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MK-5108

Phase 1

Cancer, Neoplasms, Tumors | Small molecule | Oncology |Merck & Company, Inc.|Last Updated: Jun 5, 2024

Success Probability
Approval Probability 71%
TA Base Rate26%
Adjusted LOA41%
ML RiskLOW_RISK
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Market & Valuation
rNPV $3.2B
Market Size $9.4B
Revenue Basis $1.6B
Competitors 6
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Trial Design
RandomizedCONTROLLEDBiomarker
Total Trials1
Total Enrollment35
FDA Designations
No designations recorded
Clinical Trials (1)
NCT IDTitlePhaseStatusEnrollmentVelocityDesignStartCompletionLast UpdatedSitesCountries
NCT00543387Treatment of Participants With Advanced and/or Refractory Solid Tumors (MK-5108-001)PHASE1 COMPLETED 35Mar 27, 2008Apr 4, 2011Jun 5, 2024 -
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Study Endpoints
Primary Endpoints
Number of Participants Who Experienced an Adverse Event (AE)
From Day 1 of study treatment until 30 days following the last dose of study treatment (up to 577 days)

An AE was defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the Sponsor's product, whether or not considered related to the use of the product. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a pre-existing condition which is temporally associated with the use of the Sponsor's product, was also an AE. The number of participants who experienced an AE was reported for each dose level group.

Number of Participants With Dose Limiting Toxicities (DLTs)
Day 1 to Day 21 of study treatment (Cycle 1 for Panel 1, Panel 2, or Crossover)

DLTs were AEs considered related to study drug that prevented escalation of the drug dose. Hematologic DLTs included any Grade 5 hematologic toxicity, Grade 4 neutropenia lasting for ≥7 days in duration, Grade 3 or Grade 4 neutropenia with fever \>38.5°C and/or infection requiring antibiotic or anti-fungal treatment, and Grade 4 thrombocytopenia (≤25.0 x 10\^9/L). Non-hematologic DLT was defined as any Grade 3, 4, or 5 non-hematologic toxicity, with the specific exceptions of: Grade 3 nausea or Grade 3 vomiting, Grade 3 diarrhea, or Grade 3 dehydration occurring in the setting of inadequate compliance with supportive care and lasting for \<48 hours, alopecia, inadequately treated hypersensitivity reactions, or Grade 3 elevated transaminases of ≤1 week in duration. Any drug-related AE leading to a dose modification of MK-5108, or any unresolved drug-related toxicity persisting\>6 weeks, was also considered a DLT.

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Study Design & Arms
AllocationRANDOMIZED
MaskingNONE
ModelPARALLEL
PurposeTREATMENT
Treatment Arms
ArmTypeDescription
MK-5108 200 mg BID (Panel 1)EXPERIMENTALParticipants receive 200 mg of MK-5108 orally twice daily (BID) the first 2 days of a 14-day cycle (cycle extended to 21 days if ≥Grade 2 toxicity observed).
MK-5108 400 mg BID (Panel 1)EXPERIMENTALParticipants receive 400 mg of MK-5108 orally BID the first 2 days of a 14-day cycle (cycle extended to 21 days if ≥Grade 2 toxicity observed).
MK-5108 800 mg BID (Panel 1)EXPERIMENTALParticipants receive 800 mg of MK-5108 orally BID the first 2 days of a 14-day cycle (cycle extended to 21 days if ≥Grade 2 toxicity observed).
MK-5108 1200 mg BID (Panel 1)EXPERIMENTALParticipants receive 1200 mg of MK-5108 orally BID the first 2 days of a 14-day cycle (cycle extended to 21 days if ≥Grade 2 toxicity observed).
MK-5108 1500 mg BID (Panel 1)EXPERIMENTALParticipants receive 1500 mg of MK-5108 orally BID the first 2 days of a 14-day cycle (cycle extended to 21 days if ≥Grade 2 toxicity observed).
MK-5108 1800 mg BID (Panel 1)EXPERIMENTALParticipants receive 1800 mg of MK-5108 orally BID the first 2 days of a 14-day cycle (cycle extended to 21 days if ≥Grade 2 toxicity observed).
MK-5108 100 mg BID + 60 mg/m^2 Docetaxel (Panel 2)EXPERIMENTALParticipants receive 100 mg of MK-5108 orally BID in combination with 60 mg/m\^2 Docetaxel administered intravenously (IV) the first 2 days of a 21-day cycle.
MK-5108 150 mg BID + 60 mg/m^2 Docetaxel (Panel 2)EXPERIMENTALParticipants receive 150 mg of MK-5108 orally BID in combination with 60 mg/m\^2 Docetaxel administered IV the first 2 days of a 21-day cycle.
MK-5108 225 mg BID + 60 mg/m^2 Docetaxel (Panel 2)EXPERIMENTALParticipants receive 150 mg of MK-5108 orally BID in combination with 60 mg/m\^2 Docetaxel administered IV the first 2 days of a 21-day cycle.
MK-5108 100 mg BID + 60 mg/m^2 Docetaxel (Crossover)EXPERIMENTALAfter receiving treatment in Panel 1, one participant crossed over to Panel 2 per protocol following disease progression to receive 100 mg of MK-5108 orally BID in combination with 60 mg/m\^2 Docetaxel administered IV the first 2 days of a 21-day cycle.
MK-5108 150 mg BID + 60 mg/m^2 Docetaxel (Crossover)EXPERIMENTALAfter receiving treatment in Panel 1, participants crossed over to Panel 2 per protocol following disease progression to receive 150 mg of MK-5108 orally BID in combination with 60 mg/m\^2 Docetaxel administered IV the first 2 days of a 21-day cycle.
Interventions
NameTypeDescription
MK-5108DRUGMK-5108 will be administered orally, every 12 hours (Q12H) during the first 2 days of each cycle. Cycle length will be 14-21 days in Panel 1 and 21 days in Panel 2.
docetaxelDRUGDocetaxel will be administered intravenously (I.V.) at a dose of 60 mg/m\^2 Q12H during the first 2 days of each 21-day cycle.
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Eligibility Criteria
Age Range18 Years — N/A
SexALL
Healthy VolunteersNo

Inclusion Criteria: \- Participant has a histologically-confirmed metastatic or locally advanced solid tumor that has failed to respond to standard therapy or progressed with standard therapy Exclusion Criteria: * Participant has had chemotherapy, radiotherapy or biological therapy within 4 weeks...

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