapy
All patientsOTHERSubjects will receive 150 mg of GSK2118436 twice daily and continue on treatment until disease progression, death, or unacceptable adverse event.
Part 1(Cohort 1): GSK2118436 225 mgEXPERIMENTALGSK2118436 (3 capsules of 75 mg) will be administered orally at the dose of 225 mg BID from Day 1 to 7 (and single dose on Day 8) under fasted conditions, either 1 hour before or 2 hours after a meal.
Part 1(Cohort 2): GSK2118436 300 mgEXPERIMENTALGSK2118436 (4 capsules of 75 mg) will be administered orally at the dose of 300 mg BID from Day 1 to 7 (and single dose on Day 8) under fasted conditions, either 1 hour before or 2 hours after a meal. If 225 mg BID is not tolerated in Part 1 /Cohort 1, then Part 1/Cohort 2 will not be initiated and 150 mg BID will be used in Part 2.
Part 2: GSK2118436 300 mg (or highest tolerated dose)EXPERIMENTALSubjects will receive a single dose of GSK2118436/placebo (4 capsules of 75 mg/highest tolerated dose) orally on the first 2 days of the study followed by 2 doses daily for 6 days and a single dose on the 9th day. There will be 1 day when a placebo will be given. All doses will be administered under fasted conditions, either 1 hour before or 2 hours after a meal.
Dose Escalation PartEXPERIMENTALDose escalation will be conducted to assess safety, tolerability, single and repeat dose PK profile and preliminary efficacy of GSK2118436 . The dose may be escalated to the overseas recommended phase III dose.
Study MedicationEXPERIMENTALGSK2118436
Part 1EXPERIMENTALPart 1 will identify the recommended Part 2 dose using a dose-escalation procedure. Escalation may proceed until either a maximum tolerated dose is established, or the toxicokinetic safety limit is reached. Subjects may dose up to three times a day.
Part 2EXPERIMENTALPart 2 will explore further the safety, tolerability, and clinical activity of GSK2118436 in subjects with BRAF mutation-positive tumors using the recommended part 2 dose identified during Part 1. Biologically active doses will be identified by measurement of pharmacodynamic markers in tumor tissue and blood across a range of doses and these doses may be explored in Part 2.

Interventions

NameTypeDescription
GSK2118436DRUG150 mg twice daily
Dacarbazine (DTIC)DRUGIntravenous (IV), 1000 mg/m2 every 3 weeks until initial progression
GSK2118436 75 mgDRUGEach capsule contains 75 mg of GSK2118436A as the mesylate salt, micronized particles as active equivalents.
PlaceboDRUGMatching placebo capsules will be administered in Part 2 of the study.
MidazolamDRUGMidazolam will be administered alone and with GSK2118436 in a sub-set of subjects in Part 2 to study the effect of GSK2118436 on CYP3A using midazolam as a probe.
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites94

Inclusion Criteria: * Adults at least 18 years of age * Has advanced (unresectable Stage III) or metastatic (Stage IV) melanoma that is BRAF mutation positive (V600E) * Is treatment naive for advanced (unresectable) or metastatic melanoma, with the exception of Interleukin 2 (IL-2) which is allowed...

Countries:United StatesAustraliaCanadaFranceGermanyHungaryIrelandItalyNetherlandsPolandRussiaSpainUnited KingdomJapan
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Frequently asked questions about GSK2118436

What is GSK2118436 used for?

GSK2118436 is an investigational small molecule being developed for oncology indications including melanoma, cancer, and melanoma with brain metastases. It is currently in Phase 3 clinical development, though all six listed trials have been completed. The drug is being studied in patients with solid tumors, including those with BRAF mutations.

Who makes GSK2118436?

GSK2118436 is being developed by GSK plc, a pharmaceutical company listed on the stock exchange under the ticker GSK. The company is conducting clinical trials to evaluate the drug's safety and efficacy in oncology indications such as melanoma and other cancers.

What phase is GSK2118436 in?

GSK2118436 is in Phase 3 clinical development for oncology indications. However, all six clinical trials listed for the drug have been completed, with no active trials currently ongoing. The drug remains investigational and has not been reported as approved by regulatory authorities.

What clinical trials is GSK2118436 in?

GSK2118436 has been studied in several completed clinical trials, including NCT00880321, a Phase 1 study in solid tumors; NCT01262963, an ADME study; NCT01340833, a bioavailability study; and NCT01582997, a study in Japanese patients with BRAF mutation positive solid tumors. All trials are completed.

What does GSK2118436 target?

GSK2118436 is being studied in patients with BRAF mutant solid tumors, as indicated by the clinical trial titles. The drug is designed to target cancers with BRAF mutations, which are commonly found in melanoma. It is an oral small molecule being evaluated for its safety and efficacy in these patient populations.